A Knowledge Based Approach to Drug Repurposing for Socially Important and Rare Diseases
RSF - DST Project # 16-45-02012 - INT/RUS/RSF/12

World wide approved drugs

Database contains information on about 4,108 medications, including the name of the drug, synonyms, the structural formula of the drug substance, pharmacotherapeutic fields and mechanisms of action.

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Structure Brand Name Target Pharmacotheraputic application Pharmacological class Approved link PDB link PASSOnline prediction
Structure Brand Name Target Pharmacotheraputic application Pharmacological class Approved link PDB link PASSOnline prediction
Click to view acalabrutinib Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210259s000lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210259s000lbl.pdf) Cytoplasmic tyrosine-protein kinase BMX (Organism: Homo sapiens, class: Kinase, accessions: P51813, gene: BMX, swissprot: BMX_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Tec (Organism: Homo sapiens, class: Kinase, accessions: P42680, gene: TEC, swissprot: TEC_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase TXK (Organism: Homo sapiens, class: Kinase, accessions: P42681, gene: TXK, swissprot: TXK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Receptor tyrosine-protein kinase erbB-4 (Organism: Homo sapiens, class: Kinase, accessions: Q15303, gene: ERBB4, swissprot: ERBB4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Acalabrutinib is a small-molecule inhibitor of BTK. Acalabrutinib and its active metabolite, ACP-5862, form a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B cell antigen receptor and cytokine receptor pathways. In B cells, BTK signaling results in activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, an adhesion. In nonclinical studies, acalabrutinib inhibited BTK mediated activation of downstream signaling proteins CD86 and CD69 and inhibited malignant B-cell proliferation and survival. Acalabrutinib is indicated for the treatment of adult patients with mantle cell lymphoma who have received at least one prior therapy. Kinase Inhibitor (Code: N0000175605) Tyrosine Kinase Inhibitors (Code: N0000020001) 2017-10-31 FDA
Click to view latanoprostene bunod Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: ) Latanoprostene bunod is thought to lower intraocular pressure by increasing outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes. Intraocular pressure is a major modifiable risk factor for glaucoma progression. Reduction of intraocular pressure reduces risk of glaucomatous visual field loss. 2017-11-02 FDA
Click to view letermovir DNA terminase complex (Organism: Human cytomegalovirus (strain Merlin), class: Enzyme, accessions: F5HC79|F5HCU8|F5HGI9, gene: TRM1|TRM2|TRM3, swissprot: TRM1_HCMVM|TRM2_HCMVM|TRM3_HCMVM) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209939Orig1s000,209940Orig1s000lbl.pdf) Letermovir inhibits the CMV DNA terminase complex (pUL51, pUL56, and pUL89) which is required for viral DNA processing and packaging. Biochemical characterization and electron microscopy demonstrated that letermovir affects the production of proper unit length genomes and interferes with virion maturation. Genotypic characterization of virus resistant to letermovir confirmed that letermovir targets the terminase complex. Cytomegalovirus DNA Terminase Complex Inhibitor (Code: N0000193800) DNA Terminase Complex Inhibitors (Code: N0000193801) Cytochrome P450 3A Inhibitors (Code: N0000190114) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Cytochrome P450 2C8 Inhibitors (Code: N0000187062) Cytochrome P450 2C9 Inducers (Code: N0000185507) Cytochrome P450 2C19 Inducers (Code: N0000185607) 2017-11-08 FDA
Click to view vaborbactam Beta-lactamase (Organism: Klebsiella pneumoniae, class: Enzyme, accessions: Q93LQ9, gene: KPC-2, swissprot: Q93LQ9_KLEPN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28848018) Beta-lactamase (Organism: Escherichia coli, class: Enzyme, accessions: Q9L5C7, gene: blaCTX-M-14, swissprot: Q9L5C7_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28848018) Beta-lactamase (Organism: Escherichia coli, class: Enzyme, accessions: A8DZJ2, gene: blaSHV, swissprot: A8DZJ2_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28848018) Vaborbactam is a non-suicidal beta-lactamase inhibitor that protects meropenem from degradation by certain serine beta-lactamases such as Klebsiella pneumoniae carbapenemase (KPC). Vaborbactam does not have any antibacterial activity. Vaborbactam does not decrease the activity of meropenem against meropenem-susceptible organisms. beta Lactamase Inhibitor (Code: N0000175930) beta Lactamase Inhibitors (Code: N0000000202) 2017-08-29 FDA 4D6
Click to view morinidazole Morinidazole is a nitroimidazole antibiotic indicated for the treatment of sensitive anaerobic bacterial infections including appendicitis and pelvic inflammatory disease caused by anaerobic bacteria. 2014-02-24 China Food and Drug Administration (CFDA)
Click to view forodesine Purine nucleoside phosphorylase (Organism: Homo sapiens, class: Enzyme, accessions: P00491, gene: PNP, swissprot: PNPH_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9628722) S-methyl-5'-thioadenosine phosphorylase (Organism: Homo sapiens, class: Enzyme, accessions: Q13126, gene: MTAP, swissprot: MTAP_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15163207) Forodesine is a transition state analogue that binds preferentially to and inhibits purine nucleotide phosphorylase (PNP), resulting in the accumulation of deoxyguanosine triphosphate and the subsequent inhibition of the enzyme ribonucleoside diphosphate reductase and DNA synthesis. This agent selectively causes apoptosis in stimulated or malignant T-lymphocytes. A transition state analogue is a substrate designed to mimic the properties or the geometry of the transition state of reaction. Forodesine is used for the treatment of different hematologic malignancies. 2017-03-30 PMDA
Click to view midostaurin Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: ) Activated CDC42 kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q07912, gene: TNK2, swissprot: ACK1_HUMAN Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN Serine/threonine-protein kinase PAK 3 (Organism: Homo sapiens, class: Kinase, accessions: O75914, gene: PAK3, swissprot: PAK3_HUMAN 3-phosphoinositide-dependent protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: O15530, gene: PDPK1, swissprot: PDPK1_HUMAN Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (Organism: Homo sapiens, class: Kinase, accessions: Q16816, gene: PHKG1, swissprot: PHKG1_HUMAN Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha (Organism: Homo sapiens, class: Kinase, accessions: Q99755, gene: PIP5K1A, swissprot: PI51A_HUMAN Ribosomal protein S6 kinase alpha-6 (Organism: Homo sapiens, class: Kinase, accessions: Q9UK32, gene: RPS6KA6, swissprot: KS6A6_HUMAN Myosin light chain kinase family member 4 (Organism: Homo sapiens, class: Kinase, accessions: Q86YV6, gene: MYLK4, swissprot: MYLK4_HUMAN Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN Tyrosine-protein kinase Yes (Organism: Homo sapiens, class: Kinase, accessions: P07947, gene: YES1, swissprot: YES_HUMAN Serine/threonine-protein kinase 25 (Organism: Homo sapiens, class: Kinase, accessions: O00506, gene: STK25, swissprot: STK25_HUMAN Tyrosine-protein kinase ZAP-70 (Organism: Homo sapiens, class: Kinase, accessions: P43403, gene: ZAP70, swissprot: ZAP70_HUMAN Phosphatidylinositol 5-phosphate 4-kinase type-2 beta (Organism: Homo sapiens, class: Kinase, accessions: P78356, gene: PIP4K2B, swissprot: PI42B_HUMAN cAMP-dependent protein kinase catalytic subunit beta (Organism: Homo sapiens, class: Kinase, accessions: P22694, gene: PRKACB, swissprot: KAPCB_HUMAN cAMP-dependent protein kinase catalytic subunit PRKX (Organism: Homo sapiens, class: Unclassified, accessions: P51817, gene: PRKX, swissprot: PRKX_HUMAN Protein-tyrosine kinase 2-beta (Organism: Homo sapiens, class: Kinase, accessions: Q14289, gene: PTK2B, swissprot: FAK2_HUMAN Dual specificity protein kinase CLK1 (Organism: Homo sapiens, class: Kinase, accessions: P49759, gene: CLK1, swissprot: CLK1_HUMAN Tyrosine-protein kinase CSK (Organism: Homo sapiens, class: Kinase, accessions: P41240, gene: CSK, swissprot: CSK_HUMAN Tyrosine-protein kinase receptor Tie-1 (Organism: Homo sapiens, class: Kinase, accessions: P35590, gene: TIE1, swissprot: TIE1_HUMAN Angiopoietin-1 receptor (Organism: Homo sapiens, class: Kinase, accessions: Q02763, gene: TEK, swissprot: TIE2_HUMAN TRAF2 and NCK-interacting protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9UKE5, gene: TNIK, swissprot: TNIK_HUMAN High affinity nerve growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P04629, gene: NTRK1, swissprot: NTRK1_HUMAN BDNF/NT-3 growth factors receptor (Organism: Homo sapiens, class: Kinase, accessions: Q16620, gene: NTRK2, swissprot: NTRK2_HUMAN NT-3 growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: Q16288, gene: NTRK3, swissprot: NTRK3_HUMAN Dual specificity protein kinase TTK (Organism: Homo sapiens, class: Kinase, accessions: P33981, gene: TTK, swissprot: TTK_HUMAN Casein kinase II subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: P68400, gene: CSNK2A1, swissprot: CSK21_HUMAN Death-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9UIK4, gene: DAPK2, swissprot: DAPK2_HUMAN Serine/threonine-protein kinase 17B (Organism: Homo sapiens, class: Kinase, accessions: O94768, gene: STK17B, swissprot: ST17B_HUMAN Dual specificity tyrosine-phosphorylation-regulated kinase 1B (Organism: Homo sapiens, class: Kinase, accessions: Q9Y463, gene: DYRK1B, swissprot: DYR1B_HUMAN Glycogen synthase kinase-3 alpha (Organism: Homo sapiens, class: Kinase, accessions: P49840, gene: GSK3A, swissprot: GSK3A_HUMAN Glycogen synthase kinase-3 beta (Organism: Homo sapiens, class: Kinase, accessions: P49841, gene: GSK3B, swissprot: GSK3B_HUMAN Inhibitor of nuclear factor kappa-B kinase subunit epsilon (Organism: Homo sapiens, class: Kinase, accessions: Q14164, gene: IKBKE, swissprot: IKKE_HUMAN Non-receptor tyrosine-protein kinase TYK2 (Organism: Homo sapiens, class: Kinase, accessions: P29597, gene: TYK2, swissprot: TYK2_HUMAN Mitogen-activated protein kinase 8 (Organism: Homo sapiens, class: Kinase, accessions: P45983, gene: MAPK8, swissprot: MK08_HUMAN Serine/threonine-protein kinase STK11 (Organism: Homo sapiens, class: Kinase, accessions: Q15831, gene: STK11, swissprot: STK11_HUMAN MAP/microtubule affinity-regulating kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: P27448, gene: MARK3, swissprot: MARK3_HUMAN Dual specificity mitogen-activated protein kinase kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: P46734, gene: MAP2K3, swissprot: MP2K3_HUMAN Maternal embryonic leucine zipper kinase (Organism: Homo sapiens, class: Kinase, accessions: Q14680, gene: MELK, swissprot: MELK_HUMAN AP2-associated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q2M2I8, gene: AAK1, swissprot: AAK1_HUMAN Serine/threonine-protein kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q13043, gene: STK4, swissprot: STK4_HUMAN Eukaryotic translation initiation factor 2-alpha kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q9P2K8, gene: EIF2AK4, swissprot: E2AK4_HUMAN Tyrosine-protein kinase HCK (Organism: Homo sapiens, class: Kinase, accessions: P08631, gene: HCK, swissprot: HCK_HUMAN Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN Interleukin-1 receptor-associated kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y616, gene: IRAK3, swissprot: IRAK3_HUMAN Tyrosine-protein kinase JAK2 (Organism: Homo sapiens, class: Kinase, accessions: O60674, gene: JAK2, swissprot: JAK2_HUMAN Tyrosine-protein kinase JAK3 (Organism: Homo sapiens, class: Kinase, accessions: P52333, gene: JAK3, swissprot: JAK3_HUMAN Mitogen-activated protein kinase 10 (Organism: Homo sapiens, class: Kinase, accessions: P53779, gene: MAPK10, swissprot: MK10_HUMAN Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN Serine/threonine-protein kinase RIO1 (Organism: Homo sapiens, class: Kinase, accessions: Q9BRS2, gene: RIOK1, swissprot: RIOK1_HUMAN Serine/threonine-protein kinase RIO3 (Organism: Homo sapiens, class: Kinase, accessions: O14730, gene: RIOK3, swissprot: RIOK3_HUMAN Serine/threonine-protein kinase SIK2 (Organism: Homo sapiens, class: Kinase, accessions: Q9H0K1, gene: SIK2, swissprot: SIK2_HUMAN SRSF protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q96SB4, gene: SRPK1, swissprot: SRPK1_HUMAN SRSF protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P78362, gene: SRPK2, swissprot: SRPK2_HUMAN Non-receptor tyrosine-protein kinase TNK1 (Organism: Homo sapiens, class: Kinase, accessions: Q13470, gene: TNK1, swissprot: TNK1_HUMAN Testis-specific serine/threonine-protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q9BXA7, gene: TSSK1B, swissprot: TSSK1_HUMAN Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN Cyclin-G-associated kinase (Organism: Homo sapiens, class: Kinase, accessions: O14976, gene: GAK, swissprot: GAK_HUMAN ALK tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: Q9UM73, gene: ALK, swissprot: ALK_HUMAN 5'-AMP-activated protein kinase catalytic subunit alpha-1 (Organism: Homo sapiens, class: Kinase, accessions: Q13131, gene: PRKAA1, swissprot: AAPK1_HUMAN 5'-AMP-activated protein kinase catalytic subunit alpha-2 (Organism: Homo sapiens, class: Kinase, accessions: P54646, gene: PRKAA2, swissprot: AAPK2_HUMAN Epithelial discoidin domain-containing receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: Q08345, gene: DDR1, swissprot: DDR1_HUMAN Myotonin-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q09013, gene: DMPK, swissprot: DMPK_HUMAN RAC-alpha serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P31749, gene: AKT1, swissprot: AKT1_HUMAN RAC-beta serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P31751, gene: AKT2, swissprot: AKT2_HUMAN Serine/threonine-protein kinase LATS1 (Organism: Homo sapiens, class: Kinase, accessions: O95835, gene: LATS1, swissprot: LATS1_HUMAN Serine/threonine-protein kinase LATS2 (Organism: Homo sapiens, class: Kinase, accessions: Q9NRM7, gene: LATS2, swissprot: LATS2_HUMAN Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN Serine/threonine-protein kinase 10 (Organism: Homo sapiens, class: Kinase, accessions: O94804, gene: STK10, swissprot: STK10_HUMAN Leukocyte tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: P29376, gene: LTK, swissprot: LTK_HUMAN Tyrosine-protein kinase Lyn (Organism: Homo sapiens, class: Kinase, accessions: P07948, gene: LYN, swissprot: LYN_HUMAN Serine/threonine-protein kinase 17A (Organism: Homo sapiens, class: Kinase, accessions: Q9UEE5, gene: STK17A, swissprot: ST17A_HUMAN Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN NUAK family SNF1-like kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: O60285, gene: NUAK1, swissprot: NUAK1_HUMAN Aurora kinase A (Organism: Homo sapiens, class: Kinase, accessions: O14965, gene: AURKA, swissprot: AURKA_HUMAN Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN Phosphorylase b kinase gamma catalytic chain, liver/testis isoform (Organism: Homo sapiens, class: Kinase, accessions: P15735, gene: PHKG2, swissprot: PHKG2_HUMAN Serine/threonine-protein kinase pim-1 (Organism: Homo sapiens, class: Kinase, accessions: P11309, gene: PIM1, swissprot: PIM1_HUMAN Serine/threonine-protein kinase pim-3 (Organism: Homo sapiens, class: Kinase, accessions: Q86V86, gene: PIM3, swissprot: PIM3_HUMAN cAMP-dependent protein kinase catalytic subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: P17612, gene: PRKACA, swissprot: KAPCA_HUMAN Mitogen-activated protein kinase kinase kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q92918, gene: MAP4K1, swissprot: M4K1_HUMAN Mitogen-activated protein kinase kinase kinase kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q8IVH8, gene: MAP4K3, swissprot: M4K3_HUMAN Aurora kinase B (Organism: Homo sapiens, class: Kinase, accessions: Q96GD4, gene: AURKB, swissprot: AURKB_HUMAN Tyrosine-protein kinase receptor UFO (Organism: Homo sapiens, class: Kinase, accessions: P30530, gene: AXL, swissprot: UFO_HUMAN BMP-2-inducible protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9NSY1, gene: BMP2K, swissprot: BMP2K_HUMAN Tyrosine-protein kinase Blk (Organism: Homo sapiens, class: Kinase, accessions: P51451, gene: BLK, swissprot: BLK_HUMAN Serine/threonine-protein kinase BRSK1 (Organism: Homo sapiens, class: Kinase, accessions: Q8TDC3, gene: BRSK1, swissprot: BRSK1_HUMAN Calcium/calmodulin-dependent protein kinase type 1D (Organism: Homo sapiens, class: Kinase, accessions: Q8IU85, gene: CAMK1D, swissprot: KCC1D_HUMAN Calcium/calmodulin-dependent protein kinase type 1G (Organism: Homo sapiens, class: Kinase, accessions: Q96NX5, gene: CAMK1G, swissprot: KCC1G_HUMAN Mitogen-activated protein kinase kinase kinase kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: O95819, gene: MAP4K4, swissprot: M4K4_HUMAN Mitogen-activated protein kinase kinase kinase kinase 5 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y4K4, gene: MAP4K5, swissprot: M4K5_HUMAN Serine/threonine-protein kinase MARK1 (Organism: Homo sapiens, class: Kinase, accessions: Q9P0L2, gene: MARK1, swissprot: MARK1_HUMAN Serine/threonine-protein kinase MARK2 (Organism: Homo sapiens, class: Kinase, accessions: Q7KZI7, gene: MARK2, swissprot: MARK2_HUMAN MAP/microtubule affinity-regulating kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q96L34, gene: MARK4, swissprot: MARK4_HUMAN Dual specificity mitogen-activated protein kinase kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P45985, gene: MAP2K4, swissprot: MP2K4_HUMAN Tyrosine-protein kinase Mer (Organism: Homo sapiens, class: Kinase, accessions: Q12866, gene: MERTK, swissprot: MERTK_HUMAN Hepatocyte growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P08581, gene: MET, swissprot: MET_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: Q9UQM7, gene: CAMK2A, swissprot: KCC2A_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit beta (Organism: Homo sapiens, class: Kinase, accessions: Q13554, gene: CAMK2B, swissprot: KCC2B_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit delta (Organism: Homo sapiens, class: Kinase, accessions: Q13557, gene: CAMK2D, swissprot: KCC2D_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit gamma (Organism: Homo sapiens, class: Kinase, accessions: Q13555, gene: CAMK2G, swissprot: KCC2G_HUMAN Calcium/calmodulin-dependent protein kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q8N5S9, gene: CAMKK1, swissprot: KKCC1_HUMAN Calcium/calmodulin-dependent protein kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q96RR4, gene: CAMKK2, swissprot: KKCC2_HUMAN Cyclin-dependent kinase 19 (Organism: Homo sapiens, class: Kinase, accessions: Q9BWU1, gene: CDK19, swissprot: CDK19_HUMAN MAP kinase-interacting serine/threonine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9HBH9, gene: MKNK2, swissprot: MKNK2_HUMAN Mitogen-activated protein kinase kinase kinase 9 (Organism: Homo sapiens, class: Kinase, accessions: P80192, gene: MAP3K9, swissprot: M3K9_HUMAN Mitogen-activated protein kinase kinase kinase 10 (Organism: Homo sapiens, class: Kinase, accessions: Q02779, gene: MAP3K10, swissprot: M3K10_HUMAN Mitogen-activated protein kinase kinase kinase 11 (Organism: Homo sapiens, class: Kinase, accessions: Q16584, gene: MAP3K11, swissprot: M3K11_HUMAN Serine/threonine-protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q13188, gene: STK3, swissprot: STK3_HUMAN Myosin light chain kinase, smooth muscle (Organism: Homo sapiens, class: Kinase, accessions: Q15746, gene: MYLK, swissprot: MYLK_HUMAN Serine/threonine-protein kinase Chk1 (Organism: Homo sapiens, class: Kinase, accessions: O14757, gene: CHEK1, swissprot: CHK1_HUMAN Dual specificity protein kinase CLK2 (Organism: Homo sapiens, class: Kinase, accessions: P49760, gene: CLK2, swissprot: CLK2_HUMAN Dual specificity protein kinase CLK4 (Organism: Homo sapiens, class: Kinase, accessions: Q9HAZ1, gene: CLK4, swissprot: CLK4_HUMAN Macrophage colony-stimulating factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P07333, gene: CSF1R, swissprot: CSF1R_HUMAN Death-associated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P53355, gene: DAPK1, swissprot: DAPK1_HUMAN Death-associated protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: O43293, gene: DAPK3, swissprot: DAPK3_HUMAN Serine/threonine-protein kinase PAK 1 (Organism: Homo sapiens, class: Kinase, accessions: Q13153, gene: PAK1, swissprot: PAK1_HUMAN Serine/threonine-protein kinase PAK 2 (Organism: Homo sapiens, class: Kinase, accessions: Q13177, gene: PAK2, swissprot: PAK2_HUMAN Tyrosine-protein kinase FRK (Organism: Homo sapiens, class: Kinase, accessions: P42685, gene: FRK, swissprot: FRK_HUMAN Aurora kinase C (Organism: Homo sapiens, class: Kinase, accessions: Q9UQB9, gene: AURKC, swissprot: AURKC_HUMAN Serine/threonine-protein kinase BRSK2 (Organism: Homo sapiens, class: Kinase, accessions: Q8IWQ3, gene: BRSK2, swissprot: BRSK2_HUMAN Calcium/calmodulin-dependent protein kinase type 1 (Organism: Homo sapiens, class: Kinase, accessions: Q14012, gene: CAMK1, swissprot: KCC1A_HUMAN STE20-like serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9H2G2, gene: SLK, swissprot: SLK_HUMAN NUAK family SNF1-like kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9H093, gene: NUAK2, swissprot: NUAK2_HUMAN Serine/threonine-protein kinase SIK1 (Organism: Homo sapiens, class: Kinase, accessions: P57059, gene: SIK1, swissprot: SIK1_HUMAN Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN Serine/threonine-protein kinase 16 (Organism: Homo sapiens, class: Kinase, accessions: O75716, gene: STK16, swissprot: STK16_HUMAN Tyrosine-protein kinase SYK (Organism: Homo sapiens, class: Kinase, accessions: P43405, gene: SYK, swissprot: KSYK_HUMAN Serine/threonine-protein kinase N1 (Organism: Homo sapiens, class: Kinase, accessions: Q16512, gene: PKN1, swissprot: PKN1_HUMAN Serine/threonine-protein kinase N2 (Organism: Homo sapiens, class: Kinase, accessions: Q16513, gene: PKN2, swissprot: PKN2_HUMAN Serine/threonine-protein kinase PLK4 (Organism: Homo sapiens, class: Kinase, accessions: O00444, gene: PLK4, swissprot: PLK4_HUMAN Protein kinase C delta type (Organism: Homo sapiens, class: Kinase, accessions: Q05655, gene: PRKCD, swissprot: KPCD_HUMAN Protein kinase C epsilon type (Organism: Homo sapiens, class: Kinase, accessions: Q02156, gene: PRKCE, swissprot: KPCE_HUMAN Protein kinase C eta type (Organism: Homo sapiens, class: Kinase, accessions: P24723, gene: PRKCH, swissprot: KPCL_HUMAN Protein kinase C theta type (Organism: Homo sapiens, class: Kinase, accessions: Q04759, gene: PRKCQ, swissprot: KPCT_HUMAN Tubulin alpha-1A chain (Organism: Rattus norvegicus, class: Structural, accessions: P68370, gene: Tuba1a, swissprot: TBA1A_RAT Tyrosine-protein kinase Fer (Organism: Homo sapiens, class: Kinase, accessions: P16591, gene: FER, swissprot: FER_HUMAN Serine/threonine-protein kinase D2 (Organism: Homo sapiens, class: Kinase, accessions: Q9BZL6, gene: PRKD2, swissprot: KPCD2_HUMAN Serine/threonine-protein kinase D3 (Organism: Homo sapiens, class: Kinase, accessions: O94806, gene: PRKD3, swissprot: KPCD3_HUMAN cGMP-dependent protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q13976, gene: PRKG1, swissprot: KGP1_HUMAN cGMP-dependent protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q13237, gene: PRKG2, swissprot: KGP2_HUMAN Interferon-induced, double-stranded RNA-activated protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P19525, gene: EIF2AK2, swissprot: E2AK2_HUMAN Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN Fibroblast growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P21802, gene: FGFR2, swissprot: FGFR2_HUMAN Fibroblast growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P22607, gene: FGFR3, swissprot: FGFR3_HUMAN Tyrosine-protein kinase Fgr (Organism: Homo sapiens, class: Kinase, accessions: P09769, gene: FGR, swissprot: FGR_HUMAN Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN Proto-oncogene tyrosine-protein kinase ROS (Organism: Homo sapiens, class: Kinase, accessions: P08922, gene: ROS1, swissprot: ROS1_HUMAN Ribosomal protein S6 kinase alpha-1 (Organism: Homo sapiens, class: Kinase, accessions: Q15418, gene: RPS6KA1, swissprot: KS6A1_HUMAN Ribosomal protein S6 kinase alpha-2 (Organism: Homo sapiens, class: Kinase, accessions: Q15349, gene: RPS6KA2, swissprot: KS6A2_HUMAN Ribosomal protein S6 kinase alpha-3 (Organism: Homo sapiens, class: Kinase, accessions: P51812, gene: RPS6KA3, swissprot: KS6A3_HUMAN Ribosomal protein S6 kinase alpha-4 (Organism: Homo sapiens, class: Kinase, accessions: O75676, gene: RPS6KA4, swissprot: KS6A4_HUMAN Ribosomal protein S6 kinase alpha-5 (Organism: Homo sapiens, class: Kinase, accessions: O75582, gene: RPS6KA5, swissprot: KS6A5_HUMAN SRSF protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q9UPE1, gene: SRPK3, swissprot: SRPK3_HUMAN Dual specificity tyrosine-phosphorylation-regulated kinase 1A (Organism: Homo sapiens, class: Kinase, accessions: Q13627, gene: DYRK1A, swissprot: DYR1A_HUMAN Ephrin type-B receptor 6 (Organism: Homo sapiens, class: Kinase, accessions: O15197, gene: EPHB6, swissprot: EPHB6_HUMAN Receptor tyrosine-protein kinase erbB-4 (Organism: Homo sapiens, class: Kinase, accessions: Q15303, gene: ERBB4, swissprot: ERBB4_HUMAN Serine/threonine-protein kinase/endoribonuclease IRE1 (Organism: Homo sapiens, class: Kinase, accessions: O75460, gene: ERN1, swissprot: ERN1_HUMAN Rhodopsin kinase (Organism: Homo sapiens, class: Kinase, accessions: Q15835, gene: GRK1, swissprot: RK_HUMAN G protein-coupled receptor kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P32298, gene: GRK4, swissprot: GRK4_HUMAN G protein-coupled receptor kinase 7 (Organism: Homo sapiens, class: Kinase, accessions: Q8WTQ7, gene: GRK7, swissprot: GRK7_HUMAN Homeodomain-interacting protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9H2X6, gene: HIPK2, swissprot: HIPK2_HUMAN Homeodomain-interacting protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q9H422, gene: HIPK3, swissprot: HIPK3_HUMAN Homeodomain-interacting protein kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q8NE63, gene: HIPK4, swissprot: HIPK4_HUMAN Hormonally up-regulated neu tumor-associated kinase (Organism: Homo sapiens, class: Kinase, accessions: P57058, gene: HUNK, swissprot: HUNK_HUMAN Inhibitor of nuclear factor kappa-B kinase subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: O15111, gene: CHUK, swissprot: IKKA_HUMAN Tyrosine-protein kinase JAK1 (Organism: Homo sapiens, class: Kinase, accessions: P23458, gene: JAK1, swissprot: JAK1_HUMAN Mitogen-activated protein kinase kinase kinase 13 (Organism: Homo sapiens, class: Kinase, accessions: O43283, gene: MAP3K13, swissprot: M3K13_HUMAN Mitogen-activated protein kinase kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y2U5, gene: MAP3K2, swissprot: M3K2_HUMAN Mitogen-activated protein kinase kinase kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q99759, gene: MAP3K3, swissprot: M3K3_HUMAN Mitogen-activated protein kinase kinase kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q12851, gene: MAP4K2, swissprot: M4K2_HUMAN Misshapen-like kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q8N4C8, gene: MINK1, swissprot: MINK1_HUMAN Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta (Organism: Homo sapiens, class: Kinase, accessions: O00750, gene: PIK3C2B, swissprot: P3C2B_HUMAN Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma (Organism: Homo sapiens, class: Kinase, accessions: O75747, gene: PIK3C2G, swissprot: P3C2G_HUMAN Protein kinase C alpha type (Organism: Homo sapiens, class: Kinase, accessions: P17252, gene: PRKCA, swissprot: KPCA_HUMAN U4/U6 small nuclear ribonucleoprotein Prp4 (Organism: Homo sapiens, class: Unclassified, accessions: O43172, gene: PRPF4, swissprot: PRP4_HUMAN Serine/threonine-protein kinase SIK3 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y2K2, gene: SIK3, swissprot: SIK3_HUMAN Serine/threonine-protein kinase RIO2 (Organism: Homo sapiens, class: Kinase, accessions: Q9BVS4, gene: RIOK2, swissprot: RIOK2_HUMAN Rho-associated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q13464, gene: ROCK1, swissprot: ROCK1_HUMAN Rho-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: O75116, gene: ROCK2, swissprot: ROCK2_HUMAN Mitogen-activated protein kinase kinase kinase 7 (Organism: Homo sapiens, class: Kinase, accessions: O43318, gene: MAP3K7, swissprot: M3K7_HUMAN Serine/threonine-protein kinase TBK1 (Organism: Homo sapiens, class: Kinase, accessions: Q9UHD2, gene: TBK1, swissprot: TBK1_HUMAN Tankyrase-2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9H2K2, gene: TNKS2, swissprot: TNKS2_HUMAN Serine/threonine-protein kinase ULK3 (Organism: Homo sapiens, class: Kinase, accessions: Q6PHR2, gene: ULK3, swissprot: ULK3_HUMAN Mitogen-activated protein kinase kinase kinase 19 (Organism: Homo sapiens, class: Kinase, accessions: Q56UN5, gene: MAP3K19, swissprot: M3K19_HUMAN Serine/threonine-protein kinase 32A (Organism: Homo sapiens, class: Kinase, accessions: Q8WU08, gene: STK32A, swissprot: ST32A_HUMAN Inhibitor of nuclear factor kappa-B kinase subunit beta (Organism: Homo sapiens, class: Kinase, accessions: O14920, gene: IKBKB, swissprot: IKKB_HUMAN Dual specificity mitogen-activated protein kinase kinase 6 (Organism: Homo sapiens, class: Kinase, accessions: P52564, gene: MAP2K6, swissprot: MP2K6_HUMAN Ribosomal protein S6 kinase beta-1 (Organism: Homo sapiens, class: Kinase, accessions: P23443, gene: RPS6KB1, swissprot: KS6B1_HUMAN Wee1-like protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P30291, gene: WEE1, swissprot: WEE1_HUMAN Serine/threonine-protein kinase PRP4 homolog (Organism: Homo sapiens, class: Kinase, accessions: Q13523, gene: PRPF4B, swissprot: PRP4B_HUMAN Dual specificity protein kinase CLK3 (Organism: Homo sapiens, class: Kinase, accessions: P49761, gene: CLK3, swissprot: CLK3_HUMAN RAC-gamma serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9Y243, gene: AKT3, swissprot: AKT3_HUMAN Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Organism: Homo sapiens, class: Kinase, accessions: P42336, gene: PIK3CA, swissprot: PK3CA_HUMAN Serine/threonine-protein kinase pim-2 (Organism: Homo sapiens, class: Kinase, accessions: Q9P1W9, gene: PIM2, swissprot: PIM2_HUMAN Serine/threonine-protein kinase Sgk3 (Organism: Homo sapiens, class: Kinase, accessions: Q96BR1, gene: SGK3, swissprot: SGK3_HUMAN Serine/threonine-protein kinase ICK (Organism: Homo sapiens, class: Kinase, accessions: Q9UPZ9, gene: ICK, swissprot: ICK_HUMAN Microtubule-associated serine/threonine-protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y2H9, gene: MAST1, swissprot: MAST1_HUMAN Serine/threonine-protein kinase 33 (Organism: Homo sapiens, class: Kinase, accessions: Q9BYT3, gene: STK33, swissprot: STK33_HUMAN Mitogen-activated protein kinase 9 (Organism: Homo sapiens, class: Kinase, accessions: P45984, gene: MAPK9, swissprot: MK09_HUMAN Myosin light chain kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q32MK0, gene: MYLK3, swissprot: MYLK3_HUMAN Leucine-rich repeat serine/threonine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q5S007, gene: LRRK2, swissprot: LRRK2_HUMAN Dual serine/threonine and tyrosine protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q6XUX3, gene: DSTYK, swissprot: DUSTY_HUMAN Calcium-dependent protein kinase 1 (Organism: Plasmodium falciparum, class: Kinase, accessions: P62344, gene: CPK1, swissprot: CDPK1_PLAF7 Midostaurin is a small molecule that inhibits multiple receptor tyrosine kinases. In vitro biochemical or cellular assays have shown that midostaurin or its major human active metabolites CGP62221 and CGP52421 inhibit the activity of wild type FLT3, FLT3 mutant kinases (ITD and TKD), KIT (wild type and D816V mutant), PDGFR-alfa/beta, VEGFR2, as well as members of the serine/threonine kinase PKC (protein kinase C) family. Midostaurin demonstrated the ability to inhibit FLT3 receptor signaling and cell proliferation, and it induced apoptosis in leukemic cells expressing ITD and TKD mutant FLT3 receptors or overexpressing wild type FLT3 and PDGF receptors. Midostaurin also demonstrated the ability to inhibit KIT signaling, cell proliferation and histamine release and induce apoptosis in mast cells. antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) Kinase Inhibitor (Code: N0000175605) Receptor Tyrosine Kinase Inhibitors (Code: N0000020000) 2017-04-28 FDA 2K2
Click to view macimorelin Growth hormone secretagogue receptor type 1 (Organism: Homo sapiens, class: GPCR, accessions: Q92847, gene: GHSR, swissprot: GHSR_HUMAN) agonist (Source: ) Macimorelin stimulates GH release by activating growth hormone secretagogue receptors present in the pituitary and hypothalamus. Growth Hormone Secretagogue Receptor Agonist (Code: N0000193785) Growth Hormone Secretagogue Receptor Agonists (Code: N0000193786) 2017-12-20 FDA
Click to view baricitinib Tyrosine-protein kinase JAK1 (Organism: Homo sapiens, class: Kinase, accessions: P23458, gene: JAK1, swissprot: JAK1_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004085/WC500223723.pdf) Tyrosine-protein kinase JAK2 (Organism: Homo sapiens, class: Kinase, accessions: O60674, gene: JAK2, swissprot: JAK2_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004085/WC500223723.pdf) Non-receptor tyrosine-protein kinase TYK2 (Organism: Homo sapiens, class: Kinase, accessions: P29597, gene: TYK2, swissprot: TYK2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20363976) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf) Baricitinib is a selective and reversible inhibitor of Janus kinase (JAK)1 and JAK2. Janus kinases (JAKs) are enzymes that transduce intracellular signals from cell surface receptors for a number of cytokines and growth factors involved in haematopoiesis, inflammation and immune function. Within the intracellular signalling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs), which activate gene expression within the cell. Baricitinib modulates these signalling pathways by partially inhibiting JAK1 and JAK2 enzymatic activity, thereby reducing the phosphorylation and activation of STATs. Baricitinib is indicated for the treatment of moderate to severe active rheumatoid arthritis in adult patients who have responded inadequately to, or who are intolerant to one or more disease-modifying anti-rheumatic drugs as monotherapy or in combination with methotrexate. 2017-02-13 EMA 3JW
Click to view rucaparib Poly [ADP-ribose] polymerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P09874, gene: PARP1, swissprot: PARP1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/209115s000lbl.pdf) Poly [ADP-ribose] polymerase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UGN5, gene: PARP2, swissprot: PARP2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/209115s000lbl.pdf) Poly [ADP-ribose] polymerase 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y6F1, gene: PARP3, swissprot: PARP3_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/209115s000lbl.pdf) Poly [ADP-ribose] polymerase 4 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UKK3, gene: PARP4, swissprot: PARP4_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Tankyrase-1 (Organism: Homo sapiens, class: Enzyme, accessions: O95271, gene: TNKS, swissprot: TNKS1_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Tankyrase-2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9H2K2, gene: TNKS2, swissprot: TNKS2_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Poly [ADP-ribose] polymerase 10 (Organism: Homo sapiens, class: Enzyme, accessions: Q53GL7, gene: PARP10, swissprot: PAR10_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Poly [ADP-ribose] polymerase 12 (Organism: Homo sapiens, class: Enzyme, accessions: Q9H0J9, gene: PARP12, swissprot: PAR12_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Poly [ADP-ribose] polymerase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q460N5, gene: PARP14, swissprot: PAR14_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Poly [ADP-ribose] polymerase 15 (Organism: Homo sapiens, class: Enzyme, accessions: Q460N3, gene: PARP15, swissprot: PAR15_HUMAN) inhibitor (Source: http://dx.doi.org/10.1021/acs.jmedchem.6b00990) Rucaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP-1, PARP-2, and PARP-3, which play a role in DNA repair. In vitro studies have shown that rucaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. Increased rucaparib-induced cytotoxicity was observed in tumor cell lines with deficiencies in BRCA1/2 and other DNA repair genes. Rucaparib has been shown to decrease tumor growth in mouse xenograft models of human cancer with or without deficiencies in BRCA. Poly(ADP-Ribose) Polymerase Inhibitor (Code: N0000191623) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Poly(ADP-ribose) Polymerase Inhibitors (Code: D000067856) 2016-12-19 FDA RPB
Click to view icotinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22088449) Icotinib is a new epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that developed and used in China for the treatment of patients with non-small cell lung cancer (NSCLC). 2011 China Food and Drug Administration (CFDA)
Click to view olmutinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/27357069) Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4835877/pdf/13075_2016_Article_988.pdf) Olmutinib is an oral, third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) for the treatment of non-small cell lung cancer (NSCLC). Third-generation EGFR TKIs with covalent binding to the receptors demonstrate irreversible enzymatic inhibition of activating EGFR mutations and T790M mutation (a common reason for acquired EGFR TKI resistance), while sparing wild-type EGFR. 2016-05 Korean Food and Drug Administration (KFDA)
Click to view crisaborole Phosphodiesterase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27815|Q07343|Q08493|Q08499, gene: PDE4A|PDE4B|PDE4C|PDE4D, swissprot: PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/207695s000lbl.pdf) High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A (Organism: Homo sapiens, class: Enzyme, accessions: Q13946, gene: PDE7A, swissprot: PDE7A_HUMAN) inhibitor (Source: https://doi.org/10.1016/j.bmcl.2009.03.007) Crisaborole is a phosphodiesterase 4 (PDE-4) inhibitor. PDE-4 inhibition results in increased intracellular cyclic adenosine monophosphate (cAMP) levels. The specific mechanism(s) by which crisaborole exerts its therapeutic action for the treatment of atopic dermatitis is not well defined. antipsoriatic (Code: CHEBI:50748) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Phosphodiesterase 4 Inhibitor (Code: N0000182961) Phosphodiesterase 4 Inhibitors (Code: N0000182960) 2016-12-14 FDA
Click to view radotinib Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/25676420) Radotinib is a second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration, radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed in Philadelphia chromosome-positive chronic myeloid leukemia (CML) cells. In addition, this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction pathways. The inhibitory effect of radotinib on these specific tyrosine kinases may decrease cellular proliferation and inhibit angiogenesis. This agent has shown potent efficacy in CML cells that are resistant to the first-generation standard tyrosine kinase inhibitors, such as imatinib, nilotinib and dasatinib. Radotinib is used as a second-line Chronic Myeloid Leukemia treatment. 2012-01-05 Korean Food and Drug Administration (KFDA)
Click to view lifitegrast Integrin alpha-L/beta-2 (Organism: Homo sapiens, class: Adhesion, accessions: P05107|P20701, gene: ITGAL|ITGB2, swissprot: ITAL_HUMAN|ITB2_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208073s000lbl.pdf) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208073Orig1s000ClinPharmR.pdf) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208073Orig1s000ClinPharmR.pdf) Lifitegrast is a lymphocyte function-associated antigen-1 ( LFA-1) antagonist, blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule-1 (ICAM-1), LFA-1/ICAM-1 interaction can contribute to the formation of an immunological synapse resulting in T-cell activation and migration to target tissues. Lifitegrast is used as an ophthalmic solution for the treatment of the signs and symptoms of dry eye disease. anti-inflammatory drug (Code: CHEBI:35472) Lymphocyte Function-Associated Antigen-1 Antagonist (Code: N0000192701) Lymphocyte Function-Associated Antigen-1 Antagonists (Code: N0000192700) Ophthalmic Solutions (Code: D009883) Pharmaceutical Solutions (Code: D019999) 2016-07-11 FDA
Click to view pemafibrate Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/17553678) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/17553678) Peroxisome proliferator-activated receptor delta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q03181, gene: PPARD, swissprot: PPARD_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/17553678) Pemafibrate is a selective PPAR-alpha modulator (SPPARM-alpha) that has antihyperlipidaemic activity. 2017-07-03 PMDA
Click to view zabofloxacin Zabofloxacin is a fluoroquinolone antibiotic with enhanced in-vitro activity against Streptococcus pneumoniae, including strains resistant to other antibiotics. The spectrum of activity of Zabofloxacin includes those bacterial strains that are responsible for most community-acquired respiratory infections. 2015-03-20 Korean Food and Drug Administration (KFDA)
Click to view imrecoxib Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/15210067) Imrecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor indicated for treatment of osteoarthritis. 2011-05-20 China Food and Drug Administration (CFDA)
Click to view enasidenib Isocitrate dehydrogenase [NADP], mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P48735, gene: IDH2, swissprot: IDHP_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209606s000lbl.pdf) Enasidenib is a small molecule inhibitor of the isocitrate dehydrogenase 2 (IDH2) enzyme. Enasidenib targets the mutant IDH2 variants R140Q, R172S, and R172K at approximately 40-fold lower concentrations than the wild-type enzyme in vitro. Inhibition of the mutant IDH2 enzyme by enasidenib led to decreased 2-hydroxyglutarate (2-HG) levels and induced myeloid differentiation in vitro and in vivo in mouse xenograft models of IDH2 mutated AML. In blood samples from patients with AML with mutated IDH2, enasidenib decreased 2-HG levels, reduced blast counts and increased percentages of mature myeloid cells. Isocitrate Dehydrogenase 2 Inhibitor (Code: N0000193615) Isocitrate Dehydrogenase 2 Inhibitors (Code: N0000193614) 2017-08-01 FDA 69Q
Click to view fluciclovine (18F) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208054Orig1s000PharmR.pdf) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MDR4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208054Orig1s000PharmR.pdf) Fluciclovine (18F) is a radiotracer containing a synthetic amino acid analogue of L-leucine radiolabeled with fluorine F 18 with diagnostic imaging use. Fluciclovine (18F) transported across mammalian cell membranes by amino acid transporters, such as LAT-1 and ASCT2, which are upregulated in prostate cancer cells, but as was shown, this compound has a higher affinity for ASCT2 in comparison with other transporters. Fluciclovine (18F) is used as a radioactive diagnostic agent indicated for positron emission tomography (PET) imaging in men with suspected prostate cancer recurrence. Radioactive Diagnostic Agent (Code: N0000177914) Positron Emitting Activity (Code: N0000175869) 2016-05-27 FDA
Click to view hydrocortisone phosphate Hydrocortisone phosphate is a steroid phosphate that is the 21-O-phospho derivative of cortisol. (See: hydrocortisone) 1960-08-06 FDA
Click to view meglumine Meglumine (N-methyl-D-glucamine) is a poorly metabolized derivative of sorbitol that has regulatory acceptance as a benign excipient for drug formulation to increase aqueous solubility of lipophilic drugs and improve their absorption. Meglumine is used in the preparation of certain radiopaque media such as diatrizoate meglumine and iodipamide meglumine. Meglumine is combined as an excipient (an inert substance) not an active ingredient. Excipients are added to ensure that the shelf-life of the active ingredients can be long enough to be active until internal use. Excipients are combined also to support the active ingredients, so that the latter can be easily administered or absorbed in the body. Examples of meglumine-combined drugs are flunixin meglumine (non-steroidal anti-inflammatory drugs, used as a veterinary anti-inflammatory and analgesic) and meglumine antimoniate (antiprotozoal to treat leishmaniasis). Meglumine is used in ion-exchange resins to chelate boron ions selectively. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 1974-04-30 FDA
Click to view cefathiamidine Cefathiamidine is a beta-lactam antibiotic that exhibits a broad spectrum of bactericidal activity against gram-positive bacteria. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cefathiamidine is used for the treatment of respiratory, liver, five senses, urinary tract infections, endocarditis and sepsis. 2012-12-11 China Food and Drug Administration (CFDA)
Click to view eldecalcitol Vitamin D3 receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11473, gene: VDR, swissprot: VDR_HUMAN) agonist (Source: http://www.kegg.jp/entry/D07578) Vitamin D3 receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P13053, gene: Vdr, swissprot: VDR_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8396500?dopt=AbstractPlus) Eldecalcitol is an analog of the active form of vitamin D. Eldecalcitol has a higher affinity for serum vitamin D-binding protein (DBP), binds more weakly to vitamin D receptor, and shows lower potency in suppression of serum parathyroid hormone. Eldecalcitol has been approved for the treatment of osteoporosis. Bone Density Conservation Agents (Code: D050071) 2011-01-21 PMDA ED9
Click to view pentapiperium metilsulfate Pentapiperium metilsulfate is a synthetic quaternary ammonium anticholinergic and antisecretory agent used especially in the treatment of peptic ulcer.
Click to view pimavanserin 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) inverse agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/207318lbl.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) inverse agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/16469866) Pimavanserin is an atypical antipsychotic. Mechanism of action of pimavanserin in the treatment of hallucinations and delusions associated with Parkinson's disease psychosis is unknown. However, the effect of pimavanserin could be mediated through a combination of inverse agonist and antagonist activity at serotonin 5-HT2A receptors and to a lesser extent at serotonin 5-HT2C receptors. Pimavanserin is indicated for the treatment of hallucinations and delusions associated with Parkinson’s disease psychosis. antipsychotic agent (Code: CHEBI:35476) serotonergic antagonist (Code: CHEBI:48279) Atypical Antipsychotic (Code: N0000175430) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin 5-HT2 Receptor Agonists (Code: D058826) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Tranquilizing Agents (Code: D014149) 2016-04-29 FDA
Click to view opicapone Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/ongentys-epar-product-information_en.pdf) Opicapone is a peripheral, selective and reversible catechol-O-methyltransferase (COMT) inhibitor. In the presence of a DOPA decarboxylase inhibitor (DDCI), COMT becomes the major metabolising enzyme for levodopa, catalysing its conversion to 3-O-methyldopa (3-OMD) in the brain and periphery. In patients taking levodopa and a peripheral DDCI, such as carbidopa or benserazide, opicapone increases levodopa plasma levels thereby improving the clinical response to levodopa. Opicapone is indicated as adjunctive therapy to preparations of levodopa/ DOPA decarboxylase inhibitors (DDCI) in adult patients with Parkinson’s disease and end-of-dose motor fluctuations who cannot be stabilised on those combinations. Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Catechol O-Methyltransferase Inhibitors (Code: D065098) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) 2016-06-24 EMA
Click to view neratinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf) Receptor tyrosine-protein kinase erbB-2 (Organism: Homo sapiens, class: Kinase, accessions: P04626, gene: ERBB2, swissprot: ERBB2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf) Receptor tyrosine-protein kinase erbB-4 (Organism: Homo sapiens, class: Kinase, accessions: Q15303, gene: ERBB4, swissprot: ERBB4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf) Neratinib is a kinase inhibitor that irreversibly binds to Epidermal Growth Factor Receptor (EGFR), Human Epidermal Growth Factor Receptor 2 (HER2), and HER4. In vitro, neratinib reduces EGFR and HER2 autophosphorylation, downstream MAPK and AKT signaling pathways, and showed antitumor activity in EGFR and/or HER2 expressing carcinoma cell lines. Neratinib human metabolites M3, M6, M7 and M11 inhibited the activity of EGFR, HER2 and HER4 in vitro. In vivo, oral administration of neratinib inhibited tumor growth in mouse xenograft models with tumor cell lines expressing HER2 and EGFR. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) P-Glycoprotein Inhibitors (Code: N0000185503) 2017-07-17 FDA
Click to view venetoclax Apoptosis regulator Bcl-2 (Organism: Homo sapiens, class: Cytosolic other, accessions: P10415, gene: BCL2, swissprot: BCL2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Bcl-2-like protein 1 (Organism: Homo sapiens, class: Cytosolic other, accessions: Q07817, gene: BCL2L1, swissprot: B2CL1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/23291630) Apoptosis regulator Bcl-W (Organism: Homo sapiens, class: Cytosolic other, accessions: Q92843, gene: BCL2L2, swissprot: B2CL2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/23291630) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208573s000lbl.pdf) Venetoclax is a selective and orally bioavailable small-molecule inhibitor of BCL-2, an anti-apoptotic protein. Overexpression of BCL-2 has been demonstrated in CLL cells where it mediates tumor cell survival and has been associated with resistance to chemotherapeutics. Venetoclax helps restore the process of apoptosis by binding directly to the BCL-2 protein, displacing pro-apoptotic proteins like BIM, triggering mitochondrial outer membrane permeabilization and the activation of caspases. In nonclinical studies, venetoclax has demonstrated cytotoxic activity in tumor cells that overexpress BCL-2. Venetoclax is indicated for the treatment of adult patients with chronic lymphocytic leukemia or small lymphocytic lymphoma. Venetoclax also is indicated in combination with azacitidine or decitabine or low-dose cytarabine for the treatment of newly-diagnosed acute myeloid leukemia in adults who are age 75 years or older, or who have comorbidities that preclude use of intensive induction chemotherapy. antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) BCL-2 Inhibitor (Code: N0000192515) Increased Cellular Death (Code: N0000009176) P-Glycoprotein Inhibitors (Code: N0000185503) 2016-04-11 FDA
Click to view brivaracetam Synaptic vesicle glycoprotein 2A (Organism: Homo sapiens, class: Transporter, accessions: Q7L0J3, gene: SV2A, swissprot: SV2A_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf) Epoxide hydrolase 1 (Organism: Homo sapiens, class: Unclassified, accessions: P07099, gene: EPHX1, swissprot: HYEP_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf) Brivaracetam displays a high and selective affinity for synaptic vesicle protein 2A (SV2A) in the brain, which may contribute to the anticonvulsant effect. Brivaracetam is indicated for the treatment of partial-onset seizures in patients 4 years of age and older. anticonvulsant (Code: CHEBI:35623) Epoxide Hydrolase Inhibitors (Code: N0000192345) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 2016-01-14 EMA
Click to view bictegravir Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q7ZJM1, gene: pol, swissprot: Q7ZJM1_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209360s000lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210251s000lbl.pdf) Bictegravir inhibits the strand transfer activity of HIV-1 integrase (integrase strand transfer inhibitor; INSTI), an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the integration of linear HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the virus. 2018-02-07 FDA
Click to view tezacaftor Cystic fibrosis transmembrane conductance regulator (Organism: Homo sapiens, class: Ion channel, accessions: P13569, gene: CFTR, swissprot: CFTR_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210491lbl.pdf) Tezacaftor facilitates the cellular processing and trafficking of normal and select mutant forms of CFTR (including F508del-CFTR) to increase the amount of mature CFTR protein delivered to the cell surface. 2018-02-12 FDA
Click to view etelcalcetide Extracellular calcium-sensing receptor (Organism: Homo sapiens, class: GPCR, accessions: P41180, gene: CASR, swissprot: CASR_HUMAN) agonist (Source: https://www.ema.europa.eu/documents/product-information/parsabiv-epar-product-information_en.pdf) Etelcalcetide is a synthetic peptide calcimimetic agent which reduces parathyroid hormone (PTH) secretion through binding and activation of the calcium-sensing receptor. The reduction in PTH is associated with a concomitant decrease in serum calcium and phosphate levels. Etelcalcetide was approved for the treatment of secondary hyperparathyroidism in adult patients with chronic kidney disease on hemodialysis. Calcium-sensing Receptor Agonist (Code: N0000175902) Increased Calcium-sensing Receptor Sensitivity (Code: N0000020081) 2016-11-11 EMA
Click to view mepiprazole Mepiprazole is a psychotropic drug exhibiting effects on the uptake and retention of monoamines. It is a pyrazolyl-alkyl-piperazine derivative. Mepiprazole mediates a weak inhibitory action on the uptake of 5-HT on hypothalamic neurons. Mepiprazole is marketed for the treatment of anxiety neuroses.
Click to view lorpiprazole Lorpiprazole is a serotonin antagonist and reuptake inhibitor used for the treatment of major depressive disorder.
Click to view elobixibat Ileal sodium/bile acid cotransporter (Organism: Homo sapiens, class: Transporter, accessions: Q12908, gene: SLC10A2, swissprot: NTCP2_HUMAN) inhibitor (Source: http://dx.doi.org/10.1016/S0016-5085(10)61017-7) Elobixibat is an ileal bile acid transporter inhibitor. By inhibiting the uptake of bile acids, elobixibat increases the bile acid concentration in the gut, and this accelerates intestinal passage and softens the stool. It is used for the treatment of chronic constipation. 2018-01-19 PMDA
Click to view apalutamide Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210951s000lbl.pdf) Apalutamide is an Androgen Receptor (AR) inhibitor that binds directly to the ligand-binding domain of the AR. Apalutamide inhibits AR nuclear translocation, inhibits DNA binding, and impedes AR-mediated transcription. A major metabolite, N-desmethyl apalutamide, is a less potent inhibitor of AR, and exhibited one-third the activity of apalutamide in an in vitro transcriptional reporter assay. Apalutamide is indicated for the treatment of patients with metastatic castration-sensitive or non-metastatic castration-resistant prostate cancer. 2018-02-14 FDA
Click to view velpatasvir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 2a (isolate JFH-1), class: Polyprotein, accessions: Q99IB8, gene: None, swissprot: POLG_HCVJF) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 4a (isolate ED43), class: Polyprotein, accessions: O39929, gene: None, swissprot: POLG_HCVED) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 3a (isolate k3a) (HCV), class: Polyprotein, accessions: Q81495, gene: None, swissprot: POLG_HCVK3) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 2b (isolate JPUT971017) (HCV), class: Polyprotein, accessions: Q9DHD6, gene: None, swissprot: POLG_HCVJP) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 5a (isolate SA13) (HCV), class: Polyprotein, accessions: O91936, gene: None, swissprot: POLG_HCVSA) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 6a (isolate 6a33) (HCV), class: Polyprotein, accessions: Q5I2N3, gene: None, swissprot: POLG_HCV6A) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208341s000lbl.pdf) pan-genotypic NS5A inhibitor for the treatment of chronic genotype 1-6 hepatitis C virus (HCV) infection antiviral drug (Code: CHEBI:36044) Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) P-Glycoprotein Inhibitors (Code: N0000185503) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Organic Anion Transporting Polypeptide 2B1 Inhibitors (Code: N0000190109) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2016-06-28 FDA
Click to view monoxerutin Monoxerutin is a flavonol which has antioxidant properties. It is used for the treatment of varicose veins and chronic venous insufficiency.
Click to view oxiglutatione Glutathione reductase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P00390, gene: GSR, swissprot: GSHR_HUMAN) (Source: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f69655c5-cf32-6461-e00e-3a5c4a761344) A GLUTATHIONE dimer formed by a disulfide bond between the cysteine sulfhydryl side chains during the course of being oxidized. 2008-07-24 FDA GDS
Click to view elbasvir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 4a (isolate ED43), class: Polyprotein, accessions: O39929, gene: None, swissprot: POLG_HCVED) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Multidrug resistance protein 1 (Organism:Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) inhibits NS5A protein of hepatitis C virus antiviral drug (Code: CHEBI:36044) hepatoprotective agent (Code: CHEBI:62868) Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2016-01-28 FDA
Click to view etimicin Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 2014-09-15 China Food and Drug Administration (CFDA)
Click to view obeticholic acid Bile acid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q96RI1, gene: NR1H4, swissprot: NR1H4_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/207999s000lbl.pdf) obeticholic acid is an agonist for FXR, a nuclear receptor expressed in the liver and intestine hepatoprotective agent (Code: CHEBI:62868) Farnesoid X Receptor Agonist (Code: N0000192561) Farnesoid X Receptor Agonists (Code: N0000192560) 2016-05-27 FDA CHC
Click to view grazoprevir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 4a (isolate ED43), class: Polyprotein, accessions: O39929, gene: None, swissprot: POLG_HCVED) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Multidrug resistance protein 1 (Organism:Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208261Orig1s000lbl.pdf) Grazoprevir is a direct acting antiviral medication used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus antiviral drug (Code: CHEBI:36044) hepatoprotective agent (Code: CHEBI:62868) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2016-01-28 FDA SUE
Click to view climbazole Climbazole is a conazole fungicide. It is also use in shampoo and cleaner as an anti-dandruff agents and anti-bacteria agent.
Click to view trenbolone hexahydrobenzylcarbonate Trenbolone hexahydrobenzylcarbonate is a synthetic anabolic-androgenic steroid. It is a prodrug of trenbolone. Trenbolone hexahydrobenzylcarbonate was voluntarily discontinued by its manufacturer in 1997.
Click to view ixazomib Proteasome subunit beta type-5 (Organism: Homo sapiens, class: Enzyme, accessions: P28074, gene: PSMB5, swissprot: PSB5_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208462lbl.pdf) Proteasome subunit beta type-2 (Organism: Homo sapiens, class: Enzyme, accessions: P49721, gene: PSMB2, swissprot: PSB2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20160034) Proteasome subunit beta type-1 (Organism: Homo sapiens, class: Enzyme, accessions: P20618, gene: PSMB1, swissprot: PSB1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20160034) Ixazomib is a small molecule proteasome inhibitor that is used in combination with other antineoplastic agents to treat refractory multiple myeloma. orphan drug (Code: CHEBI:71031) proteasome inhibitor (Code: CHEBI:52726) antineoplastic agent (Code: CHEBI:35610) Proteasome Inhibitors (Code: N0000175075) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 2015-11-20 FDA 6V8
Click to view alfadolone acetate Alfadolone acetate is a neuroactive steroid and general anesthetic. It was often used in combination with alfaxalobe as intravenous anesthetic.
Click to view cobimetinib Dual specificity mitogen-activated protein kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q02750, gene: MAP2K1, swissprot: MP2K1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206192s000lbl.pdf) Dual specificity mitogen-activated protein kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P36507, gene: MAP2K2, swissprot: MP2K2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206192s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26384788) Cobimetinib is a reversible inhibitor of mitogen-activated protein kinase (MAPK)/extracellular signal regulated kinase 1 (MEK1) and MEK2. MEK proteins are upstream regulators of the extracellular signal-related kinase (ERK) pathway, which promotes cellular proliferation. BRAF V600E and K mutations result in constitutive activation of the BRAF pathway which includes MEK1 and MEK2. In mice implanted with tumor cell lines expressing BRAF V600E, cobimetinib inhibited tumor cell growth. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) 2015-11-10 FDA EUI
Click to view saroglitazar Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/26171220) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/26171220) Saroglitazar is a dual peroxisome proliferator-activated receptor (PPAR) agonist indicated for the treatment of hypertriglyceridemia in Type II diabetics. hypoglycemic agent (Code: CHEBI:35526) 2013-02-25 CDSCO (INDIA)
Click to view pitolisant Histamine H3 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5N1, gene: HRH3, swissprot: HRH3_HUMAN) inverse agonist (Source: https://www.ema.europa.eu/documents/product-information/wakix-epar-product-information_en.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/wakix-epar-product-information_en.pdf) Pitolisant is a potent, orally active histamine H3-receptor antagonist/inverse agonist which, via its blockade of histamine auto-receptors enhances the activity of brain histaminergic neurons, a major arousal system with widespread projections to the whole brain. Pitolisant also modulates various neurotransmitter systems, increasing acetylcholine, noradrenaline and dopamine release in the brain. 2016-03-31 EMA
Click to view flibanserin 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022526lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022526lbl.pdf) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022526lbl.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022526lbl.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022526lbl.pdf) a serotonin receptor modulator with high affinity for the following serotonin (5-hydroxytryptamine or 5-T) receptors: agonist activity at 5-HT1A and antagonist activity at 5-HT2A. Flibanserin also has moderate antagonist activities at the 5-HT2B, 5-HT2C, and dopamine D4 receptors, used in the treatment of premenopausal women with hypoactive sexual desire disorder serotonergic agonist (Code: CHEBI:35941) serotonergic antagonist (Code: CHEBI:48279) antidepressant (Code: CHEBI:35469) P-Glycoprotein Inhibitors (Code: N0000185503) 2015-08-18 FDA
Click to view trelagliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26115728) Trelagliptin is an orally active dipeptidyl peptidase (DPP)-4 inhibitor developed by Takeda and approved in Japan for the treatment of type 2 diabetes mellitus. 2015-03-26 PMDA 6RL
Click to view gluconolactone Gluconolactone is a naturally occurring polyhydroxy acid (PHA) with metal chelating, moisturizing and antioxidant activity. Gluconolactone can be produced by enzymatic oxidation of D-glucose oxidation. Its ability in free radicals scavenging accounts for its antioxidant property. It is used in cosmetic product and as a coagulant in tofu processing. Gluconolactone is also used for skin protection from some of the damaging effects of UV radiation. Gluconolactone in combination with Citric Acid and Magnesium Carbonate is indicated for dissolution of bladder calculi of the struvite or apatite variety by local intermittent irrigation and for prevention encrustations of indwelling urethral catheters and cystostomy tubes. Calculi Dissolution Agent (Code: N0000175835) Irrigation (Code: N0000175534) 1990-10-02 FDA LGC
Click to view angiotensin II Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209360s000lbl.pdf) Type-2 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P50052, gene: AGTR2, swissprot: AGTR2_HUMAN) agonist (Source: ) Angiotensin II is a naturally occurring peptide hormone of the renin-angiotensin-aldosterone system (RAAS) that causes vasoconstriction and an increase in blood pressure. Angiotensin II raises blood pressure by vasoconstriction and increased aldosterone release. Direct action of angiotensin II on the vessel wall is mediated by binding to the G-protein-coupled angiotensin II receptor type 1 on vascular smooth muscle cells, which stimulates Ca2+/calmodulin-dependent phosphorylation of myosin and causes smooth muscle contraction. Vasoconstrictor (Code: N0000192562) Vasoconstriction (Code: N0000009908) Cardiovascular Agents (Code: D002317) Vasoconstrictor Agents (Code: D014662) 2017-12-21 FDA
Click to view faropenem medoxil Faropenem medoxomil is a prodrug of faropenem, the first oral penem-type antibiotic. (See: faropenem)
Click to view UREA C14 Urease (Organism: Helicobacter pylori, class: Enzyme, accessions: Q8KT33, gene: ureB, swissprot: Q8KT33_HELPY) substrate (Source: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=13148b04-9295-41bb-bd8b-76dbd4ce7c00) Urea 14C is a urea molecule radiolabelled with a radioactive carbon-14. To detect H. pylori, urea labeled with 14C is swallowed by the patient. If gastric urease from H. pylori is present, urea is split to form CO2 and NH3 at the interface between the gastric epithelium and lumen and 14CO2 is absorbed into the blood and exhaled in the breath. It is currently used for the Urea Breath Test (UBT) and is available as a rapid diagnostic test (marketed as PyTest) for the detection of Helicobacter pylori infections. 1997-05-09 FDA URE
Click to view copanlisib Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Organism: Homo sapiens, class: Kinase, accessions: P42336, gene: PIK3CA, swissprot: PK3CA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209936s000lbl.pdf) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Organism: Homo sapiens, class: Kinase, accessions: O00329, gene: PIK3CD, swissprot: PK3CD_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209936s000lbl.pdf) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (Organism: Homo sapiens, class: Kinase, accessions: P42338, gene: PIK3CB, swissprot: PK3CB_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24170767) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Organism: Homo sapiens, class: Kinase, accessions: P48736, gene: PIK3CG, swissprot: PK3CG_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24170767) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209936s000lbl.pdf) Copanlisib is an inhibitor of phosphatidylinositol-3-kinase (PI3K) with inhibitory activity predominantly against PI3K-alpha and PI3K-delta isoforms expressed in malignant B cells. Copanlisib has been shown to induce tumor cell death by apoptosis and inhibition of proliferation of primary malignant B cell lines. Copanlisib inhibits several key cell-signaling pathways, including B-cell receptor (BCR) signaling, CXCR12 mediated chemotaxis of malignant B cells, and NFkB signaling in lymphoma cell lines. Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) 2017-09-14 FDA 6E2
Click to view sacubitril Neprilysin (Organism: Homo sapiens, class: Enzyme, accessions: P08473, gene: MME, swissprot: NEP_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207620Orig1s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207620Orig1s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207620Orig1s000lbl.pdf) inhibits neprilysin (neutral endopeptidase; NEP) via LBQ657, the active metabolite of the prodrug sacubitril and leads to increased levels of peptides that are degraded by neprilysin such as natriuretic peptides 2015-07-07 FDA
Click to view rolapitant Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206500s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206500s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206500s000lbl.pdf) An orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life. antiemetic (Code: CHEBI:50919) Neurokinin 1 Antagonists (Code: N0000010262) Substance P/Neurokinin-1 Receptor Antagonist (Code: N0000175786) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) P-Glycoprotein Inhibitors (Code: N0000185503) 2015-09-01 FDA
Click to view uridine triacetate Uridine triacetate is an acetylated pro-drug of uridine. Following oral administration, uridine triacetate is deacetylated by nonspecific esterases present throughout the body, yielding uridine in the systemic circulation of patients with hereditary orotic aciduria who cannot synthesize adequate quantities of uridine due to a genetic defect in uridine nucleotide synthesis. prodrug (Code: CHEBI:50266) neuroprotective agent (Code: CHEBI:63726) orphan drug (Code: CHEBI:71031) Pyrimidine Analog (Code: N0000191809) Pyrimidines (Code: N0000007587) Analogs/Derivatives (Code: N0000175452) 2015-09-04 FDA
Click to view olanexidine Olanexidine is a monobiguanide compound with bactericidal activity. 2015-07-03 PMDA
Click to view tivozanib Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004131/WC500239033.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004131/WC500239033.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004131/WC500239033.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/fotivda-epar-product-information_en.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/fotivda-epar-product-information_en.pdf) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Hepatocyte growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P08581, gene: MET, swissprot: MET_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Ephrin type-B receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P29323, gene: EPHB2, swissprot: EPHB2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Angiopoietin-1 receptor (Organism: Homo sapiens, class: Kinase, accessions: Q02763, gene: TEK, swissprot: TIE2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Insulin-like growth factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P08069, gene: IGF1R, swissprot: IGF1R_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/16982756) Tivozanib is an oral, once-daily, vascular endothelial growth factor (VEGF) tyrosine kinase inhibitor (TKI). It is a potent, selective and long half-life inhibitor of all three VEGF receptors and is designed to optimize VEGF blockade while minimizing off-target toxicities, potentially resulting in improved efficacy and minimal dose modifications. Tivozanib is indicated as first line treatment of adult patients with advanced renal cell carcinoma (RCC) and for adult patients who are VEGFR and mTOR pathway inhibitor-naive following disease progression after one prior treatment with cytokine therapy for advanced RCC. 2017-08-24 EMA
Click to view menadiol sodium diphosphate a Vitamin K derivative, it has been found to have carcinogenic potential in mammalian cells as well as cytotoxic properties. Studies involving the active metabolite of this formulation, menadione, showed oocyte toxicity in a study of mice. 1941 FDA
Click to view brexpiprazole D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/24947465) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205422s000lbl.pdf) an atypical antipsychotic the efficacy of brexpiprazole may be mediated through a combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors, and antagonist activity at serotonin 5-HT2A receptors Atypical Antipsychotic (Code: N0000175430) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) 2015-07-10 FDA
Click to view eluxadoline Kappa-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P41144, gene: OPRK1, swissprot: OPRK_CAVPO) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940s000lbl.pdf) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940s000lbl.pdf) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940s000lbl.pdf) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206940s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25491493) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25491493) Eluxadoline is a mu-opioid receptor agonist; eluxadoline is also a delta opioid receptor antagonist and a kappa opioid receptor agonist. The binding affinities (Ki) of eluxadoline for the human mu and delta opioid receptors are 1.8 nM and 430 nM, respectively. The binding affinity (Ki) of eluxadoline for the human kappa opioid receptor has not been determined; however, the Ki for guinea pig cerebellum kappa opioid receptor is 55 nM. In animals, eluxadoline interacts with opioid receptors in the gut. mu-opioid receptor agonist (Code: CHEBI:55322) delta-opioid receptor antagonist (Code: CHEBI:59283) kappa-opioid receptor agonist (Code: CHEBI:59282) gastrointestinal drug (Code: CHEBI:55324) Gastrointestinal Agents (Code: D005765) Opioid mu-Receptor Agonists (Code: N0000191866) 2015-05-27 FDA
Click to view deoxycholic acid Cell membrane (Organism: None, class: Cell membrane, accessions: None, gene: None, swissprot: None) other (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206333Orig1s000lbl.pdf) fMet-Leu-Phe receptor (Organism: Homo sapiens, class: GPCR, accessions: P21462, gene: FPR1, swissprot: FPR1_HUMAN) antagonist (Source: ) G-protein coupled bile acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDU6, gene: GPBAR1, swissprot: GPBAR_HUMAN) agonist (Source: ) Steroid Delta-isomerase (Organism: Pseudomonas putida, class: Enzyme, accessions: P07445, gene: ksi, swissprot: SDIS_PSEPU) (Source: https://www.ncbi.nlm.nih.gov/pubmed/?term=11007792) Choloylglycine hydrolase (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: P54965, gene: cbh, swissprot: CBH_CLOPE) (Source: https://www.ncbi.nlm.nih.gov/pubmed/?term=15823032) Lactaldehyde dehydrogenase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P25553, gene: aldA, swissprot: ALDA_ECOLI) (Source: https://www.rcsb.org/structure/2OPX) Troponin C, slow skeletal and cardiac muscles (Organism: Homo sapiens, class: Cytosolic other, accessions: P63316, gene: TNNC1, swissprot: TNNC1_HUMAN) (Source: https://www.ncbi.nlm.nih.gov/pubmed/?term=21920370) Protein PrgI (Organism: Salmonella typhimurium (strain LT2 / SGSC1412 / ATCC 700720), class: Transporter, accessions: P41784, gene: prgI, swissprot: PRGI_SALTY) (Source: https://www.ncbi.nlm.nih.gov/pubmed/?term=21829362) Multidrug efflux pump subunit AcrB (Organism: Escherichia coli (strain K12), class: Transporter, accessions: P31224, gene: acrB, swissprot: ACRB_ECOLI) (Source: https://www.ncbi.nlm.nih.gov/pubmed/?term=19023693) A bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent. Cytolytic Agent (Code: N0000191548) Decreased Cell Membrane Integrity (Code: N0000008476) Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765) 2015-04-29 FDA DXC
Click to view triamcinolone hexacetonide Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/016466s046lbl.pdf) synthetic glucocorticoid analog used for anti-inflammatory effects in disorders of many organ systems Anti-Inflammatory Agents (Code: D000893) 1969-07-29 FDA
Click to view ombitasvir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206619s003lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206619s003lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/viekirax-epar-product-information_en.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/viekirax-epar-product-information_en.pdf) an orally available inhibitor of the hepatitis C virus (HCV) non-structural protein 5A (NS5A) replication complex, with potential activity against HCV. Upon oral administration and after intracellular uptake, ombitasvir binds to and blocks the activity of the NS5A protein. This results in the disruption of the viral RNA replication complex, blockage of HCV RNA production, and inhibition of viral replication. NS5A, a zinc-binding and proline-rich hydrophilic phosphoprotein, plays a crucial role in HCV RNA replication. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family; HCV infection is associated with the development of hepatocellular carcinoma (HCC). antiviral drug (Code: CHEBI:36044) Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) UGT1A1 Inhibitors (Code: N0000191272) 2014-11-20 EMA
Click to view isavuconazonium Aspergillus fumigatus (Organism: None, class: Fungi, accessions: None, gene: None, swissprot: None) minimum inhibitory concentration (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207500Orig1s000lbl.pdf) Candida albicans (Organism: None, class: Fungi, accessions: None, gene: None, swissprot: None) minimum inhibitory concentration (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207500Orig1s000lbl.pdf) Isavuconazonium sulfate is the prodrug of isavuconazole, an azole antifungal drug. Isavuconazole inhibits the synthesis of ergosterol, a key component of the fungal cell membrane, through the inhibition of cytochrome P-450 dependent enzyme lanosterol 14-alpha-demethylase. This enzyme is responsible for the conversion of lanosterol to ergosterol. An accumulation of methylated sterol precursors and a depletion of ergosterol within the fungal cell membrane weakens the membrane structure and function. Mammalian cell demethylation is less sensitive to isavuconazole inhibition. prodrug (Code: CHEBI:50266) orphan drug (Code: CHEBI:71031) Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Organic Cation Transporter 2 Inhibitors (Code: N0000187061) P-Glycoprotein Inhibitors (Code: N0000185503) 2015-03-06 FDA
Click to view isoflupredone acetate Isoflupredone acetate is a derivative of Isoflupredone. Isoflupredone acetate belongs to the class of corticosteroids and exerts its therapeutic effect by binding to glucocorticoid and mineralocorticoid receptors. Isoflupredone acetate is ussualy used in veterinary medicine.
Click to view drofenine Transient receptor potential cation channel subfamily V member 3 (Organism: Homo sapiens, class: Ion Channel, accessions: Q8NET8, gene: TRPV3, swissprot: TRPV3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25089200) Drofenine is an atropine-like antispasmodic drug, like papaverine, that acts directly on smooth muscles to stop muscle spasms. Drofenine is used for relaxing smooth muscle, treating dysmenorrhea, and relieving pain in the gastrointestinal tract, biliary passages, and urogenital tract.
Click to view tenofovir alafenamide a phosphonoamidate prodrug of tenofovir (2'deoxyadenosine monophosphate analog). Plasma exposure to tenofovir alafenamide allows for permeation into cells and then tenofovir alafenamide is intracellularly converted to tenofovir through hydrolysis by cathepsin A. Tenofovir is subsequently phosphorylated by cellular kinases to the active metabolite tenofovir diphosphate. Tenofovir diphosphate inhibits HIV replication through incorporation into viral DNA by the HIV reverse transcriptase, which results in DNA chain-termination antiviral drug (Code: CHEBI:36044) prodrug (Code: CHEBI:50266) 2015-05-11 FDA
Click to view avibactam Beta-lactamase TEM (Organism: Escherichia coli, class: Enzyme, accessions: P62593, gene: bla; blaT-3; blaT-4;, swissprot: BLAT_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20921316) Beta-lactamase (Organism: Enterobacter cloacae, class: Enzyme, accessions: P05364, gene: ampC, swissprot: AMPC_ENTCL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20921316) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206494s005,s006lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206494s005,s006lbl.pdf) Avibactam is a non-beta-lactam beta-lactamase inhibitor that inactivates some beta-lactamases and protects ceftazidime from degradation by certain beta-lactamases. Avibactam in combination with ceftazidime is used for the treatment of complicated intra-abdominal infections (caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Enterobacter cloacae, Klebsiella oxytoca, Citrobacter freundii complex, and Pseudomonas aeruginosa), complicated urinary tract infections (caused by Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Citrobacter freundii complex, Proteus mirabilis, and Pseudomonas aeruginosa) and hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia (caused by Klebsiella pneumoniae, Enterobacter cloacae, Escherichia coli, Serratia marcescens, Proteus mirabilis, Pseudomonas aeruginosa, and Haemophilus influenzae). antibacterial drug (Code: CHEBI:36047) beta Lactamase Inhibitor (Code: N0000175930) beta Lactamase Inhibitors (Code: N0000000202) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) beta-Lactamase Inhibitors (Code: D065093) Enzyme Inhibitors (Code: D004791) 2015-02-25 FDA
Click to view daclatasvir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206843s008lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion Channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24521299) Daclatasvir is an inhibitor of hepatitis C virus nonstructural protein 5A (NS5A). Daclatasvir binds to the N-terminus of NS5A and inhibits both viral RNA replication and virion assembly. Daclatasvir is indicated for use with sofosbuvir, with or without ribavirin, for the treatment of chronic HCV genotype 1 or 3 infection. antiviral drug (Code: CHEBI:36044) Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) P-Glycoprotein Inhibitors (Code: N0000185503) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2014-09-15 EMA
Click to view palbociclib Cyclin-dependent kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P11802, gene: CDK4, swissprot: CDK4_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Cyclin-dependent kinase 6 (Organism: Homo sapiens, class: Kinase, accessions: Q00534, gene: CDK6, swissprot: CDK6_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207103s000lbl.pdf) Palbociclib is an inhibitor of cyclin-dependent kinases (CDK) 4 and 6. Cyclin D1 and CDK4/6 are downstream of signaling pathways which lead to cellular proliferation. In vitro, palbociclib reduced cellular proliferation of estrogen receptor (ER)-positive breast cancer cell lines by blocking progression of the cell from G1 into S phase of the cell cycle. Treatment of breast cancer cell lines with the combination of palbociclib and antiestrogens leads to decreased retinoblastoma (Rb) protein phosphorylation resulting in reduced E2F expression and signaling, and increased growth arrest compared to treatment with each drug alone. In vitro treatment of ER-positive breast cancer cell lines with the combination of palbociclib and antiestrogens led to increased cell senescence compared to each drug alone, which was sustained for up to 6 days following palbociclib removal and was greater if antiestrogen treatment was continued. In vivo studies using a patient-derived ER-positive breast cancer xenograft model demonstrated that the combination of palbociclib and letrozole increased the inhibition of Rb phosphorylation, downstream signaling, and tumor growth compared to each drug alone. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) Cytochrome P450 3A Inhibitors (Code: N0000190114) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2015-02-03 FDA LQQ
Click to view lenvatinib Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf1) Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Fibroblast growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P21802, gene: FGFR2, swissprot: FGFR2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Fibroblast growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P22607, gene: FGFR3, swissprot: FGFR3_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Fibroblast growth factor receptor 4 (Organism: Homo sapiens, class: Kinase, accessions: P22455, gene: FGFR4, swissprot: FGFR4_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206947s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206947s009lbl.pdf) Lenvatinib is orally available multi-kinase inhibitor and antineoplastic agent that is used in treatment of advanced, metastatic medullary thyroid cancer and refractory renal cell carcinoma. Lenvatinib is associated with a modest rate of serum enzyme elevations during treatment and has been implicated to rare instances of clinically apparent, acute liver injury some of which have been fatal. orphan drug (Code: CHEBI:71031) antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Receptor Tyrosine Kinase Inhibitors (Code: N0000020000) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2015-02-13 FDA LEV
Click to view decamethoxine Decamethoxin is a bisquaternary ammonium salt, which close to ethonium in chemical structure and antimicrobial effect. It has a wide range of antimicrobial effects on gram-positive (staphylococcus, streptococcus, pneumococcus), gram-negative (gonococcus, meningococcus) cocci, corynebacteria diphtheria, enterobacteria, pseudomonas, protozoa, dermatophytes, yeast-like fungi of the genus Candida. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 2008-10-17 Ministry of Health of the Russian Federation
Click to view finafloxacin DNA gyrase (Organism: Staphylococcus aureus subsp. aureus, class: Enzyme, accessions: P20831|P0A0K8, gene: gyrA|gyrB, swissprot: GYRA_STAAU|GYRB_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206307s000lbl.pdf) DNA gyrase (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: P48372|Q9I7C2, gene: gyrA|gyrB, swissprot: GYRA_PSEAE|GYRB_PSEAE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206307s000lbl.pdf) Topoisomerase IV (Organism: Staphylococcus aureus subsp. aureus, class: Enzyme, accessions: P0C1U9|P0C1S7, gene: parC|parE, swissprot: PARC_STAAU|PARE_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206307s000lbl.pdf) Topoisomerase IV (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: Q9HUK1|Q9HUJ8, gene: parC|parE, swissprot: PARC_PSEAE|PARE_PSEAE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206307s000lbl.pdf) Finafloxacin belongs to the fluoroquinolone class of antibacterials which involves the inhibition of bacterial type II topoisomerase enzymes, DNA gyrase and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair and recombination. antibacterial drug (Code: CHEBI:36047) Quinolone Antimicrobial (Code: N0000175937) Quinolones (Code: N0000007606) 2014-12-17 FDA
Click to view safinamide Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/207145lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/207145lbl.pdf) Safinamide acts through both dopaminergic and non-dopaminergic mechanisms of action. Safinamide is a highly selective and reversible MAO-B inhibitor causing an increase in extracellular levels of dopamine in the striatum. Safinamide is associated with state-dependent inhibition of voltage-gated sodium (Na+) channels, and modulation of stimulated release of glutamate. To what extent the nondopaminergic effects contribute to the overall effect has not been established. Monoamine Oxidase Type B Inhibitor (Code: N0000175762) Monoamine Oxidase-B Inhibitors (Code: N0000175761) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2014-03-30 EMA
Click to view ceftolozane Peptidoglycan D,D-transpeptidase FtsI (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD68, gene: ftsI, swissprot: FTSI_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206829lbl.pdf) Peptidoglycan D,D-transpeptidase FtsI (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: Q51504, gene: pbpB, swissprot: Q51504_PSEAI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206829lbl.pdf) Penicillin-binding protein 1B (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: Q9X6W0, gene: ponB, swissprot: Q9X6W0_PSEAI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/206829lbl.pdf) Ceftolozane belongs to the cephalosporin class of antibacterial drugs. The bactericidal action of ceftolozane results from inhibition of cell wall biosynthesis, and is mediated through binding to penicillin-binding proteins (PBPs). Ceftolozane is an inhibitor of PBPs of P. aeruginosa (e.g., PBP1b, PBP1c, and PBP3) and E. coli (e.g., PBP3). Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) 2014-12-19 FDA
Click to view acotiamide Acetylcholinesterase (Organism: Rattus norvegicus (Rat), class: Enzyme, accessions: P37136, gene: Ache, swissprot: ACES_RAT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21651906) A prokinetic agent with gastrointestinal (GI) motility-enhancing activity. Although the exact mechanism by which acotiamide exerts its effect has yet to be fully elucidated, this agent appears to inhibit acetylcholinesterase (AchE), an enzyme responsible for the breakdown of acetylcholine (Ach). Increased Ach concentrations lead to an improvement of gastric emptying and GI motility and eventually to a reduction of dyspepsia symptoms. 2013-03-25 PMDA
Click to view felypressin Vasopressin V1a receptor (Organism: Homo sapiens, class: GPCR, accessions: P37288, gene: AVPR1A, swissprot: V1AR_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/18655903) A synthetic analog of LYPRESSIN with a PHENYLALANINE substitution at residue 2. Felypressin is a vasoconstrictor with reduced antidiuretic activity. vasoconstrictor agent (Code: CHEBI:50514) vasopressin receptor agonist (Code: CHEBI:59727) Cardiovascular Agents (Code: D002317) Vasoconstrictor Agents (Code: D014662) 1969-12-31 New Zealand Medicines and Medical Devices Safety Authority
Click to view netupitant Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205718s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205718s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205718s000lbl.pdf) a selective antagonist of human substance P/neurokinin 1 (NK1) receptors, inhibits substance P mediated emesis responses antiemetic (Code: CHEBI:50919) Neurokinin 1 Antagonists (Code: N0000010262) Substance P/Neurokinin-1 Receptor Antagonist (Code: N0000175786) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) P-Glycoprotein Inhibitors (Code: N0000185503) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2014-10-10 FDA
Click to view ledipasvir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205834s000lbl.pdf) Ledipasvir is an inhibitor of the Hepatitis C Virus (HCV) NS5A protein required for viral RNA replication and assembly of HCV virions. Ledipasvir is indicated in combination with sofosbuvir for the treatment of HCV genotype 1 with or without cirrhosis. antiviral drug (Code: CHEBI:36044) Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) P-Glycoprotein Inhibitors (Code: N0000185503) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2014-10-10 FDA
Click to view diquafosol P2Y purinoceptor 2 (Organism: Homo sapiens, class: GPCR, accessions: P41231, gene: P2RY2, swissprot: P2RY2_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/18232657) P2Y purinoceptor 6 (Organism: Homo sapiens, class: GPCR, accessions: Q15077, gene: P2RY6, swissprot: P2RY6_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22107038) Diquafosol is an agonist for purinergic P2Y2 receptor. Diquafosol stimulated water and mucin secretion by acting on the conjunctival epithelial and goblet cell membrane and elevating intracellular calcium ion concentrations. Diquafosol is approved for the treatment of dry eye. 2010-02-26 PMDA
Click to view belinostat Histone deacetylase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P56524, gene: HDAC4, swissprot: HDAC4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/12939461) Histone deacetylase 10 (Organism: Homo sapiens, class: Enzyme, accessions: Q969S8, gene: HDAC10, swissprot: HDA10_HUMAN) inhibitor (Source: ) Histone deacetylase 11 (Organism: Homo sapiens, class: Enzyme, accessions: Q96DB2, gene: HDAC11, swissprot: HDA11_HUMAN) inhibitor (Source: ) Histone deacetylase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BY41, gene: HDAC8, swissprot: HDAC8_HUMAN) inhibitor (Source: ) Histone deacetylase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UKV0, gene: HDAC9, swissprot: HDAC9_HUMAN) inhibitor (Source: ) Histone deacetylase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBN7, gene: HDAC6, swissprot: HDAC6_HUMAN) inhibitor (Source: ) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: ) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) inhibitor (Source: ) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: ) Histone deacetylase 5 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UQL6, gene: HDAC5, swissprot: HDAC5_HUMAN) inhibitor (Source: ) Histone deacetylase 7 (Organism: Homo sapiens, class: Enzyme, accessions: Q8WUI4, gene: HDAC7, swissprot: HDAC7_HUMAN) inhibitor (Source: ) Belinostat is a hydroxamate-type histone deacetylase inhibitor. Belinostat causes the accumulation of acetylated histones and other proteins, inducing cell cycle arrest and/or apoptosis of some transformed cells. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase. Belinostat is indicated for the treatment of relapsed or refractory peripheal T-cell lymphoma. antineoplastic agent (Code: CHEBI:35610) Histone Deacetylase Inhibitor (Code: N0000175588) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Histone Deacetylase Inhibitors (Code: D056572) 2014-07-03 FDA 5OG
Click to view imidafenacin Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17396619) Muscarinic acetylcholine receptor M3 (Organism: Rattus norvegicus, class: GPCR, accessions: P10980, gene: Chrm3, swissprot: ACM3_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17396619) Muscarinic acetylcholine receptor M2 (Organism: Rattus norvegicus, class: GPCR, accessions: P08483, gene: Chrm2, swissprot: ACM2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17396619) Imidafenacin antagonizes subtypes M3 and M1 in vitro. In the urinary bladder, imidafenacin inhibits acetylcholine release by antagonizing subtype M1 and contraction of smooth muscles by antagonizing subtype M3. 2007-04-18 PMDA
Click to view nintedanib Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Fibroblast growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P21802, gene: FGFR2, swissprot: FGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Fibroblast growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P22607, gene: FGFR3, swissprot: FGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Tyrosine-protein kinase Lyn (Organism: Homo sapiens, class: Kinase, accessions: P07948, gene: LYN, swissprot: LYN_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/205832s000lbl.pdf) Nintedanib is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Nintedanib is a drug indicated for the treatment of idiopathic pulmonary fibrosis (IPF). antineoplastic agent (Code: CHEBI:35610) angiogenesis inhibitor (Code: CHEBI:48422) Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) 2014-10-15 FDA XIN
Click to view cetilistat Pancreatic triacylglycerol lipase (Organism: Homo sapiens, class: Enzyme, accessions: P16233, gene: PNLIP, swissprot: LIPP_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/18500680) Cetilistat is a pancreatic lipase inhibitor. Cetilistat is used for the treatment of obesity in patients with or without diabetes. Anti-Obesity Agents (Code: D019440) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Lipid Regulating Agents (Code: D057847) 2013-09-20 PMDA
Click to view efinaconazole Lanosterol 14-alpha demethylase (Organism: Trichophyton rubrum, class: Enzyme, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/203567s000lbl.pdf) Lanosterol 14-alpha demethylase (Organism: Trichophyton mentagrophytes, class: Enzyme, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/203567s000lbl.pdf) Efinaconazole is an azole antifungal. Efinaconazole inhibits fungal lanosterol 14-alpha demethylase involved in the biosynthesis of ergosterol, a constituent of fungal cell membranes. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 2014-06-06 FDA
Click to view favipiravir Favipiravir is an anti-viral compound with a unique mechanism of action that is active against a wide range of RNA-based viruses in laboratory tests. Favipiravir is phosphoribosylated by cellular enzymes to its active form, favipiravir-ribofuranosyl-5'- triphosphate (RTP). Favipiravir is active against a broad range of influenza viruses, including A(H1N1)pdm09, A(H5N1) and A(H7N9) avian virus. It also inhibits influenza strains resistant to current antiviral drugs, and shows a synergistic effect in combination with oseltamivir, thereby expanding influenza treatment options. In addition to its anti-influenza activity, favipiravir blocks the replication of many other RNA viruses, including arenaviruses (Junin, Machupo and Pichinde); phleboviruses (Rift Valley fever, sandfly fever and Punta Toro); hantaviruses (Maporal, Dobrava, and Prospect Hill); flaviviruses (yellow fever and West Nile); enteroviruses (polio- and rhinoviruses); an alphavirus, Western equine encephalitis virus; a paramyxovirus, respiratory syncytial virus; and noroviruses. 2014-02-03 PMDA
Click to view topiroxostat Xanthine dehydrogenase/oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P47989, gene: XDH, swissprot: XDH_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/19783139) Topiroxostat is a xanthine oxidase inhibitor. Topiroxostat could reduce the production of uric acid in the body through the inhibition of xanthine oxidase. Topiroxostat is used for the treatment of gout and hyperuricemia. Enzyme Inhibitors (Code: D004791) 2013-04-26 PMDA FYX
Click to view asunaprevir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Genome polyprotein (Organism: Hepatitis C virus genotype 2a (isolate HC-J6), class: Polyprotein, accessions: P26660, gene: None, swissprot: POLG_HCVJ6) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00037935.PDF) Asunaprevir is an inhibitor of the HCV NS3/4A serine protease complex. This NS3/4A enzyme complex is responsible for processing the HCV polyprotein to yield mature viral proteins required for viral replication. Studies in vitro demonstrated a significant antiviral activity in HCV replicon cell systems with an EC50 of 4nm and 1nm against the HCV genotype 1a and 1b respectively.2 These studies showed a limited activity against the genotypes 2 and 3. This property makes asunaprevir a highly selective anti-HCV agent that is not effective against HCV closely related virus. Asunaprevir is indicated in combination with other agents for the treatment of chronic hepatitis C in adult patients with hepatitis C virus genotypes 1 or 4 and compensated liver cirrhosis. Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 2014-06-24 PMDA 2R9
Click to view ipragliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22139434) Sodium/glucose cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P13866, gene: SLC5A1, swissprot: SC5A1_HUMAN) Sodium/glucose cotransporter 1 (Organism: Mus musculus, class: Transporter, accessions: Q8C3K6, gene: Slc5a1, swissprot: SC5A1_MOUSE) inhibitor (Source: ) Sodium/glucose cotransporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53790, gene: Slc5a1, swissprot: SC5A1_RAT) inhibitor (Source: ) Sodium/glucose cotransporter 2 (Organism: Mus musculus, class: Transporter, accessions: Q923I7, gene: Slc5a2, swissprot: SC5A2_MOUSE) inhibitor (Source: ) Sodium/glucose cotransporter 2 (Organism: Rattus norvegicus, class: Transporter, accessions: P53792, gene: Slc5a2, swissprot: SC5A2_RAT) inhibitor (Source: ) Ipragliflozin is a selective sodium-glucose cotransporter 2 (SGLT2) inhibitor approved for the treatment of type 2 diabetes mellitus. 2014-11-29 PMDA
Click to view luseogliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20302302) Sodium/glucose cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P13866, gene: SLC5A1, swissprot: SC5A1_HUMAN) Luseogliflozin is a sodium-dependent glucose cotransporter (SGLT) 2 inhibitior. Luseogliflozin exhibits a blood glucose lowering effect, excellent urinary glucose excretion properties, and promising pharmacokinetics profiles in animals. Luseogliflozin is used as monotherapy or in combination with other antihyperglycaemic agents for the treatment of patients with type 2 diabetes mellitus. 2014-03-24 PMDA
Click to view suvorexant Orexin receptor type 1 (Organism: Homo sapiens, class: GPCR, accessions: O43613, gene: HCRTR1, swissprot: OX1R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Orexin receptor type 2 (Organism: Homo sapiens, class: GPCR, accessions: O43614, gene: HCRTR2, swissprot: OX2R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204569s005lbl.pdf) Suvorexant is a selective dual antagonist of orexin receptors OX1R and OX2R that promotes sleep by reducing wakefulness and arousal. It has been approved for the treatment of insomnia. central nervous system depressant (Code: CHEBI:35488) Orexin Receptor Antagonist (Code: N0000191000) P-Glycoprotein Inhibitors (Code: N0000185503) Cytochrome P450 3A Inhibitors (Code: N0000190114) Neurotransmitter Agents (Code: D018377) Orexin Receptor Antagonists (Code: D000068796) Sleep Aids, Pharmaceutical (Code: D000068776) 2014-08-13 FDA SUV
Click to view istradefylline Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) antagonist Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN Adenosine receptor A2a (Organism: Rattus norvegicus, class: GPCR, accessions: P30543, gene: Adora2a, swissprot: AA2AR_RAT Adenosine receptor A1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25099, gene: Adora1, swissprot: AA1R_RAT Istradefylline is an adenosine A2A receptor antagonist. Istradefylline is indicated for the improvement of wearing-off phenomena in patients with Parkinson’s disease on concomitant treatment with levodopa-containing products. Adenosine A2 Receptor Antagonists (Code: D058917) Neurotransmitter Agents (Code: D018377) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P1 Receptor Antagonists (Code: D058915) 2013-03-8 PMDA
Click to view simetride Simetride is a analgesic agent indicated for low back pain, symptomatic neuralgia, headache, menstrual pain, pharyngalgia/earache due to inflammation, toothache, postoperative pain, combined with caffeine. 1965 PMDA
Click to view tedizolid phosphate Tedizolid phosphate a phosphate prodrug, is converted to tedizolid in the presence of phosphatases. The antibacterial activity of tedizolid is mediated by binding to the 50S subunit of the bacterial ribosome resulting in inhibition of protein synthesis. Tedizolid has been shown to be active against most isolates of the following bacteria: Staphylococcus aureus (including methicillin-resistant and methicillin-susceptible isolates), Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus anginosus Group (including S. anginosus, S. intermedius, and S. constellatus), Enterococcus faecalis. prodrug (Code: CHEBI:50266) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Oxazolidinone Antibacterial (Code: N0000175495) Oxazolidinones (Code: N0000007568) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2014-06-20 FDA
Click to view tavaborole Leucine--tRNA ligase, cytoplasmic (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P26637, gene: CDC60, swissprot: SYLC_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588934) Tavaborole is a boron-based pharmaceutical agent. The mechanism of action of tavaborole is inhibition of fungal protein synthesis. Tavaborole inhibits protein synthesis by inhibition of an aminoacyl-transfer ribonucleic acid (tRNA) synthetase (AARS). Tavaborole is indicated for the topical treatment of toenail onychomycosis, a fungal infection of the nail and nail bed due to Trichophyton rubrum or Trichophyton mentagrophytes infection. Oxaborole Antifungal (Code: N0000191279) Protein Synthesis Inhibitors (Code: N0000000150) Boron Compounds (Code: N0000008253) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 2014-07-07 FDA
Click to view idelalisib Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Organism: Homo sapiens, class: Kinase, accessions: O00329, gene: PIK3CD, swissprot: PK3CD_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20959606) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (Organism: Homo sapiens, class: Kinase, accessions: P48736, gene: PIK3CG, swissprot: PK3CG_HUMAN) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (Organism: Homo sapiens, class: Kinase, accessions: P42338, gene: PIK3CB, swissprot: PK3CB_HUMAN) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Organism: Homo sapiens, class: Kinase, accessions: P42336, gene: PIK3CA, swissprot: PK3CA_HUMAN) DNA-dependent protein kinase catalytic subunit (Organism: Homo sapiens, class: Kinase, accessions: P78527, gene: PRKDC, swissprot: PRKDC_HUMAN Idelalisib is an inhibitor of PI3K-delta kinase, which is expressed in normal and malignant B-cells. Idelalisib induced apoptosis and inhibited proliferation in cell lines derived from malignant B-cells and in primary tumor cells. Idelalisib inhibits several cell signaling pathways, including B-cell receptor (BCR) signaling and the CXCR4 and CXCR5 signaling, which are involved in trafficking and homing of B-cells to the lymph nodes and bone marrow. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) Cytochrome P450 3A Inhibitors (Code: N0000190114) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) 2014-07-23 FDA 40L
Click to view ataluren Ataluren is approved for the treatment of Duchenne muscular dystrophy caused by a nonsense mutation. A nonsense mutation in DNA results in a premature stop codon within an mRNA. This premature stop codon in the mRNA causes disease by terminating translation before a full-length protein is generated. Ataluren interacts with the ribosome enabling it to read through premature nonsense stop signals on mRNA and allowing the cell to produce a full-length, functional protein. 2014-07-31 EMA
Click to view mebanazine Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/5889715) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/5889715) Mebanazine is a monoamine oxidase inhibitor. Mebanazine was previously used as an antidepressant, but later was withdrawn due to hepatotoxicity.
Click to view ceritinib ALK tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: Q9UM73, gene: ALK, swissprot: ALK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Insulin-like growth factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P08069, gene: IGF1R, swissprot: IGF1R_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Proto-oncogene tyrosine-protein kinase ROS (Organism: Homo sapiens, class: Kinase, accessions: P08922, gene: ROS1, swissprot: ROS1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211225s000lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Cyclin-dependent kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P24941, gene: CDK2, swissprot: CDK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Cyclin-dependent kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P11802, gene: CDK4, swissprot: CDK4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Fibroblast growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P22607, gene: FGFR3, swissprot: FGFR3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Fibroblast growth factor receptor 4 (Organism: Homo sapiens, class: Kinase, accessions: P22455, gene: FGFR4, swissprot: FGFR4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Fibroblast growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P21802, gene: FGFR2, swissprot: FGFR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase JAK2 (Organism: Homo sapiens, class: Kinase, accessions: O60674, gene: JAK2, swissprot: JAK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase JAK1 (Organism: Homo sapiens, class: Kinase, accessions: P23458, gene: JAK1, swissprot: JAK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Hepatocyte growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P08581, gene: MET, swissprot: MET_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase Lyn (Organism: Homo sapiens, class: Kinase, accessions: P07948, gene: LYN, swissprot: LYN_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) MAP kinase-interacting serine/threonine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9HBH9, gene: MKNK2, swissprot: MKNK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase SYK (Organism: Homo sapiens, class: Kinase, accessions: P43405, gene: SYK, swissprot: KSYK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Rho-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: O75116, gene: ROCK2, swissprot: ROCK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Testis-specific serine/threonine-protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q9BXA7, gene: TSSK1B, swissprot: TSSK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Tyrosine-protein kinase ZAP-70 (Organism: Homo sapiens, class: Kinase, accessions: P43403, gene: ZAP70, swissprot: ZAP70_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23742252) Insulin receptor (Organism: Homo sapiens, class: Kinase, accessions: P06213, gene: INSR, swissprot: INSR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/23742252) Ceritinib is a kinase inhibitor. Targets of ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among these, ceritinib is most active against ALK. Ceritinib inhibited autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK-dependent cancer cells in in vitro and in vivo assays. Ceritinib is used for the treatment of ALK-positive metastatic non-small cell lung cancer. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Tyrosine Kinase Inhibitors (Code: N0000020001) Cytochrome P450 3A Inhibitors (Code: N0000190114) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2014-04-29 FDA 4MK
Click to view umifenovir Umifenovir is a small indole-derivative molecule, used for prophylaxis and treatment of influenza and other respiratory viral infections. Umifenovir is known to inhibit haemagglutinin-mediated membrane fusion events in influenza A and B virus replication. 1988-03-23 Ministry of Health of the Russian Federation 75U
Click to view furazidin Furazidine is a nitrofuran derivative, acting as an antibacterial medicine with bacteriostatic action. It is active against both gram-positive (Staphylococcus epidermidis, Staphylococcus aureus, Staphylococcus faecalis) and gram-negative microorganisms (Enterobacteriaceae – Salmonella, Shygella, Proteus, Klebsiella, Escherichia, Enterobacter, etc.). It is used for the treatment of urinary tract, skin and soft tissues infections. antibacterial drug (Code: CHEBI:36047) antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076) 2007-08-07 Ministry of Health of the Russian Federation
Click to view naloxegol Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204760s000lbl.pdf) Naloxegol is a peripherally acting opioid receptor antagonist specific for mu-opioid receptors. Naloxegol is used for the treatment of chronic noncancer pain. Opioid Antagonist (Code: N0000175691) Opioid Antagonists (Code: N0000000154) Central Nervous System Agents (Code: D002491) Narcotic Antagonists (Code: D009292) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2014-09-16 FDA
Click to view gemigliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27298192) Dipeptidyl peptidase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q86TI2, gene: DPP9, swissprot: DPP9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27298192) Dipeptidyl peptidase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q6V1X1, gene: DPP8, swissprot: DPP8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27298192) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/24304170) Gemigliptin, a novel dipeptidyl peptidase (DPP)-4 inhibitor, is approved for use as a monotherapy or in combination therapy to treat hyperglycemia in patients with type 2 diabetes mellitus. 2012-06-27 Korean Food and Drug Administration (KFDA)
Click to view eliglustat Ceramide glucosyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: Q16739, gene: UGCG, swissprot: CEGT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205494s003lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205494s003lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205494s003lbl.pdf) Eliglustat tartrate is a small molecule inhibitor of glucosylceramide synthase that resembles the ceramide substrate for the enzyme. Gaucher disease is caused by a deficiency of the lysosomal enzyme acid beta-glucosidase. Acid beta-glucosidase catalyzes the conversion of the sphingolipid glucocerebroside into glucose and ceramide. The enzymatic deficiency causes an accumulation of glucosylceramide (GL-1) primarily in the lysosomal compartment of macrophages, giving rise to foam cells or "Gaucher cells". Glucosylceramide Synthase Inhibitor (Code: N0000175783) Glucosylceramide Synthase Inhibitors (Code: N0000020019) P-Glycoprotein Inhibitors (Code: N0000185503) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Enzyme Inhibitors (Code: D004791) 2014-08-19 FDA
Click to view ethacizine Ethacizine is an antiarrhythmic. It is used for the treatment of severe or refractory ventricular and supraventricular arrhythmias, refractory tachycardia associated with Wolff–Parkinson–White (WPW) syndrome. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1984-06-14 Ministry of Health of the Russian Federation
Click to view octisalate Octisalate is an organic compound used as an ingredient in sunscreens and cosmetics to absorb UVB (ultraviolet) rays from the sun. FDA
Click to view omarigliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/24660890) Dipeptidyl peptidase 4 (Organism: Mus musculus, class: Enzyme, accessions: P28843, gene: Dpp4, swissprot: DPP4_MOUSE Omarigliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor used for the treatment of type 2 diabetes. It potently but reversibly inhibits DPP-4 enzyme, which prolongs the circulating half-life of glucagon-like peptide-1 that increases insulin secretion in a glucose-dependent manner. 2015-09-28 PMDA
Click to view apremilast cAMP-specific 3',5'-cyclic phosphodiesterase 4D (Organism: Homo sapiens, class: Enzyme, accessions: Q08499, gene: PDE4D, swissprot: PDE4D_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) cAMP-specific 3',5'-cyclic phosphodiesterase 4C (Organism: Homo sapiens, class: Enzyme, accessions: Q08493, gene: PDE4C, swissprot: PDE4C_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) cAMP-specific 3',5'-cyclic phosphodiesterase 4B (Organism: Homo sapiens, class: Enzyme, accessions: Q07343, gene: PDE4B, swissprot: PDE4B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205437Orig1s007lbl.pdf) Apremilast is an oral small-molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels. The specific mechanism(s) by which apremilast exerts its therapeutic action in psoriatic arthritis patients and psoriasis patients is not well defined. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2014-03-21 FDA
Click to view empagliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) UDP-glucuronosyltransferase 1-8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW9, gene: UGT1A8, swissprot: UD18_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204629s019lbl.pdf) Empagliflozin is a C-glycosyl compound and a sodium-glucose co-transporter 2 inhibitor used as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. By inhibiting SGLT2, empagliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion. Empagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control with type 2 diabetes mellitus and to reduce the risk of cardiovascular death in adult patients with type 2 diabetes mellitus and established cardiovascular disease. hypoglycemic agent (Code: CHEBI:35526) Sodium-Glucose Cotransporter 2 Inhibitor (Code: N0000187059) Sodium-Glucose Transporter 2 Inhibitors (Code: N0000187058) Hypoglycemic Agents (Code: D007004) 2014-05-22 EMA
Click to view aripiprazole lauroxil Aripiprazole lauroxil is a prodrug of aripiprazole, following intramuscular injection is converted by enzyme-mediated hydrolysis to N-hydroxymethyl aripiprazole which is then hydrolyzed to aripiprazole. (See: aripiprazole) H1-receptor antagonist (Code: CHEBI:37955) second generation antipsychotic (Code: CHEBI:65191) serotonergic agonist (Code: CHEBI:35941) prodrug (Code: CHEBI:50266) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 2015-10-05 FDA
Click to view amino(diphenylhydantoin) valeric acid Amino(diphenylhydantoin) valeric acid is a hydantoin derivative. It was used for the treatment of epilepsy.
Click to view meprotixol Meprotixol is a derivative of the thiazanthene group. Meprotixol has a antitussive effect. Meprotixol showed an antitussive effect equal to that of codeine phosphate.
Click to view vintafolide Vintafolide is a water-soluble derivative of folic acid and the vinca alkaloid desacetylvinblastine hydrazide. Vintafolide is targeting the folate receptor, which is overexpressed on certain cancers, such as ovarian cancer. In 2014 manufactures stopped a late-stage study of vintafolide in treating ovarian cancer on the recommendation of a data safety monitoring board, saying that the drug failed to improve progression-free survival.
Click to view etilefrine pivalate Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/4396765) Etilefrine pivalate is a prodrug of etilefrine, an adrenergic agonist with vasoconstrictive activity. Etilefrine pivalate is hydrolyzed to etilefrine, which binds to and activates alpha-1-adrenergic receptors of the arteriolar and venous vasculature. (See: etilefrine)
Click to view laquinimod Laquinimod is an immunomodulator for oral treatment for multiple sclerosis. 2013-07-05 Ministry of Health of the Russian Federation
Click to view iodohippurate sodium I125 Iodohippurate sodium I125 is an isotopically modified compound, an organic sodium salt and a sodium 2-iodohippurate. It derives from a N-benzoylglycine. It is used as a radiopharmaceutical. It is used for the measurement of effective renal plasma flow in subjects with renal failure. radiopharmaceutical (Code: CHEBI:35232)
Click to view luliconazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10520160) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204153s004s005lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204153s004s005lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204153s004s005lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204153s004s005lbl.pdf) Luliconazole is an antifungal that belongs to the azole class. Luliconazole appears to inhibit ergosterol synthesis by inhibiting the enzyme lanosterol demethylase, inhibition of this enzyme's activity by azoles results in decreased amounts of ergosterol, a constituent of fungal cell membranes, and a corresponding accumulation of lanosterol. Luliconazole is indicated for the topical treatment of interdigital tinea pedis, tinea cruris, and tinea corporis caused by the organisms Trichophyton rubrum and Epidermophyton floccosum. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) 2013-11-14 FDA
Click to view iodohippurate sodium I131 Iodohippurate sodium I131 is a diagnostic aid in determining renal function, renal blood flow, ar urinary tract obstruction, and a renal imaging agent. radiopharmaceutical (Code: CHEBI:35232) 1968-05-24 FDA
Click to view laninamivir octanoate hydrate Neuraminidase (Organism: Influenza A virus (A/RI/5+/1957(H2N2)), class: Enzyme, accessions: Q194T1, gene: None, swissprot: Q194T1_9INFA Neuraminidase (Organism: Influenza A virus (A/WSN/1933(H1N1)), class: Enzyme, accessions: B4URF0, gene: NA, swissprot: B4URF0_9INFA Laninamivir octanoate hydrate is a prodrug of a new neuraminidase inhibitor, laninamivir. Laninamivir octanoate hydrate is used for the treatment and prevention of influenza. 2010-07-29 PMDA LVO
Click to view peramivir Neuraminidase (Organism: Influenza A virus (strain A/Puerto Rico/8/1934 H1N1), class: Enzyme, accessions: P03468, gene: NA, swissprot: NRAM_I34A1) inhibitor (Source: ) Neuraminidase (Organism: Influenza B virus (strain B/Lee/1940), class: Enzyme, accessions: P03474, gene: NA, swissprot: NRAM_INBLE) inhibitor (Source: ) Neuraminidase (Organism: Influenza A virus (strain A/Breig Mission/1/1918 H1N1), class: Enzyme, accessions: Q9IGQ6, gene: NA, swissprot: NRAM_I18A0) inhibitor (Source: ) Neuraminidase (Organism: Influenza A virus (A/WSN/1933(H1N1)), class: Enzyme, accessions: B4URF0, gene: NA, swissprot: B4URF0_9INFA) Peramivir is an inhibitor of influenza virus neuraminidase, an enzyme that releases viral particles from the plasma membrane of infected cells. EC 3.2.1.18 (exo-alpha-sialidase) inhibitor (Code: CHEBI:52425) antiviral drug (Code: CHEBI:36044) Neuraminidase Inhibitor (Code: N0000175524) Neuraminidase Inhibitors (Code: N0000175436) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) 2014-12-19 FDA BCZ
Click to view florbetaben F18 Amyloid beta A4 protein (Organism: Homo sapiens, class: Unclassified, accessions: P05067, gene: APP, swissprot: A4_HUMAN Florbetaben F18 is a F18-labeled stilbene derivative, which binds to beta-amyloid plaques in the brain. The F 18 isotope produces a positron signal that is detected by a PET scanner. Radioactive Diagnostic Agent (Code: N0000177914) Positron Emitting Activity (Code: N0000175869) 2014-03-19 FDA
Click to view delamanid Delamanid is a nitro-dihydro-imidazooxazoles derivative. The pharmacological mode of action of delamanid involves inhibition of the synthesis of the mycobacterial cell wall components, methoxy-mycolic and keto-mycolic acid. The identified metabolites of delamanid do not show anti-mycobacterial activity. Delamanid is indicated for use as part of an appropriate combination regimen for pulmonary multi-drug resistant tuberculosis (MDR-TB) in adult patients when an effective treatment regimen cannot otherwise be composed for reasons of resistance or tolerability. 2014-04-28 EMA
Click to view nordefrin Nordefrin is a structural isomer of epinephrine and has a primary amine group. Corbadrine (Levonordefrin) is a L-isomer of nordefrin and used as a vasoconstrictor in local anesthetic solutions. It has pharmacologic activity similar to that of epinephrine but it is more stable than epinephrine. Levonordefrin is used as a nasal decongestant and vasoconstrictor, most often in dentistry. Cardiovascular Agents (Code: D002317) Vasoconstrictor Agents (Code: D014662) 1960-01-06 FDA
Click to view tasimelteon Melatonin receptor type 1A (Organism: Homo sapiens, class: GPCR, accessions: P48039, gene: MTNR1A, swissprot: MTR1A_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/22640220) Melatonin receptor type 1B (Organism: Homo sapiens, class: GPCR, accessions: P49286, gene: MTNR1B, swissprot: MTR1B_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/22640220) an agonist at melatonin MT1 and MT2 receptors, these receptors are thought to be involved in the control of circadian rhythms Melatonin Receptor Agonist (Code: N0000175743) Melatonin Receptor Agonists (Code: N0000000250) 2014-01-31 FDA
Click to view rifamycin DNA-directed RNA polymerase subunit beta (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A8V2, gene: rpoB, swissprot: RPOB_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16595711) Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10648470) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12404239) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 1A4 (Organism: Rattus norvegicus, class: Transporter, accessions: O35913, gene: Slco1a4, swissprot: SO1A4_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210910s000lbl.pdf) Rifamycin SV is a derivative of antibiotic rifamycin B (the natural fermentation product of S. mediterranei broths). Rifamycin is a commonly used antimycobacterial drug that inhibits prokaryotic DNA-dependent RNA synthesis and protein synthesis; it blocks RNA-polymerase transcription initiation. Rifamycin has an activity spectrum against Gram-positive and Gram-negative bacteria, but is mainly used for the treatment of travelers’ diarrhea caused by noninvasive strains of Escherichia coli. antitubercular agent (Code: CHEBI:33231) Antirheumatic Agents (Code: D018501) 1988-10-03 Swissmedic (Switzerland)
Click to view olodaterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) UDP-glucuronosyltransferase 1-7 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW7, gene: UGT1A7, swissprot: UD17_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203108s008lbl.pdf) Olodaterol is a long-acting beta2-adrenergic agonist. The compound exerts its pharmacological effects by binding and activation of beta2-adrenoceptors after topical administration by inhalation. Olodaterol is indicated for the long-term, once-daily maintenance bronchodilator treatment of airflow obstruction in patients with chronic obstructive pulmonary disease, including chronic bronchitis and emphysema. beta-adrenergic agonist (Code: CHEBI:35522) bronchodilator agent (Code: CHEBI:35523) beta2-Adrenergic Agonist (Code: N0000175779) Adrenergic beta2-Agonists (Code: N0000009922) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 2014-07-31 FDA
Click to view umeclidinium Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205382s010lbl.pdf) Umeclidinium is a long-acting muscarinic antagonist. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptors at the smooth muscle leading to bronchodilation. Umeclidinium is indicated for the long-term maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease. muscarinic antagonist (Code: CHEBI:48876) Anticholinergic (Code: N0000175574) Cholinergic Antagonists (Code: N0000175370) 2013-12-18 FDA
Click to view vortioxetine 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) partial agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204447s018lbl.pdf) Vortioxetine is an antidepressant. The mechanism of the antidepressant effect of vortioxetine is not fully understood, but is thought to be related to its enhancement of serotonergic activity in the CNS through inhibition of the reuptake of serotonin. It also has several other activities including 5-HT3 receptor antagonism and 5-HT1A receptor agonism. The contribution of these activities to vortioxetine’s antidepressant effect has not been established. Vortioxetine binds with high affinity to the human serotonin transporter, but not to the norepinephrine or dopamine transporters. Vortioxetine potently and selectively inhibits reuptake of serotonin. Vortioxetine binds to 5-HT3, 5-HT1A, 5-HT7, 5-HT1D, and 5-HT1B, receptors and is a 5-HT3, 5-HT1D, and 5-HT7 receptor antagonist, 5-HT1B receptor partial agonist, and 5-HT1A receptor agonist. Vortioxetine is indicated for the treatment of major depressive disorder. antidepressant (Code: CHEBI:35469) anxiolytic drug (Code: CHEBI:35474) serotonergic agonist (Code: CHEBI:35941) serotonergic antagonist (Code: CHEBI:48279) Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin 5-HT1 Receptor Agonists (Code: D058825) Serotonin 5-HT1 Receptor Antagonists (Code: D058829) Serotonin 5-HT3 Receptor Antagonists (Code: D058831) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Serotonin Receptor Agonists (Code: D017366) Serotonin Uptake Inhibitors (Code: D017367) Tranquilizing Agents (Code: D014149) 2013-09-30 FDA
Click to view riociguat Guanylate cyclase soluble subunit beta-1 (Organism: Homo sapiens, class: Enzyme, accessions: Q02153, gene: GUCY1B3, swissprot: GCYB1_HUMAN) positive allosteric modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204819s011lbl.pdf) Riociguat is a stimulator of guanylate cyclase which causes relaxation of vascular smooth muscle and is used to treat severe pulmonary arterial hypertension. antihypertensive agent (Code: CHEBI:35674) Guanylate Cyclase Stimulators (Code: N0000190484) Soluble Guanylate Cyclase Stimulator (Code: N0000190485) Enzyme Activators (Code: D020536) 2013-10-08 FDA
Click to view sofosbuvir Lysosomal protective protein (Organism: Homo sapiens, class: Enzyme, accessions: P10619, gene: CTSA, swissprot: PPGB_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212480s000lbl.pdf) Liver carboxylesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23141, gene: CES1, swissprot: EST1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212480s000lbl.pdf) Histidine triad nucleotide-binding protein 1 (Organism: Homo sapiens, class: Enzyme, accessions: P49773, gene: HINT1, swissprot: HINT1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212480s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212480s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212480s000lbl.pdf) Sofosbuvir is an inhibitor of the HCV NS5B RNA-dependent RNA polymerase, which is essential for viral replication. Sofosbuvir is a nucleotide prodrug that undergoes intracellular metabolism to form the pharmacologically active uridine analog triphosphate (GS-461203), which can be incorporated into HCV RNA by the NS5B polymerase and acts as a chain terminator. Sofosbuvir is indicated for the treatment of adult and pediatric patients with genotype 1, 2, 3 or 4 chronic HCV infection without cirrhosis or with compensated cirrhosis. prodrug (Code: CHEBI:50266) antiviral drug (Code: CHEBI:36044) Hepatitis C Virus Nucleotide Analog NS5B Polymerase Inhibitor (Code: N0000191493) RNA Replicase Inhibitors (Code: N0000191258) Nucleoside Analog (Code: N0000175459) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2013-12-06 FDA
Click to view simeprevir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Ileal sodium/bile acid cotransporter (Organism: Homo sapiens, class: Transporter, accessions: Q12908, gene: SLC10A2, swissprot: NTCP2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/205123s014lbl.pdf) Simeprevir is an inhibitor of the HCV NS3/4A protease which is essential for viral replication. It is used in the treatment of chronic hepatitis C genotype 1 infection in adults with compensated liver disease, including cirrhosis. Hepatitis C Virus NS3/4A Protease Inhibitor (Code: N0000182639) HCV NS3/4A Protease Inhibitors (Code: N0000182638) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) P-Glycoprotein Inhibitors (Code: N0000185503) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 2013-11-22 FDA 30B
Click to view ipidacrine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://onlinelibrary.wiley.com/doi/abs/10.1111/j.1527-3458.1998.tb00067.x) Ipidacrine is a nonselective inhibitor of acetylcholinesterase and butyrilcholinesterase. Ipidacrine has a direct stimulating effect on the conduct of the pulse along the nerve fibers, interneuronal and neuromuscular synapses of the CNS and peripheral nervous system. 1988-07-15 Ministry of Health of the Russian Federation
Click to view macitentan Endothelin-1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25101, gene: EDNRA, swissprot: EDNRA_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204410s017lbl.pdf) Endothelin B receptor (Organism: Homo sapiens, class: GPCR, accessions: P24530, gene: EDNRB, swissprot: EDNRB_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204410s017lbl.pdf) Macitentan is an endothelin receptor antagonist that is used in the therapy of pulmonary arterial hypertension. endothelin receptor antagonist (Code: CHEBI:51451) antihypertensive agent (Code: CHEBI:35674) orphan drug (Code: CHEBI:71031) Endothelin A Receptor Antagonists (Code: D065130) Endothelin B Receptor Antagonists (Code: D065131) Endothelin Receptor Antagonists (Code: D065128) 2013-10-18 FDA
Click to view ibrutinib Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/17154430) Tyrosine-protein kinase Blk (Organism: Homo sapiens, class: Kinase, accessions: P51451, gene: BLK, swissprot: BLK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Fgr (Organism: Homo sapiens, class: Kinase, accessions: P09769, gene: FGR, swissprot: FGR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase HCK (Organism: Homo sapiens, class: Kinase, accessions: P08631, gene: HCK, swissprot: HCK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Yes (Organism: Homo sapiens, class: Kinase, accessions: P07947, gene: YES1, swissprot: YES_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase ITK/TSK (Organism: Homo sapiens, class: Kinase, accessions: Q08881, gene: ITK, swissprot: ITK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase Tec (Organism: Homo sapiens, class: Kinase, accessions: P42680, gene: TEC, swissprot: TEC_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase TXK (Organism: Homo sapiens, class: Kinase, accessions: P42681, gene: TXK, swissprot: TXK_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Receptor tyrosine-protein kinase erbB-2 (Organism: Homo sapiens, class: Kinase, accessions: P04626, gene: ERBB2, swissprot: ERBB2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Receptor tyrosine-protein kinase erbB-4 (Organism: Homo sapiens, class: Kinase, accessions: Q15303, gene: ERBB4, swissprot: ERBB4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Tyrosine-protein kinase JAK3 (Organism: Homo sapiens, class: Kinase, accessions: P52333, gene: JAK3, swissprot: JAK3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/26641137) Ibrutinib is a small-molecule inhibitor of BTK. Ibrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. BTK's role in signaling through the B-cell surface receptors results in activation of pathways necessary for B-cell trafficking, chemotaxis, and adhesion. Nonclinical studies show that ibrutinib inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) 2013-11-13 FDA 1E8
Click to view dolutegravir Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q7ZJM1, gene: pol, swissprot: Q7ZJM1_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210192s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210192s000lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210192s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/210192s000lbl.pdf) Dolutegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid (DNA) integration which is essential for the HIV replication cycle. Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor (Code: N0000175887) Multidrug and Toxin Extrusion Transporter 1 Inhibitors (Code: N0000191423) Organic Cation Transporter 2 Inhibitors (Code: N0000187061) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) HIV Integrase Inhibitors (Code: D019428) 2013-08-12 FDA DLU
Click to view dimethyl fumarate Dimethyl fumarate is a fumarate derivative. The mechanism by which dimethyl fumarate (DMF) exerts its therapeutic effect in multiple sclerosis is unknown. DMF have been shown to activate the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway in vitro and in vivo in animals and humans. The Nrf2 pathway is involved in the cellular response to oxidative stress. Dimethyl fumarate also appears to inhibit the nuclear factor-kappa B (NF-kB)-mediated pathway, modulates the production of certain cytokines and induces apoptosis in certain T-cell subsets. Its radiosensitizing activity is due to this agent's ability to bind to and sequester intracellular GSH, thereby depleting intracellular GSH and preventing its anti-oxidative effects. Dimethyl fumarate is indicated for the treatment of patients with relapsing forms of multiple sclerosis. immunomodulator (Code: CHEBI:50846) antipsoriatic (Code: CHEBI:50748) Dermatologic Agents (Code: D003879) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Radiation-Sensitizing Agents (Code: D011838) 2013-03-27 FDA
Click to view canagliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204353s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204353s000lbl.pdf) A glucoside-derived sodium-glucose transporter 2 inhibitor that stimulates urinary excretion of glucose by suppressing renal glucose reabsorption. It is used to manage blood glucose levels in patients with type 2 diabetes. hypoglycemic agent (Code: CHEBI:35526) Sodium-Glucose Cotransporter 2 Inhibitor (Code: N0000187059) Sodium-Glucose Transporter 2 Inhibitors (Code: N0000187058) P-Glycoprotein Inhibitors (Code: N0000185503) Hypoglycemic Agents (Code: D007004) 2013-03-29 FDA
Click to view glycerol phenylbutyrate Glycerol phenylbutyrate is a nitrogen-binding agent. It is a triglyceride containing 3 molecules of phenylbutyrate linked to a glycerol backbone. Phenylacetate, the major metabolite of phenylbutyrate, is the active moiety of this drug. Phenylacetate conjugates with glutamine (which contains 2 molecules of nitrogen) via acetylation in the liver and kidneys to form phenylacetylglutamine, which is excreted by the kidneys. On a molar basis, phenylacetylglutamine, like urea, contains 2 moles of nitrogen and provides an alternate vehicle for waste nitrogen excretion. Glycerol phenylbutyrate is indicated for use as a nitrogen-binding agent for chronic management of patients with urea cycle disorders (UCDs) who cannot be managed by dietary protein restriction and/or amino acid supplementation alone. (See: phenylbutanoic acid) 2013-02-01 FDA
Click to view pomalidomide Protein cereblon (Organism: Homo sapiens, class: Cytosolic other, accessions: Q96SW2, gene: CRBN, swissprot: CRBN_HUMAN) modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26131937) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204026s017lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204026s017lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204026s017lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204026s017lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/204026s017lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17308870) Pomalidomide is an analogue of thalidomide with immunomodulatory, antiangiogenic, and antineoplastic properties. Cellular activities of pomalidomide are mediated through its target cereblon, a component of a cullin ring E3 ubiquitin ligase enzyme complex. In vitro, in the presence of drug, substrate proteins (including Aiolos and Ikaros) are targeted for ubiquitination and subsequent degradation leading to direct cytotoxic and immunomodulatory effects. In in vitro cellular assays, pomalidomide inhibited proliferation and induced apoptosis of hematopoietic tumor cells. Additionally, pomalidomide inhibited the proliferation of lenalidomideresistant multiple myeloma cell lines and synergized with dexamethasone in both lenalidomide-sensitive and lenalidomide-resistant cell lines to induce tumor cell apoptosis. Pomalidomide enhanced T cell- and natural killer (NK) cell-mediated immunity and inhibited production of pro-inflammatory cytokines (e.g., TNF-? and IL-6) by monocytes. angiogenesis inhibitor (Code: CHEBI:48422) antineoplastic agent (Code: CHEBI:35610) immunomodulator (Code: CHEBI:50846) Angiogenesis Inhibitors (Code: D020533) Angiogenesis Modulating Agents (Code: D043924) Antineoplastic Agents (Code: D000970) Growth Inhibitors (Code: D006131) Growth Substances (Code: D006133) Immunologic Factors (Code: D007155) Thalidomide Analog (Code: N0000184014) 2013-02-08 FDA Y70
Click to view quifenadine Quifenadine is a quinuclidine derivative and a non-sedating antihistamines, which combines a high selective activity to block histamine type 1 receptors and an ability to block serotonin and to break down histamine directly in tissues. Quifenadine is used for the treatment of different allergic conditions. Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Neurotransmitter Agents (Code: D018377) 2006-02-17 Ministry of Health of the Russian Federation
Click to view ospemifene Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) modulator an estrogen agonist/antagonist with tissue selective effects, its biological actions are mediated through binding to estrogen receptors, this binding results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism) estrogen receptor modulator (Code: CHEBI:50739) antineoplastic agent (Code: CHEBI:35610) anti-inflammatory agent (Code: CHEBI:67079) Estrogen Agonist/Antagonist (Code: N0000175826) Selective Estrogen Receptor Modulators (Code: N0000000168) 2013-02-26 FDA
Click to view cetyl alcohol has been used for eczema, skin irritations; RN given refers to parent cpd; structure 1990-08-02 FDA PL3
Click to view regorafenib Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Fibroblast growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P21802, gene: FGFR2, swissprot: FGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Angiopoietin-1 receptor (Organism: Homo sapiens, class: Kinase, accessions: Q02763, gene: TEK, swissprot: TIE2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Discoidin domain-containing receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: Q16832, gene: DDR2, swissprot: DDR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) High affinity nerve growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P04629, gene: NTRK1, swissprot: NTRK1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) RAF proto-oncogene serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P04049, gene: RAF1, swissprot: RAF1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Serine/threonine-protein kinase B-raf (Organism: Homo sapiens, class: Kinase, accessions: P15056, gene: BRAF, swissprot: BRAF_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Mitogen-activated protein kinase 11 (Organism: Homo sapiens, class: Kinase, accessions: Q15759, gene: MAPK11, swissprot: MK11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Tyrosine-protein kinase FRK (Organism: Homo sapiens, class: Kinase, accessions: P42685, gene: FRK, swissprot: FRK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Ephrin type-A receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P29317, gene: EPHA2, swissprot: EPHA2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Bifunctional epoxide hydrolase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P34913, gene: EPHX2, swissprot: HYES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23726028) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/204369lbl.pdf) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) potentiator (Source: https://www.ncbi.nlm.nih.gov/pubmed/25790278) Regorafenib is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment. In in vivo models, regorafenib demonstrated anti-angiogenic activity in a rat tumor model, and inhibition of tumor growth as well as anti-metastatic activity in several mouse xenograft models including some for human colorectal carcinoma. Regorafenib is indicated for the treatment of patients with Metastatic colorectal cancer who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy; Locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate and sunitinib malate. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) 2012-09-27 FDA
Click to view tedisamil Potassium voltage-gated channel subfamily A member 7 (Organism: Mus musculus, class: Unclassified, accessions: Q17ST2, gene: Kcna7, swissprot: KCNA7_MOUSE) blocker (Source: ) a multiple potassium channel blocker which blocks the rapid (IKr), slow (IKs) and ultrarapid (IKur) components of the delayed rectifier potassium current, the transient outward potassium current (Ito) and the ATP (IKATP) sensitive and the acetylcholine-activated (IKACH) potassium currents Anti-Arrhythmia Agents (Code: D000889) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Protective Agents (Code: D020011) 2008-05-21 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view metabutethamine Metabutethamine is a local anesthetic used in dentistry to produce infiltration and nerve block anesthesia. Anesthetics (Code: D000777)
Click to view metamizole Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/25765567) Glucose-6-phosphate 1-dehydrogenase (Organism: Homo sapiens, class: Enzyme, accessions: P11413, gene: G6PD, swissprot: G6PD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11440730) Metamizole has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, an antirheumatic drug, a peripheral nervous system drug, an antipyretic, a prodrug and a cyclooxygenase 3 inhibitor. It was withdrawn from US market in 1977 on the basis of reports of agranulocytosis. Withdrawn from the Canadian market in 1963. prodrug (Code: CHEBI:50266) non-narcotic analgesic (Code: CHEBI:35481) antirheumatic drug (Code: CHEBI:35842) peripheral nervous system drug (Code: CHEBI:49110) antipyretic (Code: CHEBI:35493) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antipyretics (Code: D058633) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1949-05-10 Swissmedic (Switzerland)
Click to view methylatropine Methylatropine is a quaternary salt of atropine. It was used for relieving pyloric spasm in infants. The drug has the same action as atropine and antagonizes muscarinic acetylcholine receptors. Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view creatine Creatine is a glycine derivative having methyl and amidino groups attached to the nitrogen. Creatine is an endogenous amino acid derivative produced by vertebrate animals and occurring primarily in muscle cells. Creatine is important for energy storage; it is phosphorylated to creatine phosphate, which serves as a phosphate donor in the conversion of ADP to ATP and supplies energy necessary for muscle contraction. Dietary supplementation with creatine may improve muscle wasting associated with cancer and other chronic diseases. CRN
Click to view benzoin Benzoin is a ketone that consists of acetophenone bearing hydroxy and phenyl substituents at the alpha-position. The parent of the class of benzoins. Benzoin was first reported in 1832 by Justus von Liebig and Friedrich Woehler during their research on oil of bitter almond, which is benzaldehyde with traces of hydrocyanic acid. This should not be confused with benzoin gum from STYRAX.
Click to view octinoxate a UV filter compound 1992-12-07 FDA
Click to view avobenzone Tyrosinase (Organism: Homo sapiens, class: Enzyme, accessions: P14679, gene: TYR, swissprot: TYRO_HUMAN) inhibitor causes allergic or photoallergic contact dermatitis; structure given in first source Cosmetics (Code: D003358) Dermatologic Agents (Code: D003879) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) Sunscreening Agents (Code: D013473) 1992-12-07 FDA
Click to view methyl salicylate Methyl salicylate is an organic ester naturally produced by many species of plants, particularly wintergreens. Methyl salicylate is used as a rubefacient and analgesic in deep heating liniments for acute joint and muscular pain. It is used as a flavoring agent in chewing gums and mints in small concentrations and added as antiseptic in mouthwash solutions. flavouring agent (Code: CHEBI:35617) insect attractant (Code: CHEBI:24850) Antirheumatic Agents (Code: D018501) Fixatives (Code: D005404) 2008-02-20 FDA
Click to view tafluprost Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/202514s003s004lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/22910791) Tafluprost is a prostaglandin analog is a selective FP prostanoid receptor agonist which is believed to reduce intraocular pressure by increasing uveoscleral outflow. Tafluprost is indicated for reducing elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Prostaglandin Analog (Code: N0000175454) Prostaglandin Receptor Agonists (Code: N0000000106) Increased Prostaglandin Activity (Code: N0000009526) Prostaglandins (Code: N0000007706) 2012-02-10 FDA
Click to view Ioflupane I-123 a radiopharmaceutical indicated for striatal dopamine transporter visualization using single photon emission computed tomography (SPECT) brain imaging to assist in the evaluation of adult patients with suspected Parkinsonian syndromes (PS) radiopharmaceutical (Code: CHEBI:35232) Radioactive Diagnostic Agent (Code: N0000177914) Radiopharmaceutical Activity (Code: N0000000205) 2011-01-14 FDA
Click to view telbivudine Telbivudine is a synthetic thymidine nucleoside analogue with activity against HBV DNA polymerase. It is phosphorylated by cellular kinases to the active triphosphate form. Telbivudine 5'-triphosphate inhibits HBV DNA polymerase (reverse transcriptase) by competing with the natural substrate, thymidine 5'-triphosphate. Incorporation of telbivudine 5'-triphosphate into viral DNA causes DNA chain termination. antiviral drug (Code: CHEBI:36044) Hepatitis B Virus Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175656) Nucleoside Analog (Code: N0000175459) Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009947) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) 2006-10-25 FDA LLT
Click to view formaldehyde Formaldehyde is a colorless poisonous gas synthesized by the oxidation of methanol and used as an antiseptic, disinfectant, histologic fixative, and general-purpose chemical reagent for laboratory applications. Formaldehyde is readily soluble in water and is commonly distributed as a 37% solution in water; formalin, a 10% solution of formaldehyde in water, is used as a disinfectant and to preserve biological specimens. Environmentally, formaldehyde may be found in the atmosphere, smoke from fires, automobile exhaust and cigarette smoke. Small amounts are produced during normal metabolic processes in most organisms, including humans. Formaldehyde vapors are toxic, upon entry formaldehyde reacts readily with macromolecules, including DNA to form DNA-protein and DNA-DNA cross-links. Anti-Infective Agents (Code: D000890) Disinfectants (Code: D004202) Fixatives (Code: D005404) Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) FDA FOR
Click to view mequinol Tyrosinase (Organism: Homo sapiens, class: Enzyme, accessions: P14679, gene: TYR, swissprot: TYRO_HUMAN) substrate (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020922s006lbl.pdf) Mequinol is 4-hydroxyanisole. The mechanism of action of mequinol is unknown. Although mequinol is a substrate for the enzyme tyrosinase and acts as a competitive inhibitor of the formation of melanin precursors, the clinical significance of these findings is unknown. Mequinol is a skin lightening agent. Mequinol is used in combination with tretinoin as an adjunct to a comprehensive skin care and sun avoidance program where the patient should primarily either avoid the sun or use protective clothing. Antineoplastic Agents (Code: D000970) Antioxidants (Code: D000975) Protective Agents (Code: D020011) Depigmenting Activity (Code: N0000175851) Melanin Synthesis Inhibitors (Code: N0000175850) Skin Lightening Agent (Code: N0000175855) 1999-12-10 FDA 4KS
Click to view vilazodone Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: ) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: ) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q13639, gene: HTR4, swissprot: 5HT4R_HUMAN) agonist (Source: ) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT D(3) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19020, gene: Drd3, swissprot: DRD3_RAT Serotonin 3 (5-HT3) receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35563|Q9JJ16, gene: Htr3a|Htr3b, swissprot: 5HT3A_RAT|5HT3B_RAT 5-hydroxytryptamine receptor 2C (Organism: Rattus norvegicus, class: GPCR, accessions: P08909, gene: Htr2c, swissprot: 5HT2C_RAT 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT D(4) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30729, gene: Drd4, swissprot: DRD4_RAT 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT 5-hydroxytryptamine receptor 1D (Organism: Rattus norvegicus, class: GPCR, accessions: P28565, gene: Htr1d, swissprot: 5HT1D_RAT Adrenergic receptor alpha-2 (Organism: Homo sapiens, class: GPCR, accessions: P08913|P18089|P18825, gene: ADRA2A|ADRA2B|ADRA2C, swissprot: ADA2A_HUMAN|ADA2B_HUMAN|ADA2C_HUMAN Adrenergic receptor alpha-1 (Organism: Homo sapiens, class: GPCR, accessions: P25100|P35348|P35368, gene: ADRA1A|ADRA1B|ADRA1D, swissprot: ADA1A_HUMAN|ADA1B_HUMAN|ADA1D_HUMAN 5-hydroxytryptamine receptor 4 (Organism: Rattus norvegicus, class: GPCR, accessions: Q62758, gene: Htr4, swissprot: 5HT4R_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT A benzofuran, indole, and piperazine derivative that functions as a SEROTONIN UPTAKE INHIBITOR and partial SEROTONIN 5-HT1 RECEPTOR AGONIST. It is used as an ANTIDEPRESSIVE AGENT. antidepressant (Code: CHEBI:35469) serotonergic agonist (Code: CHEBI:35941) serotonin uptake inhibitor (Code: CHEBI:50949) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin 5-HT1 Receptor Agonists (Code: D058825) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Serotonin Uptake Inhibitors (Code: D017367) 2011-01-21 FDA
Click to view pirfenidone Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf) Pirfenidone is an immunosuppresant. It is used for the treatment of idiopathic pulmonary fibrosis. It has a role as a non-narcotic analgesic, a non-steroidal anti-inflammatory drug and an antipyretic. non-narcotic analgesic (Code: CHEBI:35481) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antipyretic (Code: CHEBI:35493) Pyridone (Code: N0000191420) Pyridones (Code: N0000007575) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antineoplastic Agents (Code: D000970) Antirheumatic Agents (Code: D018501) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2008-09-16 PMDA
Click to view axitinib Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202324s008lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24398510) Axitinib is an indazole derivative and a second generation tyrosine kinase inhibitor that works by selectively inhibiting vascular endothelial growth factor receptors (VEGFR-1, VEGFR-2, VEGFR-3). Through this mechanism of action, axitinib blocks angiogenesis, tumour growth and metastases. It is reported to exhibit potency that is 50-450 times higher than that of the first generation VEGFR inhibitors. Axitinib is indicated for the treatment of advanced renal cell carcinoma after failure of one prior systemic therapy. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Receptor Tyrosine Kinase Inhibitors (Code: N0000020000) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2012-01-27 FDA AXI
Click to view ingenol mebutate Protein kinase C delta type (Organism: Homo sapiens, class: Kinase, accessions: Q05655, gene: PRKCD, swissprot: KPCD_HUMAN) activator (Source: http://www.ncbi.nlm.nih.gov/pubmed/15126366) Protein kinase C alpha type (Organism: Homo sapiens, class: Kinase, accessions: P17252, gene: PRKCA, swissprot: KPCA_HUMAN) Protein kinase C beta type (Organism: Homo sapiens, class: Kinase, accessions: P05771, gene: PRKCB, swissprot: KPCB_HUMAN) Protein kinase C epsilon type (Organism: Homo sapiens, class: Kinase, accessions: Q02156, gene: PRKCE, swissprot: KPCE_HUMAN) Serine/threonine-protein kinase D1 (Organism: Homo sapiens, class: Kinase, accessions: Q15139, gene: PRKD1, swissprot: KPCD1_HUMAN) Protein kinase C gamma type (Organism: Homo sapiens, class: Kinase, accessions: P05129, gene: PRKCG, swissprot: KPCG_HUMAN) activator (Source: ) protein kinase C agonist and antineoplastic antineoplastic agent (Code: CHEBI:35610) Cell Death Inducer (Code: N0000184015) Increased Cellular Death (Code: N0000009176) 2012-01-23 FDA
Click to view icatibant B2 bradykinin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30411, gene: BDKRB2, swissprot: BKRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022150s000lbl.pdf) Aminopeptidase N (Organism: Homo sapiens, class: Enzyme, accessions: P15144, gene: ANPEP, swissprot: AMPN_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17026984) B1 bradykinin receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P97583, gene: Bdkrb1, swissprot: BKRB1_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10422787) B1 bradykinin receptor (Organism: Homo sapiens, class: GPCR, accessions: P46663, gene: BDKRB1, swissprot: BKRB1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10422787) Icatibant is a competitive antagonist selective for the bradykinin B2 receptor, with an affinity similar to bradykinin. Hereditary angioedema is caused by an absence or dysfunction of C1-esterase-inhibitor, a key regulator of the Factor XII/kallikrein proteolytic cascade that leads to bradykinin production. Bradykinin is a vasodilator which is thought to be responsible for the characteristic HAE symptoms of localized swelling, inflammation, and pain. Icatibant inhibits bradykinin from binding the B2 receptor and thereby treats the clinical symptoms of an acute, episodic attack of HAE. beta-adrenergic antagonist (Code: CHEBI:35530) Bradykinin B2 Receptor Antagonist (Code: N0000182965) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Bradykinin B2 Receptor Antagonists (Code: D065094) Bradykinin Receptor Antagonists (Code: D065168) Complement Inactivating Agents (Code: D051056) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2008-07-11 EMA
Click to view crizotinib Hepatocyte growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P08581, gene: MET, swissprot: MET_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202570s027lbl.pdf) Proto-oncogene tyrosine-protein kinase ROS (Organism: Homo sapiens, class: Kinase, accessions: P08922, gene: ROS1, swissprot: ROS1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202570s027lbl.pdf) Macrophage-stimulating protein receptor (Organism: Homo sapiens, class: Kinase, accessions: Q04912, gene: MST1R, swissprot: RON_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202570s027lbl.pdf) ALK tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: Q9UM73, gene: ALK, swissprot: ALK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202570s027lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23686600) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23686600) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23686600) Insulin receptor (Organism: Homo sapiens, class: Kinase, accessions: P06213, gene: INSR, swissprot: INSR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21708465) Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins. The formation of ALK fusion proteins results in activation and dysregulation of the gene's expression and signaling which can contribute to increased cell proliferation and survival in tumors expressing these proteins. Crizotinib demonstrated concentration-dependent inhibition of ALK, ROS1, and c-Met phosphorylation in cell-based assays using tumor cell lines and demonstrated antitumor activity in mice bearing tumor xenografts that expressed echinoderm microtubule-associated protein-like 4 (EML4)- or nucleophosmin (NPM)-ALK fusion proteins or c-Met. antineoplastic agent (Code: CHEBI:35610) biomarker (Code: CHEBI:59163) Kinase Inhibitor (Code: N0000175605) Cytochrome P450 3A Inhibitors (Code: N0000190114) Receptor Tyrosine Kinase Inhibitors (Code: N0000020000) Cytochrome P450 2B6 Inhibitors (Code: N0000182139) P-Glycoprotein Inhibitors (Code: N0000185503) Organic Cation Transporter 1 Inhibitors (Code: N0000191265) Organic Cation Transporter 2 Inhibitors (Code: N0000187061) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2011-08-26 FDA VGH
Click to view deferiprone iron (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021825s003lbl.pdf) UDP-glucuronosyltransferase 1-6 (Organism: Homo sapiens, class: Enzyme, accessions: P19224, gene: UGT1A6, swissprot: UD16_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021825s004lbl.pdf) Deferiprone is a chelating agent with an affinity for ferric ion (iron III). Deferiprone binds with ferric ions to form neutral 3:1 (deferiprone:iron) complexes that are stable over a wide range of pH values. Deferiprone has a lower binding affinity for other metals such as copper, aluminum and zinc than for iron. Deferiprone is indicated for the treatment of patients with transfusional iron overload due to thalassemia syndromes when current chelation therapy is inadequate. protective agent (Code: CHEBI:50267) Iron Chelating Activity (Code: N0000000144) Iron Chelator (Code: N0000175522) Chelating Agents (Code: D002614) Iron Chelating Agents (Code: D007502) Sequestering Agents (Code: D064449) 2011-10-14 FDA
Click to view hydroxyprogesterone caproate Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18060946) Hydroxyprogesterone caproate is a synthetic progestin. It is an ester derivative of 17alpha-hydroxyprogesterone formed from caproic acid (hexanoic acid). Mimicking the action of progesterone, hydroxyprogesterone caporate binds to and activates nuclear progesterone receptors in the reproductive system and causes the ligand-receptor complex to be translocated to the nucleus where it binds to and promotes expression of target genes. Hydroxyprogesterone caproate is used as a contraceptive and to reduce the risk of preterm birth in women with a singleton pregnancy who have a history of singleton spontaneous preterm birth. Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Progestins (Code: D011372) 1974-12-26 FDA
Click to view talbutal Talbutal is a short to intermediate-acting barbiturate. Talbutal has been used as a sedative and hypnotic, but then this usage was discontinued. 1954-09-21 FDA
Click to view ethanol Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15285839) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12824820) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9929510) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9929510) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9929510) Kir3.1/Kir3.4 (Organism: Homo sapiens, class: Ion channel, accessions: P48544|P48549, gene: KCNJ3|KCNJ5, swissprot: KCNJ3_HUMAN|KCNJ5_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10570486) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) potentiator (Source: https://www.ncbi.nlm.nih.gov/pubmed/8700149) Glycine receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: P23416, gene: GLRA2, swissprot: GLRA2_HUMAN) potentiator (Source: https://www.ncbi.nlm.nih.gov/pubmed/8700149) Gamma-aminobutyric acid receptor subunit delta (Organism: Homo sapiens, class: Ion channel, accessions: O14764, gene: GABRD, swissprot: GBRD_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17591544) Ethanol is a primary alcohol that is ethane in which one of the hydrogens is substituted by a hydroxy group. Ethanol affects the brain’s neurons in several ways. It alters their membranes as well as their ion channels, enzymes, and receptors. Alcohol also binds directly to the receptors for acetylcholine, serotonin, GABA, and the NMDA receptors for glutamate. The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). It also inhibits NMDA receptor functioning. In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in alcoholic beverages. antiseptic drug (Code: CHEBI:48218) polar solvent (Code: CHEBI:48354) central nervous system depressant (Code: CHEBI:35488) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Solvents (Code: D012997) 1946-01-17 FDA EOH
Click to view guanidine Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12089365) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9632645) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9618255) Solute carrier family 22 member 4 (Organism: Homo sapiens, class: Transporter, accessions: Q9H015, gene: SLC22A4, swissprot: S22A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215651) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Potassium voltage-gated channel subfamily A member 2 (Organism: Oncorhynchus mykiss, class: Ion channel, accessions: Q9I830, gene: kcna2, swissprot: KCNA2_ONCMY) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21926190) Guanidine is a small basic compound. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. Guanidine stimulates the neuromuscular junction presynaptically by inhibiting voltage-gated potassium channels, leading to the enhanced release of acetylcholine in the synaptic cleft. This stimulatory effect of guanidine underlies its use in the therapy for the neuromuscular diseases. The hydrochloride salt of guanidine was approved for the reduction of the symptoms of muscle weakness and easy fatigability associated with the myasthenic syndrome of Eaton-Lambert. Acetylcholine Releasing Agent (Code: N0000175772) Increased Acetylcholine Activity (Code: N0000009079) 1939-10-02 FDA GAI
Click to view corticorelin ovine used in diagnosis of adrenocortical insufficiency & Cushing's syndrome; AA sequence given in first source; MF C205-H339-N59-O63-S; RN given refers to triflutate salt; RN for parent cpd not avail 3/94 diagnostic agent (Code: CHEBI:33295) 1996-05-23 FDA
Click to view vinyl ether Vinyl ether is a clear, nearly colorless, volatile liquid which was used as an inhalation anesthetic. Vinyl ether's only strengths compared to ethyl ether are favorable induction and recovery. During anesthesia vinyl ether has no particularly wonderful properties and is harder to control than other agents. Therefore, vinyl ether was commonly used as a preliminary anesthetic before administration of diethyl ether. Additionally, vinyl ether was only used for short operations or analgesia, e.g. dentistry and obstetrics. Vinyl ether was used infrequently for long operations because of toxicity, cost, and superior alternatives. Anesthetics (Code: D000777) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492)
Click to view propiolactone Propiolactone (beta-propiolactone) is disinfectant which was used in vapor form to sterilize vaccines, grafts, etc. It is no longer used for medical disinfection. Dermal exposure to beta-propiolactone causes the burning or blistering of the skin, and ingestion of this substance burns the mouth and stomach while exposure to its vapors causes severe irritation of the eyes, throat and respiratory tract. This substance is reasonably anticipated to be a human carcinogen. Anti-Infective Agents (Code: D000890) Disinfectants (Code: D004202) 1959-06-12 FDA
Click to view ethyl chloride Ethyl chloride is the simplest and least toxic member of the class of chloroethanes, that is ethane in which a single hydrogen is substituted by a chlorine. A colourless gas at room temperature and pressure (boiling point 12?), it is used as a mild topical anaesthetic to numb the skin prior to ear piercing, skin biopsies, etc., and is also used in the treatment of sports injuries. It was formerly used in the production of tetraethyllead. It is still used in the treatment of cellulose to make ethylcellulose for commercial products. Also ethyl chloride is used as a diagnostic tool to detect a dead tooth with nonviable pulp. Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1965-07-01 Spanish Agency of Medicines and Medical Products (AEMPS) MCE
Click to view glycine Glycine N-acyltransferase (Organism: Homo sapiens, class: Transporter, accessions: Q6IB77, gene: GLYAT, swissprot: GLYAT_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22475485) Glycine amidinotransferase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P50440, gene: GATM, swissprot: GATM_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/3800397) Glycine receptor (alpha-1/beta) (Organism: Homo sapiens, class: Ion channel, accessions: P23415|P48167, gene: GLRA1|GLRB, swissprot: GLRA1_HUMAN|GLRB_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/14551753) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/14551753) Sodium-coupled neutral amino acid transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q96QD8, gene: SLC38A21, swissprot: S38A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10930503) Sodium-coupled neutral amino acid transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q9H2H9, gene: SLC38A1, swissprot: S38A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11342143) Sodium-coupled neutral amino acid transporter 5 (Organism: Homo sapiens, class: Transporter, accessions: Q8WUX1, gene: SLC38A5, swissprot: S38A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11243884) Glycine (Gly) is a natural amino acid neurotransmitter that acts as a co-agonist at Glutamate receptors in the brain and is an activator of glycine receptors, GLRA1-3, GLRB. The abnormal Gly levels have been implicated in neuropsychiatric disorders. Alterations in Gly levels are implicated in several diseases of the central nervous system. Glycine is a component of a nutrients mixture for peripheral administration to well-nourished mildly catabolic adult patients who require only short-term parenteral nutrition. nutraceutical (Code: CHEBI:50733) hepatoprotective agent (Code: CHEBI:62868) NMDA receptor agonist (Code: CHEBI:64571) Glycine Agents (Code: D018684) Neurotransmitter Agents (Code: D018377) 1976-05-25 FDA GLY
Click to view acetohydroxamic acid Urease (Organism: Sporosarcina pasteurii, class: Enzyme, accessions: P41020|P41021|P41022, gene: ureC|ureB|ureA, swissprot: URE1_SPOPA|URE2_SPOPA|URE3_SPOPA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/29913313) Acetohydroxamic Acid, a synthetic drug derived from hydroxylamine and ethyl acetate, is similar in structure to urea. In the urine, it acts as an antagonist of the bacterial enzyme urease. This inhibits the hydrolysis of urea and production of ammonia in urine infected with urea-splitting organisms, leading to a decrease in pH and ammonia levels. As antimicrobial agents are more effective in such conditions, the effectiveness of these agents is amplified, resulting in a higher cure rate. Acetohydroxamic Acid has no direct antimicrobial action and does not acidify urine directly. It is used, in addition to antibiotics or medical procedures, to treat chronic urea-splitting urinary infections. Urease Inhibitor (Code: N0000175611) Urease Inhibitors (Code: N0000175087) Enzyme Inhibitors (Code: D004791) 1983-05-31 FDA HAE
Click to view hydroxycarbamide Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16759856) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16759856) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16759856) Ribonucleoside-diphosphate reductase subunit M2 (Organism: Homo sapiens, class: Enzyme, accessions: P31350, gene: RRM2, swissprot: RIR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15670581) Ribonucleoside-diphosphate reductase large subunit (Organism: Homo sapiens, class: Enzyme, accessions: P23921, gene: RRM1, swissprot: RIR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15670581) Hydroxyurea is an antimetabolite. The precise mechanism by which hydroxyurea produces its antineoplastic effects cannot, at present, be described. The reports of various studies in tissue culture in rats and humans lend support to the hypothesis that hydroxyurea causes an immediate inhibition of DNA synthesis by acting as a ribonucleotide reductase inhibitor, without interfering with the synthesis of ribonucleic acid or of protein. This hypothesis explains why, under certain conditions, hydroxyurea may induce teratogenic effects. Hydroxyurea is indicated for the treatment of resistant chronic myeloid leukemia or locally advanced squamous cell carcinomas of the head and neck (excluding the lip) in combination with chemoradiation. antineoplastic agent (Code: CHEBI:35610) immunomodulator (Code: CHEBI:50846) Antimetabolite (Code: N0000180853) Urea (Code: N0000006999) Antineoplastic Agents (Code: D000970) Antisickling Agents (Code: D000986) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Nucleic Acid Synthesis Inhibitors (Code: D019384) 1967-12-07 FDA NHY
Click to view propylene glycol Propylene glycol (1, 2-propanediol) is an organic compound (a diol alcohol), usually a tasteless, odorless, and colorless clear oily liquid that is hygroscopic and miscible with water, acetone, and chloroform. Propylene glycol is used as a solvent for intravenous, oral, and topical pharmaceutical preparations It is generally considered safe. However in large doses it can be toxic, especially if given over a short period of time. Propylene glycol is metabolized by the liver to form lactate, acetate, and pyruvate. Propylene glycol toxicity includes development of serum hyperosmolality, lactic acidosis, and kidney failure. It has been suggested that proximal tubular necrosis is the cause of acute kidney injury from propylene glycol. Propylene glycol induced intoxication can also mimic sepsis or systemic inflammatory response syndrome (SIRS). Propylene glycol also is used for the temporary relief of burning and irritation due to dryness of the eye. protic solvent (Code: CHEBI:48356) Pharmaceutic Aids (Code: D010592) Pharmaceutical Vehicles (Code: D014677) Solvents (Code: D012997) PGO
PGR
Click to view mercaptamine cystine (Organism: None, class: Unnatural amino acid, accessions: None, gene: None, swissprot: None) cleavage (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200740s000lbl.pdf) Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/2829860) Mercaptamine (cysteamine) is a cystine-depleting agent which lowers the cystine content of cells in patients with cystinosis. Cysteamine acts as a cystine-depleting agent by converting cystine to cysteine and cysteine-cysteamine mixed disulfides and reduces corneal cystine crystal accumulation. Mercaptamine indicated for the treatment of corneal cystine crystal accumulation in patients with cystinosis. Cystine Depleting Agents (Code: D065104) Cystine Depleting Agent (Code: N0000187051) Cystine Disulfide Reduction (Code: N0000175549) 1994-08-15 FDA DHL
Click to view dimethyl sulfoxide Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159803) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159803) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159803) Dimethyl sulfoxide (DMSO) is a highly polar organic liquid, that is used widely as a chemical solvent. Because of its ability to penetrate biological membranes, it is used as a vehicle for topical application of pharmaceuticals. It is also used to protect tissue during cryopreservation. The mechanism of dimethyl sulfoxide's actions is not well understood. Dimethyl sulfoxide shows a range of pharmacological activity including analgesia and anti-inflammation. Dimethyl sulfoxide is indicated for the symptomatic relief of patients with interstitial cystitis. polar aprotic solvent (Code: CHEBI:48358) non-narcotic analgesic (Code: CHEBI:35481) antidote (Code: CHEBI:50247) Antioxidants (Code: D000975) Cryoprotective Agents (Code: D003451) Free Radical Scavengers (Code: D016166) Protective Agents (Code: D020011) Solvents (Code: D012997) 1978-04-04 FDA DMS
Click to view fomepizole Alcohol dehydrogenase (Organism: Homo sapiens, class: Enzyme, accessions: P00325|P07327|P00326, gene: ADH1A|ADH1B|ADH1C, swissprot: ADH1A_HUMAN|ADH1B_HUMAN|ADH1G_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00041975.PDF) Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. Fomepizole is indicated as an antidote for ethylene glycol (such as antifreeze) or methanol poisoning, or for use in suspected ethylene glycol or methanol ingestion, either alone or in combination with hemodialysis. antidote (Code: CHEBI:50247) protective agent (Code: CHEBI:50267) Antidotes (Code: D000931) Protective Agents (Code: D020011) 1997-12-04 FDA 4PZ
Click to view piperazine Piperazine is a cyclic organic compound possessing two nitrogen atoms in opposite positions within a 6-member heterocyclic ring that serves as a backbone for piperazine derivatives and acts as a gamma-amino-butyric acid (GABA) receptor agonist in nematodes, with potential anti-helminthic activity. Upon administration, piperazine binds to the GABA inhibitory receptors in susceptible nematodes, thereby inducing chloride channel opening and hyperpolarization. This results in paralysis of the worm musculature and allows normal peristalsis to dislodge the worm from the intestinal lumen, which causes the worm to be expelled from the body. Unlike vertebrates where GABA is restricted to the central nervous system (CNS), the GABA receptors in helminths are also expressed in the peripheral nervous system. Piperazine was first introduced as an anthelmintic in 1953. Piperazine has been withdrawn from use on the grounds that other more effective and less toxic drugs are now available. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) 1954-07-12 FDA PZE
Click to view cyverine Cyverine is an antispasmodic drugs. It is used for the treatment of gastric ulcer.
Click to view deanol Deanol (dimethylaminoethanol (DMAE) or dimethylethanolamine (DMEA)) holds tertiary amine and primary alcohol groups as functional groups. Deanol has been used in the treatment of attention deficit-hyperactivity disorder (ADHD), Alzheimer's disease, autism, and tardive dyskinesia. It has been also used as an ingredient in skin care, and in cognitive function- and mood-enhancing products. The mechanism of action is not well understood. Now deanol is used for the treatment of general fatigue (asthenia). curing agent (Code: CHEBI:75358) Anti-Dyskinesia Agents (Code: D018726) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1972-09-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view benzyl alcohol Benzyl Alcohol is a colorless liquid with a sharp burning taste and slight odor. Benzyl Alcohol is an aromatic alcohol used in a wide variety of cosmetic formulations as a fragrance component, preservative, solvent, and viscosity-decreasing agent. Benzyl Alcohol is metabolized to Benzoic Acid, which reacts with glycine and excreted as hippuric acid in the human body. Acceptable daily intakes were established by the World Health Organization at 5 mg/kg for Benzyl Alcohol. It is used as a local anesthetic and to reduce pain associated with Lidocaine injection. Also, it is used in the manufacture of other benzyl compounds, as a pharmaceutical aid, and in perfumery and flavoring. Benzyl alcohol is approved for the treatment of head lice. The drug acts on head lice by inhibiting them from closing their respiratory spiracles, allowing the vehicle to obstruct the spiracles and causing the lice to asphyxiate. solvent (Code: CHEBI:46787) fragrance (Code: CHEBI:48318) Pediculicide (Code: N0000181811) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2009-04-09 FDA 010
Click to view lactic acid Lactic Acid is the racemic isomer of lactic acid, the biologically active isoform in humans. Lactic acid or lactate is produced during fermentation from pyruvate by lactate dehydrogenase. This reaction, in addition to producing lactic acid, also produces nicotinamide adenine dinucleotide (NAD) that is then used in glycolysis to produce energy source adenosine triphosphate (ATP). Lactic Acid is primarily indicated as a source of bicarbonate for prevention or control of mild to moderate metabolic acidosis in patients with restricted oral intake whose oxidative processes are not seriously impaired. Sodium Lactate is most commonly associated with an E number of “E325” Sodium Lactate blends are commonly used in meat and poultry products to extend shelf life and increase food safety. 2006-10-25 FDA LAC
2OP
Click to view glycerol Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/9113273) Glycerol is a triol with a structure of propane substituted at positions 1, 2 and 3 by hydroxy groups. Glycerol is commonly classified as an osmotic laxative but may act additionally or alternatively through its local irritant effects; it may also have lubricating and fecal softening actions. When administered rectally, glycerol exerts a hygroscopic and/or local irritant action, drawing water from the tissues into the feces and reflexively stimulating evacuation. Glycerol decreases intraocular pressure by creating an osmotic gradient between the blood and intraocular fluid, causing fluid to move out of the aqueous and vitreous humors into the bloodstream. It is used as a solvent, emollient, pharmaceutical agent, and sweetening agent. solvent (Code: CHEBI:46787) detergent (Code: CHEBI:27780) Non-Standardized Chemical Allergen (Code: N0000185370) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Increased IgG Production (Code: N0000185001) Allergens (Code: N0000171131) Glycerol (Code: N0000006566) Cryoprotective Agents (Code: D003451) Protective Agents (Code: D020011) Solvents (Code: D012997) 1979-01-31 ANSM (French National Agency for Medicines and Health Products Safety) GOL
Click to view methylpentynol Methylpentynol is a tertiary hexanol with hypnotic, sedative and anticonvulsant effects. It was used for the treatment of insomnia and as sedaive agent, but its use was quickly phased out in response to newer drugs with more favorable safety profiles. Methylpentynol is no longer available.
Click to view secretin porcine stimulate pancreatic ductal cells to secrete pancreas fluid in large volumes that contain bicarbonate 2002-04-04 FDA
Click to view loxoprofen Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: ) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: ) Loxoprofen is a propionic acid derivative and a non-steroidal anti-inflammatory drug. After oral administration loxoprofen sodium hydrate is absorbed from the gastrointestinal tract as an unchanged compound with only a modest gastric-mucosal irritation. It is then rapidly biotransformed into the active metabolite trans-OH form (SRS coordination) with a potent inhibitory effect on prostaglandin biosynthesis to exert its pharmacologic effects. It is used to treat rheumatoid arthritis, osteoarthritis, to reduce pain and inflammation after surgery, wounds and tooth removal. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) prodrug (Code: CHEBI:50266) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2005-12-22 PMDA
Click to view aminopicoline Nitric oxide synthase, brain (Organism: Homo sapiens, class: Enzyme, accessions: P29475, gene: NOS1, swissprot: NOS1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8937711) Nitric oxide synthase, endothelial (Organism: Homo sapiens, class: Enzyme, accessions: P29474, gene: NOS3, swissprot: NOS3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8937711) Nitric oxide synthase, inducible (Organism: Homo sapiens, class: Enzyme, accessions: P35228, gene: NOS2, swissprot: NOS2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8937711) Nitric oxide synthase, inducible (Organism: Mus musculus, class: Enzyme, accessions: P29477, gene: Nos2, swissprot: NOS2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8937711) Aminopicoline (2-Amino-4-methylpyridine) acts as ligand and forms methoxo-bridged copper(II) complexes. Aminopicoline is potent inhibitor of inducible nitric oxide synthase (iNOS) in vitro. Aminopicoline is used in the synthesis of 2-amino-4-methyl­pyridinium 2-hy­droxy­benzoate. BVF
Click to view glutaral Glutaral (glutaraldehyde) is used as an antimicrobial agent in sugar mills and as a fixing agent in the immobilisation of glucose isomerase enzyme preparations for use in the manufacture of high fructose corn syrup A polymerized isomer of glutaraldehyde known as polycycloglutaracetal is a fertilizer for aquatic plants. It is claimed that it provides a bioavailable source of carbon for higher plants that is not available to algae. Though not marketed as such due to federal regulations, the biocidal effect of glutaraldehyde kills most algae at concentrations of 0. 5 - 5. 0 ppm. These levels are not harmful to most aquatic fauna and flora. Adverse reactions have been observed by some aquarists at these concentrations in some aquatic mosses, liverworts, and vascular plants. Glutaraldehyde is a colorless liquid with a pungent odor used to disinfect medical and dental equipment. It is also used for industrial water treatment and as a chemical preservative. It is used as a tissue fixative in electron microscopy. It is employed as an embalming fluid, is a component of leather tanning solutions, and occurs as an intermediate in the production of certain industrial chemicals. Glutaraldehyde is frequently used in biochemistry applications as an amine-reactive homobifunctional crosslinker. The oligomeric state of proteins can be examined through this application. However, it is toxic, causing severe eye, nose, throat and lung irritation, along with headaches, drowsiness and dizziness. It is a main source of occupational asthma among health care providers. cross-linking reagent (Code: CHEBI:50684) Anti-Infective Agents (Code: D000890) Cross-Linking Reagents (Code: D003432) Disinfectants (Code: D004202) Fixatives (Code: D005404) Indicators and Reagents (Code: D007202) 1984-08-01 PMDA PTD
Click to view cycloserine Alanine racemase (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WQA9, gene: alr, swissprot: ALR_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12499203) D-alanine--D-alanine ligase (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WP31, gene: ddl, swissprot: DDL_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12499203) Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q9R1M7|Q8VHN2, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3A_RAT|NMD3B_RAT) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2157524) Cycloserine is a 4-amino-1,2-oxazolidin-3-one that has R configuration. It is an antibiotic produced by Streptomyces garyphalus or S. orchidaceus. Cycloserine suppresses the synthesis of bacterial wall by inhibitin two enzymes: alanine racemase and d-alanine ligase. Cycloserine is used as part of a multi-drug regimen for the treatment of tuberculosis when resistance to, or toxicity from, primary drugs has developed. NMDA receptor agonist (Code: CHEBI:64571) antiinfective agent (Code: CHEBI:35441) antitubercular agent (Code: CHEBI:33231) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Antibiotics, Antitubercular (Code: D000904) Antimetabolites (Code: D000963) Antitubercular Agents (Code: D000995) Noxae (Code: D009676) Renal Agents (Code: D012076) 1964-06-29 FDA 4AX
Click to view gamma-aminobutyric acid Gamma-aminobutyric acid receptor subunit rho-1 (Organism: Homo sapiens, class: Ion channel, accessions: P24046, gene: GABRR1, swissprot: GBRR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23294161) GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47870|P18507, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23294161) GABA-A receptor alpha-2/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P47870|P18507, gene: GABRA2|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23294161) Aminobutyric acid (GABA), a naturally occurring substance, which is a product of decarboxylation of the amino acid glutamate mediated by the synthesizing enzyme glutamic acid decarboxylase. GABA is a major inhibitory neurotransmitter of the brain and acts mainly through the GABAA receptor. GABA is locally produced by the pancreatic beta cells. GABAARs are also expressed in various immune cells, including T-cells, peripheral blood mononuclear cells, and exerted immune-inhibitory effects. GABA is sold as a dietary supplement. GABA Agents (Code: D018682) Neurotransmitter Agents (Code: D018377) FDA ABU
Click to view choline Choline O-acetyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P28329, gene: CHAT, swissprot: CLAT_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17144655) Choline/ethanolamine kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9Y259, gene: CHKB, swissprot: CHKB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19915674) Choline kinase alpha (Organism: Homo sapiens, class: Kinase, accessions: P35790, gene: CHKA, swissprot: CHKA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19915674) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12089365) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10385678) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10385678) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9632645) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9618255) Solute carrier family 22 member 4 (Organism: Homo sapiens, class: Transporter, accessions: Q9H015, gene: SLC22A4, swissprot: S22A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215651) Choline transporter-like protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q8WWI5, gene: SLC44A1, swissprot: CTL1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16319125) Vesicular acetylcholine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q62666, gene: Slc18a3, swissprot: VACHT_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15485505) Choline is a major part of the polar head group of phosphatidylcholine. Phosphatidylcholine's role in the maintenance of cell membrane integrity is vital to all of the basic biological processes: information flow, intracellular communication and bioenergetics. Inadequate choline intake would negatively affect all these processes. Choline is also a major part of sphingomyelin also important for the maintenance of cell structure and function. Choline deficiency in cell culture causes apoptosis or programmed cell death. This appears to be due to abnormalities in cell membrane phosphatidylcholine content and an increase in ceramide, a precursor, as well as a metabolite, of sphingomyelin. Ceramide accumulation, which is caused by choline deficiency, appears to activate Caspase that mediates apoptosis. Betaine or trimethylglycine is derived from choline via an oxidation reaction. Choline is a precursor to acetylcholine. Choline is also needed for gallbladder regulation, liver function and lecithin (a key lipid) formation. Adequate acetylcholine levels in the brain are believed to be protective against certain types of dementia, including Alzheimer's disease. Choline is used for nutritional supplementation, also for treating dietary shortage or imbalance. Antimetabolites (Code: D000963) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Lipotropic Agents (Code: D008082) Nootropic Agents (Code: D018697) CHT
Click to view nicotinyl alcohol Nicotinyl alcohol is an alcohol analog of nicotinic acid which is a direct-acting peripheral vasodilator that causes flushing and may decrease blood pressure. Nicotinyl alcohol (pyridylcarbinol) is rapidly oxidized to nicotinic acid. Nicotinyl alcohol is used as a vasodilator agent and an antilipemic drug. (See: nicotinic acid) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1964 CDSCO (INDIA) PYF
Click to view resorcinol Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501600) Prostaglandin G/H synthase 1 (Organism: Ovis aries, class: Enzyme, accessions: P05979, gene: PTGS1, swissprot: PGH1_SHEEP) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15568761) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase (Organism: Dicentrarchus labrax, class: Unclassified, accessions: Q2PCB5, gene: ca, swissprot: Q2PCB5_DICLA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21669522) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Resorcinol is a benzenediol that is benzene dihydroxylated at positions 1 and 3. It is used as an antiseptic and disinfectant in topical pharmaceutical products in the treatment of skin disorders and infections such as acne, seborrheic dermatitis, eczema, psoriasis, corns, calluses, and warts. 1956-02-01 Spanish Agency of Medicines and Medical Products (AEMPS) RCO
Click to view hydroquinone Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase (Organism: Dicentrarchus labrax, class: Unclassified, accessions: Q2PCB5, gene: ca, swissprot: Q2PCB5_DICLA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501600) Polyphenol oxidase 2 (Organism: Agaricus bisporus, class: Enzyme, accessions: O42713, gene: PPO2, swissprot: PPO2_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19181523) Hydroquinone is a melanin synthesis inhibitor. It is prepared from the reduction of p-benzoquinone with sodium bisulfite. Hydroquinone is used as a topical application in skin whitening to reduce the color of skin.The FDA stated that hydroquinone cannot be ruled out as a potential carcinogen. skin lightening agent (Code: CHEBI:85046) Antioxidants (Code: D000975) Mutagens (Code: D009153) Noxae (Code: D009676) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) Depigmenting Activity (Code: N0000175851) Melanin Synthesis Inhibitor (Code: N0000175854) Melanin Synthesis Inhibitors (Code: N0000175850) 2002-01-18 FDA HQE
Click to view histamine Histamine H4 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9H3N8, gene: HRH4, swissprot: HRH4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21044842) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12626648) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21044842) Histamine H3 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5N1, gene: HRH3, swissprot: HRH3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21044842) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12089365) Histamine is a depressor amine derived by enzymatic decarboxylation of histidine. Histamine physiological functions are mediated by four 7-transmembrane G protein-coupled receptors (H1R, H2R, H3R, H4R) that are all targets of pharmacological intervention. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and a centrally acting neurotransmitter. Phosphate salt of histamine was used as a diagnostic aid for evaluation of gastric acid secretory function. In addition, this compound is used as a positive control in evaluation of allergenic (immediate hypersensitivity or "Type I") skin testing. Histamine Agents (Code: D018494) Histamine Agonists (Code: D017442) Neurotransmitter Agents (Code: D018377) 1939-04-25 FDA HSM
Click to view betazole Betazole is a histamine H2 receptor agonist with diagnostic application. Betazole selectively targets and binds to the H2 receptor, thereby mimicking the effect of histamine on these receptors. This may lead to an increase in gastric secretions. Betazole can be used in gastric function tests. histamine agonist (Code: CHEBI:35678) diagnostic agent (Code: CHEBI:33295) gastrointestinal drug (Code: CHEBI:55324) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Agonists (Code: D017442) Neurotransmitter Agents (Code: D018377) 1982-01-01 FDA
Click to view thiamazole Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9172960) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9172960) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9172960) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9172960) Thyroid peroxidase (Organism: Sus scrofa, class: Enzyme, accessions: P09933, gene: TPO, swissprot: PERT_PIG) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10365684) Thiamazole is a thionamide antithyroid agent that inhibits the synthesis of thyroid hormones. Thiamazole is indicated for the treatment of hyperthyroidism; for the amelioration of hyperthyroid symptoms in preparation for thyroidectomy or radioactive iodine therapy. antithyroid drug (Code: CHEBI:50671) Antithyroid Agents (Code: D013956) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Thyroid Hormone Synthesis Inhibitor (Code: N0000175918) Thyroid Hormone Synthesis Inhibitors (Code: N0000175917) 1950-06-21 FDA MMZ
Click to view tuaminoheptane Tuaminoheptane is a vasoconstrictor and a sympathomimetic amine. Tuaminoheptane acts similarly to ephedrine. Tuaminoheptane is used as a nasal decongestant in combination with other drugs. 1983-04-22 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view methylhexaneamine Methylhexaneamine is an amphetamine derivative. It was used as a nasal decongestant. Now methylhexaneamine is used as a dietary supplement with stimulant properties.
Click to view cacodylic acid Cacodylic acid (dimethylarsinic acid) is classified as a member of the Pentaorganoarsanes. Cacodylic acid induces an organ-specific lesion-single strand breaks in DNA. Mechanistic studies have suggested that this damage is due mainly to the peroxyl radical of cacodylic acid and production of active oxygen species by pulmonary tissues. Multi-organ initiation-promotion studies have demonstrated that cacodylic acid acts as a promotor of urinary bladder, kidney, liver and thyroid gland cancers in rats and as a promotor of lung tumors in mice. Cacodylic acid is used as a buffering agent in the preparation and fixation of biological samples for electron microscopy. Also cacodylic acid is used as a non-selective herbicide and defoliant for general weed control. Herbicides (Code: D006540) Pesticides (Code: D010575) CAC
CAD
Click to view fumaric acid Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19962903) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19962903) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19962903) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19962903) Transmembrane prolyl 4-hydroxylase (Organism: Homo sapiens, class: Enzyme, accessions: Q9NXG6, gene: P4HTM, swissprot: P4HTM_HUMAN) inhbiitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17182618) Fumaric acid, naturally found in organisms, is a well-known intermediate of the citric acid cycle. Fumaric acid has been identified as an oncometabolite or an endogenous, cancer causing metabolite. High levels of this organic acid can be found in tumors or biofluids surrounding tumors. Oncogenic action of fumarate appears to due to its ability to inhibit prolyl hydroxylase-containing enzymes. Fumaric acid is found to be associated with fumarase deficiency, which is an inborn error of metabolism. food acidity regulator (Code: CHEBI:64049) FUM
Click to view succinic acid Succinate receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q9BXA5, gene: SUCNR1, swissprot: SUCR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15141213) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11306713) Succinic acid is a dicarboxylic acid, which has multiple biological roles as a metabolic intermediate being converted into fumarate by the enzyme succinate dehydrogenase in complex 2 of the electron transport chain which is involved in making ATP, and as a signaling molecule reflecting the cellular metabolic state. Succinate is generated in mitochondria via the tricarboxylic acid cycle (TCA), an energy-yielding process shared by all organisms. Succinate can exit the mitochondrial matrix and function in the cytoplasm as well as the extracellular space, changing gene expression patterns, modulating epigenetic landscape or demonstrating hormone-like signaling. Dysregulation of succinate synthesis, and therefore ATP synthesis, happens in some genetic mitochondrial diseases, such as Leigh's disease, and Mela's disease and degradation can lead to pathological conditions, such as malignant transformation, inflammation and tissue injury. Succinic acid is a precursor to some polyesters and a component of some alkyd resins. Succinic acid is used primarily as an acidity regulator in the food and beverage industry. anti-ulcer drug (Code: CHEBI:49201) nutraceutical (Code: CHEBI:50733) 1971-11-16 FDA SIN
Click to view betaine Betaine is a naturally occurring compound that has been of interest for its role in osmoregulation. Betaine acts as a methyl group donor in the remethylation of homocysteine to methionine in patients with homocystinuria. Betaine occurs naturally in the body. It is a metabolite of choline and is present in small amounts in foods such as beets, spinach, cereals, and seafood. Betaine is indicated for the treatment of homocystinuria to decrease elevated homocysteine blood concentrations. Included within the category of homocystinuria are cystathionine beta-synthase (CBS) deficiency, 5,10-methylenetetrahydrofolate reductase (MTHFR) deficiency, cobalamin cofactor metabolism (cbl) defect. Antimetabolites (Code: D000963) Gastrointestinal Agents (Code: D005765) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Lipotropic Agents (Code: D008082) Methylating Activity (Code: N0000175804) Methylating Agent (Code: N0000175805) 1996-10-25 FDA BET
Click to view aminohydroxybutyric acid Gamma-aminobutyric acid receptor subunit rho-1 (Organism: Homo sapiens, class: Ion channel, accessions: P24046, gene: GABRR1, swissprot: GBRR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23019493) Aminohydroxybutyric acid (or gamma-Amino-beta-hydroxybutyric acid) is an endogenous ligand found in the central nervous system in mammals. Aminohydroxybutyric acid is a derivative of the neurotransmitter GABA. Aminohydroxybutyric acid is used for the treatment of stress and anxiety, for improvement learning and boost memory function. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Anticonvulsants (Code: D000927) 1961-06-27 Italian Medicines Agency (AIFA)
Click to view oxymethurea Oxymethurea is an antiseptic included in multi-ingredient preparations intended for the topical treatment of ear infections.
Click to view noxytiolin Noxythiolin is local antibacterial agent that probably acts by releasing formaldehyde in aqueous solutions. It is used for irrigation of infected body cavities - bladder, peritoneum, etc. and as a spray for burns. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 1977-02-03 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view trometamol Trometamol is a proton acceptor with a pK of 7.8, it is an effective buffer that can be used to maintain the pH of body fluids. Trometamol is indicated for the prevention and correction of metabolic acidosis. Trometamol also acts as an osmotic diuretic, increasing urine flow, urinary pH, and excretion of fixed acids, carbon dioxide and electrolytes. Buffers (Code: D002021) Excipients (Code: D005079) Pharmaceutic Aids (Code: D010592) Pharmaceutical Vehicles (Code: D014677) 1965-12-16 FDA TRS
Click to view cysteine Cysteine is a non-essential sulfur-containing amino acid in humans, related to cystine, Cysteine is important for protein synthesis, detoxification, and diverse metabolic functions. Found in beta-keratin, the main protein in nails, skin, and hair, Cysteine is important in collagen production, as well as skin elasticity and texture. Also required in the manufacture of amino acid taurine, Cysteine is a component of the antioxidant glutathione, and plays a role in the metabolism of essential biochemicals such as coenzyme A, heparin, and biotin. Amino Acid (Code: N0000175780) Amino Acids (Code: N0000006806) 1986-10-22 FDA CYS
DCY
Click to view nicotinamide Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081432) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081432) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081432) NAD-dependent protein deacetylase sirtuin-2 (Organism: Homo sapiens, class: Enzyme, accessions: Q8IXJ6, gene: SIRT2, swissprot: SIR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17149860) NAD-dependent deacetylase sirtuin 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q9NTG7, gene: SIRT3, swissprot: SIR3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19700324) NAD-dependent protein deacetylase sirtuin-1 (Organism: Homo sapiens, class: Enzyme, accessions: Q96EB6, gene: SIRT1, swissprot: SIR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19700324) NAD-dependent protein deacylase sirtuin-5, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9NXA8, gene: SIRT5, swissprot: SIR5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24900427) Nicotinamide ia an important compound functioning as a component of the coenzyme NAD. Its primary significance is in the prevention and/or cure of blacktongue and pellagra. Most animals cannot manufacture this compound in amounts sufficient to prevent nutritional deficiency and it therefore must be supplemented through dietary intake. neuroprotective agent (Code: CHEBI:63726) anti-inflammatory agent (Code: CHEBI:67079) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) Vitamin B Complex (Code: D014803) 1953-02-20 FDA NCA
Click to view nicotinic acid Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081432) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12724351) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Hydroxycarboxylic acid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDS4, gene: HCAR2, swissprot: HCAR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17358052) Hydroxycarboxylic acid receptor 2 (Organism: Rattus norvegicus, class: GPCR, accessions: Q80Z39, gene: Hcar2, swissprot: HCAR2_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19309152) Nicotinic acid (niacin) is a water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has pellagra-curative, vasodilating, and antilipemic properties. Niacin in gram doses reduces LDL-C, Apo B, Lp(a), TG, and TC, and increases HDL-C. The mechanism by which niacin alters lipid profiles is not completely understood and may involve several actions, including partial inhibition of release of free fatty acids from adipose tissue, and increased lipoprotein lipase activity. Niacin decreases the rate of hepatic synthesis of VLDL-C and LDL-C, and does not appear to affect fecal excretion of fats, sterols, or bile acids. Nicotinic acid is indicated to reduce elevated TC, LDL-C, Apo B and TG, and to increase HDL-C in patients with primary hyperlipidemia and mixed dyslipidemia, to reduce the risk of recurrent nonfatal myocardial infarction in patients with a history of myocardial infarction and hyperlipidemia. In combination with a bile acid binding resin nicotinic acid slows progression or promotes regression of atherosclerotic disease in patients with a history of coronary artery disease and hyperlipidemia. Nicotinic acid also indicated to reduce TG in adult patients with severe hypertriglyceridemia. B vitamin (Code: CHEBI:75769) vasodilator agent (Code: CHEBI:35620) antidote (Code: CHEBI:50247) antilipemic drug (Code: CHEBI:35679) Nicotinic Acid (Code: N0000175594) Nicotinic Acids (Code: N0000007641) Antimetabolites (Code: D000963) Cardiovascular Agents (Code: D002317) Growth Substances (Code: D006133) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Micronutrients (Code: D018977) Vitamins (Code: D014815) Vasodilator Agents (Code: D014665) Vitamin B Complex (Code: D014803) 1957-07-24 FDA NIO
Click to view mecysteine Mecysteine is known as a mucolytic agent. Mecysteine works by breaking some of the chemical bonds between the molecules in mucus. Mecysteine is used as an adjunct in the management of conditions such as chronic obstructive pulmonary disease, when characterised by thick viscid or glutinous mucus, including the symptomatic relief of cough with sputum. Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) 2006-02-24 UK Medicines and Healthcare Products Regulatory Agency (MHRA) CMT
Click to view pyrazinamide Aldehyde oxidase 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: Q9Z0U5, gene: Aox1, swissprot: AOXA_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8216357) Probable fatty acid synthase Fas (Fatty acid synthetase) (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P95029, gene: fas, swissprot: P95029_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17485499) Pyrazinamide is a synthetic pyrazinoic acid amide derivative with bactericidal property. Pyrazinamide is indicated for the initial treatment of active tuberculosis in adults and children. antitubercular agent (Code: CHEBI:33231) prodrug (Code: CHEBI:50266) Antimycobacterial (Code: N0000175483) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antitubercular Agents (Code: D000995) 1971-06-03 FDA PZA
Click to view guaiacol Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231207) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231207) Guaiacol is a naturally occurring organic compound. Although it is biosynthesized by a variety of organisms, this yellowish aromatic oil is usually derived from guaiacum or wood creosote. Guaiacol is used as a reducing co-substrate for COX reactions. It is mainly used as expectorant, antiseptic. expectorant (Code: CHEBI:77035) 2006-10-27 UK Medicines and Healthcare Products Regulatory Agency (MHRA) JZ3
Click to view dimercaprol arsenic (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: https://www.ncbi.nlm.nih.gov/pubmed/20717537) cadmium (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: https://www.ncbi.nlm.nih.gov/pubmed/20717537) mercury (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: https://www.ncbi.nlm.nih.gov/pubmed/20717537) Dimercaprol is an anti-gas warfare agent that is effective against Lewisite (dichloro(2-chlorovinyl)arsine) and formerly known as British Anti-Lewisite or BAL. It acts as a chelating agent and is used in the treatment of arsenic, gold, and other heavy metal poisoning. Metal Chelating Activity (Code: N0000175472) Metal Chelator (Code: N0000175473) Chelating Agents (Code: D002614) Sequestering Agents (Code: D064449) 1946-05-06 FDA 9DC
Click to view foscarnet DNA polymerase catalytic subunit (Organism: Human herpesvirus 1 (strain 17), class: Enzyme, accessions: P04293, gene: None, swissprot: DPOL_HHV11) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020068s023lbl.pdf) Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72549, gene: pol, swissprot: Q72549_9HIV1) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15189038) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15745821) Foscarnet is a phosphonoformic acid. Foscarnet is an antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet exerts its antiviral activity by a selective inhibition at the pyrophosphate binding site on virus-specific DNA polymerases at concentrations that do not affect cellular DNA polymerases. Foscarnet does not require activation (phosphorylation) by thymidine kinase or other kinases. Foscarnet also shows activity against human herpesviruses and HIV. antiviral drug (Code: CHEBI:36044) DNA Polymerase Inhibitors (Code: N0000020060) Pyrophosphate Analog (Code: N0000175469) Pyrophosphate Analog DNA Polymerase Inhibitor (Code: N0000175470) Chelating Activity (Code: N0000000087) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 1991-09-27 FDA PPF
Click to view fluroxene Fluroxene, is a volatile, inhalational anesthetic. It was voluntarily withdrawn from the market in 1974 due to its potential flammability and accumulating evidence that it could cause organ toxicity.
Click to view phloroglucinol Prostaglandin G/H synthase 1 (Organism: Ovis aries, class: Enzyme, accessions: P05979, gene: PTGS1, swissprot: PGH1_SHEEP) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16252923) Beta-secretase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P56817, gene: BACE1, swissprot: BACE1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20462757) Phloroglucinol is a phenol derivative with antispasmodic properties that is used primarily as a laboratory reagent. The mechanism of action is most likely based on the direct inhibition of the voltage-dependent calcium channels of smooth muscle; however, the modulation of prostaglandin or nitric oxide release has also been suggested. Although it has long been used in clinical practice as an antispasmodic for painful urogenital and gastrointestinal conditions, in an early study on anesthetized rats, phloroglucinol was found to be inactive toward the contraction of the duodenum, ileum and colon. However in Irritable bowel syndrome (IBS) patients iv phloroglucinol effectively reduced postprandial rectosigmoid motility increases after a test meal, compared to placebo. Phloroglucinol is indicated for the treatment of pain in the intestine, bile ducts, bladder and uterus caused by spasm. Indicators and Reagents (Code: D007202) 2007-10-30 ANSM (French National Agency for Medicines and Health Products Safety) 13X
Click to view orazamide Orazamide is composed of one molecule of 5-aminoimidazole-4-carboxamide (AICA), one molecule of orotic acid and two molecules of water. The nucleoside of AICA is internalized and becomes phosphorylated by adenosine kinase to form AICAR mono-phosphate, an intermediate in the late steps of de novo purine biosynthesis. In hepatocytes, AICA can inhibit the fatty acid synthesis, sterol synthesis, and gluconeogenesis. Orazamide is used clinically for the treatment of hepatitis and cirrhosis. 1971 YEAR INTRODUCED 5AC
Click to view chloral hydrate GABA-A receptor alpha-2/beta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P18505, gene: GABRA2|GABRB1, swissprot: GBRA1_HUMAN|GBRB1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) Chloral Hydrate is a synthetic monohydrate of chloral with sedative, hypnotic, and anticonvulsive properties. Chloral hydrate is converted to the active compound trichloroethanol by hepatic alcohol dehydrogenase. The agent interacts with various neurotransmitter-operated ion channels, thereby enhancing gamma-aminobutyric acid (GABA)-A receptor mediated chloride currents and inhibiting amino acid receptor-activated ion currents. In addition, chloral hydrate enhances the agonistic effects of glycine receptors, inhibits AMPA-induced calcium influx in cortical neurons, and facilitates 5-HT 3 receptor-mediated currents in ganglionic neurons. Overall, this results in a depressive effect on the central nervous system. Chloral Hydrate is used in the treatment of insomnia. The safety margin is too narrow for chloral hydrate to be used as a general anesthetic in humans, but it is commonly used for that purpose in animal experiments. It is no longer considered useful as an anti-anxiety medication. sedative (Code: CHEBI:35717) general anaesthetic (Code: CHEBI:38869) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1840-01-01 YEAR INTRODUCED
Click to view pyrithione Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22365761) Pyrithione is the common name of an organosulfur compound with molecular formula C5H5NOS. It exists as a pair of tautomers, the major form being the thione 1-hydroxy-2(1H)-pyridinethione and the minor form being the thiol 2-mercaptopyridine N-oxide. It is used to prepare zinc pyrithione, which is used primarily to treat dandruff and seborrhoeic dermatitis in medicated shampoos. (See: pyrithione zinc) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935)
Click to view thiouracil Nitric oxide synthase, brain (Organism: Rattus norvegicus, class: Enzyme, accessions: P29476, gene: Nos1, swissprot: NOS1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11094150) Thiouracil is a sulfur-containing uracil. Thiouracil occurs in seeds of Brassica and Crucifera species. An established antithyroid drug and highly selective inhibitor of nitric oxide synthase (NOS), thiouracil also covalently binds to dopaquinone, produced by tyrosinase catalyzed oxidation of tyrosine, thereby selectively accumulating in de novo-synthesized melanin in overactive melanin-producing cells and providing a means to localize melanoma cells. It is known to cause blood dyscrasias and suspected of terato- and carcinogenesis. Antithyroid Agents (Code: D013956) Cardiovascular Agents (Code: D002317) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Vasodilator Agents (Code: D014665) 3CJ
Click to view dichloroacetic acid [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial (Organism: Rattus norvegicus, class: Kinase, accessions: Q63065, gene: Pdk1, swissprot: PDK1_RAT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9405293) [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial (Organism: Rattus norvegicus, class: Kinase, accessions: Q64536, gene: Pdk2, swissprot: PDK2_RAT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9405293) [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrial (Organism: Homo sapiens, class: Kinase, accessions: Q15120, gene: PDK3, swissprot: PDK3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9405293) [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial (Organism: Rattus norvegicus, class: Kinase, accessions: O54937, gene: Pdk4, swissprot: PDK4_RAT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9405293) Dichloroacetic acid (dichloroacetate) is an acid analog of acetic acid. Salts of dichloroacetate are used as drugs since they inhibit the enzyme pyruvate dehydrogenase kinase. Dichloroacetate is a noncompetitive inhibitor of the endoplasmic reticulum enzyme HMG CoA reductase, which catalyzes the rate limiting step in cholesterol biosynthesis. dichloroacetate has been researched in adults, children, animals, and cells as a monotherapy as well as in combination with other therapies for the treatment of severe metabolic disorders including diabetes and hypercholesterolemia, lactic acidosis, certain heart conditions, and cancer. TF4
Click to view flucytosine Cytosine deaminase (Organism: Candida albicans, class: Enzyme, accessions: P78594, gene: FCA1, swissprot: FCA1_CANAX) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/017001s033lbl.pdf) Flucytosine is a fluorinated cytosine analog that is used as an antifungal agent. Inside the fungal cell, flucytosine is rapidly converted to fluorouracil by the enzyme cytosine deaminase. Fluorouracil exerts its antifungal activity through the subsequent conversion into several active metabolites, which inhibit protein synthesis by being falsely incorporated into fungal RNA or interfere with the biosynthesis of fungal DNA through the inhibition of the enzyme thymidylate synthetase. Flucytosine has been shown to be active against most strains of Candida albicans and Cryptococcus neoformans. Flucytosine is indicated only in the treatment of serious infections caused by susceptible strains of Candida and/or Cryptococcus. prodrug (Code: CHEBI:50266) Nucleoside Analog (Code: N0000175459) Nucleoside Analog Antifungal (Code: N0000175467) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antimetabolites (Code: D000963) Noxae (Code: D009676) 1971-11-26 FDA 1LD
Click to view vigabatrin 4-aminobutyrate aminotransferase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P80404, gene: ABAT, swissprot: GABT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020427s020,022006s022lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020427s020,022006s022lbl.pdf) Vigabatrin is a gamma-amino acid having a gamma-vinyl GABA structure.The precise mechanism of vigabatrin's anti-seizure effect is unknown, but it is believed to be the result of its action as an irreversible inhibitor of gamma-aminobutyric acid transaminase (GABA-T), the enzyme responsible for the metabolism of the inhibitory neurotransmitter GABA. This action results in increased levels of GABA in the central nervous system. Vigabatrin is indicated for the treatment of refractory complex partial seizures as adjunctive therapy and infantile spasms -monotherapy in infants 1 month to 2 years of age for whom the potential benefits outweigh the potential risk of vision loss. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) GABA Agents (Code: D018682) Neurotransmitter Agents (Code: D018377) 2009-08-21 FDA
Click to view metformin 5'-AMP-activated protein kinase subunit beta-1 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y478, gene: PRKAB1, swissprot: AAKB1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/14871885) Mitochondrial complex I (NADH dehydrogenase) (Organism: Homo sapiens, class: Enzyme, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22117616) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23435786) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23435786) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23435786) Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15842525) Metformin is an antihyperglycemic agent which improves glucose tolerance in patients with type 2 diabetes mellitus, lowering both basal and postprandial plasma glucose. Metformin decreases hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. With metformin therapy, insulin secretion remains unchanged while fasting insulin levels and day-long plasma insulin response may decrease. hypoglycemic agent (Code: CHEBI:35526) Biguanide (Code: N0000175565) Biguanides (Code: N0000007698) Hypoglycemic Agents (Code: D007004) 1995-03-03 FDA MF8
Click to view octodrine Octodrine is a stimulant that is structurally similar to amphetamine and is included in several so-called “pre-workout” and “fat-burning” supplements. Originally developed as a remedy to nasal congestion and as a possible anti-tumor drug, Octodrine has resurfaced as a key ingredient in dietary supplements for its stimulant and thermogenic benefits.
Click to view oxiniacic acid Oxiniacic acid is a nicotinic acid derivative and an antihyperlipidemic agent.
Click to view fluorouracil Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15901346) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18820913) Solute carrier family 22 member 8 (Organism: Mus musculus, class: Transporter, accessions: O88909, gene: Slc22a8, swissprot: S22A8_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15100168) Fluorouracil is an antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine with antineoplastic activity. Fluorouracil and its metabolites possess a number of different mechanisms of action. In vivo, fluoruracil is converted to the active metabolite 5-fluoroxyuridine monophosphate (F-UMP); replacing uracil, F-UMP incorporates into RNA and inhibits RNA processing, thereby inhibiting cell growth. Another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase, resulting in the depletion of thymidine triphosphate (TTP), one of the four nucleotide triphosphates used in the in vivo synthesis of DNA. Other fluorouracil metabolites incorporate into both RNA and DNA; incorporation into RNA results in major effects on both RNA processing and functions. Fluorouracil is used for the topical treatment of multiple actinic or solar keratoses, superficial basal cell carcinomas, for palliative management of some types of cancer, including colon, esophageal, gastric, rectum, breast, biliary tract, stomach, head and neck, cervical, pancreas, renal cell, and carcinoid. radiosensitizing agent (Code: CHEBI:132992) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Noxae (Code: D009676) 1962-04-25 FDA URF
Click to view aminolevulinic acid Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9637710) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9637710) Aminolevulinic acid is a porphyrin precursor. Photoactivation following topical application occurs when aminolevulinic acid (prodrug) is metabolized to protoporphyrin IX (PpIX), a photoactive compound which accumulates in the skin. When exposed to red light of a suitable wavelength and energy, PpIX is activated resulting in an excited state of porphyrin molecules. In the presence of oxygen, reactive oxygen species are formed which causes damage to cellular components, and eventually destroys the cells. Aminolevulinic acid is indicated for the lesion-directed and field-directed treatment of actinic keratoses of mild-to-moderate severity on the face and scalp. antineoplastic agent (Code: CHEBI:35610) photosensitizing agent (Code: CHEBI:47868) dermatologic drug (Code: CHEBI:50177) prodrug (Code: CHEBI:50266) Porphyrin Precursor (Code: N0000175846) Porphyrinogens (Code: N0000171207) Dermatologic Agents (Code: D003879) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) 1999-12-03 FDA FVT
Click to view leucine Large neutral amino acids transporter small subunit 3 (Organism: Homo sapiens, class: Transporter, accessions: O75387, gene: SLC43A1, swissprot: LAT3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12930836) Large neutral amino acids transporter small subunit 1 (Organism: Homo sapiens, class: Transporter, accessions: Q01650, gene: SLC7A5, swissprot: LAT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12930836) Sodium-coupled neutral amino acid transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q96QD8, gene: SLC38A2, swissprot: S38A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10930503) Sodium-coupled neutral amino acid transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q969I6, gene: SLC38A4, swissprot: S38A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11342143) Leucine is an alpha-amino acid used in the biosynthesis of proteins. Leucine is an essential hydrophobic amino acid. Leucine is an mTOR activator. It is a dietary amino acid with the capacity to directly stimulate muscle protein synthesis. As a dietary supplement, leucine has been found to slow the degradation of muscle tissue by increasing the synthesis of muscle proteins in aged rats. Long-term leucine supplementation does not increase muscle mass or strength in healthy elderly men. Leucine potently activates the mammalian target of rapamycin kinase that regulates cell growth. Infusion of leucine into the rat brain has been shown to decrease food intake and body weight via activation of the mTOR pathway. Leucine is also found in fish, meat, and poultry. In the pharmaceutical industry, L-leucine is used for parenteral and enteral nutrition and feeding, and is also used as a flavoring product and tablet lubricant in manufacturing. 1971-09-24 FDA LEU
DLE
Click to view aminocaproic acid Tissue-type plasminogen activator (Organism: Homo sapiens, class: Enzyme, accessions: P00750, gene: PLAT, swissprot: TPA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/015197s043,015230s035lbl.pdf) Aminocaproic acid is an antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties. Aminocaproic acid is useful in enhancing hemostasis when fibrinolysis contributes to bleeding. antifibrinolytic drug (Code: CHEBI:48675) hematologic agent (Code: CHEBI:50248) Antifibrinolytic Agent (Code: N0000175634) Decreased Fibrinolysis (Code: N0000175632) Antifibrinolytic Agents (Code: D000933) Coagulants (Code: D003029) Fibrin Modulating Agents (Code: D050299) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) 1964-06-03 FDA ACA
Click to view paraldehyde Paraldehyde is a hypnotic and sedative with anticonvulsant effects. It is believed to depress many levels of the central nervous system (CNS), including the ascending reticular activating system to cause an imbalance between inhibitory and facilitatory mechanisms. In sub-hypnotic doses, paraldehyde has anticonvulsant actions, although the dose margin between the anticonvulsant and hypnotic effects is small. At sub-anaesthetic doses, it is not an analgesic and may produce excitement or delirium in the presence of pain. Paraldehyde has been used as a sedative and hypnotic in a variety of clinical situations, although it has been largely replaced by safer and/ or more effective agents. It may also be used in the treatment of convulsive episodes arising from tetanus, status epilepticus and poisoning by convulsive drugs, when other agents are inappropriate or ineffective. Paraldehyde may be effective in reducing the anxiety associated with withdrawal from drugs such as narcotics or barbiturates, as well as in the management of acute agitation or delirium tremens due to alcohol withdrawal. Paraldehyde is only recommended for use in these conditions when other treatments are ineffective or deemed inappropriate. sedative (Code: CHEBI:35717) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 2009-08-31 Therapeutic Goods Administration (TGA)
Click to view ornithine G-protein coupled receptor family C group 6 member A (Organism: Homo sapiens, class: GPCR, accessions: Q5T6X5, gene: GPRC6A, swissprot: GPC6A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15576628) Ornithine is a non-essential and nonprotein amino acid, ornithine is critical for the production of the body's proteins, enzymes and muscle tissue. Ornithine plays a central role in the urea cycle and is important for the disposal of excess nitrogen (ammonia). Ornithine is the starting point for the synthesis of many polyamines such as putrescine and spermine. Ornithine supplements are claimed to enhance the release of growth hormone and to burn excess body fat. Ornithine is necessary for proper immune function and good liver function. Ornithine is a naturally occurring amino acid found in meat, fish, dairy and eggs. Ornithine is also a precursor of citrulline and arginine. Ornithine is used for nutritional supplementation, also for treating dietary shortage or imbalance. It has been claimed that ornithine improves athletic performance, has anabolic effects, has wound-healing effects, and is immuno-enhancing. 1979-11-16 ANSM (French National Agency for Medicines and Health Products Safety) ORN
ORD
Click to view prenderol Prenderol ia an anticonvulsant drug and it has a depressant action on multisynaptic reflexes. Prenderol has been used as a drug to relieve anxiety in patients with mental disorders. It has also been used to treat absence crisis. anticonvulsant (Code: CHEBI:35623)
Click to view aspartic acid Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q9R1M7|Q8VHN2, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3A_RAT|NMD3B_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15703381) Aspartate aminotransferase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P00505, gene: GOT2, swissprot: AATM_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/26902786) Aspartic acid (aspartate) is a non-essential alpha-amino acid that is used in the biosynthesis of proteins. Aspartic acid acts as a neurotransmitter by stimulation of the NMDA receptors. In medicine, aspartic acid was studied as an activator of brain L-asparaginase to treat opiate abstinence syndrom. Supplements of aspartic acid was shown to improve condition of newborns with jaundice due to inhibition of beta-glucuronidase. L-aspartate is formed by the transamination of the Krebs cycle intermediate oxaloacetate. The amino acid serves as a precursor for synthesis of proteins, oligopeptides, purines, pyrimidines, nucleic acids and L-arginine. L-aspartate is a glycogenic amino acid, and it can also promote energy production via its metabolism in the Krebs cycle. These latter activities were the rationale for the claim that supplemental aspartate has an anti-fatigue effect on skeletal muscle, a claim that was never confirmed. FDA ASP
IAS
Click to view timonacic Timonacic (4-Thiazolidinecarboxylic acid) is the product of condensation between cysteine and formaldehyde. Dietary timonacic slows the aging process in mammals and prolongs their life span. It exerts antioxidant and antineoplastic actions however its mechanism of action is elusive. Timonacic is hydrolyzed in the licer to N-formyl-cysteine which contains the free -SH group. Timonacic is used for the treatment of liver diseases. hepatoprotective agent (Code: CHEBI:62868) antidote (Code: CHEBI:50247) 1993-05-24 Office for Registration of Medicinal Products, Medical Devices and Biocidal Products (Poland) PRS
Click to view tranylcypromine Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/012342s064lbl.pdf) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/012342s064lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15049511) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15049511) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15049511) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11181487) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11181487) Tranylcypromine is a nonhydrazine monamine oxidase inhibitor. The mechanism of action of tranylcypromine as an antidepressant is not fully understood, but is presumed to be linked to potentiation of monoamine neurotransmitter activity in the central nervous system. Tranylcypromine is indicated for the treatment of major depressive disorder. antidepressant (Code: CHEBI:35469) anxiolytic drug (Code: CHEBI:35474) Monoamine Oxidase Inhibitor (Code: N0000175744) Anti-Anxiety Agents (Code: D014151) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1961-02-21 FDA GJZ
Click to view adenine Xanthine dehydrogenase/oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P47989, gene: XDH, swissprot: XDH_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17379526) Adenine is a purine base. Adenine is found in both DNA and RNA. Adenine is a fundamental component of adenine nucleotides. Adenine forms adenosine, a nucleoside, when attached to ribose, and deoxyadenosine when attached to deoxyribose; it forms adenosine triphosphate (ATP), a nucleotide, when three phosphate groups are added to adenosine. Adenosine triphosphate is used in cellular metabolism as one of the basic methods of transferring chemical energy between chemical reactions. Adenine is used for nutritional supplementation, also for treating dietary shortage or imbalance. 1980-06-11 FDA ADE
Click to view acetanilide Acetanilide is a fever-reducing drug. Acetanilide exhibited an unacceptable profile of toxic effects, the most alarming being cyanosis due to methemoglobinemia. Acetanilide is no longer used as a drug in its own right, although its primary metabolite, paracetamol, has been widely succesful. analgesic (Code: CHEBI:35480)
Click to view amfetamine Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00043799.PDF) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00043799.PDF) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00043799.PDF) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00043799.PDF) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/28936885) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9830022) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9618255) Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22037049) Amphetamine is a powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l-form (levamfetamine) has less central nervous system activity but stronger cardiovascular effects. L-Amphetamine succinate was sold between 1952 and 1955 under the brand name Cydril. Amphetamine is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity. Amphetamine is one of the more restricted controlled drugs. sympathomimetic agent (Code: CHEBI:35524) dopaminergic agent (Code: CHEBI:48560) adrenergic agent (Code: CHEBI:37962) dopamine uptake inhibitor (Code: CHEBI:51039) adrenergic uptake inhibitor (Code: CHEBI:35640) bronchodilator agent (Code: CHEBI:35523) Central Nervous System Stimulant (Code: N0000175739) Central Nervous System Stimulation (Code: N0000175729) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1955-09-09 FDA FRD
1WE
Click to view allopurinol Xanthine dehydrogenase/oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P47989, gene: XDH, swissprot: XDH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/016084s044lbl.pdf) Solute carrier family 22 member 8 (Organism: Mus musculus, class: Transporter, accessions: O88909, gene: Slc22a8, swissprot: S22A8_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15100168) Solute carrier family 22 member 7 (Organism: Mus musculus, class: Transporter, accessions: Q91WU2, gene: Slc22a7, swissprot: S22A7_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12065749) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/29342419) Allopurinol is a structural analogue of the natural purine base, hypoxanthine. It is an inhibitor of xanthine oxidase, the enzyme responsible for the conversion of hypoxanthine to xanthine and of xanthine to uric acid, the end product of purine metabolism in man. Allopurinol is metabolized to the corresponding xanthine analogue, oxipurinol (alloxanthine), which also is an inhibitor of xanthine oxidase. Allopurinol is indicated in the management of patients with signs and symptoms of primary or secondary gout (acute attacks, tophi, joint destruction, uric acid lithiasis, and/or nephropathy), in the management of patients with leukemia, lymphoma and malignancies who are receiving cancer therapy which causes elevations of serum and urinary uric acid levels and in the management of patients with recurrent calcium oxalate calculi. gout suppressant (Code: CHEBI:35845) Antimetabolites (Code: D000963) Antioxidants (Code: D000975) Antirheumatic Agents (Code: D018501) Enzyme Inhibitors (Code: D004791) Free Radical Scavengers (Code: D016166) Gout Suppressants (Code: D006074) Noxae (Code: D009676) Xanthine Oxidase Inhibitor (Code: N0000175698) Xanthine Oxidase Inhibitors (Code: N0000000206) 1966-08-19 FDA
Click to view pentaerythritol Pentaerythritol is a white crystalline polyhydric alcohol containing four primary hydroxyl groups. Pentaerythritol causes hyperhydration of the intestinal contents. Pentaerythritol is osmotically acting laxatives. It was used for treatment of constipation. 1991-07-01 ANSM (French National Agency for Medicines and Health Products Safety) 3SY
Click to view phenylpropanol Phenylpropanol (1-phenyl-1-propanol) is a choleretic agent.
Click to view phenelzine Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020682s010lbl.pdf) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020682s010lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16669850) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16669850) Membrane primary amine oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q16853, gene: AOC3, swissprot: AOC3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20690686) Phenelzine is a hydrazine derivative. Phenelzine is a potent inhibitor of monoamine oxidase by phenelzine relieves depressive symptoms by causing an increase in the levels of serotonin, norepinephrine, and dopamine in the neuron. Phenelzine is used in depressed patients clinically characterized as “atypical,” “nonendogenous,” or “neurotic.” These patients often have mixed anxiety and depression and phobic or hypochondriacal features. Monoamine Oxidase Inhibitor (Code: N0000175744) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) 1961-06-09 FDA
Click to view betahistine Histamine H3 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5N1, gene: HRH3, swissprot: HRH3_HUMAN) antagonist (Source: https://pdf.hres.ca/dpd_pm/00045254.PDF) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) partial agonist (Source: https://pdf.hres.ca/dpd_pm/00045254.PDF) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00045254.PDF) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00045254.PDF) Betahistine is is an antivertigo drug first used for treating vertigo assosicated with Meniere's disease. It is also commonly used for patients with balance disorders. Betahistine primarily acts as a histamine H1-agonist with 0. 07 times the activity of histamine. Stimulating the H1-receptors in the inner ear causes a vasodilatory effect and increased permeability in the blood vessels which results in reduced endolymphatic pressure. Betahistine is believed to act by reducing the asymmetrical functioning of sensory vestibular organs as well as by increasing vestibulocochlear blood flow. Doing so aids in decreasing symptoms of vertigo and balance disorders. Betahistine also acts as a histamine H3-receptor antagonist which causes an increased output of histamine from histaminergic nerve endings which can further increase the direct H1-agonist activity. Furthermore, H3-receptor antagonism increases the levels of neurotransmitters such as serotonin in the brainstem, which inhibits the activity of vestibular nuclei, helping to restore proper balance and decrease in vertigo symptoms. H1-receptor agonist (Code: CHEBI:71173) vasodilator agent (Code: CHEBI:35620) Cardiovascular Agents (Code: D002317) Histamine Agents (Code: D018494) Histamine Agonists (Code: D017442) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) 1970-06-08 Ministry of Health, Welfare and Sport (Netherlands)
Click to view isopromethazine Isopromethazine is an impurity of promethazine, an antihistamine used as an central nervous system depressant.
Click to view homonicotinic acid Hydroxycarboxylic acid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDS4, gene: HCAR2, swissprot: HCAR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12522134) Homonicotinic acid is a breakdown product of nicotine (and other tobacco alkaloids). Homonicotinic acid acid is an analog of nicotinic acid and used as a hypolipidemic agent. Italian Medicines Agency (AIFA)
Click to view bethanechol Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Bethanechol is a synthetic cholinergic agent with is structurally and pharmacologically related to acetylcholine. Bethanechol is a slowly hydrolysed muscarinic agonist with no nicotinic effects, it is used as its chloride salt to increase smooth muscle tone, as in the gastrointestinal tract following abdominal surgery, treatment of gastro-oesophageal reflux disease, and as an alternative to catheterisation in the treatment of non-obstructive urinary retention. muscarinic agonist (Code: CHEBI:38325) Cholinergic Muscarinic Agonist (Code: N0000175840) Cholinergic Muscarinic Agonists (Code: N0000000104) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Muscarinic Agonists (Code: D018721) Neurotransmitter Agents (Code: D018377) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) 1948-10-12 FDA
Click to view methyl nicotinate Methyl nicotinate is the methyl ester of niacin. Methyl nicotinate is present in guava fruit, papaya, strawberry, soursop (Annona muricata), beer, grape brandy, coffee, roasted filbert, roasted peanut and Bourbon vanill. The action of methyl nicotinate as a rubefacient is thought to involve peripheral vasodilation. Methyl nicotinate is used in combination with other drugs for the symptomatic treatment of muscle stiffness, muscular rheumatism, lumbago, sciatica, fibrositis, sprains and chilblains. 1983-12-29 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view salicylamide Salicylamide is a non-prescription drug with analgesic and antipyretic properties. It has similar medicinal uses to aspirin. Salicylamide blocks cyclooxygenase, breaks the metabolism of arachidonic acid, reduces the amount of prostaglandins both in the inflammation focus and in healthy tissues, suppresses the exudative and proliferative phase of inflammation. Reduces the permeability of capillaries; stabilizes the lysosomal membranes; inhibits the production of macroergers (primarily ATP) in the processes of oxidative phosphorylation; inhibits synthesis or inactivates mediators of inflammation, incl. histamine, bradykinin, lymphokines, complement factor and other nonspecific endogenous "damaging factors". It blocks the interaction of bradykinin with tissue receptors, restores disturbed microcirculation and reduces pain sensitivity in the inflammatory focus. Salicylamide is used in combination with both aspirin and caffeine in the over-the-counter pain remedies. non-narcotic analgesic (Code: CHEBI:35481) antirheumatic drug (Code: CHEBI:35842) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1964-04-30 Ministry of Health of the Russian Federation OHB
Click to view aminobenzoic acid Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22172310) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21402476) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21402476) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21402476) Aminobenzoic acid is an intermediate in the synthesis of folate by bacteria, plants, and fungi. Many bacteria, including those found in the human intestinal tract such as E. coli, generate Aminobenzoic acid from chorismate by the combined action of the enzymes 4-amino-4-deoxychorismate synthase and 4-amino-4-deoxychorismate lyase. Plants produce Aminobenzoic acid in their chloroplasts, and store it as a glucose ester (pABA-Glc) in their tissues. Humans lack the enzymes to convert Aminobenzoic acid to folate, so require folate from dietary sources such as green leafy vegetables. In humans, Aminobenzoic acid is considered nonessential and, although it has been referred to historically as "vitamin Bx", is no longer recognized as a vitamin, because most people have colon bacteria that generate Aminobenzoic acid. It used to be common in sunscreening agents until found to also be a sensitizer. The potassium salt is used therapeutically in fibrotic skin disorders. Vitamin B Complex Compounds (Code: N0000175715) Vitamin B Complex Member (Code: N0000175714) 1987-02-26 ANSM (French National Agency for Medicines and Health Products Safety) PAB
Click to view isoniazid Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28197313) Enoyl-[acyl-carrier-protein] reductase [NADH] (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WGR1, gene: inhA, swissprot: INHA_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15908576) Antibacterial agent used primarily as a tuberculostatic, inhibits the synthesis of mycoloic acids, an essential component of the bacterial cell wall. It remains the treatment of choice for tuberculosis. drug allergen (Code: CHEBI:88188) antitubercular agent (Code: CHEBI:33231) Antimycobacterial (Code: N0000175483) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antimetabolites (Code: D000963) Antitubercular Agents (Code: D000995) Fatty Acid Synthesis Inhibitors (Code: D054872) Hypolipidemic Agents (Code: D000960) 1952-09-29 FDA NIZ
Click to view dimetofrine proposed cardiovascular stimulant; minor descriptor (75-85); on-line & Index Medicus search ETHANOLAMINES (75-85); RN given refers to parent cpd without isomeric designation
Click to view pralidoxime Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021983s023lbl.pdf) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/24571195) Pralidoxime is an antidote to organophosphate pesticides and chemicals. If given within 24 hours, after organophosphate exposure, pralidoxime reactivates the enzyme cholinesterase by cleaving the phosphate-ester bond formed between the organophosphate and acetylcholinesterase. Pralidoxime in combination with atropine or alone is indicated for the treatment of poisoning by organophosphorus nerve agents as well as organophosphorus insecticides. cholinergic drug (Code: CHEBI:38323) antidote to organophosphate poisoning (Code: CHEBI:90753) antidote to sarin poisoning (Code: CHEBI:136860) Cholinesterase Reactivator (Code: N0000175742) Antidotes (Code: D000931) Cholinergic Agents (Code: D018678) Cholinesterase Reactivators (Code: D002801) Enzyme Reactivators (Code: D004793) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1964-03-11 FDA
Click to view phenylethanolamine Phenylethanolamine is the simplest member of the class of phenylethanolamines that is 2-aminoethanol bearing a phenyl substituent at the 1-position. It has a role as a human metabolite in the brain. Its derivatives are adrenergic agonists and antagonists. It can be used as a modulator of sympathetic functions.
Click to view tyramine Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18602830) Equilibrative nucleoside transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q7RTT9, gene: SLC29A4, swissprot: S29A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16099839) Tyramine is a monoamine compound derived from the amino acid tyrosine. Foods containing considerable amounts of tyramine include fish, chocolate, alcoholic beverages, cheese, soy sauce, sauerkraut, and processed meat. A large dietary intake of tyramine can cause an increase in systolic blood pressure of 30 mmHg or more. Tyramine acts as a neurotransmitter via a G protein-coupled receptor with high affinity for tyramine called TA1. The TA1 receptor is found in the brain as well as peripheral tissues including the kidney. An indirect sympathomimetic, Tyramine can also serve as a substrate for adrenergic uptake systems and monoamine oxidase so it prolongs the actions of adrenergic transmitters. It also provokes transmitter release from adrenergic terminals. Tyramine is a biomarker for the consumption of cheese. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Autonomic Agents (Code: D001337) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) AEF
Click to view isaxonine Isaxonine (isopropyl-amino-2-pyrimidinephosphate) is a neurotropic agent. Isaxonine is believed to have a positive effect on nerve regeneration by increasing the axonal transport, enhancing polymerization of tubuline in the peripheral nerves and stimulating axonal sprouting. Isaxonine is activated cytochromes P-450 into a reactive metabolite that is conjugated with glutathione or covalently binds to hepatic proteins. Isaxonine was used for the treatment of peripheral neuropathie. Also isaxonine was used for protection against the neurotoxic side-effect of vincristine. It is no longer commercially available due to its severe hepatotoxicity. 1981 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view fosfomycin UDP-N-acetylglucosamine 1-carboxyvinyltransferase 1 (Organism: Enterococcus faecalis (strain ATCC 700802 / V583), class: Enzyme, accessions: Q836E5, gene: murA1, swissprot: MURA1_ENTFA) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050717s009lbl.pdf) UDP-N-acetylglucosamine 1-carboxyvinyltransferase 2 (Organism: Enterococcus faecalis (strain ATCC 700802 / V583), class: Enzyme, accessions: Q831A8, gene: murA2, swissprot: MURA2_ENTFA) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050717s009lbl.pdf) UDP-N-acetylglucosamine 1-carboxyvinyltransferase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A749, gene: murA, swissprot: MURA_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050717s009lbl.pdf) UDP-N-acetylglucosamine 1-carboxyvinyltransferase (Organism: Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG 12228), class: Unclassified, accessions: Q9HVW7, gene: murA, swissprot: MURA_PSEAE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16945528) Fosfomycin is an antibiotic produced by Streptomyces fradiae. Fosfomycin has in vitro activity against a broad range of gram-positive and gram-negative aerobic microorganisms which are associated with uncomplicated urinary tract infections. Fosfomycin is bactericidal in urine at therapeutic doses. The bactericidal action of fosfomycin is due to its inactivation of the enzyme enolpyruvyl transferase, thereby irreversibly blocking the condensation of uridine diphosphate-N-acetylglucosamine with p-enolpyruvate, one of the first steps in bacterial cell wall synthesis. It also reduces adherence of bacteria to uroepithelial cells. There is generally no cross-resistance between fosfomycin and other classes of antibacterial agents such as beta-lactams and aminoglycosides. Fosfomycin has been shown to be active in clinical infections against Enterococcus faecalis and Escherichia coli. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1996-12-19 FDA FCN
Click to view salicylic acid High mobility group protein B1 (Organism: Homo sapiens, class: Unclassified protein, accessions: P09429, gene: HMGB1, swissprot: HMGB1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26101955) Aldo-keto reductase family 1 member C1 (Organism: Homo sapiens, class: Enzyme, accessions: Q04828, gene: AKR1C1, swissprot: AK1C1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18045204) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049739) Solute carrier family 22 member 19 (Organism: Mus musculus, class: Transporter, accessions: Q8VCA0, gene: Slc22a19, swissprot: S22AJ_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15068970) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11306713) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15640378) Solute carrier family 22 member 7 (Organism: Mus musculus, class: Transporter, accessions: Q91WU2, gene: Slc22a7, swissprot: S22A7_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12065749) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Solute carrier family 22 member 20 (Organism: Mus musculus, class: Transporter, accessions: Q80UJ1, gene: Slc22a20, swissprot: S22AK_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17553798) Solute carrier family 22 member 6 (Organism: Mus musculus, class: Transporter, accessions: Q8VC69, gene: Slc22a6, swissprot: S22A6_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17553798) Salicylic acid is a compound obtained from the bark of the white willow and wintergreen leaves, and also prepared synthetically. It has bacteriostatic, fungicidal, and keratolytic actions. Its salts, the salicylates, are used as analgesics. Salicylic acid directly irreversibly inhibits COX-1 and COX-2 to decrease conversion of arachidonic acid to precursors of prostaglandins and thromboxanes. Salicylic acid competitively inhibits oxidation of uridine-5-diphosphoglucose (UDPG) with nicotinamide adenosine dinucleotide (NAD) and noncompetitively with UDPG. It also competitively inhibits the transferring of the glucuronyl group of uridine-5-phosphoglucuronic acid (UDPGA) to a phenolic acceptor. Inhibition of mucopoly saccharide synthesis is likely responsible for the slowing of wound healing with salicylates. Salicylic acid is a key additive in many skin-care products for the treatment of acne, psoriasis, callouses, corns, keratosis pilaris and warts. antiinfective agent (Code: CHEBI:35441) keratolytic drug (Code: CHEBI:50176) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Infective Agents (Code: D000890) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antifungal Agents (Code: D000935) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Dermatologic Agents (Code: D003879) Enzyme Inhibitors (Code: D004791) Keratolytic Agents (Code: D007641) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1898-01-01 YEAR INTRODUCED SAL
Click to view phenoxyethanol Phenoxyethanol is a glycol ether used as a insect repellent, antiseptic, solvent, preservative, and also as an anesthetic in fish aquaculture. Phenoxyethanol is used as an antimicrobial and preservative. Also it is used in vaccines and shown to inactivate bacteria, and several types of yeast. antiinfective agent (Code: CHEBI:35441) central nervous system depressant (Code: CHEBI:35488) Anesthetics (Code: D000777) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) FDA 268
Click to view pentetrazol GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47870|P18507, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11504794) Pentetrazol is a pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive gamma-aminobutyric acid (GABA) antagonist. Pentetrazol has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility. GABA is thought to play a role in promoting sleep and its function is believed to be elevated in idiopathic hypersomnia. By blocking GABA’s function, pentetrazo is expected to reduce excessive daytime sleepiness. Pentetrazole in combination with dihydrocodeine rhodanate is used as cough suppressant. Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Convulsants (Code: D003292) GABA Agents (Code: D018682) GABA Antagonists (Code: D018756) Neurotransmitter Agents (Code: D018377) 1969-08-12 Italian Medicines Agency (AIFA)
Click to view methazolamide Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991988) Carbonic anhydrase 13 (Organism: Homo sapiens, class: Enzyme, accessions: Q8N1Q1, gene: CA13, swissprot: CAH13_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21620713) Carbonic anhydrase 2 (Organism: Cryptococcus neoformans var. grubii, class: Unclassified, accessions: Q3I4V7, gene: CAN2, swissprot: Q3I4V7_CRYNV) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Enzyme, accessions: P40881, gene: None, swissprot: CAH_METTE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15546717) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Methazolamide is a sulfonamide derivative and a potent inhibitor of the enzyme carbonic anhydrase. The oral administration of the drug inhibits ocular carbonic anhydrase therefore decreasing formation of aqueous humor and intraocular pressure. Methazolamide does have a weak transient diuretic effect. Methazolamide is indicated for adjunctive treatment of chronic simple (open-angle) glaucoma, secondary glaucoma and preoperatively in acute angle closure glaucoma, where delay of surgery is desired in order to lower intraocular pressure. Carbonic Anhydrase Inhibitors (Code: D002257) Diuretics (Code: D004232) Enzyme Inhibitors (Code: D004791) Natriuretic Agents (Code: D045283) 1959-01-26 FDA MZM
Click to view irofulven Serine/threonine-protein kinase Chk2 (Organism: Homo sapiens, class: Kinase, accessions: O96017, gene: CHEK2, swissprot: CHK2_HUMAN) Irofulven is a semisynthetic sesquiterpene derivative of illudin S, a natural toxin isolated from the fungus Omphalotus illudens. Irofulven alkylates DNA and protein macromolecules, forms adducts, and arrests cells in the S-phase of the cell cycle. This agent requires NADPH-dependent metabolism by alkenal/one oxidoreductase for activity. Irofulven is more active in vitro against tumor cells of epithelial origin and is more resistant to deactivation by p53 loss and MDR1 than other alkylating agents. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) Radiation-Sensitizing Agents (Code: D011838)
Click to view methenamine Methenamine is a heterocyclic organic compound with antibiotic activity. Methenamine most commonly used in the treatment of urinary tract infections. Its anti-infective action derives from the slow release of formaldehyde by hydrolysis at acidic pH. (From Martindale, The Extra Pharmacopoeia, 30th ed, p173) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076) 1967-07-05 FDA
Click to view furtrethonium Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Furtrethonium is an cholinergic agent. Furtrethonium iodide is used for the treatment of glaucoma. Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Neurotransmitter Agents (Code: D018377)
Click to view ethosuximide Voltage-dependent T-type calcium channel subunit alpha-1G (Organism: Homo sapiens, class: Ion channel, accessions: O43497, gene: CACNA1G, swissprot: CAC1G_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/11641441) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/11641441) Voltage-dependent T-type calcium channel subunit alpha-1I (Organism: Homo sapiens, class: Ion channel, accessions: Q9P0X4, gene: CACNA1I, swissprot: CAC1I_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/11641441) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12637244) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12637244) Ethosuximide is a succinimide anticonvulsant. Ethosuximide suppresses the paroxysmal three cycle per second spike and wave activity associated with lapses of consciousness which is common in absence (petit mal) seizures. The frequency of epileptiform attacks is reduced, apparently by depression of the motor cortex and elevation of the threshold of the central nervous system to convulsive stimuli. Ethosuximide is on the World Health Organization's List of Essential Medicines. Ethosuximide is indicated for the control of absence (petit mal) epilepsy. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1960-11-02 FDA
Click to view isometheptene Isometheptene is a sympathomimetic drug which causes vasoconstriction. Isometheptene's vasoconstricting properties arise through activation of the sympathetic nervous system via epinephrine and norepinephrine. It is used for treating migraines and tension headaches. FDA
Click to view cyclopentamine Cyclopentamine is a sympathomimetic alkylamine, classified as a vasoconstrictor. Cyclopentamine acts as a releasing agent of the catecholamine neurotransmitters norepinephrine (noradrenaline), epinephrine (adrenaline), and dopamine. Cyclopentamine was indicated in the past as a nasal decongestant, but has now been largely discontinued.
Click to view metyrapone Cytochrome P450 11B1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P15538, gene: CYP11B1, swissprot: C11B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25874338) Cytochrome P450 11B2, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P19099, gene: CYP11B2, swissprot: C11B2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25874338) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11465421) Metopirone is an inhibitor of endogenous adrenal corticosteroid synthesis. The pharmacological effect of Metopirone is to reduce cortisol and corticosterone production by inhibiting the 11-betahydroxylation reaction in the adrenal cortex. Metopirone is used as a diagnostic test, with urinary 17-hydroxycorticosteroids measured as an index of pituitary adrenocorticotropic hormone responsiveness. Metopirone may also suppress biosynthesis of aldosterone, resulting in a mild natriuresis. diagnostic agent (Code: CHEBI:33295) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Noxae (Code: D009676) Adrenal Steroid Synthesis Inhibitor (Code: N0000175928) Adrenal Steroid Synthesis Inhibitors (Code: N0000175921) 1961-12-04 FDA MYT
Click to view kojic acid Polyphenol oxidase (Organism: Agaricus bisporus, class: Enzyme, accessions: Q00024|O42713|C7FF04|C7FF05, gene: PPO1|PPO2|PPO3|PPO4, swissprot: PPO1_AGABI|PPO2_AGABI|PPO3_AGABI|PPO4_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16513349) D-amino-acid oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P14920, gene: DAO, swissprot: OXDA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23683589) Kojic acid is a pyranone that has been isolated from the fungus Aspergillus oryzae. It has a role as a NF-kappaB inhibitor, an Aspergillus metabolite, a skin lightening agent, an catechol oxidase inhibitor, an laccase inhibitor, an quercetin 2,3-dioxygenase inhibitor, an tyrosinase inhibitor and an D-amino-acid oxidase inhibitor. it is used to treat skin diseases like melasma. Kojic acid also has antibacterial and antifungal properties. skin lightening agent (Code: CHEBI:85046) Antioxidants (Code: D000975) Protective Agents (Code: D020011) KOJ
Click to view piracetam Piracetam is a nootropic drug in the racetams group, with chemical name 2-oxo-1-pyrrolidine acetamide. It shares the same 2-oxo-pyrrolidone base structure with pyroglutamic acid and is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA). However its mechanism of action differ from that of endogenous GABA.Piracetam has neuroprotective and anticonvulsant properties and is reported to improve neural plasticity. Its efficacy is documented in cognitive disorders and dementia, vertigo, cortical myoclonus, dyslexia, and sickle cell anemia although the clinical application in these conditions is not yet established. Piracetam has effects on the vascular system by reduce erythrocyte adhesion to vascular endothelium, hinder vasospasm and facilitate microcirculation. Piracetam is indicated in adult patients suffering from myoclonus of cortical origin, irrespective of aetiology, and should be used in combination with other antimyoclonic therapies. Central Nervous System Agents (Code: D002491) Neuroprotective Agents (Code: D018696) Nootropic Agents (Code: D018697) Protective Agents (Code: D020011) 1975-06-01 Spanish Agency of Medicines and Medical Products (AEMPS) PZI
Click to view methylthiouracil Methylthiouracil is a thiourea antithyroid agent that inhibits the synthesis of thyroid hormone. Methylthiouracil was introduced for the treatment of hyperthyroidism. Methylthiouracil is no longer in clinical use in most countries. Methylthiouracil is possibly carcinogenic to humans. Antithyroid Agents (Code: D013956) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1958 YEAR INTRODUCED
Click to view mesna Mesna is a sulfhydryl compound that is used to reduce the incidence of hemorrhagic cystitis associated with certain chemotherapeutic agents. Mesna is converted to a free thiol compound in the kidney, where it binds to and inactivates acrolein and other urotoxic metabolites of ifosfamide and cyclophosphamide, thereby reducing their toxic effects on the urinary tract during urinary excretion. Protective Agents (Code: D020011) 1988-12-30 FDA COM
Click to view trimethadione Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14651673) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14651673) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14651673) Trimethadione is an oxazolidinedione compound and an antiepileptic agent. Trimethadione has been shown to prevent pentylenetetrazol-induced and thujone-induced seizures in experimental animals. Unlike the hydantoins and antiepileptic barbiturates, trimethadione does not modify the maximal seizure pattern in patients undergoing electroconvulsive therapy. Trimethadione is rapidly absorbed from the gastrointestinal tract. It is demethylated by liver microsomes to the active metabolite, dimethadione. Trimethadione is indicated for the control of petit mal seizures that are refractory to treatment with other drugs. Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1946-01-25 FDA
Click to view valpromide Valpromide is a derivative of valproic acid. Valpromide has been shown to decrease aggressivity in stress-induced animals, to regulate anxious induced behaviours, as well as to potentiate central sedative compounds. It produces a significant increase of cognitive functions. Valpromide is indicated for the treatment of bipolar disorder (manic episodes). Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1999-12-23 Italian Medicines Agency (AIFA) VPR
Click to view valnoctamide Valnoctamide is a valproic acid derivative associated with a decreased risk for congenital abnormalities and developed for treatment mania. Valnoctamide has been marketed as an anxiolytic and sedative. It is no longer available. Italian Medicines Agency (AIFA)
Click to view betanaphthol Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15916432) Betanaphthol is a monatomic phenol occurring in coal-tar, but usually prepared artificially from naphthalene. Betanaphthol is antiseptic, antifermentative, deodorant, and may also be considered a disinfectant. Its action closely resembles that of phenol, but is less poisonous. Betanaphthol (in combination with salicylic acid) is used for the treatment of skin dermatomycosis of sleek skin and hairy parts of the head. 2010-10-22 Bulgarian Drug Agency (BDA) 03V
Click to view trichloroacetic acid Trichloroacetic acid (TCA; also known as trichloroethanoic acid) is an analogue of acetic acid. In clinical chemistry and biochemistry, it is used as a precipitant of macromolecules including proteins, DNA and RNA. Trichloroacetate is also found in cosmetic treatments and topical formulations as a cauterant, which removes condyloma or warts on the skin. Caustics (Code: D002424) Noxae (Code: D009676) 1993-12-01 Italian Medicines Agency (AIFA)
Click to view octanoic acid Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12063169) Octanoic acid (caprylic acid) is a saturated medium-chain fatty acid with an 8-carbon backbone. Octanoic acid is found naturally in the milk of various mammals and is a minor component of coconut oil and palm kernel oil. Octanoic acid is an antimicrobial pesticide used as a disinfectant agent. OCA
Click to view valproic acid Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BY41, gene: HDAC8, swissprot: HDAC8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20602621) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18838507) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18838507) UDP-glucuronosyltransferase 1-8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW9, gene: UGT1A8, swissprot: UD18_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18838507) UDP-glucuronosyltransferase 1-10 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW8, gene: UGT1A10, swissprot: UD110_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18838507) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9228014) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10525100) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Valproic acid is a carboxylic acid designated as 2-propylpentanoic acid. It is also known as dipropylacetic acid. Valproic acid dissociates to the valproate ion in the gastrointestinal tract. The mechanisms by which valproate exerts its therapeutic effects have not been established. It has been suggested that its activity in epilepsy is related to increased brain concentrations of gamma-aminobutyric acid (GABA). Valproic acid is indicated as monotherapy and adjunctive therapy in the treatment of patients with complex partial seizures that occur either in isolation or in association with other types of seizures. Valproic acid also is indicated for use as sole and adjunctive therapy in the treatment of simple and complex absence seizures, and adjunctively in patients with multiple seizure types which include absence seizures. GABA agent (Code: CHEBI:51374) anticonvulsant (Code: CHEBI:35623) psychotropic drug (Code: CHEBI:35471) neuroprotective agent (Code: CHEBI:63726) antimanic drug (Code: CHEBI:35477) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Mood Stabilizer (Code: N0000175751) Anticonvulsants (Code: D000927) Antimanic Agents (Code: D018692) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Enzyme Inhibitors (Code: D004791) GABA Agents (Code: D018682) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1978-02-28 FDA 2PP
Click to view octamoxin Octamoxin (2-octylhydrazine) is both an irreversible and nonselective monoamine oxidase enzyme inhibitor (MAOI) of the hydrazine chemical class. This drug was used in the past as an antidepressant agent in the 1960s, however, has since been discontinued.
Click to view ethchlorvynol Ethchlorvynol is a sedative and hypnotic drug. Ethchlorvynol is a schedule IV (USA) controlled substance. It produces cerebral depression, however the exact mechanism of action is not known. Ethchlorvynol appears to depress the central nervous system in a manner similar to that of barbiturates. It has been used to treat insomnia, but has been largely superseded and is only offered where an intolerance or allergy to other drugs exists. sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1961-05-10 FDA
Click to view methyl aminolevulinate Methyl aminolevulinate is the methyl ester of 5-aminolevulinic acid. Methyl aminolevulinate is a prodrug, it is metabolised to protoporphyrin IX, a photosensitizer. Topical application (often as the hydrochloride salt) results in an accumulation of protoporphyrin IX in the skin lesions to which the cream has been applied. Subsequent illumination with red light results in the generation of toxic singlet oxygen that destroys cell membranes and thereby kills the tumour cells. Methyl aminolevulinate is used in the photodynamic treatment of non-melanoma skin cancer (including basal cell carcinoma). Methyl aminolevulinate is also used for the treatment of thin and moderately thick, non-hyperkeratotic, non-pigmented actinic keratoses of the face and scalp in immunocompetent patients when used in conjunction with lesion preparation in the physician’s office when other therapies are considered medically less appropriate. antineoplastic agent (Code: CHEBI:35610) photosensitizing agent (Code: CHEBI:47868) prodrug (Code: CHEBI:50266) dermatologic drug (Code: CHEBI:50177) Porphyrin Precursor (Code: N0000175846) Porphyrinogens (Code: N0000171207) 2004-07-27 FDA
Click to view camphor Methionine aminopeptidase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P50579, gene: METAP2, swissprot: MAP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621724) Methionine aminopeptidase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P53582, gene: METAP1, swissprot: MAP11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621724) Methionine aminopeptidase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AE18, gene: map, swissprot: MAP1_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621724) Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Camphor is an antiseptic with mild fungistatic, bacteriostatic, anthelmintic, and amebicidal action. It is also used as a reagent and metal chelator, as a carrier for radio-indium for diagnostic purposes, and its halogenated derivatives are used in addition as topical anti-infective agents and oral antiamebics. antiseptic drug (Code: CHEBI:48218) antifungal agrochemical (Code: CHEBI:86328) 1964-04-30 Ministry of Health of the Russian Federation HQY
Click to view emylcamate Emylcamate is an anxiolytic and muscle relaxant. It is used for the treatment of anxiety and tension. It is no longer prescribed.
Click to view heptaminol Heptaminol is an amino alcohol that has been used as a myocardial stimulant and vasodilator and to relieve bronchospasm. Its most common therapeutic use is in orthostatic hypotension. The mechanism of heptaminol's therapeutic actions is not well understood although it has been suggested to affect catecholamine release or calcium metabolism.
Click to view trioxsalen Trioxsalen (trimethylpsoralen, trioxysalen or trisoralen) is a furanocoumarin and a psoralen derivative. It is obtained from several plants, mainly Psoralea corylifolia. Like other psoralens it causes photosensitization of the skin. The photoactivated form produces interstrand linkages in DNA resulting in cell apoptosis. It is administered either topically or orally in conjunction with UV-A (the least damaging form of ultraviolet light) for phototherapy treatment of vitiligo and hand eczema. dermatologic drug (Code: CHEBI:50177) photosensitizing agent (Code: CHEBI:47868) Psoralen (Code: N0000175879) Psoralens (Code: N0000007909) Dermatologic Agents (Code: D003879) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) 1964-07-24 FDA
Click to view gimeracil Dihydropyrimidine dehydrogenase [NADP(+)] (Organism: Homo sapiens, class: Enzyme, accessions: Q12882, gene: DPYD, swissprot: DPYD_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21668582) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inducer (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inducer (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Gimeracil is a dihydropyrimidine dehydrogenase (DPD) inhibitor which used to prevent degradation of 5-fluorouracil (5-FU) by the body. Gimeracil inhibits the metabolism of 5-FU by reversibly and selectively inhibiting DPD, the primary metabolic enzyme for 5-FU, so that higher plasma concentrations of 5-FU are achieved with the administration of a lower dose of tegafur. Gimeracil is indicated in combination with tegaflur and oteracil for the treatment of advanced gastric cancer. 2011-03-14 EMA
Click to view adipic acid Solute carrier family 22 member 6 (Organism: Mus musculus, class: Transporter, accessions: Q8VC69, gene: Slc22a6, swissprot: S22A6_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17553798) Solute carrier family 22 member 20 (Organism: Mus musculus, class: Transporter, accessions: Q80UJ1, gene: Slc22a20, swissprot: S22AK_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17553798) Adipic acid is an alpha,omega-dicarboxylic acid that is the 1,4-dicarboxy derivative of butane. It has a role as a food acidity regulator and a human xenobiotic metabolite. It is used to make plastics and foams and for other uses. Adipic acid in the urine and in the blood is typically exogenous in origin and is a good biomarker of jello consumption. In fact, a condition known as adipic aciduria is actually an artifact of jello consumption. However, certain disorders (such as diabetes and glutaric aciduria type I) can lead to elevated levels of adipic acid snd other dicarboxcylic acids (such as suberic acid) in urine. Moreover, adipic acid is also found to be associated with 3-hydroxy-3-methylglutaryl-CoA lyase deficiency, carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency, and medium Chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism. food acidity regulator (Code: CHEBI:64049) 0L1
Click to view isosorbide Isosorbide is an effective hyperosmotic agent which can be administered orally without gastrointestinal irritation. Isosorbide (Ismotic, Hydronol) is a dihydric alcohol formed by the removal of two molecules of water from sorbitol. Its actions are similar to those of glycerol. Hyperosmotic agents lower intraocular pressure by creating an osmotic gradient between the blood and the ocular fluids. Isosorbide is used for the short-term reduction of intraocular pressure. May be used prior to and after intraocular surgery. May be used to interrupt an acute attack of glaucoma. Diuretics (Code: D004232) Diuretics, Osmotic (Code: D004234) Natriuretic Agents (Code: D045283) 1974-01-30 FDA
Click to view coumarin Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19206230) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19206230) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19206230) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19206230) Amine oxidase [flavin-containing] A (Organism: Rattus norvegicus, class: Enzyme, accessions: P21396, gene: Maoa, swissprot: AOFA_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11123983) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11123983) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15658857) Coumarin and its derivatives are alpha-benzopyrones. Coumarin is metabolized in humans to 7-hydroxycoumarin. Coumarin is isolated from the tonka bean Coumarouna odorata. Coumarin is a secondary phytochemical with hepatotoxic and carcinogenic properties. Coumarin has been reported to exhibit antioxidant, analgesic, anti-inflammatory, and antimutagenic properties. Coumarin is used in the pharmaceutical industry as a precursor reagent in the synthesis of a number of synthetic anticoagulant pharmaceuticals. Also it was used as a homeopatic drug for temporary relief of allergies caused products. fluorescent dye (Code: CHEBI:51121) 1995 CDSCO (INDIA) COU
Click to view glutamine Glutamine is a non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from glutamic acid and ammonia. It is the principal carrier of nitrogen in the body and is an important energy source for many cells. L-glutamine is an optically active form of glutamine having L-configuration. L-glutamine appears to play a major role in protecting the integrity of the gastrointestinal tract and, in particular, the large intestine. L-glutamine is the preferred respiratory fuel for enterocytes, colonocytes and lymphocytes. The exact mechanism of the possible immunomodulatory action of supplemental L-glutamine remains unclear. It is conceivable that the major effect of L-glutamine occurs at the level of the intestine. Perhaps enteral L-glutamine acts directly on intestine-associated lymphoid tissue and stimulates overall immune function by that mechanism, without passing beyond the splanchnic bed. Glutamine is used for nutritional supplementation, also for treating dietary shortage or imbalance. Amino Acid (Code: N0000175780) Amino Acids (Code: N0000006806) 2004-06-10 FDA DGN
GLN
Click to view acetylpheneturide Acetylpheneturide suppresses epileptic attacks by acting on the central nerves. Acetylpheneturide is used as an anticonvulsant in the treatment of epilepsy.
Click to view lysine G-protein coupled receptor family C group 6 member A (Organism: Homo sapiens, class: GPCR, accessions: Q5T6X5, gene: GPRC6A, swissprot: GPC6A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15576628) Mitochondrial ornithine transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y619, gene: SLC25A15, swissprot: ORNT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12807890) Mitochondrial ornithine transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9BXI2, gene: SLC25A2, swissprot: ORNT2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12807890) Sodium-coupled neutral amino acid transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q969I6, gene: SLC38A4, swissprot: S38A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11342143) Lysine is one of nine essential amino acids in humans required for growth and tissue repair, Lysine is supplied by many foods, especially red meats, fish, and dairy products. L-Lysine is a nutritional supplement containing the biologically active L-isomer of the essential amino acid lysine, with potential anti-mucositis activity. Upon oral intake, L-lysine promotes healthy tissue function, growth and healing and improves the immune system. L-Lysine promotes calcium uptake, is essential for carnitine production and collagen formation. As collagen is essential for connective tissue maintenance, this agent may also help heal mucosal wounds. This may help decrease and prevent mucositis induced by radiation or chemotherapy. nutraceutical (Code: CHEBI:50733) anticonvulsant (Code: CHEBI:35623) 1971-09-24 FDA LYS
DLY
Click to view oxapropanium Oxapropanium is a synthetic cholinomimetics.
Click to view acetylcholine Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224827) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22677319) Vesicular acetylcholine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q62666, gene: Slc18a3, swissprot: VACHT_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15485505) Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P17787, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/26225816) Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Rattus norvegicus, class: Ion channel, accessions: P04757|P12392, gene: Chrna3|Chrnb4, swissprot: ACHA3_RAT|ACHB4_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19027295) Solute carrier family 22 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63089, gene: Slc22a1, swissprot: S22A1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8898084) Acetylcholine (ACh) is a neurotransmitter. Acetylcholine in vertebrates is the major transmitter at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system. Various nicotinic and muscarinic ACh receptors are present in both afferent nerve endings and glomus cells. Therefore, ACh can depolarize or hyperpolarize the cell membrane depending on the available receptor type in the vicinity. Binding of ACh to its receptor can create a wide variety of cellular responses including opening cation channels (nicotinic ACh receptor activation), releasing Ca2+ from intracellular storage sites (via muscarinic ACh receptors), and modulating activities of K+ and Ca2+ channels. Acetylcholine is used to obtain miosis of the iris in seconds after delivery of the lens in cataract surgery, in penetrating keratoplasty, iridectomy and other anterior segment surgery where rapid miosis may be required. vasodilator agent (Code: CHEBI:35620) muscarinic agonist (Code: CHEBI:38325) Cardiovascular Agents (Code: D002317) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) Cholinergic Receptor Agonist (Code: N0000175884) 1973-10-09 FDA ACH
Click to view trientine copper (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.ncbi.nlm.nih.gov/pubmed/6121964) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590092) Trientine ( triethylenetatramine, TETA) is a chelating compound for removal of excess copper from the body. Its salt form, trientine (triethylenetetramine dihydrochloride or 2,2,2-tetramine) was introduced as an alternative to D-penicillamine. It consists of a polyamine-like structure different from D-penicillamine, as it lack sulfhydryl groups. Although penicillamine treatment is believed to be more extensive, TETA therapy has been shown to be an effective initial therapy, even with patients with decompensated liver disease at the outset, and prolonged TETA treatment is not associated with adverse effects as expected in penicillamine treatment. Trietine is indicated in the treatment of patients with Wilson's disease who are intolerant of penicillamine. Metal Chelating Activity (Code: N0000175472) Metal Chelator (Code: N0000175473) Chelating Agents (Code: D002614) Sequestering Agents (Code: D064449) 1985-11-08 FDA 104
Click to view ambazone Ambazone is an antiseptic agent with potential antibacterial and antileukemic activity. Although the exact mechanism of action remains to be fully elucidated, ambazone appears to interfere with the membrane-bound nucleotide system by increasing the intracellular concentration of cAMP in leukemia cells and macrophages, which potentially contributes to this agent's antineoplastic activity. Furthermore, this agent's affinity for various cellular targets, i.e. membranes, nucleic acids and proteins, may contribute to the overall antibacterial effect. Ambazone is used as an adjunct in the treatment of acute infectious oral and pharyngeal infections (eg, gingivitis, stomatitis, tonsillitis) and after removal of tonsils or teeth. 2008-03-01 NAMMDR (National Agency for Medicines and Medical Devices of Romania)
Click to view glutamic acid Metabotropic glutamate receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q14416, gene: GRM2, swissprot: GRM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10530814) Metabotropic glutamate receptor 3 (Organism: Homo sapiens, class: GPCR, accessions: Q14832, gene: GRM3, swissprot: GRM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10530814) Metabotropic glutamate receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q13255, gene: GRM1, swissprot: GRM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10443583) Metabotropic glutamate receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q14833, gene: GRM4, swissprot: GRM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10443583) Metabotropic glutamate receptor 5 (Organism: Homo sapiens, class: GPCR, accessions: P41594, gene: GRM5, swissprot: GRM5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10443583) Metabotropic glutamate receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: O15303, gene: GRM6, swissprot: GRM6_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10443583) Metabotropic glutamate receptor 8 (Organism: Homo sapiens, class: GPCR, accessions: O00222, gene: GRM8, swissprot: GRM8_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10443583) Sodium-coupled neutral amino acid transporter 3 (Organism: Homo sapiens, class: Transporter, accessions: Q99624, gene: SLC38A3, swissprot: S38A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10823827) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Glutamic acid is a non-essential aminoacid used in biosynthesis of proteins. Besides being a building block of proteins, glutamic acid plays a principal role in neural activation. Glutamic acid is also responsible for the umami (savory) flavor of certain foods. In medicine, glutamate is used as a metabolic supplemnet in patients undergoing coronary surgery. Glutamic acid activates both ionotropic and metabotropic glutamate receptors. The ionotropic ones being non-NMDA (AMPA and kainate) and NMDA receptors. Free glutamic acid cannot cross the blood-brain barrier in appreciable quantities; instead it is converted into L-glutamine, which the brain uses for fuel and protein synthesis. It is conjectured that glutamate is involved in cognitive functions like learning and memory in the brain, though excessive amounts may cause neuronal damage associated in diseases like amyotrophic lateral sclerosis, lathyrism, and Alzheimer's disease. Also, the drug phencyclidine (more commonly known as PCP) antagonizes glutamate at the NMDA receptor, causing behavior reminiscent of schizophrenia. Glutamic acid in action is extremely difficult to study due to its transient nature. 1985 FDA GLU
Click to view meldonium Gamma-butyrobetaine dioxygenase (Organism: Homo sapiens, class: Enzyme, accessions: O75936, gene: BBOX1, swissprot: BODG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24571165) Meldonium is an ammonium betaine that is beta-alaninate in which one of the amino hydrogens is replaced by a trimethylamino group. Meldonium is a cardioprotective drug that is used for treatment of heart failure, myocardial infarction, arrhythmia, atherosclerosis and diabetes. Meldonium was added to the World Anti-Doping Agency’s (WADA) list of banned substances. cardioprotective agent (Code: CHEBI:77307) neuroprotective agent (Code: CHEBI:63726) 1998-05-20
Click to view carbachol Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12505062) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Carbachol is a synthetic choline ester and a positively charged quaternary ammonium compound. Carbachol is a parasympathomimetic that mimics the effect of acetylcholine on both the muscarinic and nicotinic receptors. Carbachol is used for the treatment of glaucoma, but is also used during ophthalmic surgery. nicotinic acetylcholine receptor agonist (Code: CHEBI:47958) muscarinic agonist (Code: CHEBI:38325) cardiotonic drug (Code: CHEBI:38147) miotic (Code: CHEBI:51068) non-narcotic analgesic (Code: CHEBI:35481) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Miotics (Code: D008916) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sensory System Agents (Code: D018689) 1972-09-28 FDA CCE
Click to view ketoxal Kethoxal (3-Ethoxy-alpha-ketobutyraldehyde) modifies guanine containing oligoribonucleotides (by reacting selectively with guanine in polynucleotides). Ketoxal was used as an antiviral drug. Now ketoxal is used for the modification bases in RNA. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998)
Click to view viloxazine Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871604) Viloxazine is a selective norepinephrine reuptake inhibitor. It structurally differs from conventional tri- or tetra-cyclic antidepressants and it does not produce sedative anticholinergic or adrenergic effects in man. It was used in some European countries as an antidepressant drug. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) 1988-04-28 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view trolamine Trolamine is the salt formed between triethanolamine and salicylic acid. It is widely used as a topical analgesic such as are creams for temporarily relief of minor aches and pains of muscles and joints associated with arthritis, simple backache, lumbago, neuralgia, strains, bruises, and sprains. Trolamine was used as triethanolamine polypeptide in otic solution drops for removal of impacted cerumen prior to ear examination, otologic therapy and/or audiometry. Now trolamine is used for the treatment and prevention of radiotherapy-induced skin erythema. It is also used for the treatment burns and any other uninfected skin wounds. 1958 FDA 211
Click to view methionine S-adenosylmethionine synthase isoform type-2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P18298, gene: Mat2a, swissprot: METK2_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/3755757) S-adenosylmethionine synthase isoform type-1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P13444, gene: Mat1a, swissprot: METK1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/3755757) Methionine is an non-polar, aliphatic, essential alpha-amino acid that is used in the biosynthesis of proteins. Methionine is sulphur containing amino acid and improves the tone and pliability of skin, hair, and strengthens nails. Involved in many detoxifying processes, sulphur provided by methionine protects cells from pollutants, slows cell aging, and is essential for absorption and bio-availability of selenium and zinc. Methionine chelates heavy metals, such as lead and mercury, aiding their excretion. It also acts as a lipotropic agent and prevents excess fat buildup in the liver. nutraceutical (Code: CHEBI:50733) 1975 FDA MED
MET
Click to view penicillamine Copper (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/19853s012,014lbl.pdf) Penicillamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, penicillamine chelates with heavy metals and increases their urinary excretion. From in vitro studies which indicate that one atom of copper combines with two molecules of penicillamine, it would appear that one gram of penicillamine should be followed by the excretion of about 200 milligrams of copper. Penicillamine is used for treatment of Wilson's disease, cystinuria and active rheumatoid arthritis. antirheumatic drug (Code: CHEBI:35842) Antidotes (Code: D000931) Antirheumatic Agents (Code: D018501) Chelating Agents (Code: D002614) Protective Agents (Code: D020011) Sequestering Agents (Code: D064449) Antirheumatic Agent (Code: N0000175713) 1970-12-04 FDA LEI
Click to view phenpromethamine Phenpromethamine is a stimulant; it is chemically and structurally related to amphetamine. Phenpromethamine is prohibited from sport under the 'S6: Stimulants' of the WADA List of Prohibited Substances and Methods as a result of its purported stimulant properties due to its structural relationship to amphetamine, its derivatives (e.g. methamphetamine) and analogues (WADA 2019).
Click to view tioxolone Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26821818) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26821818) Tioxolone is a metalloenzyme carbonic anhydrase I inhibitor. Tioxolone has cytostatic, antipsoriatic, antibacterial and anti-mycotic properties. It has been used topically for many years, in the treatment of various skin and scalp disorders. It is used in anti-acne and rinse-off products respectively. The substance has also been used for seborrheic dermatitis. antiseborrheic (Code: CHEBI:59010)
Click to view phentermine Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022580s016lbl.pdf) Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18602830) Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11071707) Sodium-dependent serotonin transporter (Organism: Mus musculus, class: Transporter, accessions: Q60857, gene: Slc6a4, swissprot: SC6A4_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11071707) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11911838) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11911838) Phentermine is a sympathomimetic amine anorectic agent. It is chemically related to amphetamine and it is commonly referred to as an atypical amphetamine. Phentermine is an indirect-acting sympathomimetic agent that acts by releasing noradrenaline from the presynaptic vesicles in the lateral hypothalamus. Phentermine is indicated, alone or in combination with topiramate, as a short-term adjunct, not pass a few weeks, in a regimen of weight reduction based on exercise, behavioral modifications and caloric restriction in the management of exogenous obesity. dopaminergic agent (Code: CHEBI:48560) adrenergic agent (Code: CHEBI:37962) sympathomimetic agent (Code: CHEBI:35524) appetite depressant (Code: CHEBI:50507) central nervous system drug (Code: CHEBI:35470) central nervous system stimulant (Code: CHEBI:35337) Appetite Suppression (Code: N0000175372) Increased Sympathetic Activity (Code: N0000175651) Sympathomimetic Amine Anorectic (Code: N0000175423) Adrenergic Agents (Code: D018663) Anti-Obesity Agents (Code: D019440) Appetite Depressants (Code: D001067) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1959-05-04 FDA
Click to view isocarboxazid Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/011961s045lbl.pdf) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/011961s045lbl.pdf) Isocarboxazid is a monoamine oxidase inhibitor. In vivo and in vitro studies demonstrated inhibition of MAO in the brain, heart, and liver. The mechanism by which MAO inhibitors act as antidepressants is not fully understood, but it is thought to involve the elevation of brain levels of biogenic amines. Isocarboxazid is indicated for the treatment of depression. Monoamine Oxidase Inhibitor (Code: N0000175744) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) 1959-07-01 FDA
Click to view methamphetamine Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22037049) Synaptic vesicular amine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q01827, gene: Slc18a2, swissprot: VMAT2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23993667) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9311621) Solute carrier family 22 member 3 (Organism: Rattus norvegicus, class: Transporter, accessions: O88446, gene: Slc22a3, swissprot: S22A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9830022) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9618255) Methamphetamine is a central nervous system stimulant and sympathomimetic. Methamphetamine is a mixture of two isomers. One isomer called Dextro, or D Methamphetamine, is active as a central nervous system stimulant. Desoxyn, a prescription drug also contains D Methamphetamine, is used for the treatment of attention deficit disorder with hyperactivity. The other isomer, levomethamphetamine, the L-enantiomer of methamphetamine is a sympathomimetic vasoconstrictor used in some over-the-counter (OTC) nasal decongestant inhalers in the United States.D-methamphetamine is the more physiologically active isomer. psychotropic drug (Code: CHEBI:35471) central nervous system stimulant (Code: CHEBI:35337) Amphetamine Anorectic (Code: N0000175425) Amphetamines (Code: N0000007883) Appetite Suppression (Code: N0000175372) Central Nervous System Stimulation (Code: N0000175729) Increased Sympathetic Activity (Code: N0000175651) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1943-12-31 FDA B40
Click to view ditiocarb Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11501186) Ditiocarb is a sulfhydryl-containing carbamate that is the primary in vivo metabolite of disulfiram. Diethyldithiocarbamate chelates zinc, thereby inhibiting metalloproteinases, thereby preventing the degradation of the extracellular matrix and inhibiting an initial step in cancer metastasis and angiogenesis. A known inhibitor of superoxide dismutase, this agent can either potentiate or protect against cell oxidative damage caused by ionizing radiation, depending on the time of administration. Adjuvants, Immunologic (Code: D000276) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Chelating Agents (Code: D002614) Immunologic Factors (Code: D007155) Sequestering Agents (Code: D064449) 1969-12-31 New Zealand Medicines and Medical Devices Safety Authority DCD
Click to view tartaric acid Tartaric acid is found in many plants such as grapes, tamarinds, pineapples, mulberries and so on. L-(+)-tartaric acid is widely used in food and beverage as acidity regulator with E number E334. Tartaric acid is used to generate carbon dioxide through interaction with sodium bicarbonate following oral administration. Carbon dioxide extends the stomach and provides a negative contrast medium during double contrast radiography. In high doses, this agent acts as a muscle toxin by inhibiting the production of malic acid, which could cause paralysis and maybe death. 1985-08-07 FDA TAR
TLA
Click to view moroxydine Moroxydine is a heterocyclic biguanidine with activity against influenza and other viral infections. Although its mechanism of action is not fully known the effects seem to be due to an influence on the virus host-cell system. bMoroxydine may be effective against a number of DNA and RNA viruses. Moroxydine is given as HCl orally or topically for treating herpes simplex and varicella-zoster infections. It is also used in the treatment of cold and influenza symptoms. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998)
Click to view xylose Xylose is a sugar originally isolated from wood. Xylose is classified as a monosaccharide of the aldopentose type, which means that it contains five carbon atoms and includes a formyl functional group. Xylose is used to sweeten products intended for use by obese and diabetic customers because it is a non-caloric sweetener. D-xylose absorbtion test has been used for diagnosis of intestinal malabsorption. 1987-03-26 FDA XYP
XYS
Click to view levofacetoperane Levofacetoperane is a sympathomimetic central nervous system stimulant and is commonly used to treat depression. Levophacetoperane is also a known analeptic.
Click to view cresatin Cresatin (m-Cresyl Acetate) is the acetic acid ester of metacresol, an agent with antiseptic and analgesic properties. Cresatin is used in an otic solution to treat bacterial and fungal infections of the outer ear, and in endodontic procedures.
Click to view paroxypropione Paroxypropione is a synthetic, non-steroidal estrogen. Paroxypropione has antigonadotropin action. Paroxypropione is a product from the oxidative splitting of stilbestrol, with a low degree of estrogenicity. As the drug possesses relatively low affinity for the estrogen receptor and must be given at high dosages to achieve significant estrogenic and antigonadotropic action.
Click to view pheniprazine Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/17404836) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/17404836) Pheniprazine is an irreversible and nonselective monoamine oxidase inhibitor (MAOI) of the hydrazine chemical class that was used as an antidepressant in the 1960s. It was also used in the treatment of angina pectoris and schizophrenia. Pheniprazine has been largely discontinued due to toxicity concerns such as jaundice, amblyopia, and optic neuritis.
Click to view ethylmethylthiambutene Ethylmethylthiambutene is a member of thiambutenes a class of opioid analgesics, around 1.3x the potency of morphine. Ethylmethylthiambutene is illegal throughout the world.
Click to view paracetamol Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17884974) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17884974) Fatty-acid amide hydrolase 1 (Organism: Homo sapiens, class: Enzyme, accessions: O00519, gene: FAAH, swissprot: FAAH1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22750843) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11095574) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/11811955) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11811955) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022450lbl.pdf) Arylamine N-acetyltransferase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P11245, gene: NAT2, swissprot: ARY2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9918139) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23897240) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501600) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501600) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501600) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579385) Myoglobin (Organism: Homo sapiens, class: Unclassified, accessions: P02144, gene: MB, swissprot: MYG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24482730) Paracetamol (acetaminophen) is the most commonly taken analgesic worldwide and is recommended as first-line therapy in pain conditions by the World Health Organization. At normal therapeutic doses, its reactive metabolite N-acetyl-p-benzoquinone imine (NAPQI) undergoes fast conjugation with glutathione and is subsequently metabolized to produce both cysteine and mercapturic acid conjugates. High doses of acetaminophen (overdoses) can lead to hepatic necrosis due to the depletion of glutathione and of binding of high levels of reactive metabolite (NAPQI) to important parts of liver cells. Paracetamol is used for the treatment of mild to moderate pain and reduction of fever. non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Antipyretics (Code: D058633) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1968-11-07 FDA TYL
Click to view aminomethylbenzoic acid Solute carrier family 15 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P51574, gene: Slc15a1, swissprot: S15A1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9882198) Aminomethylbenzoic acid is an unnatural amino acid derivative and is an antifibrinolytic agent. It is used for the treatment of bleeding caused by hyperfibrinolysis. Antifibrinolytic Agents (Code: D000933) Coagulants (Code: D003029) Enzyme Inhibitors (Code: D004791) Fibrin Modulating Agents (Code: D050299) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) Protease Inhibitors (Code: D011480) 1983-08-04 Ministry of Health of the Russian Federation
Click to view phenicarbazide Phenicarbazide, also known as phenylsemicarbazide, is an antipyretic compound. It has analgetic and antipyretic activity. It has been withdrawn from the market on grounds of its adverse effect profile (phenicarbazide can cause hemolytic anemia in human).
Click to view phenylpropanolamine Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12238918) Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12238918) Alpha-1B adrenergic receptor (Organism: Mesocricetus auratus, class: GPCR, accessions: P18841, gene: ADRA1B, swissprot: ADA1B_MESAU) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12238918) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3961266) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3961266) Phenylpropanolamine (norephedrine) is a sympathomimetic agent that acts as a nonselective adrenergic receptor agonist. It has been used as a decongestant and appetite suppressant. Currently, it is withdrawn from the market in Canada and the United States due to the risk for hemorrahgic strokes. The compound exists as 4 stereoisomers, which include d- and l-norephedrine and d- and l-norpseudoephedrine. Cathine (d-Phenylpropanolamine or pseudonorephedrine) is found naturally in Catha edulis. Cathine is a Schedule III drug under the Convention on Psychotropic Substances. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Anti-Obesity Agents (Code: D019440) Appetite Depressants (Code: D001067) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Nasal Decongestants (Code: D014663) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 2000-09-29 FDA NPU
Click to view hydroxyamfetamine Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22037049) Hydroxyamfetamine is an amphetamine metabolite with sympathomimetic effects. It is sometimes called alpha-methyltyramine, which may also refer to the meta isomer, gepefrine. Hydroxyamphetamine, when applied topically to the eye, stimulates the release of norepinephrine from postganglionic adrenergic nerves resulting in the stimulation of both alpha and beta adrenergic receptors. Local alpha stimulatory effects include dilation of the pupil, increased flow of aqueous humor, and vasoconstriction; whereas beta stimulatory effects include relaxation of the ciliary muscle and a decreased production in aqueous humor. The main use of hydroxyamphetamines as eye drops is the diagnosis of Horner's syndrome which is characterized by nerve lesions. Adrenergic Agonists (Code: N0000000122) Adrenergic Receptor Agonist (Code: N0000175883) 1969-07-16 FDA AEG
Click to view gepefrine isomer of PARA-HYDROXYAMPHETAMINE which is also called alpha-methyl-tyramine
Click to view amantadine Glutamate [NMDA] receptor (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q12879|Q13224|Q14957|O15399|Q8TCU5|O60391, gene: GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B, swissprot: NMDZ1_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMDE4_HUMAN|NMD3A_HUMAN|NMD3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208944lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208944lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208944lbl.pdf) Matrix protein 2 (Organism: Influenza A virus (strain A/Udorn/307/1972 H3N2), class: Ion channel, accessions: P63231, gene: M, swissprot: M2_I72A2) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/016023s041,018101s016lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12089365) Amantadine is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A. The mechanisms of its effects in movement disorders are not well understood but probably reflect an increase in synthesis and release of dopamine, with perhaps some inhibition of dopamine uptake. It is also used as an antiparkinsonian agent, to treat extrapyramidal reactions, and for postherpetic neuralgia. antiviral drug (Code: CHEBI:36044) antiparkinson drug (Code: CHEBI:48407) dopaminergic agent (Code: CHEBI:48560) analgesic (Code: CHEBI:35480) non-narcotic analgesic (Code: CHEBI:35481) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Dyskinesia Agents (Code: D018726) Anti-Infective Agents (Code: D000890) Antiparkinson Agents (Code: D000978) Antiviral Agents (Code: D000998) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Influenza A M2 Protein Inhibitor (Code: N0000175543) M2 Protein Inhibitors (Code: N0000175542) 1968-02-14 FDA 308
Click to view methylparaben Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Transient receptor potential cation channel subfamily A member 1 (Organism: Mus musculus, class: Unclassified, accessions: Q8BLA8, gene: Trpa1, swissprot: TRPA1_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17351650) Methylparaben (E number E218) is preservative in the food, cosmetic, and pharmaceutical industries. It is completely absorbed through the skin or after ingestion and and it is hydrolyzed to para-hydroxybenzoic acid, and metabolites are rapidly excreted in the urine. Methylparaben is used in allergenic testing. Also methylparaben in combination with other drugs used for short term treatment of chronic wounds including stage III & IV pressure sores, leg ulcers. antimicrobial food preservative (Code: CHEBI:65256) neuroprotective agent (Code: CHEBI:63726) Pharmaceutic Aids (Code: D010592) Preservatives, Pharmaceutical (Code: D011310) Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) 2010-07-06 CDSCO (INDIA) MPB
Click to view mandelic acid Mandelic Acid is an aromatic alpha hydroxy acid. In an acid urine, mandelic acid exerts its antibacterial action and also contributes to the acidification of the urine. Mandelic acid is excreted by both glomerular filtration and tubular excretion. Mandelic acid is used for the treatment of urinary tract infections. 1951-12-31 Health Canada SMN
RMN
Click to view hydroxymethylnicotinamide Hydroxymethylnicotinamide the amide derivative of nicotinic acid and formaldehyde. Has a choleretic effect, and also promotes the secretion of bile. In addition, it has a bacteriostatic and bactericidal action, which is due to the fact that during the metabolism, the formaldehyde part of the drug molecule is cleaved. The other part of the molecule (nicotinamide) has the properties of vitamin PP, increases the secretory function of the liver parenchyma, enhancing the secretion of bile and facilitating its entry into the intestine. Hydroxymethylnicotinamide is used in complex treatment violations of the liver, with cholecystitis, as well as infections of the urinary tract and gastroenteritis. It is effective in the treatment of infections caused by E. coli. 1964-04-30 Ministry of Health of the Russian Federation
Click to view tisopurine Thiopurinol inhibited aggregation of platelets induced by ADP and arachidonic acid but did not inhibit superoxide generation. Tisopurine has been shown to reduce effectively both the plasma and urinary uric acid levels of hyperexcretors, but plasma levels only of normal excretors. Tisopurine reduces uric acid concentrations by interfering with the early stages of its synthesis, thus avoiding increased blood concentrations of hypoxanthine and xanthine. Thiopurinol was used for the treatment of gout. Antirheumatic Agents (Code: D018501) Gout Suppressants (Code: D006074)
Click to view debrisoquine Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2601584) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2601584) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12023534) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12023534) Debrisoquin is an antihypertensive drug having guanethidine-like properties. Debrisoquin acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine, rather than acting at the effector cell by inhibiting the association of norepinephrine with its receptors. Debrisoquine was used for the treatment of hypertension. Debrisoquine hydroxylation has been used test in humans to evaluate CYP2D6 activity. antihypertensive agent (Code: CHEBI:35674) adrenergic agent (Code: CHEBI:37962) sympatholytic agent (Code: CHEBI:66991) Adrenergic Agents (Code: D018663) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1965-01-01 YEAR INTRODUCED
Click to view mercaptopurine Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12358729) Mercaptopurine activation occurs via hypoxanthine-guanine phosphoribosyl transferase (HGPRTase) and several enzymes to form 6-thioguanine nucleotides (6-TGNs). Incorporation of 6-TGN into nucleic acids (instead of purine bases) results in cell-cycle arrest and cell death. Mercaptopurine competes with hypoxanthine and guanine for HGPRTase and is itself converted to thioinosinic acid (TIMP). This intracellular nucleotide inhibits several reactions involving inosinic acid (IMP), including the conversion of IMP to xanthylic acid (XMP) and the conversion of IMP to adenylic acid (AMP) via adenylosuccinate (SAMP). In addition, 6-methylthioinosinate (MTIMP) is formed by the methylation of TIMP. Both TIMP and MTIMP have been reported to inhibit glutamine-5-phosphoribosylpyrophosphate amidotransferase, the first enzyme unique to the de novo pathway for purine ribonucleotide synthesis. Experiments indicate that radiolabeled mercaptopurine may be recovered from the DNA in the form of deoxythioguanosine. Some mercaptopurine is converted to nucleotide derivatives of 6-thioguanine (6-TG) by the sequential actions of inosinate (IMP) dehydrogenase and xanthylate (XMP) aminase, converting TIMP to thioguanylic acid (TGMP). antineoplastic agent (Code: CHEBI:35610) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Noxae (Code: D009676) Nucleic Acid Synthesis Inhibitors (Code: D019384) 1953-09-11 FDA
Click to view homocamfin Homocamfin is a stimulant. It has cardiopulmonary effect (increase output). It is no longer available.
Click to view camphor Transient receptor potential cation channel subfamily V member 1 (Organism: Rattus norvegicus, class: Unclassified, accessions: O35433, gene: Trpv1, swissprot: TRPV1_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16192383) Transient receptor potential cation channel subfamily A member 1 (Organism: Mus musculus, class: Unclassified, accessions: Q8BLA8, gene: Trpa1, swissprot: TRPA1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16192383) A bicyclic monoterpene ketone found widely in plants, especially cinnamomum camphora. It is used topically as a skin antipruritic and as an anti-infective agent. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 1970-11-12 Ministry of Health of the Russian Federation
Click to view aminosalicylic acid Dihydrofolate reductase (Organism: Mycobacterium tuberculosis, class: Enzyme, accessions: P9WNX1, gene: folA, swissprot: DYR_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23779105) Aminosalicylic acid is bacteriostatic against Mycobacterium tuberculosis. It inhibits the onset of bacterial resistance to streptomycin and isoniazid. The mechanism of action has been postulated to be inhibition of folic acid synthesis (but without potentiation with antifolic compounds) and/or inhibition of synthesis of the cell wall component, mycobactin, thus reducing iron uptake by M. tuberculosis. Aminosalicylic acid is indicated for the treatment of tuberculosis in combination with other active agents. It is most commonly used in patients with Multi-drug Resistant TB or in situations when therapy with isoniazid and rifampin is not possible due to a combination of resistance and/or intolerance. antitubercular agent (Code: CHEBI:33231) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antitubercular Agents (Code: D000995) 1982-01-01 FDA BHA
Click to view mesalazine Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15824083) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12950415) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12950415) Mitogen-activated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P28482, gene: MAPK1, swissprot: MK01_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12950415) Mitogen-activated protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: P27361, gene: MAPK3, swissprot: MK03_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12950415) Mitogen-activated protein kinase 8 (Organism: Homo sapiens, class: Kinase, accessions: P45983, gene: MAPK8, swissprot: MK08_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12950415) Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/6131674) Nitric oxide synthase, inducible (Organism: Homo sapiens, class: Enzyme, accessions: P35228, gene: NOS2, swissprot: NOS2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10493988) Intermediate conductance calcium-activated potassium channel protein 4 (Organism: Homo sapiens, class: Ion channel, accessions: O15554, gene: KCNN4, swissprot: KCNN4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23516517) Mesalamine is an agent derived from sulfasalazine, an antiinflammatory agent. Mesalamine may reduce inflammation through inhibition of cyclooxygenase and prostaglandin production. Mesalamine is used for the treatment of ulcerative colitis to both induce and maintain remissions in disease. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Aminosalicylate (Code: N0000175781) Aminosalicylic Acids (Code: N0000005760) 1987-12-24 FDA
Click to view octopamine Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18524885) Octopamine is an organic chemical closely related to norepinephrine. Octopamine exerts adrenergic effects. Octopamine is an endogenous selective beta(3)-AR agonist. In humans Octopamine is a trace amine found endogenously in the human brain where it interacts with signalling of catecholamines; it is structurally similar to synephrine and tyramine, being a metabolite of the latter (via dopamine beta-hydroxylase) and substrate for the synthesis of the former (via phenethanolamine N-methyltransferase) while being perhaps the closest in structure to noradrenaline. Octopamine is used as dietary supplements.Octopamine was used as a nootropic. All optical isomers (enantiomers) of octopamine are on the World Anti-Doping Agency (WADA) 2014 list of substances prohibited in competition. It was used for the treatment of hypotension. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasoconstrictor Agents (Code: D014662) OTS
OTR
Click to view enbucrilate A tissue adhesive that is applied as a monomer to moist tissue and polymerizes to form a bond. It is slowly biodegradable and used in all kinds of surgery, including dental.
Click to view norfenefrine Norfenefrine (meta-octopamine) is an adrenergic agent. Along with its structural isomer p-octopamine and the tyramines, norfenefrine is a naturally occurring, endogenous trace amine and plays a role as a minor neurotransmitter in the brain. Norfenefrine is used for the treatment of acute hypotension. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Neurotransmitter Agents (Code: D018377)
Click to view dopamine D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17301410) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17301410) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17301410) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17301410) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17301410) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11071707) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11071707) One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action. cardiotonic drug (Code: CHEBI:38147) beta-adrenergic agonist (Code: CHEBI:35522) dopaminergic agent (Code: CHEBI:48560) sympathomimetic agent (Code: CHEBI:35524) Catecholamine (Code: N0000175570) Catecholamines (Code: N0000007715) Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Dopamine Agents (Code: D015259) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sympathomimetics (Code: D013566) 1974-02-25 FDA LDP
Click to view gentisic acid Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Gentisic acid is a dihydroxybenzoic acid. Gentisic acid is an active metabolite of salicylic acid degradation. Gentisic acid is also a byproduct of tyrosine and benzoate metabolism. The antioxidant activity and radioprotective properties of gentisic acid are exerted by its phenoxyl group. It is also used in cosmetics as a skin-whitening agent for the treatment of skin pigmentary disorders by influencing the synthesis of melanin through inhibition of melanosomal tyrosinase activity. In the laboratory, it is used as a sample matrix in matrix-assisted laser desorption/ionization (MALDI) mass spectrometry, and has been shown to conveniently detect peptides incorporating the boronic acid moiety by MALDI. MALDI matrix material (Code: CHEBI:64345) GTQ
Click to view acipimox Hydroxycarboxylic acid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDS4, gene: HCAR2, swissprot: HCAR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12522134) Acipimox is a niacin derivative used as a hypolipidemic agent. It is used in low doses and may have less marked adverse effects, although it is unclear whether the recommended dose is as effective as are standard doses of nicotinic acid. Acipimox inhibits the production of triglycerides by the liver and the secretion of VLDL, which leads indirectly to a modest reduction in LDL and increase in HDL. Long-term administration is associated with reduced mortality, but unwanted effects limit its clinical use. Acipimox is indicated as alternative or adjunct treatment to reduce triglyceride levels in patients who have not responded adequately to other treatments such as statin or fibrate treatment for hypertriglyceridaemia (Fredrickson type IV hyperlipoproteinaemia) or hypercholesterolaemia and hypertriglyceridaemia (Fredrickson type IIB hyperlipoproteinaemia). Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) 1991-01-16 Austrian Medicines and Medical Devices Agency
Click to view guancidine Guancidine is an antihypertensive agent.
Click to view allomethadione Allomethadione (aloxidone) is an anticonvulsivant N-allyl derivatives of hydantoin. It was used for the treatment of epilepsy.
Click to view chlorphenesin carbamate A centrally acting muscle relaxant. Its mode of action is unknown. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1203) muscle relaxant (Code: CHEBI:51371) Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 1965-06-14 FDA
Click to view histidine Histidine decarboxylase (Organism: Homo sapiens, class: Enzyme, accessions: P19113, gene: HDC, swissprot: DCHS_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17965265) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17499996) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17499996) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17499996) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18627905) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18627905) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Solute carrier family 15 member 4 (Organism: Homo sapiens, class: Transporter, accessions: Q8N697, gene: SLC15A4, swissprot: S15A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16289537) Solute carrier family 15 member 3 (Organism: Rattus norvegicus, class: Transporter, accessions: Q924V4, gene: Slc15a3, swissprot: S15A3_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11336635) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16730978) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/19464888) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20061162) Histidine is an essential amino acid. L-histidine is converted to histamine by histidine decarboxylase, a pyridoxal 5'-phosphate-dependent enzyme. The efficacy of L-histidine in protecting inflamed tissue is attributed to the capacity of the imidazole ring to scavenge reactive oxygen species generated by cells during acute inflammatory response. Histidine, when administered in therapeutic quantities is able to inhibit cytokines and growth factors involved in cell and tissue damage. 1975 FDA DHI
HIS
Click to view bemegride Bemegride is a CNS stimulant that is used to induce convulsions in experimental animals. It has also been used as a respiratory stimulant and in the treatment of barbiturate overdose. Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Convulsants (Code: D003292) Respiratory System Agents (Code: D019141) 1970-03-30 Ministry of Health of the Russian Federation
Click to view valdetamide Sedative
Click to view propylhexedrine Propylhexedrine is considered to be an agonist of alpha-adrenergic receptors. Exact mechanism of action unknown but thought to be similar to amphetamine. It is used for temporary symptomatic relief of nasal decongestion due to colds, allergies and allergic rhinitis.
Click to view pempidine A nicotinic antagonist most commonly used as an experimental tool. It has been used as a ganglionic blocker in the treatment of hypertension but has largely been supplanted for that purpose by more specific drugs. Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Ganglionic Blockers (Code: D005730) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373)
Click to view bucolome Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10497145) Bucolome (Paramidine) is a barbiturate derivative. It is a non-steroidal anti-inflammatory drug. It has been used as a uricosuric and/or anti-inflammatory agent. Bucolome is used to treatment inflammation, pain, fever in rheumatoid arthritis, osteoarthritis, cystitis, erythema multiforme, acute sinusitis, otitis media, appendicitis and for the treatment of gout hyperuricemia. 1989-01-01 PMDA
Click to view mechlorethamine Mechlorethamine, also known as nitrogen mustard, is an alkylating agent which inhibits rapidly proliferating cells. Nitrogen mustard (a member of a family of chemotherapy agents including cyclophosphamide and chlorambucil) is an irritant and carcinogenic agent metabolized to a highly reactive ethylene immonium derivative; the ethylene immonium derivative alkylates DNA and inhibits DNA replication. This agent also exhibits lympholytic properties. Mechlorethamine has been in clinical use for more than 60 years, given systemically in combination with other antineoplastic agents to treat Hodgkin disease, chronic leukemias, lung cancer and polycythemia vera. Currently, however, it is used largely as a topical gel for therapy of cutaneous T-cell lymphomas and mycosis fungoides. Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Chemical Warfare Agents (Code: D002619) Irritants (Code: D007509) Noxae (Code: D009676) Poisons (Code: D011042) 1949-03-15 FDA
Click to view orotic acid Uridine 5'-monophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P11172, gene: UMPS, swissprot: UMPS_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/26059769) Orotic acid appears as minor dietary constituent. Indeed, until it was realized that it could be synthesized by humans, orotic acid was known as vitamin B-13. but it is now known that it is not a vitamin and is synthesized in the body, where it arises as an intermediate in the pathway for the synthesis of pyrimidine nucleotides. The richest dietary sources of orotic acid are cow's milk and other dairy products as well as root vegetables such as carrots and beets. Orotic acid levels are elevated in the urea cycle defects ornithine transcarbamylase (OTC) deficiency, citrullinemia and argininosuccinic acidemia, as well as the mitochondrial transport disorder hyperornithinemia-hyperammonemia-homocitrullinuria (HHH) syndrome. 1968-04-30 Ministry of Health of the Russian Federation ORO
Click to view nifuroxime Nifuroxime is anti-infective agent used in protozoal and fungal infections. It works by adsorbing (binding) large numbers of bacteria and toxins and reducing the loss of water. Nifuroxime has been withdrawm from the market in many countries.
Click to view diethadione Diethadione is an analeptics with a strong stimulating action on the CNS and especially on the respiratory center.
Click to view ectylurea Ectylurea (2-ethyl-cis crotonylurea) is a sedative and psychotherapeutic drug that produces mild depression of the central nervous system, an action shared with other substituted urea compounds. It was used for the treatment of anxiety and tension. 1956 YEAR INTRODUCED
Click to view iprazochrome used in prophylaxis of migraine Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702)
Click to view chloroxylenol Chloroxylenol (para-chloro-meta-xylenol) is an antiseptic and disinfectant agent. It is bactericidal against most Gram-positive bacteria but less effective against Staphylococci and Gram-negative bacteria, and often inactive against Pseudomonas species. It is ineffective against bacterial spores. The hydroxyl -OH groups of the chloroxylenol molecule binds to certain proteins on the cell membrane of bacteria, and disrupts the membrane. This allows chloroxylenol to enter the bacterial cell to bind further with more proteins and enzymes. At particularly high concentrations of chloroxylenol, the protein and nucleic acid content of targeted bacterial cells become coagulated and cease to function, leading to rapid cell death. Chloroxylenol is used for cleaning and disinfecting wounds, abrasions and abscesses, for minor cuts and scratches, insect bites, burns, inflammation of the skin. It is also found in hair conditioners, toilet cleaners, deodorants, soaps and paste. molluscicide (Code: CHEBI:33904) antiseptic drug (Code: CHEBI:48218) Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Disinfectants (Code: D004202) Schistosomicides (Code: D012556) 1951-12-31 Health Canada
Click to view oteracil Uridine 5'-monophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P11172, gene: UMPS, swissprot: UMPS_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Oteracil is an orotate phosphoribosyltransferase (OPRT) inhibitor that decreases the activity of 5-fluorouracil in normal gastrointestinal mucosa. It is used in combination with Gimeracil and Tegafur as an adjunct to antineoplastic therapy, used to reduce the toxic side effects associated with chemotherapy. 2011-03-14 EMA
Click to view furamicid Furamicid (2-methoxymethyl-5-nitrofuran) is an derivative of 5-nitrofuran and an antifungal agent.
Click to view paramethadione Paramethadione is an anticonvulsant in the oxazolidinedione class. Paramethadione acts to reduce T-type calcium currents in thalamic neurons. Paramethadione is used for the control of absence (petit mal) seizures that are refractory to treatment with other medications. 1949-06-15 FDA
Click to view nitrefazole Nitrefazole is a nitroimidazole derivative with the ability to inhibit aldehyde dehydrogenase. Nitrefazole was used in the treatment of alcoholism and withdrawn following reports of hepatotoxicity.
Click to view ethadione Ethadione is an oxazolidine derivative and an anticonvulsant. Ethadione was used as an anti-seizure preparation.
Click to view tranexamic acid Plasminogen (Organism: Homo sapiens, class: Enzyme, accessions: P00747, gene: PLG, swissprot: PLMN_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019281s041lbl.pdf) Tranexamic Acid is a synthetic derivative of the amino acid lysine with antifibrinolytic activity. With strong affinity for the five lysine-binding sites of plasminogen, tranexamic acid competitively inhibits the activation of plasminogen to plasmin, resulting in inhibition of fibrinolysis; at higher concentrations, this agent noncompetitively inhibits plasmin. This agent has a longer half-life, is approximately ten times more potent, and is less toxic than aminocaproic acid, which possesses similar mechanisms of action. Tranexamic Acid is indicated in patients with hemophilia for short-term use (two to eight days) to reduce or prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction. hematologic agent (Code: CHEBI:50248) antifibrinolytic drug (Code: CHEBI:48675) Antifibrinolytic Agent (Code: N0000175634) Decreased Fibrinolysis (Code: N0000175632) Antifibrinolytic Agents (Code: D000933) Coagulants (Code: D003029) Fibrin Modulating Agents (Code: D050299) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) 1986-12-30 FDA AMH
Click to view oxanamide Oxanamide is a central nervous system depressant resembling short-acting barbiturates. The exact mechanism of action of oxanamide is unknown.
Click to view buformin Solute carrier family 22 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63089, gene: Slc22a1, swissprot: S22A1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130709) Buformin is an agent belonging to the biguanide class of antidiabetics with antihyperglycemic activity. Buformin exerts its activity via activation of AMPK and inhibition of the mTOR signaling pathways. Buformin is used for the treatment of type 2 diabetes mellitus. Buformin was withdrawn from the market in many countries due to an elevated risk of causing lactic acidosis. Hypoglycemic Agents (Code: D007004) 2007-09-14 PMDA
Click to view isovaleryl diethylamide -
Click to view methylphenidate Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17228864) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17228864) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) (Source: https://www.ncbi.nlm.nih.gov/pubmed/17228864) Liver carboxylesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23141, gene: CES1, swissprot: EST1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15082749) Methylphenidate is a central nervous system (CNS) stimulant. Methylphenidate is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space.Methylphenidate is a racemic mixture comprised of the d-and l-threo enantiomers. The d-threo enantiomer is more pharmacologically active than the l-threo enantiomer. Methylphenidate is indicated for the treatment of attention deficit hyperactivity disorder and narcolepsy. adrenergic agent (Code: CHEBI:37962) adrenergic uptake inhibitor (Code: CHEBI:35640) dopamine uptake inhibitor (Code: CHEBI:51039) central nervous system stimulant (Code: CHEBI:35337) sympathomimetic agent (Code: CHEBI:35524) psychotropic drug (Code: CHEBI:35471) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Central Nervous System Stimulation (Code: N0000175729) methylphenidate: 1955-12-05 FDA dexmethylphenidate: 2001-11-13 FDA
Click to view oxiracetam Oxiracetam is an ampakine of the nootropic racetam chemical class. Oxiracetam is a positive AMPA modulator similar in mechanism and potency (but not the binding site) to both piracetam and aniracetam but may have an additional benefit of increasing glutamate, acetylcholine, and D-aspartic acid release from activated but not resting neurons. Oxiracetam has been proved as an efficient memory enhancer if taken consistently. Thus, the drug enhances an overall quality of life of patients suffering from ADHD, dementia, and other neurological problems. Central Nervous System Agents (Code: D002491) Nootropic Agents (Code: D018697) Psychotropic Drugs (Code: D011619) 1988 Italian Medicines Agency (AIFA)
Click to view tiliquinol Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Tiliquinol is an antiprotozoal agent that is used in combination with tibroquinol. The combination agent was withdrawn in some countries because of hepatoxicity. 1997-06-30 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view citiolone Citiolone is a derivative of the amino acid cysteine.Citiolone is a mucolytic agent. Citiolone is used for the treatment of hepatic disorders. 1976 Italian Medicines Agency (AIFA)
Click to view pregabalin Voltage-dependent calcium channel subunit alpha-2/delta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P54289, gene: CACNA2D1, swissprot: CA2D1_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021446s036,022488s014lbl.pdf) Voltage-dependent calcium channel subunit alpha-2/delta-2 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NY47, gene: CACNA2D2, swissprot: CA2D2_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021446s036,022488s014lbl.pdf) Large neutral amino acids transporter small subunit 1 (Organism: Homo sapiens, class: Transporter, accessions: Q01650, gene: SLC7A5, swissprot: LAT1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021446s036,022488s014lbl.pdf) Pregabalin is a 3-isobutyl derivative of gamma-amino butyric acid (GABA) with anti-convulsant, anti-epileptic, anxiolytic, and analgesic activities. Pregabalin binds with high affinity to the alpha2-delta site of voltage-gated calcium channels in central nervous system tissues. Pregabalin is indicated for the treatment neuropathic pain associated with diabetic peripheral neuropathy, postherpetic neuralgia, fibromyalgia, neuropathic pain associated with spinal cord injury and for adjunctive therapy for patients with partial onset seizures. anticonvulsant (Code: CHEBI:35623) Analgesics (Code: D000700) Anti-Anxiety Agents (Code: D014151) Anticonvulsants (Code: D000927) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Membrane Transport Modulators (Code: D049990) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) Tranquilizing Agents (Code: D014149) 2004-07-06 EMA
Click to view pargyline Pargyline is a monoamine oxidase (MAO) inhibitor with antidepressant activity. Pargyline selectively inhibits MAO type B, an enzyme catalyzing the oxidative deamination and inactivation of certain catecholamines, such as norepinephrine and dopamine, within the presynaptic nerve terminals. By inhibiting the metabolism of these biogenic amines in the brain, pargyline increases their concentration and binding to postsynaptic receptors. Increased receptor stimulation may cause downregulation of central receptors which may attribute to pargyline's antidepressant effect. It was approved for the treatment hypertension, but then this drug was discontinued. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) 1982-01-01 FDA
Click to view methylchromone Methylchromone (3-methylchromone) is the first synthetic chromone to be used clinically. It has both antispasmodic and coronary vasodilator actions. It was recommended for the treatment of angina pectoris but it doesn’t produce any remarkable improvements and its clinical use has been discontinued.
Click to view hydralazine Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28197313) Hydralazine is a selective dilator of arterial smooth muscle. Animal data suggests that hydralazine may also mitigate tolerance to nitrates. It inhibits membrane-bound enzymes that form reactive oxygen species, such as superoxides. Excessive superoxide counteracts NO-induced vasodilation. Hydralazine is used for the treatment of essential hypertension, alone or as an adjunct. Also for the management of severe hypertension when the drug cannot be given orally or when blood pressure must be lowered immediately, congestive heart failure (in combination with cardiac glycosides and diuretics and/or with isosorbide dinitrate), and hypertension secondary to pre-eclampsia/eclampsia. antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) Arteriolar Vasodilation (Code: N0000175379) Arteriolar Vasodilator (Code: N0000175564) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1953-01-15 FDA HLZ
Click to view tolazoline Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9605427) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9605427) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9605427) Tolazoline is a vasodilator that apparently has direct actions on blood vessels and also increases cardiac output. Tolazoline can interact to some degree with histamine, adrenergic, and cholinergic receptors, but the mechanisms of its therapeutic effects are not clear. It is used in treatment of persistent pulmonary hypertension of the newborn. alpha-adrenergic antagonist (Code: CHEBI:37890) antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) 1948-03-17 FDA
Click to view methacholine Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9622546) Muscarinic acetylcholine receptor M3 (Organism: Rattus norvegicus, class: GPCR, accessions: P08483, gene: Chrm3, swissprot: ACM3_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9622546) Methacholine is a parasympathomimetic (cholinergic) bronchoconstrictor agent. Methacholine agonizes the muscarinic receptors which eventually induce bronchoconstriction. It is hydrolyzed by acetylcholinesterase at a considerably slower rate than acetylcholine and is more resistant to hydrolysis by nonspecific cholinesterases so that its actions are more prolonged. Methacholine is indicated for the diagnosis of bronchial airway hyperreactivity (methacholine challenge test). muscarinic agonist (Code: CHEBI:38325) bronchoconstrictor agent (Code: CHEBI:50141) cholinergic agonist (Code: CHEBI:38324) vasodilator agent (Code: CHEBI:35620) Cholinergic Receptor Agonist (Code: N0000175884) Autonomic Agents (Code: D001337) Bronchoconstrictor Agents (Code: D016085) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Miotics (Code: D008916) Muscarinic Agonists (Code: D018721) Neurotransmitter Agents (Code: D018377) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1986-10-31 FDA
Click to view carpronium a hair growth reagent with a vasodilatory action. Carpronium chloride has local vasodilating effect and hair growth stimulatory effect to improve alopecia and vitiligo. It is usually used for the prevention of hair loss, for hair growth stimulation, and in the treatment of seborrhea sicca and vitiligo vulgaris. 1987 PMDA
Click to view clomethiazole Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs/d6d032495d6cf95a02c5f40d74aa45e2559809fd) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs/d6d032495d6cf95a02c5f40d74aa45e2559809fd) Clomethiazole is a short acting hypnotic and sedative with anticonvulsant effect. Clomethiazole interacts with the picrotoxin/barbiturate site of the GABAA-receptor-chloride channel complex. It is used for the management of restlessness and agitation in the elderly, short term treatment of severe insomnia in the elderly and treatment of alcohol withdrawal symptoms where close hospital supervision is also provided. Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neuroprotective Agents (Code: D018696) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1968-05-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view meglutol Meglutol (3-Hydroxy-3-methylglutaric acid, HMGA) is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutaryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol. It acts by interfering with the enzymatic steps involved in the conversion of acetate to hydroxymethylglutaryl coenzyme A. Meglutol is used as a hypolipidaemic agent. anticholesteremic drug (Code: CHEBI:35821) Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Hydroxymethylglutaryl-CoA Reductase Inhibitors (Code: D019161) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) 1983 Italian Medicines Agency (AIFA) MAH
Click to view fenadiazole Fenadiazole is a hypnotic drug with a unique oxadiazole-based structure.
Click to view aminorex An amphetamine-like anorectic agent. It may cause pulmonary hypertension.
Click to view levocarnitine Carnitine O-palmitoyltransferase 1, liver isoform (Organism: Homo sapiens, class: Enzyme, accessions: P50416, gene: CPT1A, swissprot: CPT1A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16362726) Levocarnitine is an amino acid derivative. Levocarnitine facilitates long-chain fatty acid entry into mitochondria, delivering substrate for oxidation and subsequent energy production. antilipemic drug (Code: CHEBI:35679) nutraceutical (Code: CHEBI:50733) nootropic agent (Code: CHEBI:66980) Carnitine (Code: N0000006688) Carnitine Analog (Code: N0000175903) 1985-12-27 FDA DCK
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Click to view oxydibutanol Oxydibutanol is an choleretic and spasmolytic agent. It is used for the treatment of constipation.
Click to view nicotine Neuronal acetylcholine receptor; alpha2/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: Q15822|P30926, gene: CHRNA2|CHRNB4, swissprot: ACHA2_HUMAN|ACHB4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Neuronal acetylcholine receptor; alpha3/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P32297|P17787, gene: CHRNA3|CHRNB2, swissprot: ACHA3_HUMAN|ACHB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P32297|P30926, gene: CHRNA3|CHRNB4, swissprot: ACHA3_HUMAN|ACHB4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P17787, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Neuronal acetylcholine receptor; alpha4/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P30926, gene: CHRNA4|CHRNB4, swissprot: ACHA4_HUMAN|ACHB4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20081230) Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/19749751) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22864238/) Cytochrome P450 2A13 (Organism: Homo sapiens, class: Enzyme, accessions: Q16696, gene: CYP2A13, swissprot: CP2AD_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22864238/) Nicotine is a plant alkaloid, found in the tobacco plant, and addictive central nervous system (CNS) stimulant that causes either ganglionic stimulation in low doses or ganglionic blockage in high doses. Nicotine acts as an agonist at the nicotinic cholinergic receptors in the autonomic ganglia, at neuromuscular junctions, and in the adrenal medulla and the brain. Nicotine's CNS-stimulating activities may be mediated through the release of several neurotransmitters, including acetylcholine, beta-endorphin, dopamine, norepinephrine, serotonin, and ACTH. As a result, peripheral vasoconstriction, tachycardia, and elevated blood pressure may be observed with nicotine intake. This agent may also stimulate the chemoreceptor trigger zone, thereby inducing nausea and vomiting. biomarker (Code: CHEBI:59163) immunomodulator (Code: CHEBI:50846) peripheral nervous system drug (Code: CHEBI:49110) psychotropic drug (Code: CHEBI:35471) anxiolytic drug (Code: CHEBI:35474) nicotinic acetylcholine receptor agonist (Code: CHEBI:47958) phytogenic insecticide (Code: CHEBI:22917) Cholinergic Nicotinic Agonist (Code: N0000175706) Nicotine (Code: N0000006496) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Ganglionic Stimulants (Code: D005731) Neurotransmitter Agents (Code: D018377) Nicotinic Agonists (Code: D018722) Peripheral Nervous System Agents (Code: D018373) 1991-11-07 FDA NCT
Click to view carsalam Carsalam is a cyclised carbamyl derivative of salicylamide. Carsalam was used as a nonsteroidal anti-inflammatory drug.
Click to view tiopronin Tiopronin is N-(2-Mercaptopropionyl) glycine which is is a reducing and cystine-binding thiol drug. Tiopronin is an active reducing agent which undergoes thiol-disulfide exchange with cystine to form a mixed disulfide of tiopronin-cysteine. From this reaction, a water-soluble mixed disulfide is formed and the amount of sparingly soluble cystine is reduced. Tiopronin is indicated, in combination with high fluid intake, alkali, and diet modification, for the prevention of cystine stone formation in patients with severe homozygous cystinuria, who are not responsive to these measures alone. Cystine Disulfide Reduction (Code: N0000175549) N-substituted Glycines (Code: N0000011378) Reducing and Complexing Thiol (Code: N0000175898) 1988-08-11 FDA WJZ
Click to view acetylcysteine Acetylcysteine is the N-acetyl derivative of the naturally occurring amino acid, L-cysteine. Acetylcysteine has been shown to reduce the extent of liver injury following acetaminophen overdose. Acetylcysteine is essentially a prodrug that is converted to cysteine (in the intestine by the enzyme aminoacylase 1) and absorbed in the intestine into the blood stream. Acetylcysteine also used as a mucolytic. (See: cysteine) antidote to paracetamol poisoning (Code: CHEBI:74529) antiinfective agent (Code: CHEBI:35441) antiviral drug (Code: CHEBI:36044) mucolytic (Code: CHEBI:77034) vulnerary (Code: CHEBI:73336) Antidote (Code: N0000175429) Antidote for Acetaminophen Overdose (Code: N0000175961) Decreased Respiratory Secretion Viscosity (Code: N0000008867) Increased Glutathione Concentration (Code: N0000175960) Reduction Activity (Code: N0000175547) Anti-Infective Agents (Code: D000890) Antioxidants (Code: D000975) Antiviral Agents (Code: D000998) Expectorants (Code: D005100) Free Radical Scavengers (Code: D016166) Respiratory System Agents (Code: D019141) 1963-09-14 FDA SC2
1ZT
Click to view cloforex carbamic ethyl ester of chlorphentermine; structure in Negwer, 5th ed, #2275
Click to view pentorex Pentorex is a phenyl-isopropylamone derivative and has an anorexigenous activity. It was used to assist with weight loss.
Click to view mephentermine Mephentermine is an amphetamine-derived phenethylamine. It is an alpha 1 adrenergic receptor agonist and a hypertensive drug. Mephentermine is mainly used as a vasopressor agent with a sympathomimetic action, primarily causing release of noradrenaline and increasing cardiac output due to positive inotropic effect on the myocardium. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-1 Receptor Agonists (Code: D058646) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1951-12-29 FDA
Click to view etilamfetamine Etilamfetamine is an amphetamine analog and was used as an appetite suppressant in the 1950s. Etilamfetamine is prohibited by WADAas a stimulant.
Click to view phenylbutanoic acid phenylbutanoic acid: Histone deacetylase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BY41, gene: HDAC8, swissprot: HDAC8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Histone deacetylase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBN7, gene: HDAC6, swissprot: HDAC6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21874153) Dihydroneopterin aldolase (Organism: Paracoccus denitrificans, class: Enzyme, accessions: P95468, gene: tyrB, swissprot: TYRB_PARDE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9930977) phenylacetate: glutamine (Organism: None, class: Amino acid, accessions: None, gene: None, swissprot: None) Binding Agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020572s016,020573s015lbl.pdf) Phenylbutanoic acid is a pro-drug and is rapidly metabolized to phenylacetate. Phenylacetate is a metabolically-active compound that conjugates with glutamine via acetylation to form phenylacetylglutamine which is excreted by the kidneys. On a molar basis, phenylacetylglutamine, like urea, contains 2 moles of nitrogen and provides an alternate vehicle for waste nitrogen excretion. Phenylbutanoic acid is indicated as adjunctive therapy in the chronic management of patients with urea cycle disorders involving deficiencies of carbamylphosphate synthetase (CPS), ornithine transcarbamylase (OTC), or argininosuccinic acid synthetase (AS). antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) Antineoplastic Agents (Code: D000970) 1996-04-30 FDA CLT
Click to view fenipentol stimulates plasma secretion & exocrine pancreatic secretion Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765) Ministry of Health of the Russian Federation
Click to view methiosulfonium chloride Methiosulfonium chloride (methylmethionine sulfonium chloride, vitamin U) is a derivative of methionine metabolism in some plants. Methylmethionine has therapeutic effects on gastrointestinal ulceration potentially via its ability to promote dermal fibroblast migration and growth. It is used in the treatment of peptic ulcers, colitis, and gastritis and has an effect on secretory, acid-forming, and enzymatic functions of the intestinal tract. 1960-06-01 PMDA
Click to view methoxyflurane Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) GABA-A receptor alpha-2/beta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P18505, gene: GABRA2|GABRB1, swissprot: GBRA1_HUMAN|GBRB1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7879937) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7879937) Methoxyflurane is a general inhalation anesthetic used for induction and maintenance of general anesthesia. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential. It was withdrawn from US market due to safety concerns. inhalation anaesthetic (Code: CHEBI:38870) non-narcotic analgesic (Code: CHEBI:35481) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) 1962 FDA
Click to view atrolactamide Atrolactamide (themisone) is an anticonvulsant. It was used for the treatment of epileptic seizures, but is no longer available due to its side effects.
Click to view phenylalanine Monocarboxylate transporter 10 (Organism: Homo sapiens, class: Transporter, accessions: Q8TF71, gene: SLC16A10, swissprot: MOT10_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11278508) Monocarboxylate transporter 10 (Organism: Homo sapiens, class: Transporter, accessions: Q8TF71, gene: SLC16A10, swissprot: MOT10_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11827462) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16214338) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16214338) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16214338) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17174092) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17174092) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20176489) Probable G-protein coupled receptor 139 (Organism: Homo sapiens, class: Unclassified, accessions: Q6DWJ6, gene: GPR139, swissprot: GP139_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24826842) Phenylalanine is an essential aromatic amino acid in humans (provided by food), Phenylalanine is a precursor of melanin; dopamine; noradrenalin (norepinephrine), and thyroxine and plays a key role in the biosynthesis of other amino acids. Phenylalanine is converted to tyrosine, used in the biosynthesis of dopamine and norepinephrine neurotransmitters. The L-form of Phenylalanine is incorporated into proteins, while the D-form acts as a painkiller. The supposed antidepressant effects of L-phenylalanine may be due to its role as a precursor in the synthesis of the neurotransmitters norepinephrine and dopamine. Elevated brain norepinephrine and dopamine levels are thought to be associated with antidepressant effects. The mechanism of L-phenylalanine's possible antivitiligo activity is not well understood. It is thought that L-phenylalanine may stimulate the production of melanin in the affected skin. 1975 FDA DPN
PHE
Click to view ethenzamide Ethenzamide is a non-steroidal anti-inflammatory drug. It is used in combination with other ingredients for the relief of fever, headaches, and other minor aches and pains. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1988-04-01 PMDA
Click to view sulfaperin Sulfaperin is a long-acting sulfanilamide antibiotic. antibacterial drug (Code: CHEBI:36047)
Click to view benzocaine Sodium channel protein type 10 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y5Y9, gene: SCN10A, swissprot: SCNAA_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/19661462) Benzocaine is a local anesthetic. Benzocaine is an ester, a compound made from the organic acid PABA (para-aminobenzoic acid) and ethanol. It acts by blocking voltage-gated sodium ion channels in nerve endings. Benzocaine is available over-the counter for local anesthesia of oral and pharyngeal mucous membranes (sore throat, cold sores, mouth ulcers, toothache, sore gums, denture irritation), otic pain, and as a local anesthetic for surgical or diagnostic procedures. Topical application of benzocaine to gums or mouth may cause rare, but serious and potentially fatal adverse effect methemoglobinemia. antipruritic drug (Code: CHEBI:59683) topical anaesthetic (Code: CHEBI:48425) Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1964-04-30 Ministry of Health of the Russian Federation
Click to view pholedrine Pholedrineis (4-Hydroxymethamphetamine) is a metabolite of methamphetamine. It was used as a topical eye drop for the purpose of dilating the pupil for diagnostic of Horner's syndrome. Also pholedrine was a frequently used drug for the treatment of severe hypotension. Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1WF
Click to view ephedrine Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208609s000lbl.pdf) Ephedrine is an alpha- and beta-adrenergic agonist that may also enhance release of norepinephrine. Ephedrine is similar in molecular structure to the well-known drugs phenylpropanolamine and methamphetamine, as well as to the important neurotransmitter epinephrine (adrenalin). Chemically, it is an alkaloid with a phenethylamine skeleton found in various plants in the genus Ephedra (family Ephedraceae). It works mainly by increasing the activity of norepinephrine (noradrenalin) on adrenergic receptors. It is most usually marketed as the hydrochloride or sulfate salt. It has been used in the treatment of several disorders including asthma, heart failure, rhinitis, and urinary incontinence, and for its central nervous system stimulatory effects in the treatment of narcolepsy and depression. It has become less extensively used with the advent of more selective agonists. Pseudoephedrine is a phenethylamine that is an isomer of ephedrine which has less central nervous system effects and usage is mainly for respiratory tract decongestion. sympathomimetic agent (Code: CHEBI:35524) vasoconstrictor agent (Code: CHEBI:50514) nasal decongestant (Code: CHEBI:77715) alpha-Adrenergic Agonist (Code: N0000175552) Adrenergic alpha-Agonists (Code: N0000000209) beta-Adrenergic Agonist (Code: N0000175555) Adrenergic beta-Agonists (Code: N0000000245) Norepinephrine Releasing Agent (Code: N0000192563) Increased Norepinephrine Activity (Code: N0000009456) Adrenergic Agents (Code: D018663) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1963-10-18 FDA
Click to view cycloguanil Bifunctional dihydrofolate reductase-thymidylate synthase (Organism: Plasmodium falciparum, class: Enzyme, accessions: P13922, gene: None, swissprot: DRTS_PLAFK) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9037017) Cycloguanil is a dihydrofolate reductase inhibitor and is a metabolite of the antimalarial drug proguanil. Cycloguanil acts on both the erythrocytic and on the pre-erythrocytic (hepatic) forms of the malaria parasites. Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) 1CY
Click to view fenoxypropazine Fenoxypropazine is a non-selective and irreversible monoamine oxidase enzyme inhibitor (MAOI), belonging to the hydrazine chemical class. It was marketed as an antidepressant in 1961 but was later withdrawn in 1966 because of its hepatotoxic potential.
Click to view edrophonium Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019677s006lbl.pdf) Edrophonium is a rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles. Also it is used in combination with atropine as a reversal agent or antagonist of nondepolarizing neuromuscular blocking agents. diagnostic agent (Code: CHEBI:33295) antidote (Code: CHEBI:50247) Cholinesterase Inhibitor (Code: N0000175723) Antidotes (Code: D000931) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1951-05-03 FDA EDR
Click to view ethionamide Polyphenol oxidase 2 (Organism: Agaricus bisporus, class: Enzyme, accessions: O42713, gene: PPO2, swissprot: PPO2_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26544630) Ethionamide is a thiocarboxamide that is pyridine-4-carbothioamide substituted by an ethyl group at position 2. Ethionamide is a prodrug that undergoes metabolic activation by conversion to the ethionamide sulphoxide. Ethionamide may be bacteriostatic or bactericidal in action, depending on the concentration of the drug attained at the site of infection and the susceptibility of the infecting organism. The exact mechanism of action of ethionamide has not been fully elucidated, but the drug appears to inhibit peptide synthesis in susceptible organisms. Its sulphoxide metabolite has been demonstrated to have antimicrobial activity against Mycobacterium tuberculosis. Ethionamide is primarily indicated for the treatment of active tuberculosis in patients with M. tuberculosis resistant to isoniazid or rifampin, or when there is intolerance on the part of the patient to other drugs. Its use alone in the treatment of tuberculosis results in the rapid development of resistance. antitubercular agent (Code: CHEBI:33231) antilipemic drug (Code: CHEBI:35679) leprostatic drug (Code: CHEBI:35816) prodrug (Code: CHEBI:50266) Antimycobacterial (Code: N0000175483) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antimetabolites (Code: D000963) Antitubercular Agents (Code: D000995) Fatty Acid Synthesis Inhibitors (Code: D054872) Hypolipidemic Agents (Code: D000960) 1965-04-30 FDA
Click to view orthocaine Orthocaine (methyl m-amino-p-hydroxybenzoate) was used as an anaesthetic for painful wounds.
Click to view aminosalicylic acid hydrazide Aminosalicylic acid hydrazide (apacizin) has activity against Mycobacterium tuberculosis.
Click to view thioguanine DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) intercalation (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/012429s028lbl.pdf) Hypoxanthine-guanine phosphoribosyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P00492, gene: HPRT1, swissprot: HPRT_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/012429s028lbl.pdf) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14643890) Thioguanine is an analogue of the nucleic acid constituent guanine, and is closely related structurally and functionally to mercaptopurine. Thioguanine is incorporated into the DNA and the RNA of human bone marrow cells. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Thioguanine is cross-resistant with mercaptopurine. Cytotoxicity is cell cycle phase-specific (S-phase). Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is itself converted to 6-thioguanilyic acid (TGMP), which reaches high intracellular concentrations at therapeutic doses. TGMP interferes with the synthesis of guanine nucleotides by its inhibition of purine biosynthesis by pseudofeedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, the first enzyme unique to the de novo pathway of purine ribonucleotide synthesis. TGMP also inhibits the conversion of inosinic acid (IMP) to xanthylic acid (XMP) by competition for the enzyme IMP dehydrogenase. Thioguanine is used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia. antineoplastic agent (Code: CHEBI:35610) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Noxae (Code: D009676) 1966-01-18 FDA DX4
Click to view oxedrine Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20217639) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20217639) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20217639) Neuromedin-U receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q9GZQ4, gene: NMUR2, swissprot: NMUR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25262941) Oxedrine (synephrine) is naturally occurring alkaloid. It is known for its longer acting adrenergic effects compared to norepinephrine. It is used as a vasoconstrictor in circulatory failure, asthma, nasal congestion, and glaucoma. Also it is used for the treatment and prevention of arterial collapse. alpha-adrenergic agonist (Code: CHEBI:35569) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Nasal Decongestants (Code: D014663) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1947-01-01 Hungary National Institute of Pharmacy and Nutrition
Click to view pyrithyldione Pyrithyldione is a sedative and hypnotic drug. It was indicated in mild cases of insomnia. Pyrithyldione was withdrawn from the marked due to several cases of agranulocytosis.
Click to view phenylephrine Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204300lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204300lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204300lbl.pdf) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10025828) Phenylephrine is a sympathomimetic amine and a postsynaptic ?1-receptor agonist with little effect on ?-receptors of the heart. Phenylephrine is mainly used to treat nasal congestion, but may also be useful in treating hypotension and shock, hypotension during spinal anaesthesia, prolongation of spinal anaesthesia, paroxysmal supraventricular tachycardia, symptomatic relief of external or internal hemorrhoids, and to increase blood pressure as an aid in the diagnosis of heart murmurs. cardiotonic drug (Code: CHEBI:38147) mydriatic agent (Code: CHEBI:50513) protective agent (Code: CHEBI:50267) vasoconstrictor agent (Code: CHEBI:50514) sympathomimetic agent (Code: CHEBI:35524) nasal decongestant (Code: CHEBI:77715) alpha-adrenergic agonist (Code: CHEBI:35569) alpha-1 Adrenergic Agonist (Code: N0000186105) Adrenergic alpha1-Agonists (Code: N0000009917) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-1 Receptor Agonists (Code: D058646) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Mydriatics (Code: D009184) Nasal Decongestants (Code: D014663) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1952-01-21 FDA
Click to view metaraminol Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist A sympathomimetic agent that acts predominantly at alpha-1 adrenergic receptors. It has been used primarily as a vasoconstrictor in the treatment of HYPOTENSION. alpha-adrenergic agonist (Code: CHEBI:35569) vasoconstrictor agent (Code: CHEBI:50514) sympathomimetic agent (Code: CHEBI:35524) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-1 Receptor Agonists (Code: D058646) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1954-09-29 FDA
Click to view ethinamate short duration hypnotic with fast onset & relatively low toxicity; may cause dependence; minor descriptor (76-85); on-line & Index Medicus search CARBAMATES (76-85) sedative (Code: CHEBI:35717) 1955-03-13 FDA
Click to view mecamylamine Neuronal acetylcholine receptor; alpha3/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P32297|P17787, gene: CHRNA3|CHRNB2, swissprot: ACHA3_HUMAN|ACHB2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11303054) Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P17787, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11303054) Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P32297|P30926, gene: CHRNA3|CHRNB4, swissprot: ACHA3_HUMAN|ACHB4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11303054) Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11303054) Mecamylamine is a nicotinic antagonist that is well absorbed from the gastrointestinal tract and crosses the blood-brain barrier. Mecamylamine has been used as a ganglionic blocker in treating hypertension, but, like most ganglionic blockers, is more often used now as a research tool. S-(+)-mecamylamine might be preferable to R-(-)-mecamylamine, because it has the decreased side effects associated with muscle-type receptors. Autonomic Ganglionic Blocker (Code: N0000175641) Decreased Autonomic Ganglionic Activity (Code: N0000175644) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Ganglionic Blockers (Code: D005730) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) 1956-03-01 FDA
Click to view desflurane Desflurane is a highly fluorinated methyl ethyl ether used for maintenance of general anaesthesia. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential. Desflurane is used as an inhalation agent for induction and/or maintenance of anesthesia for inpatient and outpatient surgery in adults. inhalation anaesthetic (Code: CHEBI:38870) General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) 1992-09-18 FDA DSF
Click to view sulfametrole Sulfametrole is a sulfonamide antibiotic. Sulfametrole inhibits folic acid formation. Sulfametrole is used in combintion with trimethoprim for the treatment of urinary tract infections, gastrointestinal infections (typhoid, paratyphoid A and B, shigellosis), diarhhea, respiratory tract infections (acute exacerbation of chronic bronchitis, otitis media, Pneumocystis jiroveci pneumonia), and ginecological infections. 1979-10-30 Austrian Medicines and Medical Devices Agency
Click to view cicrotoic acid Cicrotoic acid is an unsaturated fatty acid. Cicrotoic acid acts on bile flow and liquid composition of human bile.
Click to view zoxazolamine Intermediate conductance calcium-activated potassium channel protein 4 (Organism: Homo sapiens, class: Ion channel, accessions: O15554, gene: KCNN4, swissprot: KCNN4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10712246) Small conductance calcium-activated potassium channel protein 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P70604, gene: Kcnn2, swissprot: KCNN2_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10712246) Zoxazolamine is a centrally acting muscle relaxant. Zoxazolamine was shown to decrease striatal dopamine turnover without directly affecting dopamine synthesis, catabolism, reuptake, or release. It was used for the relief of muscle spasm in conditions such as musculoskeletal disorders and neurological diseases. Later, it was submitted for the drug's use as a uricosuric agent to treat gout. It was withdrawn from the market due to hepatotoxicity. Antirheumatic Agents (Code: D018501) Central Nervous System Agents (Code: D002491) Gout Suppressants (Code: D006074) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) Renal Agents (Code: D012076) Uricosuric Agents (Code: D014528) 1956-01-13 FDA 36R
Click to view pyridoxine Pyridoxine is the 4-methanol form of vitamin B6, an important water-soluble vitamin that is naturally present in many foods. As its classification as a vitamin implies, pyridoxine are essential nutrients required for normal functioning of many biological systems within the body. While many plants and microorganisms are able to synthesize pyridoxine through endogenous biological processes, animals must obtain it through their diet. More specifically, pyridoxine is converted to pyridoxal 5-phosphate in the body. Pyridoxine is indicated for the treatment of vitamin B6 deficiency and for the prophylaxis of Isoniazid-induced peripheral neuropathy. It is also approved for the treatment of nausea and vomiting. Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) Vitamin B6 Analog (Code: N0000192800) Vitamin B 6 (Code: N0000005657) Analogs/Derivatives (Code: N0000175452) 1947-07-28 FDA UEG
Click to view norepinephrine Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/007513Orig1s024lbl.pdf) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16722247) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9812985) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9776363) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9830022) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10454528) Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P22909|P19328|P22086, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8230093) Adrenergic receptor beta (Organism: Rattus norvegicus, class: GPCR, accessions: P18090|P10608|P26255, gene: Adrb1|Adrb2|Adrb3, swissprot: ADRB1_RAT|ADRB2_RAT|ADRB3_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8230093) Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P43140|P15823|P23944, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8230093) Norepinephrine is a naturally occurring catecholamine hormone that functions as a neurotransmitter in the sympathetic nervous system. Norepinephrine directly stimulates adrenergic receptors. Stimulation of alpha-adrenergic receptors causes vasoconstriction of the radial smooth muscle of the iris, arteries, arterioles, veins, urinary bladder, and the sphincter of the gastrointestinal tract. Stimulation of beta-1 adrenergic receptors causes an increase in myocardial contractility, heart rate, automaticity, and atrioventricular (AV) conduction while stimulation of beta-2 adrenergic receptors causes bronchiolar and vascular smooth muscle dilatation. Norepinephrine may be used for blood pressure control in certain acute hypotensive states (e.g., pheochromocytomectomy, sympathectomy, poliomyelitis, spinal anesthesia, myocardial infarction, septicemia, blood transfusion, and drug reactions) and as an adjunct in the treatment of cardiac arrest and profound hypotension. Catecholamine (Code: N0000175570) Catecholamines (Code: N0000007715) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1950-07-13 FDA LNR
E5E
Click to view dichlorobenzyl alcohol Dichlorobenzyl alcohol is a mild antiseptic with a broad spectrum for bacterial and virus associated with mouth and throat infections. Dichlorobenzyl alcohol is considered as an active ingredient found in several marketed OTC products. On the other hand, dichlorobenzyl alcohol is categorized by the FDA in the inactive ingredient for approved drug products. The local anesthetic action of dichlorobenzyl alcohol is thought to be due to a reduced sodium channel blockade. The antiseptic mechanism of action of dichlorobenzyl alcohol is not fully understood but it is thought to be related to a denaturation of external proteins and rearrangement of the tertiary structure proteins. Dichlorobenzyl alcohol in combination with Amylmetacresol is available in over-the-counter products used for symptomatic relief of acute sore throat and postoperative sore throat. antiseptic drug (Code: CHEBI:48218) 1996-12-31 Health Canada
Click to view piperidione Piperidione has a sedative and hypnotic properties. Piperidione was used as an antitussive, but piperidione inhibited respiration.
Click to view chlorzoxazone Intermediate conductance calcium-activated potassium channel protein 4 (Organism: Homo sapiens, class: Ion channel, accessions: O15554, gene: KCNN4, swissprot: KCNN4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10712246) Small conductance calcium-activated potassium channel protein 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P70604, gene: Kcnn2, swissprot: KCNN2_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10712246) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7550365) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7550365) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10534312) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10534312) Chlorzoxazone is a benzoxazolone derivative with mild sedative and centrally-acting muscle relaxant activities. Although its exact mechanism of action is unknown, chlorzoxazone appears to act at the spinal cord and subcortical levels of the brain to inhibit multisynaptic reflex arcs involved in producing and maintaining muscle spasms. The clinical result is a reduction of the skeletal muscle spasm with relief of pain and increased mobility of the involved muscles. Chlorzoxazone is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions. Chlorzoxazone does not directly relax tense skeletal muscles in man. muscle relaxant (Code: CHEBI:51371) sedative (Code: CHEBI:35717) Centrally-mediated Muscle Relaxation (Code: N0000175730) Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 1958-08-15 FDA CLW
Click to view levetiracetam Synaptic vesicle glycoprotein 2A (Organism: Homo sapiens, class: Transporter, accessions: Q7L0J3, gene: SV2A, swissprot: SV2A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17461889) Voltage-dependent N-type calcium channel subunit alpha-1B (Organism: Homo sapiens, class: Ion channel, accessions: Q00975, gene: CACNA1B, swissprot: CACNA1B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207958s008lbl.pdf) Levetiracetam is a pyrrolidine with antiepileptic activity. Levetiracetam inhibits burst firing without affecting normal neuronal excitability, which suggests that it may selectively prevent hyper-synchronization of epileptiform burst firing and propagation of seizure activity. The antiepileptic activity of levetiracetam was assessed in a number of animal models of epileptic seizures. Levetiracetam did not inhibit single seizures induced by maximal stimulation with electrical current or different chemoconvulsants and showed only minimal activity in submaximal stimulation and in threshold tests. Protection was observed, however, against secondarily generalized activity from focal seizures induced by pilocarpine and kainic acid, two chemoconvulsants that induce seizures that mimic some features of human complex partial seizures with secondary generalization. Levetiracetam also displayed inhibitory properties in the kindling model in rats, another model of human complex partial seizures, both during kindling development and in the fully kindled state. anticonvulsant (Code: CHEBI:35623) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) 1999-11-30 FDA
Click to view propylthiouracil Thyroid peroxidase (Organism: Homo sapiens, class: Enzyme, accessions: P07202, gene: TPO, swissprot: PERT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26509551) Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26509551) Dopamine beta-hydroxylase (Organism: Bos taurus, class: Unclassified, accessions: P15101, gene: DBH, swissprot: DOPO_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/880264) Propylthiouracil (PTU) is a thiourea derivative with antithyroid property. Propylthiouracil interferes with the oxidation of iodine possibly by interaction with peroxidase or a peroxidase-mediated complex reaction, thereby inhibiting synthesis of thyroid hormones tri-iodothyronine (T3) and thyroxine (T4). In addition, this agent inhibits the Type I 5'-deiodinase (D1), an enzyme involved in the peripheral conversion of thyroxine to tri-iodothyronine. Propylthiouracil is used to manage hyperthyroidism which is due to Grave's disease. antithyroid drug (Code: CHEBI:50671) hormone antagonist (Code: CHEBI:49020) antidote to paracetamol poisoning (Code: CHEBI:74529) Antimetabolites (Code: D000963) Antithyroid Agents (Code: D013956) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Noxae (Code: D009676) Thyroid Hormone Synthesis Inhibitor (Code: N0000175918) Thyroid Hormone Synthesis Inhibitors (Code: N0000175917) 1947-07-28 FDA 3CJ
Click to view sobrerol Sobrerol is a cyclic terpene derivative. Sobrerol may increase mucus production and volume but reduce overall viscosity. (-)-trans-sobrerol enantiomer has a central antitussive activity, which has never been described for racemic sobrerol, as well as a lower toxicity than the latter. Sobrerol is used as mucolitic for the treatment of chronic obstructive pulmonary diseases. Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) 1970 Italian Medicines Agency (AIFA)
Click to view metronidazole Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23813797) Metronidazole, a nitroimidazole, exerts antibacterial effects in an anaerobic environment against most obligate anaerobes. Once metronidazole enters the organism by passive diffusion and activated in the cytoplasm of susceptible anaerobic bacteria, it is reduced; this process includes intracellular electron transport proteins such as ferredoxin, transfer of an electron to the nitro group of the metronidazole, and formation of a short-lived nitroso free radical. Because of this alteration of the metronidazole molecule, a concentration gradient is created and maintained which promotes the drug’s intracellular transport. The reduced form of metronidazole and free radicals can interact with DNA leading to inhibition of DNA synthesis and DNA degradation leading to death of the bacteria. The precise mechanism of action of metronidazole is unclear. Metronidazole has been shown to be active against: Clostridium species, Eubacterium species, Peptococcus species, Peptostreptococcus species, Bacteroides fragilis group (B. fragilis, B. distasonis, B. ovatus, B. thetaiotaomicron, B.vulgatus), Fusobacterium species, Entamoeba histolytica and Trichomonas vaginalis. Metronidazole is indicated for the treatment of trichomoniasis, amebiasis, intra-abdominal infections, skin and skin structure infections, gynecologycal infections, septicimia, bone and joint infections, CNS infections, lower respiratory tract infections, endocarditis. antitrichomonal drug (Code: CHEBI:50685) prodrug (Code: CHEBI:50266) antibacterial drug (Code: CHEBI:36047) antiparasitic agent (Code: CHEBI:35442) radiosensitizing agent (Code: CHEBI:132992) Nitroimidazole Antimicrobial (Code: N0000175435) Nitroimidazoles (Code: N0000007663) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Radiation-Sensitizing Agents (Code: D011838) 1963-07-18 FDA 2MN
Click to view gabapentin Voltage-dependent calcium channel subunit alpha-2/delta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P54289, gene: CACNA2D1, swissprot: CA2D1_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020235s064_020882s047_021129s046lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020235s064_020882s047_021129s046lbl.pdf) Potassium voltage-gated channel subfamily KQT member 3 (Organism: Homo sapiens, class: Ion channel, accessions: O43525, gene: KCNQ3, swissprot: KCNQ3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/30021858) Potassium voltage-gated channel subfamily KQT member 5 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NR82, gene: KCNQ5, swissprot: KCNQ5_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/30021858) Branched-chain-amino-acid aminotransferase, cytosolic (Organism: Homo sapiens, class: Enzyme, accessions: P54687, gene: BCAT1, swissprot: BCAT1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16141215) L-type amino acid transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q01650, gene: SLC7A5, swissprot: LAT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23567998) Gabapentin is gamma-amino-2-cyclohexyl-butyric acid. Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid), but it does not modify GABAA or GABAB radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. The mechanism of action by which gabapentin exerts its analgesic action is unknown but in animal models of analgesia, gabapentin prevents allodynia and hyperalgesia. The relevance of these models to human pain is not known. Gabapentin is indicated for the management of postherpetic neuralgia and for adjunctive therapy in the treatment of partial onset seizures, with/without secondary generalization. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Analgesics (Code: D000700) Anti-Anxiety Agents (Code: D014151) Anti-Dyskinesia Agents (Code: D018726) Anticonvulsants (Code: D000927) Antimanic Agents (Code: D018692) Antiparkinson Agents (Code: D000978) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) Tranquilizing Agents (Code: D014149) 1993-12-30 FDA GBN
Click to view rasagiline Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021641s020lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021641s020lbl.pdf) Apoptosis regulator Bcl-2 (Organism: Homo sapiens, class: Cytosolic other, accessions: P10415, gene: BCL2, swissprot: BCL2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12057839) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15027867) Rasagiline is an inhibitor of monamine oxidase used as adjunctive therapy in combination with levodopa and carbidopa in the management of Parkinson’s disease. neuroprotective agent (Code: CHEBI:63726) Monoamine Oxidase Inhibitor (Code: N0000175744) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Neuroprotective Agents (Code: D018696) Protective Agents (Code: D020011) 2005-02-21 EMA RAU
Click to view iproheptine Iproheptine is a vasoconstrictor, antihistamine, and nasal decongestant.
Click to view menadione M-phase inducer phosphatase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P30307, gene: CDC25C, swissprot: MPIP3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15501045) M-phase inducer phosphatase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P30305, gene: CDC25B, swissprot: MPIP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19028102) NAD(P)H dehydrogenase [quinone] 1 (Organism: Homo sapiens, class: Enzyme, accessions: P15559, gene: NQO1, swissprot: NQO1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17850125) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22996261) Trypanothione reductase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P28593, gene: TPR, swissprot: TYTR_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11170645) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22071524) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22071524) Menadione is a synthetic form of vitamin K. Menadione is prescribed for the treatment of hemorrhage, vitamin K deficiency, moderate to severe forms of hypoprothrombinaemia in adults and children. Large doses of menadione have been reported to cause adverse outcomes including hemolytic anemia due to glucose-6-phosphate dehydrogenase deficiency, neonatal brain or liver damage, or neonatal death in some rare cases. nutraceutical (Code: CHEBI:50733) 1940 FDA VK3
Click to view sulfanilamide Dihydropteroate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AC13, gene: folP, swissprot: DHPS_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9127492) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15149691) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14971907) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14971907) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14971907) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686895) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686895) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Enzyme, accessions: P40881, gene: None, swissprot: CAH_METTE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15546717) Carbonic anhydrase (Organism: Helicobacter pylori (strain ATCC 700392 / 26695), class: Enzyme, accessions: O24855, gene: cynT, swissprot: CYNT_HELPY) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16459077) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source:https://www.ncbi.nlm.nih.gov/pubmed/19338333) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Delta carbonic anhydrase (Organism: Thalassiosira weissflogii, class: Unclassified, accessions: Q5U9J1, gene: ca1, swissprot: Q5U9J1_THAWE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24314394) Sulfanilamide is an organic sulfur compound structurally similar to p-aminobenzoic acid (PABA) with antibacterial property. Sulfanilamide competes with PABA for the bacterial enzyme dihydropteroate synthase, thereby preventing the incorporation of PABA into dihydrofolic acid, the immediate precursor of folic acid. This leads to an inhibition of bacterial folic acid synthesis and de novo synthesis of purines and pyrimidines, ultimately resulting in cell growth arrest and cell death. Sulfanilamide is used for the treatment of vulvovaginitis caused by Candida albicans. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1965-06-05 FDA SAN
Click to view sodium hexacyclonate used in treatment of hyperlipoproteinemia
Click to view terpin Terpin is derived from oil of turpentine, oregano, thyme and eucalyptus. It was banned by FDA in the 1990s due to lack of proof of efficacy but is a medicine available in a number of countries worldwide commonly used in combination with codein. Terpin is an expectorant which used to loosen mucus in patients presenting with acute or chronic bronchitis, and related conditions. Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) 2004-06-01 Ministry of Health of the Russian Federation
Click to view loprodiol Loprodiol (2,2-bis(chloromethyl)-1,3-propanediol) was used as a sedative agent.
Click to view oxaceprol Oxaceprol is a structural analog of hydroxyproline. It was shown that oxaceprol does not inhibit the synthesis of prostaglandins in vitro, but acts predominantly by inhibiting leukocyte adhesion and migration, thus inhibiting inflammation at an early stage and helps in pain relief. Oxaceprol is used for the treatment of osteoarthritis and rheumatoid arthritis. Antirheumatic Agents (Code: D018501) Dermatologic Agents (Code: D003879) 2011-03-15 CDSCO (INDIA)
Click to view acexamic acid Acexamic acid is a wound-healing agent component of plasmutan.
Click to view acetylleucine Acetylleucine is a modified amino acid used for treating vestibular-related imbalance and vertigo. L-Acetylleucine is enantiomer of acetylleucine and the active part of the racemate component since it induces a significant acceleration of the vestibular compensation process similar and even better than that observed under treatment with the racemate component only. Acetylleucine may act as a precursor of a peptidic neuromediator responsible for activation of vestibular afferents. 1992-09-30 ANSM (French National Agency for Medicines and Health Products Safety) LAY
Click to view menadiol sodium sulfate Menadiol sodium sulfate (Menadiol disulfate, Vitamin k4 sodium sulfate) is a synthetic vitamin K analogue and a prothrombogenic agent.
Click to view ascorbic acid Solute carrier family 23 member 1 (Organism: Homo sapiens, class: Unclassified, accessions: Q9UHI7, gene: SLC23A1, swissprot: S23A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18094143) Solute carrier family 23 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UGH3, gene: SLC23A2, swissprot: S23A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19216494) Ascorbic acid is a six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C or L-ascorbic acid, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant. Ascorbic acid is used to treat vitamin C deficiency, scurvy, delayed wound and bone healing, urine acidification, and in general as an antioxidant. It has also been suggested to be an effective antiviral agent. vitamin C (Code: CHEBI:21241) flour treatment agent (Code: CHEBI:64577) food antioxidant (Code: CHEBI:77962) Ascorbic Acid (Code: N0000006439) Antioxidants (Code: D000975) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Protective Agents (Code: D020011) Vitamins (Code: D014815) 1947-07-28 FDA ASC
ISD
Click to view arginine Nitric oxide synthase, inducible (Organism: Homo sapiens, class: Enzyme, accessions: P35228, gene: NOS2, swissprot: NOS2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11527735) Glycine amidinotransferase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P50440, gene: GATM, swissprot: GATM_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/27233232) Arginase-2 (Organism: Homo sapiens, class: Enzyme, accessions: P78540, gene: ARG2, swissprot: ARGI2_HUMAN) substrate (Source: https://www.uniprot.org/uniprot/P78540) Arginine is an essential amino acid that is physiologically active in the L-form. In mammals, arginine is formally classified as a semi-essential or conditionally essential amino acid, depending on the developmental stage and health status of the individual. Arginine helps dispose of ammonia, is used to make compounds such as nitric oxide, creatine, L-glutamate, and L-proline, and it can be converted into glucose and glycogen if needed. In large doses, L-arginine also stimulates the release of the hormones growth hormone and prolactin. Catabolic disease states such as sepsis, injury, and cancer cause an increase in arginine utilization, which can exceed normal body production, leading to arginine depletion. Arginine is found in plant and animal proteins, such as dairy products, meat, poultry, fish, and nuts. 1973-02-28 FDA ARG
DAR
Click to view carfimate Carfimate (?-Ethynylbenzenemethanol carbamate) is a carboxylic ester. It derives from a benzyl alcohol. Carfimate has sedative and hypnotic activities.
Click to view citrulline Argininosuccinate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P00966, gene: ASS1, swissprot: ASSY_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/27287393) Citrulline is an amino acid. It is made from ornithine and carbamoyl phosphate in one of the central reactions in the urea cycle. It is a non-essential amino acid and a precursor of arginine. L-citrulline is converted into L-arginine by the enzymes argininosuccinate synthetase and argininosuccinate lyase in the presence of L-aspartate and ATP. Subsequently, L-arginine is converted to nitric oxide by nitric oxide synthase and L-citrulline is regenerated as a by-product. Citrulline supplements have been claimed to promote energy levels, stimulate the immune system and help detoxify ammonia (a cell toxin). 2000-03-15 Spanish Agency of Medicines and Medical Products (AEMPS) CIR
Click to view benzalamide Benzalamide is a hypocholesterolemic and hypolipemic agent reducing the biosynthesis of cholesterol and fatty acids.
Click to view tidiacic Tidiacic is a hepatoprotective drug that acts as an antioxidant and a sulfur donor. Tidiacic is a component of tidiacic arginine that used for the treatment of toxic liver damage. 1988-02-22 ANSM (French National Agency for Medicines and Health Products Safety) 5XB
Click to view glucurolactone Glucurolactone (Glucuronolactone) is a naturally occurring metabolite of glucose. It is used as an additive in energy drinks, because it increases alertness and decreases sleepiness. Glucurolactone is also used as a conventional hepatoprotective drug that is used in epidemical hepatitis, cirrhosis of the liver and poisoning due to food and drugs. It acts as a hepatic antidote and immune regulator. 2014 China Food and Drug Administration (CFDA)
Click to view hymecromone Testosterone 17-beta-dehydrogenase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P37058, gene: HSD17B3, swissprot: DHB3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19954971) Aldose reductase (Organism: Homo sapiens, class: Enzyme, accessions: P15121, gene: AKR1B1, swissprot: ALDR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20805028) Hymecromone is a choleretic with spasmolytic activity on the gallbladder (sphincter of Oddi) and without spasmolytic effect on other organs. It is used as choleretic and antispasmodic drug. antineoplastic agent (Code: CHEBI:35610) Indicators and Reagents (Code: D007202) 1970-06-30 Italian Medicines Agency (AIFA) 4MU
Click to view pemoline Pemoline is an oxazolidine compound with central nervous system (CNS) stimulant property. Although pemoline has pharmacological activity similar to other CNS stimulants, the exact mechanism and site of action are unknown. This agent has minimal sympathomimetic properties, but animal studies indicate it may work through dopaminergic mechanisms. Pemoline has been withdrawn from the market because of the agent's association with life threatening hepatic failure. Pemoline was used for the treatment of Attention Deficit Hyperactivity Disorder (ADHD). central nervous system stimulant (Code: CHEBI:35337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) 1975-01-27 FDA
Click to view cotinine Cotinine is the major metabolite of nicotine. Cotinine has antipsychotic, anxiolytic, and antidepressant properties and modulates the serotonergic, cholinergic and dopaminergic systems. Cotinine behaves as a positive allosteric modulator of the nicotinic acetylcholine receptors and has anti-inflammatory effects. Measuring cotinine in people’s blood is the most reliable way to determine exposure to nicotine for both smokers and nonsmokers exposed to environmental tobacco smoke. biomarker (Code: CHEBI:59163) antidepressant (Code: CHEBI:35469) Indicators and Reagents (Code: D007202)
Click to view meptazinol Acetylcholinesterase (Organism: Mus musculus, class: Enzyme, accessions: P21836, gene: Ache, swissprot: ACES_MOUSE) Cholinesterase (Organism: Mus musculus, class: Enzyme, accessions: Q03311, gene: Bche, swissprot: CHLE_MOUSE) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) partial agonist (Source: ) A narcotic antagonist with analgesic properties. It is used for the control of moderate to severe pain. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotic Antagonists (Code: D009292) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1983-01-01 YEAR INTRODUCED
Click to view metamfepramone Metamfepramone (dimethylcathinone, dimethylpropion, and dimepropion) is a sympathomimetic agent that was used for the treatment of the common cold and hyptonic conditions. Metamfepramone is considered to be an analogue of dimethylamphetamine and is a controlled substance.
Click to view phenmetrazine Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12106802) Phenmetrazine is an anti-obesity drug. It is suggested that the drug exerts its effect by inhibiting the monoamine transport. Later on the drug was withdrawn from the market due to the reported cases of abuse. Anti-Obesity Agents (Code: D019440) Appetite Depressants (Code: D001067) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1982-01-01 FDA
Click to view betanidine Betanidine is a guanidinium antihypertensive agent that acts by blocking adrenergic transmission. Betanidine is a peripherally acting antiadrenergic agent which primarily acts as an alpha2a adrenergic agonist. Betanidine effectively decreases blood pressure by suppressing renin secretion or interfering with function of the sympathetic nervous system. antihypertensive agent (Code: CHEBI:35674) adrenergic antagonist (Code: CHEBI:37887) Adrenergic Agents (Code: D018663) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1981-05-29 FDA
Click to view rimantadine Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Rimantadine is a cyclic amine and alpha-methyl derivative of amantadine with antiviral activity. Rimantadine appears to exert its inhibitory effect early in the viral replicative cycle, possibly inhibiting the uncoating of the virus. Genetic studies suggest that a virus protein specified by the virion M2 gene plays an important role in the susceptibility of influenza A virus to inhibition by rimantadine. Rimantadine inhibits the replication in cell culture of influenza A virus isolates from each of the three antigenic subtypes, i.e., H1N1, H2N2 and H3N2, that have been isolated from man. Rimantadine has little or no activity against influenza B virus. Influenza A M2 Protein Inhibitor (Code: N0000175543) M2 Protein Inhibitors (Code: N0000175542) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) 1993-09-17 FDA RIM
EU7
Click to view lidocaine Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/8786356) Sodium channel protein type 2 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q99250, gene: SCN2A, swissprot: SCN2A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/8799190) Sodium channel protein type 5 subunit alpha (Organism: Rattus norvegicus, class: Unclassified, accessions: P15389, gene: Scn5a, swissprot: SCN5A_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/2546048) Sodium channel protein type 9 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q15858, gene: SCN9A, swissprot: SCN9A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/17430993) Sodium channel protein type 4 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35499, gene: SCN4A, swissprot: SCN4A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/24440379) Sodium channel protein type 3 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9NY46, gene: SCN3A, swissprot: SCN3A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/24440379) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16551906) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215663) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27906699) A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Lidocaine stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting the ionic fluxes required for the initiation and conduction of impulses and effecting local anesthesia. Amide Local Anesthetic (Code: N0000175682) Amides (Code: N0000007681) Antiarrhythmic (Code: N0000175426) Local Anesthesia (Code: N0000175976) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Anti-Arrhythmia Agents (Code: D000889) drug allergen (Code: CHEBI:88188) local anaesthetic (Code: CHEBI:36333) anti-arrhythmia drug (Code: CHEBI:38070) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Membrane Transport Modulators (Code: D049990) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1948-11-19 FDA LQZ
Click to view chlorobutanol Chlorobutanol, or chlorbutol, is an alcohol-based preservative with no surfactant activity. Similar in nature to chloral hydrate, it is formed by the simple nucleophilic addition of chloroform and acetone. It also elicits sedative-hypnotic and weak local anesthetic actions in addition to antibacterial and antifungal properties. Due to the long terminal half-life of 37 days, the use of chlorobutanol as a sedative is limited because of the considerable accumulation which will occur following multiple dosing. Chlorobutanol is a common detergent preservative in eye drops and other ophthalmic therapeutic formulations. Chlorobutanol is used as a local anesthetic in combination with hexetidine, chlorhexidine or levomenthol for the treatment of bacterial infections. Pharmaceutic Aids (Code: D010592) Preservatives, Pharmaceutical (Code: D011310) 1971-12-31 Health Canada
Click to view phenacemide Sodium channel protein type 1 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35498, gene: SCN1A, swissprot: SCN1A_HUMAN) blocker anti-epileptic drug; structure 1951-06-28 FDA
Click to view nikethamide Nikethamide is a central nervous system stimulant. It was used as a medical countermeasure against tranquilizer overdoses, before the advent of endotracheal intubation and positive-pressure lung expansion. In some sports, nikethamide is listed by the World Anti-Doping Agency as a banned substance. Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Convulsants (Code: D003292) 1967-07-11 Ministry of Health of the Russian Federation
Click to view propofol GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47869|P34903|P48169|P31644|Q16445|P18505|P47870|P28472|O14764|P78334|Q8N1C3|P18507|Q99928|O00591|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) positive allosteric modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019627s066lbl.pdf) Fatty-acid amide hydrolase 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P97612, gene: Faah, swissprot: FAAH1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18983142) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231207) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231207) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9764927) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9764927) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9764927) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9764927) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7772432) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7772432) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7772432) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17697043) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17697043) Propofol is an intravenous general anesthetic and sedation drug for use in the induction and maintenance of anesthesia or sedation. The mechanism of action is poorly understood. However, propofol is thought to produce its sedative/anesthetic effects by the positive modulation of the inhibitory function of the neurotransmitter GABA through the ligand-gated GABAA receptors. Propofol is used for induction and maintenance of anaesthesia and for management of refractory status epilepticus. intravenous anaesthetic (Code: CHEBI:38877) sedative (Code: CHEBI:35717) antiemetic (Code: CHEBI:50919) anticonvulsant (Code: CHEBI:35623) General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1989-10-02 FDA PFL
Click to view fluostigmine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20189400) Fluostigmine (isoflurophate) is a long acting cholinesterase inhibitor and potent miotic. It works as an indirect acting parasympathomimetic agent to reduce intraocular pressure. Isoflurophate has been replaced by the more stable anticholinesterase agents. Now fluostigmine is used as a research tool in neuroscience for its ability to inhibit cholinesterase (by phosphorylation) on an acute/sub-acute basis and to produce a delayed neuropathy. Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Protease Inhibitors (Code: D011480) 1957-04-02 FDA
Click to view glucosamine Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Glucosamine is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. Glucosamine is one of the most abundant monosaccharides. Oral glucosamine is a dietary supplement. D-Glucosamine is made naturally in the form of glucosamine-6-phosphate, and is the biochemical precursor of all nitrogen-containing sugars. Glucosamine is commonly used as a treatment for osteoarthritis, although its acceptance as a medical therapy varies. 1989-11-02 Italian Medicines Agency (AIFA) GCS
Click to view salacetamide Salacetamide is a derivative of salicylic acid. It is analgesic, anti-inflammatory and antipyretic agent.
Click to view phenprobamate Muscle relaxant & tranquiliser 1964 CDSCO (INDIA)
Click to view phenacetin Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14592552) Arylacetamide deacetylase (Organism: Homo sapiens, class: Enzyme accessions: P22760, gene: AADAC, swissprot: AAAD_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22207054) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22331994) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8474022) Cytochrome P450 2A13 (Organism: Homo sapiens, class: Enzyme, accessions: Q16696, gene: CYP1A13, swissprot: CP2AD_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17178771) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10421611) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10548449) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991954) Phenacetin was the first NSAID and fever reducer to go on the market. It acts as an analgesic at the spinal cord as well as a negative inotrope at the heart. Human ingestion of phenacetin can result in a bluish discoloration of the skin due to a lack of oxygen in the blood (cyanosis), dizziness and respiratory depression. It is reasonably anticipated to be a human carcinogen. It is used in research as the preferred marker for detecting CYP1A2-based inhibition potential in vitro. In medicine phenacetin is used for the relief of mild to moderate pain, fever. non-narcotic analgesic (Code: CHEBI:35481) peripheral nervous system drug (Code: CHEBI:49110) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1951-05-15 Hungary National Institute of Pharmacy and Nutrition N4E
Click to view homarylamine Homarylamine is a sympathomimetic agent proposed as an antitussive.
Click to view glucose Hexokinase HKDC1 (Organism: Homo sapiens, class: Enzyme, accessions: Q2TB90, gene: HKDC1, swissprot: HKDC1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/30517626) Solute carrier family 2, facilitated glucose transporter member 2 (Organism: Homo sapiens, class: Transporter, accessions: P11168, gene: SLC2A2, swissprot: GTR2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 3 (Organism: Homo sapiens, class: Transporter, accessions: P11169, gene: SLC2A3, swissprot: GTR3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 4 (Organism: Homo sapiens, class: Transporter, accessions: P14672, gene: SLC2A4, swissprot: GTR4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 5 (Organism: Homo sapiens, class: Transporter, accessions: P22732, gene: SLC2A5, swissprot: GTR5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q9UGQ3, gene: SLC2A6, swissprot: GTR6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q6PXP3, gene: SLC2A7, swissprot: GTR7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q9NY64, gene: SLC2A8, swissprot: GTR8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 9 (Organism: Homo sapiens, class: Transporter, accessions: Q9NRM0, gene: SLC2A9, swissprot: GTR9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 10 (Organism: Homo sapiens, class: Transporter, accessions: O95528, gene: SLC2A10, swissprot: GTR10_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9BYW1, gene: SLC2A11, swissprot: GTR11_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 12 (Organism: Homo sapiens, class: Transporter, accessions: Q8TD20, gene: SLC2A12, swissprot: GTR12_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23506862) Solute carrier family 2, facilitated glucose transporter member 1 (Organism: Homo sapiens, class: Transporter, accessions: P11166, gene: SLC2A1, swissprot: GTR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/27078104) Glucose is a sugar. The D-isomer (D-glucose), also known as dextrose, occurs widely in nature. Glucose is the human body's key source of energy, through aerobic respiration, providing about 3.75 kilocalories (16 kilojoules) of food energy per gram. Use of glucose as an energy source in cells is by either aerobic respiration, anaerobic respiration, or fermentation. All of these processes follow from an earlier metabolic pathway known as glycolysis. Glucose is synthesized in the liver and kidneys from non-carbohydrate intermediates, such as pyruvate and glycerol, by a process known as gluconeogenesis. D-Glucose is found to be associated with 3-methyl-crotonyl-glycinuria, growth hormone deficiency, and primary hypomagnesemia, which are inborn errors of metabolism. Glucose is used to manage hypoglycemia and for intravenous feeding. Nausea may occur after ingesting glucose, but this also may be an effect of the hypoglycemia which is present just prior to ingestion. Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Sweetening Agents (Code: D013549) 1946-01-17 FDA BGC
GLC
GLO
Click to view iproniazid Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19267475) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24793878) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16669850) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16669850) Iproniazid is an irreversible inhibitor of monoamine oxidase types A and B that is used as an antidepressive agent. It has also been used as an antitubercular agent, but its use is limited by its toxicity. Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) 1991-12-02 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view fudosteine Mucin-5AC (Organism: Homo sapiens, class: Unclassified protein, accessions: P98088, gene: MUC5AC, swissprot: MUC5A_HUMAN) gene expression inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18579549) Fudosteine is a derivative of cysteine. Fudosteine acts as a mucoactive agent, enabling mucin secretion. Fudosteine is a MUC5AC mucin hypersecretion inhibitor. It is indicated for use in patients with chronic respiratory diseases (bronchial asthma, chronic bronchitis, bronchiectasis). 2001-10-01 PMDA
Click to view methylephedrine Methylephedrine is a member of amphetamines. Methylephedrine is one of the ephedra alkaloids that is found in varying amounts in different species of the plant genus Ephedra. Methylephedrine is a sympathomimetic amine that appears in various over-the-counter cough and cold medications throughout the world. 2013 China Food and Drug Administration (CFDA)
Click to view protionamide Polyphenol oxidase 2 (Organism: Agaricus bisporus, class: Enzyme, accessions: O42713, gene: PPO2, swissprot: PPO2_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26544630) Protionamide is a thioamide derivative with antitubercular activity. Protionamide forms a covalent adduct with bacterial nicotinamide adenine dinucleotide (NAD), PTH-NAD, which competitively inhibits 2-trans-enoyl-ACP reductase (inhA), an enzyme essential for mycolic acid synthesis. This results in increased cell wall permeability and decreased resistance against cell injury eventually leading to cell lysis. Protionamide is used for the treatment multidrug resistance tuberculosis and leprosy. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antitubercular Agents (Code: D000995) 2005-07-09 Ministry of Health of the Russian Federation
Click to view mexiletine Sodium channel protein type 4 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35499, gene: SCN4A, swissprot: SCN4A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/14608007) Sodium channel protein type 9 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q15858, gene: SCN9A, swissprot: SCN9A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/26068619) Sodium channel protein type 10 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y5Y9, gene: SCN10A, swissprot: SCNAA_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501613) Sodium channel protein type 2 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q99250, gene: SCN2A, swissprot: SCN2A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501613) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501613) Sodium channel protein type 11 subunit alpha (Organism: Rattus norvegicus, class: Ion channel, accessions: O88457, gene: Scn11a, swissprot: SCNBA_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501613) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Aryl hydrocarbon receptor (Organism: Homo sapiens, class: Transcription factor, accessions: P35869, gene: AHR, swissprot: AHR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17327465) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9690950) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9690950) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12519691) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12519691) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215663) Mexiletine is a local anesthetic, antiarrhythmic agent (Class Ib), structurally similar to lidocaine, but orally active. Mexiletine, like lidocaine, inhibits the inward sodium current required for the initiation and conduction of impulses, thus reducing the rate of rise of the action potential, Phase 0. Mexiletine is used for the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation. anti-arrhythmia drug (Code: CHEBI:38070) Antiarrhythmic (Code: N0000175426) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1985-12-30 FDA 505
Click to view methoxyphenamine Methoxyphenamine (2-methoxy-N-methylamphetamine) is an amphetamine methylated on nitrogen and with the phenyl ring methoxylated at C-2. Methoxyphenamine is a beta adrenergic receptor agonist. Methoxyphenamine is used as a bronchodilator to treat asthma, chronic bronchitis, respiratory tract infections with cough and. In addition, methoxyphenamine using is prohibited in sports according to the regulations of the World Anti-Doping Agency (WADA). Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Neurotransmitter Agents (Code: D018377) 1969-12-31 New Zealand Medicines and Medical Devices Safety Authority
Click to view memantine Glutamate receptor ionotropic, NMDA 3A (Organism: Homo sapiens, class: Ion channel, accessions: Q8TCU5, gene: GRIN3A, swissprot: NMD3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q05586, gene: GRIN1, swissprot: NMDZ1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 2A (Organism: Homo sapiens, class: Ion channel, accessions: Q12879, gene: GRIN2A, swissprot: NMDE1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 2B (Organism: Homo sapiens, class: Ion channel, accessions: Q13224, gene: GRIN2B, swissprot: NMDE2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 2C (Organism: Homo sapiens, class: Ion channel, accessions: Q14957, gene: GRIN2C, swissprot: NMDE3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 2D (Organism: Homo sapiens, class: Ion channel, accessions: O15399, gene: GRIN2D, swissprot: NMDE4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Glutamate receptor ionotropic, NMDA 3B (Organism: Homo sapiens, class: Ion channel, accessions: O60391, gene: GRIN3B, swissprot: NMD3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021487s025lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15378224) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15378224) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Memantine is an oral N-methyl-D-aspartate glutamate receptor antagonist used in the therapy of Alzheimer disease and dementia. dopaminergic agent (Code: CHEBI:48560) antiparkinson drug (Code: CHEBI:48407) neuroprotective agent (Code: CHEBI:63726) antidepressant (Code: CHEBI:35469) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Neurotransmitter Agents (Code: D018377) NMDA Receptor Antagonists (Code: N0000020015) N-methyl-D-aspartate Receptor Antagonist (Code: N0000175745) 2003-10-16 FDA 377
Click to view cloxiquine Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Methionine aminopeptidase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P50579, gene: METAP2, swissprot: MAP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22391578) Methionine aminopeptidase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P53582, gene: METAP1, swissprot: MAP11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22391578) Potassium channel subfamily K member 18 (Organism: Homo sapiens, class: Ion channel, accessions: Q7Z418, gene: KCNK18, swissprot: KCNKI_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/24383077) Cloxyquin is a monohalogenated 8-hydroxyquinoline with activity against bacteria, fungi, and protozoa. Cloxyquin is reported to have activity against Mycobacterium tuberculosis, including strains that show resistance to common first-line antibacterial agents.
Click to view flurotyl Flurothyl is a volatile convulsant acting as a GABAA antagonist that was extensively used historically to induce seizures in severely depressed patients as an alternative to electroconvulsive shock therapy. The main current use of flurothyl is in scientific research for inducing seizures in laboratory animals. Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Convulsants (Code: D003292) 1964 FDA
Click to view inositol Sodium/myo-inositol cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q8WWX8, gene: SLC5A11, swissprot: SC5AB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12133831) Inositol is a collection of nine different stereoisomers but the name is usually used to describe only the most common type of inositol, myo-inositol. Myo-inositol is the cis-1,2,3,5-trans-4,6-cyclohexanehexol and it is prepared from an aqueous extract of corn kernels by precipitation and hydrolysis of crude phytate. These molecules have structural similarities to glucose and are involved in cellular signaling. It is considered a pseudovitamin as it is a molecule that does not qualify to be an essential vitamin because even though its presence is vital in the body, a deficiency in this molecule does not translate into disease conditions. Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) Vitamin B Complex (Code: D014803) 1949 FDA INS
Click to view galactose An aldohexose that occurs naturally in the D-form in lactose, cerebrosides, gangliosides, and mucoproteins. Deficiency of galactosyl-1-phosphate uridyltransferase (GALACTOSE-1-PHOSPHATE URIDYL-TRANSFERASE DEFICIENCY DISEASE) causes an error in galactose metabolism called GALACTOSEMIA, resulting in elevations of galactose in the blood.
Click to view fructose Solute carrier family 2, facilitated glucose transporter member 2 (Organism: Homo sapiens, class: Transporter, accessions: P11168, gene: SLC2A2, swissprot: GTR2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23396969) Solute carrier family 2, facilitated glucose transporter member 8 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9JJZ1, gene: Slc2a8, swissprot: GTR8_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23396969) Ketohexokinase (Organism: Homo sapiens, class: Enzyme, accessions: P50053, gene: KHK, swissprot: KHK_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12941785) Sorbitol dehydrogenase (Organism: Homo sapiens, class: Enzyme, accessions: Q00796, gene: SORD, swissprot: DHSO_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12962626) Hexokinase-4 (Organism: Homo sapiens, class: Enzyme, accessions: P35557, gene: GCK, swissprot: HXK4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7742312) Fructose is a monosaccharide in sweet fruits and honey that is soluble in water, alcohol, or ether. Fructose is one of the three dietary monosaccharides, along with glucose and galactose, that are absorbed directly into the bloodstream. It is used as a preservative and an intravenous infusion in parenteral feeding. Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Sweetening Agents (Code: D013549) 1953 FDA Z9N
FRU
Click to view acetylsalicylic acid Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/200671s000lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17480099) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10220563) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/24107783) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24692216) Endothelin-1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25101, gene: EDNRA, swissprot: EDNRA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10727528) Acid-sensing ion channel 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UHC3, gene: ASIC3, swissprot: ASIC3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11588175) Acetylsalicylic acid (also known as aspirin) is a prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Acetylsalicylic acid is indicated for the relief of pain, fever and inflammation of a variety of conditions such as influenza, common cold, low back and neck pain, dysmenorrhea, headache, toothache, sprains and strains, fractures, myositis, neuralgia, synovitis, arthritis, bursitis, burns, injuries, following surgical and dental procedures. Acetylsalicylic acid also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. plant activator (Code: CHEBI:73182) drug allergen (Code: CHEBI:88188) platelet aggregation inhibitor (Code: CHEBI:50427) antipyretic (Code: CHEBI:35493) prostaglandin antagonist (Code: CHEBI:49023) anticoagulant (Code: CHEBI:50249) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Decreased Prostaglandin Production (Code: N0000008836) Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Decreased Platelet Aggregation (Code: N0000008832) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antipyretics (Code: D058633) Antirheumatic Agents (Code: D018501) Cardiovascular Agents (Code: D002317) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Fibrin Modulating Agents (Code: D050299) Fibrinolytic Agents (Code: D005343) Hematologic Agents (Code: D006401) Peripheral Nervous System Agents (Code: D018373) Platelet Aggregation Inhibitors (Code: D010975) Sensory System Agents (Code: D018689) 1898-01-01 YEAR INTRODUCED AIN
Click to view clorindione Arachidonate 5-lipoxygenase (Organism: Rattus norvegicus, class: Enzyme, accessions: P12527, gene: Alox5, swissprot: LOX5_RAT) inhibitor (Source: https://www.sciencedirect.com/science/article/pii/S0960894X0080236X) Clorindione is a vitamin K antagonists, and is a derivative of phenindione. It has been demonstrated as effective in reducing prothrombin levels in humans. Clorindione is used as a long-acting anticoagulant.
Click to view theophylline cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12421478) cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Organism: Homo sapiens, class: Enzyme, accessions: Q14432, gene: PDE3A, swissprot: PDE3A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12887610) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12070353) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12070353) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12070353) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019211s042lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019211s042lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019211s042lbl.pdf) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7619675) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15708966) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15708966) Adenosine receptor A2b (Organism: Homo sapiens, class: GPCR, accessions: P29275, gene: ADORA2B, swissprot: AA2BR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12014951) Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6279840) Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6279840) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Organism: Homo sapiens, class: Kinase, accessions: O00329, gene: PIK3CD, swissprot: PK3CD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12145276) Theophylline is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Physiologically, this agent relaxes bronchial smooth muscle, produces vasodilation (except in cerebral vessels), stimulates the CNS, stimulates cardiac muscle, induces diuresis, and increases gastric acid secretion; it may also suppress inflammation and improve contractility of the diaphragm. muscle relaxant (Code: CHEBI:51371) bronchodilator agent (Code: CHEBI:35523) vasodilator agent (Code: CHEBI:35620) immunomodulator (Code: CHEBI:50846) anti-inflammatory agent (Code: CHEBI:67079) anti-asthmatic drug (Code: CHEBI:49167) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Phosphodiesterase Inhibitors (Code: D010726) Protective Agents (Code: D020011) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P1 Receptor Antagonists (Code: D058915) Respiratory System Agents (Code: D019141) Vasodilator Agents (Code: D014665) Methylxanthine (Code: N0000175790) Xanthines (Code: N0000008118) 1947-10-17 FDA TEP
Click to view theobromine 3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9) vasodilator agent (Code: CHEBI:35620) bronchodilator agent (Code: CHEBI:35523) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiovascular Agents (Code: D002317) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Vasodilator Agents (Code: D014665) 37T
Click to view propylparaben Propylparaben is an ester of p-hydroxybenzoic acid. Propylparaben is a chemical allergen capable of producing immunologically mediated hypersensitivity reactions. It is used as a bacteriostatic, fungistatic agent and preservative in cosmetic products, food and drugs. It has the number E216 as a food additive. Also propylparaben is used in allergenic testing. Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) Pharmaceutic Aids (Code: D010592) Preservatives, Pharmaceutical (Code: D011310) 36M
Click to view mephenesin Mephenesin is a centrally acting muscle relaxant with a short duration of action. The exact mechanism of action of mephenesin is not known. It has been observed to block both inward sodium and inward calcium currents in neurons. It is used as an adjunctive treatment of muscle pain. Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 1996-06-24 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view rilmenidine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27265687) Nischarin (Organism: Homo sapiens, class: Cytosolic other, accessions: Q9Y2I1, gene: NISCH, swissprot: NISCH_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12065769) Rilmenidine is a centrally-acting antihypertensive. It acts through stimulation of central imidazoline receptors and has alpha2-adrenoceptor agonist activity. Rilmenidine is used for the treatment of hypertension. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 1995-02-21 CDSCO (INDIA)
Click to view tyrosine A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin. 1975 FDA DTY
TYR
Click to view styramate Styramate is a centrally acting skeletal muscle relaxant that was used in the symptomatic treatment of painful muscle spasm associated with musculoskeletal conditions.
Click to view adrenalone Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21885739) Adrenalone is a keton form of the natural epinephrine. It is an adrenergic receptor agonist. Adrenalone inhibits the norepinephrine synthesis and dopamine beta oxidase. Adrenalone has the high radioprotective effect. Adrenalone has hemostatic, sympathomimetic and vasoconstrictor properties. It was used as a topical nasal decongestant. Cardiovascular Agents (Code: D002317) Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) Vasoconstrictor Agents (Code: D014662)
Click to view acamprosate Glutamate NMDA receptor; GRIN1/GRIN2A (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q12879, gene: GRIN1|GRIN2A, swissprot: NMDE1_HUMAN|NMDZ1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11369029) Glutamate NMDA receptor; GRIN1/GRIN2B (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q13224, gene: GRIN1|GRIN2B, swissprot: NMDE2_HUMAN|NMDZ1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11369029) Acamprosate is a synthetic compound with a chemical structure similar to that of the endogenous amino acid homotaurine, which is a structural analogue of the amino acid neurotransmitter gamma-aminobutyric acid and the amino acid neuromodulator taurine. The mechanism of action of acamprosate in maintenance of alcohol abstinence is not completely understood. In vitro and in vivo studies in animals have provided evidence to suggest acamprosate may interact with glutamate and GABA neurotransmitter systems centrally, and has led to the hypothesis that acamprosate restores balance between neuronal excitation and inhibition. Acamprosate is indicated for the maintenance of abstinence from alcohol in patients with alcohol dependence who are abstinent at treatment initiation. neurotransmitter agent (Code: CHEBI:35942) Alcohol Deterrents (Code: D000427) Central Nervous System Agents (Code: D002491) 2004-07-29 FDA
Click to view pyridostigmine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/17398s015lbl.pdf) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2738887) Pyridostigmine is a cholinesterase inhibitor with a slightly longer duration of action than neostigmine. It is used in the treatment of myasthenia gravis and to reverse the actions of muscle relaxants. Cholinesterase Inhibitor (Code: N0000175723) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) 1955-04-06 FDA
Click to view oxilofrine Oxilofrine is a metabolite of p-methoxymethamphetamine. Oxilofrine is a stimulant and a sympathomimetic. It was used to treat hypotensive states, with actions similar to those of ephedrine.
Click to view hexapropymate Hexapropymate is a carbamate hypnotic substance with properties similar to those of the barbiturates. Hexapropymate produces CNS depressant effects through an unknown mechanism. Hexapropymate was used as a hypnotic and sedative drug.
Click to view etilefrine Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/4396765) A phenylephrine-related beta-1 adrenergic and alpha adrenergic agonist used as a cardiotonic and antihypotensive agent. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Adrenergic beta-1 Receptor Agonists (Code: D058665) Adrenergic beta-Agonists (Code: D000318) Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1929-01-01 YEAR INTRODUCED
Click to view eflornithine Ornithine decarboxylase (Organism: Homo sapiens, class: Enzyme, accessions: P11926, gene: ODC1, swissprot: DCOR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/21145lbl.pdf) Eflornithine is a difluoromethylated ornithine compound with antineoplastic activity. Eflornithine irreversibly inhibits skin ODC activity. This enzyme is necessary in the synthesis of polyamines. Animal data indicate that inhibition of ornithine decarboxylase inhibits cell division and synthetic functions, which affect the rate of hair growth. Eflornithine is indicated for the reduction of unwanted facial hair in women. Eflornithine is on the World Health Organization's List of Essential Medicines as the drug for the treatment of Trypanosoma brucei gambiense infection. Antiprotozoal (Code: N0000175485) Decarboxylase Inhibitor (Code: N0000175845) Decarboxylase Inhibitors (Code: N0000175844) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Enzyme Inhibitors (Code: D004791) Ornithine Decarboxylase Inhibitors (Code: D065108) Trypanocidal Agents (Code: D014344) 1990-11-28 FDA DMO
Click to view mannitol Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12954186) Mannitol is an osmotic diuretic that is metabolically inert in humans and occurs naturally, as a sugar or sugar alcohol, in fruits and vegetables. Mannitol elevates blood plasma osmolality, resulting in enhanced flow of water from tissues, including the brain and cerebrospinal fluid, into interstitial fluid and plasma. As a result, cerebral edema, elevated intracranial pressure, and cerebrospinal fluid volume and pressure may be reduced. Sorbitol is an isomer of mannitol, the two differ only in the orientation of the hydroxyl group on carbon 2. While similar, the two sugar alcohols have very different uses. Mannitol is used for the promotion of diuresis before irreversible renal failure becomes established, the reduction of intracranial pressure, the treatment of cerebral edema, and the promotion of urinary excretion of toxic substances. Also mannitol is indicated for the assessment of bronchial hyperresponsiveness in patients 6 years of age or older who do not have clinically apparent asthma. Sorbitol is used as a non-stimulant laxative via an oral suspension or enema. In addition, sorbitol has one-third fewer calories and 60 % the sweetening activity of sucrose and is used as a sugar replacement in diabetes. Increased Diuresis (Code: N0000175359) Osmotic Activity (Code: N0000010288) Osmotic Diuretic (Code: N0000175810) Diuretics (Code: D004232) Diuretics, Osmotic (Code: D004234) Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Natriuretic Agents (Code: D045283) Sweetening Agents (Code: D013549) mannitol: 1964-06-08 FDA sorbitol: 1971-08-20 FDA MTL
SOR
Click to view glycol salicylate component of Piadar; topical ointment of the above including 1% methanol in base FDA
Click to view sparteine A quinolizidine alkaloid isolated from several FABACEAE including LUPINUS; SPARTIUM; and CYTISUS. It has been used as an oxytocic and an anti-arrhythmia agent. It has also been of interest as an indicator of CYP2D6 genotype. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102)
Click to view flopropione Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) inhibitor (Source: http://eisai.jp/medical/products/di/EPI/CSP_C_EPI.pdf) The mechanism of action is considered to be based on the inhibition of catechol-o-methyl-transferase (COMT), resulting in an adrenergic action, and anti-serotonin action
Click to view dacarbazine 6-phosphogluconate dehydrogenase, decarboxylating (Organism: Homo sapiens, class: Enzyme, accessions: P52209, gene: PGD, swissprot: 6PGD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20235752) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10473105) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10473105) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10473105) Dacarbazine is a cell-cycle, non-specific antineoplastic agent. It is a structural analogue of 5-amino-imidazole-4-carboxamide which is an intermediate in purine biosynthesis. The exact mechanism of action of dacarbazine is not known. It may function as an alkylating agent, possibly after activation by metabolism in the liver, but other hypotheses, including inhibition of DNA synthesis by acting as a purine analogue and interaction with sulfhydryl groups, have also been proposed. Dacarbazine is inactive until metabolized in the liver by cytochromes P450 to form the reactive N-demethylated species 5-[3-hydroxymethyl-3-methyl-triazen-1-yl]-imidazole-4-carboxamide (HMMTIC) and 5-[3-methyl-triazen-1-yl]-imidazole-4-carboxamide (MTIC). Dacarbazine is used for the palliative therapy of metastatic malignant melanoma. In addition, this drug also is indicated for Hodgkin’s disease as a second-line therapy when used in combination with other effective agents. antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) 1975-05-27 FDA
Click to view succimer lead (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2007/019998s013lbl.pdf) Succimer is a mercaptodicarboxylic acid used as an antidote to heavy metal poisoning because it forms strong chelates with them. Succimer is an analogue of dimercaprol. The advantages of succimer are that it is effective by oral administration because it is soluble in water, it is well-tolerated, has relatively low toxicity and can be given at the same time as iron supplements to treat iron deficiency anaemia. It is used in the management of poisoning by lead and other heavy metals. Lead Chelating Activity (Code: N0000175962) Lead Chelator (Code: N0000175963) Antidotes (Code: D000931) Chelating Agents (Code: D002614) Protective Agents (Code: D020011) Sequestering Agents (Code: D064449) 1991-01-30 FDA
Click to view guanacline Guanacline is a sympatholytic agent with limited post-ganglionic sympathetic blocking action and prolonged catecholamine depletion. It was used for the treatment of hypotension. Its use was discontinued due to cases of persistent orthostatic hypotension after treatment with guanacline.
Click to view chlorphentermine Chlorphentermine is a synthetic amphetamine derivative which exerts anorectic properties. Chlorphentermine is a relatively weak stimulant with little abuse potential. It presents a prominent serotonergic profile leading to pulmonary hypertension and cardiac fibrosis after prolonged use. It was used as an appetite suppressant but is no longer used. Autonomic Agents (Code: D001337) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1982-01-01 FDA
Click to view epinephrine Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019430s074lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19356039) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19356039) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19356039) Amine oxidase [flavin-containing] A (Organism: Rattus norvegicus, class: Enzyme, accessions: P21396, gene: Maoa, swissprot: AOFA_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8138937) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8138937) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9812985) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9776363) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17127057) Chromaffin granule amine transporter (Organism: Homo sapiens, class: Transporter, accessions: P54219, gene: SLC18A1, swissprot: VMAT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8643547) Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8643547) Epinephrine (adrenaline) is a sympathomimetic catecholamine. Epinephrine is produced by the adrenal glands and used as a drug due to its various important functions.Epinephrine acts on both alpha-and beta-adrenergic receptors. Through its action on alpha-adrenergic receptors, epinephrine lessens the vasodilation and increased vascular permeability that occurs during anaphylaxis, which can lead to loss of intravascular fluid volume and hypotension. Through its action on beta-adrenergic receptors, epinephrine causes bronchial smooth muscle relaxation and helps alleviate bronchospasm, wheezing and dyspnea that may occur during anaphylaxis. Racepinephrine is a racemic mixture consisting of inactive d-Epinephrine and active l-Epinephrine enantiomers. Epinephrine is indicated in the emergency treatment of allergic reactions (Type I) including anaphylaxis. Epinephrine's cardiac effects may be of use in restoring cardiac rhythm in cardiac arrest due to various causes but is not used in cardiac failure or in hemorrhagic, traumatic, or cardiogenic shock. Epinephrine also is used as a hemostatic agent. It is also used in treating mucosal congestion of hay fever, rhinitis, and acute sinusitis; to relieve bronchial asthmatic paroxysms; in syncope due to complete heart block or carotid sinus hypersensitivity; for symptomatic relief of serum sickness, urticaria, angioneurotic edema; for resuscitation in cardiac arrest following anesthetic accidents; in simple (open angle) glaucoma; for relaxation of uterine musculature and to inhibit uterine contractions. Epinephrine injection can be utilized to prolong the action of local anesthetics. alpha-Adrenergic Agonist (Code: N0000175552) beta-Adrenergic Agonist (Code: N0000175555) Catecholamine (Code: N0000175570) Catecholamines (Code: N0000007715) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiovascular Agents (Code: D002317) Mydriatics (Code: D009184) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1948-11-19 FDA ALE
XDE
Click to view methyprylon Methyprylon, a piperidinedione CNS depressant, is close to barbituric acid in structure, but different enough to be called a "non-barbiturate" sedative-hynotic. Methyprylon depresses the activity of muscle tissues, the heart, and the respiratory system. Methyprylon binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. Methyprylon was used for the treatment of insomnia and daytime tension but was withdrawn from the market due to adverse events. 1955-01-18 FDA
Click to view epomediol marked choleretic activity in Wistar rats; mechanism of action may be related to increases in both the bile salt dependent & independent fractions of bile Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765)
Click to view clortermine Clortermine is a sympathomimetic amine with infrequent and mild CNS stimulant activity. Clortermine is an appetite suppressant. It was used for the adjunctivetreatment of exogenous obesity. Now it is a a "controlled substance" in schedule II of the US Federal Controlled Substances Act.
Click to view domiodol Domiodol (4-hydroxymethyl-2-indomethyl-2,3-dioxolane) is a compound containing organically bound iodine. In animal studies domiodol induced a dose-related increase in respiratory tract fluid and reduced the viscosity of sputum.
Click to view phosphorylcholine Phosphorylcholine (PC) is a small zwitterionic amino alcohol, which is composed of a negatively charged phosphate bonded to a small, positively charged choline group. Phosphorylcholine is the precursor metabolite of choline in the glycine, serine, and threonine metabolism pathways and in intermediate between choline and cytidine-diphosphate choline in the glycerophospholipid metabolism pathway. Phosphorylcholine is an immunodominant determinant of pneumococcal teichoic acids and also a major prerequisite for proinflammatory effects of PAF and PAF-like lipids. PC is also a component of some bacteria, apoptotic cells, and OxLDL, which, if exposed, is immunogenic. PC has several properties that could in principle both promote and protect against disease, depending on the pathogen and type of inflammatory reaction. In the field of interventional cardiology, phosphorylcholine is used as a synthetic polymer-based coating, applied to drug-eluting stents, to prevent the occurrence of coronary artery restenosis. PC
Click to view azelaic acid 3-oxo-5-alpha-steroid 4-dehydrogenase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P31213, gene: SRD5A2, swissprot: S5A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3207614) Azelaic acid is a naturally occurring dicarboxylic acid produced by Malassezia furfur and found in whole grain cereals, rye, barley and animal products. Azelaic acid possesses antibacterial, keratolytic, comedolytic, and anti-oxidant activity. Azelaic acid is bactericidal against Proprionibacterium acnes and Staphylococcus epidermidis due to its inhibitory effect on the synthesis of microbial cellular proteins. Azelaic acid exerts its keratolytic and comedolytic effects by reducing the thickness of the stratum corneum and decreasing the number of keratohyalin granules by reducing the amount and distribution of filaggrin in epidermal layers. Azelaic acid also possesses a direct anti-inflammatory effect due to its scavenger activity of free oxygen radical. This drug is used topically to reduce inflammation associated with acne and rosacea. antineoplastic agent (Code: CHEBI:35610) dermatologic drug (Code: CHEBI:50177) Decreased Protein Synthesis (Code: N0000008841) Decreased Sebaceous Gland Activity (Code: N0000009982) Antineoplastic Agents (Code: D000970) Dermatologic Agents (Code: D003879) 1995-09-13 FDA AZ1
Click to view barbital A long-acting barbiturate that depresses most metabolic processes at high doses. It is used as a hypnotic and sedative and may induce dependence. Barbital is also used in veterinary practice for central nervous system depression. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377)
Click to view mitoguazone S-adenosylmethionine decarboxylase proenzyme (Organism: Rattus norvegicus, class: Enzyme, accessions: P17708, gene: Amd1, swissprot: DCAM_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8421290) Amiloride-sensitive amine oxidase [copper-containing] (Organism: Rattus norvegicus, class: Enzyme, accessions: P36633, gene: Aoc1, swissprot: AOC1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8421290) Mitoguazone is a guanylhydrazone with potential antineoplastic activity. Mitoguazone is obtained by formal condensation of the two carbonyl groups of methylglyoxal with the primary amino groups of two molecules of aminoguanidine. Mitoguazone competitively inhibits S-adenosyl-L-methionine decarboxylase (SAMD), an enzyme involved in the synthesis of polyamines, resulting in decreased proliferation of tumor cells, antimitochondrial effects, and p53-independent apoptosis. Mitoguazone has been used for the treatment of Hodgkin's disease, Non-Hodgkin's leukemias and malignant lymphomas and of Squamous cell carcinomas of the upper respiratory tract. Mitoguazone is no longer available. antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) 1998-04-17 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view enflurane Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8689955) Enflurane is a general inhalation anesthetic drug. Induction of and recovery from anesthesia with enflurane are rapid. Enflurane has a mild, sweet odor. Enflurane may provide a mild stimulus to salivation or tracheobronchial secretions. Pharyngeal and laryngeal reflexes are readily obtunded. The level of anesthesia can be changed rapidly by changing the inspired enflurane concentration. Enflurane reduces ventilation as depth of anesthesia increases. Enflurane may be used for induction and maintenance of general anesthesia. Enflurane may be used to provide analgesia for vaginal delivery. Low concentrations of enflurane may also be used to supplement other general anesthetic agents during delivery by Cesarean section. Higher concentrations of enflurane may produce uterine relaxation and an increase in uterine bleeding. It was increasingly used for inhalational anesthesia during the 1970s and 1980s but is no longer in common use. anaesthetic (Code: CHEBI:38867) General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) 1972-08-28 FDA
Click to view apronal Apronal was used as a hypnotic drug. It has been withdrawn due to patient development of thrombocytopenic purpura.
Click to view undecylenic acid a fatty acid with a terminal double bond FDA
Click to view piroctone 2(1H)-pyridinone, 1-hydroxy-4-methyl-6-(2,4,4-trimethylpentyl)- combined with 2-aminoethanol; used to treat pityriasis; structure given in first source antiseborrheic (Code: CHEBI:59010)
Click to view guanazodine synonyms EGYT-739 & Sanegyt (Sanegit) refers to sulfate; RN given refers to parent cpd
Click to view isoflurane Potassium channel subfamily K member 17 (Organism: Homo sapiens, class: Ion channel, accessions: Q96T54, gene: KCNK17, swissprot: KCNKH_HUMAN) opener (Source: https://www.ncbi.nlm.nih.gov/pubmed/11263999) Transient receptor potential cation channel subfamily A member 1 (Organism: Rattus norvegicus, class: Ion channel, accessions: Q6RI86, gene: Trpa1, swissprot: TRPA1_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18574153) Potassium channel subfamily K member 3 (Organism: Homo sapiens, class: Ion channel, accessions: O14649, gene: KCNK3, swissprot: KCNK3_HUMAN) opener (Source: https://www.ncbi.nlm.nih.gov/pubmed/10321245) Potassium channel subfamily K member 2 (Organism: Mus musculus, class: Ion channel, accessions: P97438, gene: Kcnk2, swissprot: KCNK2_MOUSE) opener (Source: https://www.ncbi.nlm.nih.gov/pubmed/10321245) GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23364597) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Isoflurane is a fluorinated ether with general anesthetic and muscle relaxant activities. Although the exact mechanism of action has not been established, inhaled isoflurane, appears to act on the lipid matrix of the neuronal cell membrane, which results in disruption of neuronal transmission. Isoflurane is a stable, non-explosive inhalation anesthetic, relatively free from significant side effects. inhalation anaesthetic (Code: CHEBI:38870) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) 1979-12-18 FDA 4LE
ICF
Click to view ribavirin Inosine-5'-monophosphate dehydrogenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P20839, gene: IMPDH1, swissprot: IMDH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020903s055,021546s011lbl.pdf) Inosine-5'-monophosphate dehydrogenase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P12268, gene: IMPDH2, swissprot: IMDH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020903s055,021546s011lbl.pdf) Adenosine kinase (Organism: Homo sapiens, class: Kinase, accessions: P55263, gene: ADK, swissprot: ADK_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17379518) Solute carrier family 28 member 3 (Organism: Homo sapiens, class: Transporter, accessions: Q9HAS3, gene: SLC28A3, swissprot: S28A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20096989) Equilibrative nucleoside transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q99808, gene: SLC29A1, swissprot: S29A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20096989) Ribavirin is a synthetic nucleoside analog of ribofuranose with activity against hepatitis C virus and other RNA viruses. Ribavirin increases the mutation frequency in the genomes of several RNA viruses and ribavirin triphosphate inhibits HCV polymerase in a biochemical reaction. Ribavirin is indicated for the treatment of chronic hepatitis C (CHC) virus infection in patients 5 years of age and older with compensated liver disease not previously treated with interferon alpha, and in adult CHC patients coinfected with HIV. Nucleoside Analog (Code: N0000175459) Nucleoside Analog Antiviral (Code: N0000175466) antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) Antimetabolites (Code: D000963) Antiviral Agents (Code: D000998) Noxae (Code: D009676) 1985-12-31 FDA RBV
Click to view secnidazole Secnidazole is a 5-nitroimidazole antimicrobial. 5-nitroimidazoles enter the bacterial cell as an inactive prodrug where the nitro group is reduced by bacterial enzymes to radical anions. It is believed that these radical anions interfere with bacterial DNA synthesis of susceptible isolates. Secnidazole is active in vitro against most isolates of the following organisms reported to be associated with bacterial vaginosis: Bacteroides spp., Gardnerella vaginalis, Prevotella spp., Mobiluncus spp., Megasphaera-like type I/II. Secnidazole is indicated for the treatment of bacterial vaginosis in adult women. Nitroimidazole Antimicrobial (Code: N0000175435) Nitroimidazoles (Code: N0000007663) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) 2017-09-15 FDA
Click to view amanozine Amanozine is a triazine-based diuretic agent. Amanozine is structurally similar to the diuretic agent chlorazanil. 7ZF
Click to view procymate Procymate is an anxiolytic.
Click to view amphenidone Amphenidone is a CNS depressant. Amphenidone was used as a mild tranquilizer. It was withdrawn in 1961 due to patient development of agranulocytosis.
Click to view selenomethionine Selenomethionine is the racemic mixture of the D and L enantiomers of Selenomethionine, that used as animal’s dietary supplement. L-isomer of selenomethionine is a major natural food-form of selenium. Selenomethionine is either metabolized directly to reactive forms of selenium or stored in place of methionine in body proteins. Se-met metabolism is closely linked to protein turnover. Selenium, which is nutritionally essential for humans, is a constituent of more than two dozen selenoproteins that play critical roles in reproduction, thyroid hormone metabolism, DNA synthesis, and protection from oxidative damage and infection. Selenomethionine is indicated in combinations with other vitamins for prophylactic or therapeutic nutritional supplementation in physiologically stressful conditions. 2007-10-01 FDA MSE
Click to view mafenide Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22370338) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22370338) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22370338) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22370338) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22370338) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Enzyme, accessions: P40881, gene: None, swissprot: CAH_METTE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15546717) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19193158) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12643899) Carbonic anhydrase 4 (Organism: Bos taurus, class: Enzyme, accessions: Q95323, gene: CA4, swissprot: CAH4_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12643899) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16302824) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16302824) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17228881) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15203157) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686931) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686895) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Mafenide is a synthetic antimicrobial agent designated chemically as "-amino-p-toluenesulfonamide monoacetate. The mechanism of action of mafenide is not known, but is different from that of the sulfonamides. Mafenide is not antagonized by pABA, serum, pus or tissue exudates, and there is no correlation between bacterial sensitivities to mafenide and to the sulfonamides. Mafenide acetate exerts broad bacteriostatic action against many gramnegative and gram-positive organisms, including Pseudomonas aeruginosa and certain strains of anaerobes. is indicated for use as an adjunctive topical antimicrobial agent to control bacterial infection when used under moist dressings over meshed autografts on excised burn wounds. Methylated Sulfonamide Antibacterial (Code: N0000175511) Methylated Sulfonamides (Code: N0000175512) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 1969-01-24 FDA 6LH
Click to view carbimazole Lactoperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P22079, gene: LPO, swissprot: PERL_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18954039) Carbimazole (thionamide) is is a sulfur-containing imidazole derivatives. Carbimazole acts as a pro-drug which undergoes rapid and virtually complete metabolism to the active metabolite, thiamazole. (See: thiamazole) prodrug (Code: CHEBI:50266) antithyroid drug (Code: CHEBI:50671) Antithyroid Agents (Code: D013956) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1958-03-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view cyclobutyrol Cyclobutyrol is a synthetic choleretic agent. It induces a transient choleresis which is accompanied by a marked reduction in cholesterol and phospholipid biliary secretion and in the biliary output of plasma-membrane enzymes. bile therapy drug (Code: CHEBI:61026)
Click to view capuride Capuride is an N-acylurea. Capuride is a monoureide sedative. Capuride has a duration of hypnotic effect similar to that of the short-acting barbiturates. It has a role as a sedative.
Click to view aminitrozole Aminitrozole is an orally available antiprotozoal agent used in the treatment of vaginal trichomoniasis. 1971-05-27 Ministry of Health of the Russian Federation
Click to view amrinone cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Organism: Homo sapiens, class: Enzyme, accessions: Q14432, gene: PDE3A, swissprot: PDE3A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10644042) cGMP-inhibited 3',5'-cyclic phosphodiesterase B (Organism: Homo sapiens, class: Enzyme, accessions: Q13370, gene: PDE3B, swissprot: PDE3B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10644042) cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Bos taurus, class: Enzyme, accessions: Q28156, gene: PDE5A, swissprot: PDE5A_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10644042) Amrinone is a synthetic bipyridine phosphodiesterase inhibitor with inotropic and vasodilator properties. Amrinone inhibits type III phosphodiesterase, which is abundant in cardiac and vascular tissues, thereby preventing the degradation of cyclic adenosine monophosphate (cAMP) and increasing intracellular concentrations of this secondary messenger. Elevated levels of cAMP increase the contractile force of the cardiac muscle and produce positive inotropic effects. Although the mechanism of action is not fully understood, amrinone causes smooth muscle relaxation, resulting in peripheral vasodilation (reduced afterload) and a decreased pulmonary vascular resistance (reduced preload). It is used in the treatment of congestive heart failure. Calcium Channel Blockers (Code: D002121) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Membrane Transport Modulators (Code: D049990) Phosphodiesterase 3 Inhibitors (Code: D058987) Phosphodiesterase Inhibitors (Code: D010726) Protective Agents (Code: D020011) Vasodilator Agents (Code: D014665) 1984-07-31 FDA
Click to view phendimetrazine Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27514281) Phendimetrazine is a phenylalkylamine sympathomimetic amine with pharmacological activity similar to the prototype drugs of this class used in obesity, the amphetamines. Actions include central nervous system stimulation and elevation of blood pressure. Phendimetrazine is indicated in the management of exogenous obesity as a short term adjunct (a few weeks) in a regimen of weight reduction based on caloric restriction. Appetite Suppression (Code: N0000175372) Increased Sympathetic Activity (Code: N0000175651) Sympathomimetic Amine Anorectic (Code: N0000175423) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) 1976-07-28 FDA
Click to view pivagabine Pivagabine is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. The effects of pivagabine are mediated by inhibition of release of corticotropin-releasing factor, a neurohormone involved in stress-generating mechanisms. Pivagabine was used as an antidepressant. It was discontinued from the market.
Click to view selegiline Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021336s014lbl.pdf) Selegiline is a selective, irreversible inhibitor of Type B monoamine oxidase. Selegiline is used in the treatment of depression and as adjunctive therapy in combination with levodopa and carbidopa in the therapy of Parkinson disease. Monoamine Oxidase Inhibitor (Code: N0000175744) Monoamine Oxidase Type B Inhibitor (Code: N0000175762) Monoamine Oxidase-B Inhibitors (Code: N0000175761) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Neuroprotective Agents (Code: D018696) Protective Agents (Code: D020011) 1989-06-05 FDA
Click to view clavulanic acid Beta-lactamase TEM (Organism: Escherichia coli, class: Enzyme, accessions: P62593, gene: bla; blaT-3; blaT-4;, swissprot: BLAT_ECOLX) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050590s069,050658s031lbl.pdf) Beta-lactamase (Organism: Escherichia coli, class: Enzyme, accessions: Q6GWS8, gene: blaTEM-125, swissprot: Q6GWS8_ECOLX) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050590s069,050658s031lbl.pdf) Beta-lactamase (Organism: Enterobacter cloacae, class: Enzyme, accessions: P05364, gene: ampC, swissprot: AMPC_ENTCL) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050590s069,050658s031lbl.pdf) Beta-lactamase (Organism: Klebsiella pneumoniae, class: Enzyme, accessions: A0ZX81, gene: blaSHV-72, swissprot: A0ZX81_KLEPN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050590s069,050658s031lbl.pdf) Beta-lactamase (Organism: Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG 12228), class: Enzyme, accessions: P24735, gene: ampC, swissprot: AMPC_PSEAE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050590s069,050658s031lbl.pdf) Beta-lactamase (Organism: Staphylococcus aureus, class: Enzyme, accessions: P00807, gene: blaZ, swissprot: BLAC_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050785s015lbl.pdf) Clavulanic acid is a ?-lactam structurally related to the penicillins which is produced by the fermentation of Streptomyces clavuligerus. Clavulanic acid has the ability to inactivate a wide variety of ?-lactamases by blocking the active sites of these enzymes. Clavulanic acid is particularly active against the clinically important plasmid-mediated ?-lactamases frequently responsible for transferred drug resistance to penicillins and cephalosporins. Clavulanic acid is used in conjunction with amoxicillin for the treatment of bronchitis and urinary tract, skin, and soft tissue infections caused by beta-lactamase producing organisms. antibacterial drug (Code: CHEBI:36047) anxiolytic drug (Code: CHEBI:35474) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) beta-Lactamase Inhibitors (Code: D065093) Enzyme Inhibitors (Code: D004791) beta Lactamase Inhibitor (Code: N0000175930) beta Lactamase Inhibitors (Code: N0000000202) 1984-08-06 FDA J01
Click to view aceglutamide Aceglutamide is an acetyl derivative of the amino acid L-glutamine. Aceglutamide is a psychostimulant and nootropic used to improve memory and concentration. Also aceglutamide aluminium salt is used for the treatment and prevention of peptic ulcers. 2013 China Food and Drug Administration (CFDA) NLQ
Click to view fluoresone Fluoresone was used as an adjunct treatment of epilepsy.
Click to view phenazone Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/25765567) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 2C18 (Organism: Homo sapiens, class: Enzyme, accessions: P33260, gene: CYP2C18, swissprot: CP2CI_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8681486) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8801065) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8801065) Phenazone is an analgesic and antipyretic that has been given by mouth and as ear drops. It inhibits cyclooxygenases and shows little anti-inflammatory activity. Phenazone is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29) opioid analgesic (Code: CHEBI:35482) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1964-01-01 YEAR INTRODUCED
Click to view promoxolane Promoxolane is a cyclic derivative of glycerol. Promoxolane produces skeletal-muscle-relaxing effects due to its depressant action on spinal inter-neural connections which relives tension and spasm without central depression. Promoxolane was used for the treatment of neuroses as a minor tranquilizer to produce sedation. Also promoxolane was used for dysmenorrhea and the menopausal syndrome.
Click to view droxidopa Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/203202s007lbl.pdf) Aromatic-L-amino-acid decarboxylase (Organism: Homo sapiens, class: Enzyme, accessions: P20711, gene: DDC, swissprot: DDC_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/203202s007lbl.pdf) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) agonist (Source: https://pubmed.ncbi.nlm.nih.gov/20966043/) Droxidopa is a synthetic amino acid precursor of norepinephrine. The exact mechanism of action of droxidopa in the treatment of neurogenic orthostatic hypotension is unknown. Droxidopa is a synthetic amino acid analog that is directly metabolized to norepinephrine by dopa-decarboxylase, which is extensively distributed throughout the body. Droxidopa is believed to exert its pharmacological effects through norepinephrine and not through the parent molecule or other metabolites. Norepinephrine increases blood pressure by inducing peripheral arterial and venous vasoconstriction. Droxidopa is indicated for the treatment of orthostatic dizziness, lightheadedness, or the “feeling that you are about to black out” in adult patients with symptomatic neurogenic orthostatic hypotension caused by primary autonomic failure (Parkinson's disease, multiple system atrophy, and pure autonomic failure), dopamine beta-hydroxylase deficiency, and non-diabetic autonomic neuropathy. prodrug (Code: CHEBI:50266) vasoconstrictor agent (Code: CHEBI:50514) antihypertensive agent (Code: CHEBI:35674) Catecholamines (Code: N0000007715) Increased Blood Pressure (Code: N0000178478) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) 2014-02-18 FDA
Click to view fenproporex an anorectic drug used in the treatment of obesity 1975 YEAR INTRODUCED
Click to view etryptamine Ethyltryptamine is a non hydrazine reversible monoamine oxidase inhibitor. It is used as an antidepressant. However, in 1962, after the discovery of an unacceptable incidence of agranulocytosis, the development of ethyltryptamine was halted and the drug was withdrawn from potential market use. Currently, ethyltryptamine is an illegal substance. 1961 YEAR INTRODUCED
Click to view unithiol Unithiol is a chelating agent used as an antidote to heavy metal poisoning. Its active sulfhydryl groups enter into reactions with thiol poisons present in blood and tissues, form not toxic complex with them eliminated with urine. The poisons fixation results in the body enzyme systems changed under the poisons effect functions restoration. It is efficient as an antidote in case of intoxications by arsenic and heavy metals salts. Antidotes (Code: D000931) Chelating Agents (Code: D002614) Protective Agents (Code: D020011) Sequestering Agents (Code: D064449) 1964-04-30 Ministry of Health of the Russian Federation
Click to view phensuximide Phensuximide is an anticonvulsant in the succinimide class. It suppresses the paroxysmal three cycle per second spike and wave EEG pattern associated with lapses of consciousness in petit mal seizures. The frequency of attacks is reduced by depression of nerve transmission in the motor cortex. IT is used for the treatment of epilepsy. 1953-09-08 FDA
Click to view azacitidine Azacitidine is a pyrimidine nucleoside analog of cytidine. Azacitidine is believed to exert its antineoplastic effects by causing hypomethylation of DNA and direct cytotoxicity on abnormal hematopoietic cells in the bone marrow. The concentration of azacitidine required for maximum inhibition of DNA methylation in vitro does not cause major suppression of DNA synthesis. The cytotoxic effects of azacitidine cause the death of rapidly dividing cells, including cancer cells that are no longer responsive to normal growth control mechanisms. Non-proliferating cells are relatively insensitive to azacitidine. Azacitidine is indicated for the treatment of patients with the following FAB myelodysplastic syndrome subtypes: Refractory anemia or refractory anemia with ringed sideroblasts (if accompanied by neutropenia or thrombocytopenia or requiring transfusions), refractory anemia with excess blasts, refractory anemia with excess blasts in transformation, and chronic myelomonocytic leukemia. Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Noxae (Code: D009676) 2004-05-19 FDA 5AE
Click to view thiotepa Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208264s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208264s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208264s000lbl.pdf) Thiotepa is a cytotoxic agent of the polyfunctional type, related chemically and pharmacologically to the nitrogen mustard. The radiomimetic action of thiotepa is believed to occur through the release of ethyleneimine radicals which, like irradiation, disrupt the bonds of DNA. One of the principle bond disruptions is initiated by alkylation of guanine at the N-7 position, which severs the linkage between the purine base and the sugar and liberates alkylated guanines. Thiotepa is a very toxic alkylating antineoplastic agent also used as an insect sterilant. Thiotepa causes skin, gastrointestinal, CNS, and bone marrow damage. Thiotepa may reasonably be anticipated to be a carcinogen. Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Myeloablative Agonists (Code: D019653) Noxae (Code: D009676) 1959-03-09 FDA
Click to view chromocarb treatment for certain forms of hemorrhagic anal inflammations
Click to view pentamethonium bromide Pentamethonium bromide is an anglioplegic agent which produces arterial vasodilation. It was used for the treatment of hypertension and circulation diseases. It is no longer available.
Click to view carglumic acid Carbamoyl-phosphate synthase [ammonia], mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P31327, gene: CPS1, swissprot: CPSM_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022562s005lbl.pdf) Carglumic acid ( N-carbamoyl-L-glutamic acid or (2S)-2-(carbamoylamino) pentanedioic acid) is a carbamoyl phosphate synthetase 1 (CPS 1) activator. Carglumic acid is a synthetic structural analogue of N-acetylglutamate (NAG) which is produced from glutamate and acetyl-CoA in a reaction catalyzed by N-acetylglutamate synthase (NAGS), a mitochondrial liver enzyme. NAG acts as an essential allosteric activator of Carbamoyl Phosphate Synthetase 1 (CPS 1), a mitochondrial liver enzyme which catalyzes the first reaction of the urea cycle. The urea cycle, whose role is the disposition of ammonia, includes a series of biochemical reactions in the liver resulting in the conversion of ammonia into urea, which is then excreted through the urine. Carglumic acid acts as a CPS1 activator in patients with NAGS deficiency, thereby removing the block in the urea cycle and facilitating ammonia detoxification and urea production. Carglumic acid is indicated as adjunctive therapy for the treatment of acute hyperammonemia or as maintenance therapy for the treatment of chronic hyperammonemia due to the deficiency of the hepatic enzyme N-acetylglutamate synthase. orphan drug (Code: CHEBI:71031) Carbamoyl Phosphate Synthetase 1 Activator (Code: N0000184144) Carbamoyl Phosphate Synthetase 1 Activators (Code: N0000184143) 2010-03-18 FDA
Click to view dioxybenzone Dioxybenzone is a derivative of benzophenone used in sunscreen to block UVB and short-wave UVA rays. FDA
Click to view nitroxoline Methionine aminopeptidase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P50579, gene: METAP2, swissprot: MAP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21088277) Cathepsin B (Organism: Homo sapiens, class: Enzyme, accessions: P07858, gene: CTSB, swissprot: CATB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21598397) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24088053) Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Nitroxoline is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. Its antibacterial activity may stem from the metal ion complexation vital for bacterial growth. This drug may also have antitumor activity by inhibition of type 2 methionine aminopeptidase (MetAP2) protein which is involved in angiogenesis. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Antifungal Agents (Code: D000935) Renal Agents (Code: D012076) 2006-06-09 Ministry of Health of the Russian Federation HNQ
Click to view procodazole Procodazole (1H-benzimidazole-2-propanoic acid) is an immunomodulator. Procodazole enhances the phagocytic activity in the liver and the spleen. 4BX
Click to view dihydralazine Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10525281) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10525281) Dihydralazine belongs to thehydrazinophthalazine chemical class and has very similar effects to hydralazine. Dihydralazine is the most frequently used antihypertensive drug in the treatment of severe hypertension in pregnancy. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) 1979-02-13 Hungary National Institute of Pharmacy and Nutrition
Click to view isosorbide mononitrate Isosorbide mononitrate is a vasodilator with effects on both arteries and veins. The principal pharmacological action of isosorbide mononitrate is relaxation of vascular smooth muscle and consequent dilatation of peripheral arteries and veins, especially the latter. Similar to other nitrites and organic nitrates, Isosorbide Mononitrate is converted to nitric oxide (NO), an active intermediate compound that activates the enzyme guanylate cyclase. Isosorbide mononitrate is rapidly and completely absorbed from the gastrointestinal tract. In humans, is not subject to first pass metabolism in the liver. Isosorbide mononitrate is indicated for the prevention and treatment of angina pectoris due to coronary artery disease. vasodilator agent (Code: CHEBI:35620) Nitrate Vasodilator (Code: N0000175415) Nitrates (Code: N0000007647) Vasodilation (Code: N0000009909) Cardiovascular Agents (Code: D002317) Nitric Oxide Donors (Code: D020030) Vasodilator Agents (Code: D014665) 1991-12-30 FDA
Click to view idrocilamide Idrocilamide is a skeletal muscle relaxant and anti-inflammatory agent. Idrocilamide is used as a topical cream to treat lumbago and other kinds of muscular pain. 1998-05-11 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view amiphenazole used as a respiratory tonic, morphine antagonist, & antidote in barbiturate poisoning; RN given refers to parent cpd; sturcture Respiratory System Agents (Code: D019141)
Click to view oxidronic acid Oxidronic acid is a calcium regulator. In complex with Technetium Tc 99m is used as diagnostic skeletal imaging agent used to demonstrate areas of altered osteogenesis in adult and pediatric patients. 1982-01-01 FDA
Click to view citric acid pH (H+ ion activity) (Organism: None, class: Unclassified, accessions: None, gene: None, swissprot: None) other (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019481s013lbl.pdf) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12724351) Citric acid is a key intermediate in metabolism. It is an acid compound found in citrus fruits. Citric acid is a natural preservative and is also used to add an acidic (sour) taste to foods and soft drinks. The salts of citric acid (citrates) can be used as anticoagulants due to their calcium chelating ability. It is also used as an acidulant to control pH. food acidity regulator (Code: CHEBI:64049) Acidifying Activity (Code: N0000175833) Calculi Dissolution Agent (Code: N0000175835) Anti-coagulant (Code: N0000175980) Decreased Coagulation Factor Activity (Code: N0000008556) Calcium Chelating Activity (Code: N0000175089) Anticoagulants (Code: D000925) Calcium Chelating Agents (Code: D065096) Chelating Agents (Code: D002614) Hematologic Agents (Code: D006401) Sequestering Agents (Code: D064449) 1982-06-22 FDA CIT
FLC
Click to view clonitrate Clonitrate (chloroglyceryl dinitrate) is an oily liquid. It has coronary-dilator effect on isolated heart and therapeutic effect on the angina pectoris patient. Chloroglyceryl dinitrate is a more potent coronary dilator than nitroglycerin. It is no longer availible.
Click to view ibufenac Amine oxidase [flavin-containing] B (Organism: Mus musculus, class: Enzyme, accessions: Q8BW75, gene: Maob, swissprot: AOFB_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22984634) Ibufenac is a nonsteroidal anti-inflammatory drug. Ibufenac has anti-inflammatory, antipyretic and analgesic properties. It was used for the treatment of rheumatoid arthritis. It was withdrawn from the market due to hepatotoxicity. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481)
Click to view tocainide Tocainide is an antiarrhythmic agent which exerts a potential- and frequency-dependent block of sodium channels. Tocainide acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation. Tocainide binds preferentially to the inactive state of the sodium channels. The antiarrhythmic actions are mediated through effects on sodium channels in Purkinje fibers. It is used in the treatment of ventricular arrhythmias. anti-arrhythmia drug (Code: CHEBI:38070) local anaesthetic (Code: CHEBI:36333) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1984-11-09 FDA
Click to view bitoscanate Bitoscanate is a tasteless, odorless, colorless, needle-like crystalline solid material prepared from mustard powder acid. Bitoscanate was used as an anthelmintic against nematodes, especially hookworms (Necator sp.) and Ancylostoma duodenale. Bitoscanate is an extremely hazardous substance. 1970-04-01 CDSCO (INDIA)
Click to view glucuronamide Glucuronamide is a hexose related to glucuronic acid. Glucuronamide in combination with caffeine and ascorbic acid has antiasthenic properties and is used against fatigue. 1996-08-28 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view carbaryl Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23632007) Carbaryl is a carbamate insecticide and parasiticide. It is a potent anticholinesterase agent belonging to the carbamate group of reversible cholinesterase inhibitors. It has a particularly low toxicity from dermal absorption and is used for control of head lice in some countries. carbamate insecticide (Code: CHEBI:38461) acaricide (Code: CHEBI:22153) agrochemical (Code: CHEBI:33286) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Insecticides (Code: D007306) Neurotransmitter Agents (Code: D018377) Pesticides (Code: D010575)
Click to view betamipron Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11426832) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11426832) Betamipron is an amino acid derivative. Betamipron reduces the nephrotoxicity by carbapenem antibiotics by inhibiting the intracellular accumulation in renal tubules. It is used in combination with panipenem for inhibition renal uptake of panipenem and also from panipenem's nephrotoxicity. 1993 PMDA BYA
Click to view actarit immunomodulator 2008-07-22 CDSCO (INDIA)
Click to view butamben Butamben is the ester of 4-aminobenzoic acid and butanol. It is used as a local anesthetic. It is one of three components in the topical anesthetic Cetacaine local anaesthetic (Code: CHEBI:36333) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) FDA
Click to view fenozolone Fenozolone is a psychostimulant drug. It exhibits an amphetamine-like effect and increases transmission of all monoamines. It was used as a psychostimulant and antidepressant. Autonomic Agents (Code: D001337) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566)
Click to view tryptophan Extracellular calcium-sensing receptor (Organism: Homo sapiens, class: GPCR, accessions: P41180, gene: CASR, swissprot: CASR_HUMAN) allosteric modulator (Source: ) Probable G-protein coupled receptor 139 (Organism: Homo sapiens, class: Unclassified, accessions: Q6DWJ6, gene: GPR139, swissprot: GP139_HUMAN) agonist (Source: ) An essential amino acid that is necessary for normal growth in infants and for NITROGEN balance in adults. It is a precursor of INDOLE ALKALOIDS in plants. It is a precursor of SEROTONIN (hence its use as an antidepressant and sleep aid). It can be a precursor to NIACIN, albeit inefficiently, in mammals. Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1975 FDA TRP
DTR
Click to view sabcomeline Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10323594) Sabcomeline is a selective M1 partial agonist. Sabcomeline improves cognitive performance. It was under development for the treatment of Alzheimer's disease, but later it was discontinued due to poor results.
Click to view etafedrine Etafedrine is a sympathomimetic agent. It acts on the sympathetic receptors of the bronchial tree relaxing spasm. Etafedrine is used in combination with hydrocodone, doxylamine, sodium citrate and alcohol for the treatment of cough associated with inflamed mucosa, which does not respond to products of lesser potency. 1983-12-31 Health Canada
Click to view temozolomide Temozolomide is not directly active but undergoes rapid nonenzymatic conversion at physiologic pH to the reactive compound 5-(3-methyltriazen1-yl)-imidazole-4-carboxamide (MTIC). The cytotoxicity of MTIC is thought to be primarily due to alkylation of DNA. It is indicated for the treatment of glioblastoma multiforme, refractory anaplastic astrocytoma. antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) 1999-08-11 FDA
Click to view ibuprofen tidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Acid-sensing ion channel 1 (Organism: Homo sapiens, class: Ion channel, accessions: P78348, gene: ASIC1, swissprot: ASIC1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/28949138) Sodium-coupled monocarboxylate transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q8N695, gene: SLC5A8, swissprot: SC5A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16729224) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9296349) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9296349) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12954186) Ibuprofen is a nonsteroidal anti-inflammatory agent with analgesic and antipyretic properties. It’s used temporarily relieves minor aches and pains due to: headache; the common cold; muscular aches; backache; toothache; minor pain of arthritis; menstrual cramps and temporarily reduces fever. The exact mechanism of action of ibuprofen is unknown. Ibuprofen is administered as a racemic mixture. The R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo. The S-enantiomer (dexibuprofen) is believed to be the more pharmacologically active enantiomer. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Central Nervous System Agents (Code: D002491) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1974-08-27 FDA IBP
IZP
Click to view aminohippuric acid Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9950961) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11669456) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10760098) Solute carrier organic anion transporter family member 3A1 (Organism: Homo sapiens, class: Transporter, accessions: Q9UIG8, gene: SLCO3A1, swissprot: SO3A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14631946) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Aminohippuric acid is a glycine amide of 4-aminobenzoic acid. Renal proximal tubules secrete various organic anions, including drugs and p-aminohippurate (PAH). Uptake of PAH from blood into tubule cells occurs by exchange with intracellular alpha-ketoglutarate and is mediated by the organic anion transporter 1. PAH exit into tubule lumen is species specific and may involve ATP-independent and -dependent transporters. Enhanced secretion of p-aminohippuric acid occurs in Fanconi's syndrome. It is used as a diagnostic aid to measure effective renal plasma flow and excretory capacity. Indicators and Reagents (Code: D007202) 1944-12-30 FDA
Click to view enprofylline Adenosine receptor A1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25099, gene: Adora1, swissprot: AA1R_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3002801) Adenosine A2 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P29276|P30543, gene: Adora2a|Adora2b, swissprot: AA2AR_RAT|AA2BR_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3002801) Adenosine receptor A2b (Organism: Homo sapiens, class: GPCR, accessions: P29275, gene: ADORA2B, swissprot: AA2BR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10496952) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10496952) Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10496952) Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10496952) Enprofylline is a derivative of theophylline which shares bronchodilator properties. iI was used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. bronchodilator agent (Code: CHEBI:35523) anti-asthmatic drug (Code: CHEBI:49167) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) anti-arrhythmia drug (Code: CHEBI:38070) Adenosine A2 Receptor Antagonists (Code: D058917) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P1 Receptor Antagonists (Code: D058915) Respiratory System Agents (Code: D019141)
Click to view caffeine Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049999) Adenosine receptor A2b (Organism: Homo sapiens, class: GPCR, accessions: P29275, gene: ADORA2B, swissprot: AA2BR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049999) Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049999) Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049999) cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20164566) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Organism: Homo sapiens, class: Kinase, accessions: O00329, gene: PIK3CD, swissprot: PK3CD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12145276) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Organism: Homo sapiens, class: Kinase, accessions: P42336, gene: PIK3CA, swissprot: PK3CA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12145276) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (Organism: Homo sapiens, class: Kinase, accessions: P42338, gene: PIK3CB, swissprot: PK3CB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12145276) Serine-protein kinase ATM (Organism: Homo sapiens, class: Kinase, accessions: Q13315, gene: ATM, swissprot: ATM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10531013) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14616429) Guanine deaminase (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2T3, gene: GDA, swissprot: GUAD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20716488) Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic and anti-inflammatory activities. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages. psychotropic drug (Code: CHEBI:35471) diuretic (Code: CHEBI:35498) food additive (Code: CHEBI:64047) adjuvant (Code: CHEBI:60809) central nervous system stimulant (Code: CHEBI:35337) Central Nervous System Stimulation (Code: N0000175729) Methylxanthine (Code: N0000175790) Xanthines (Code: N0000008118) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Phosphodiesterase Inhibitors (Code: D010726) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P1 Receptor Antagonists (Code: D058915) 1948-11-26 FDA CFF
Click to view phenamine Phenocoll is an antineuralgic, analgesic and antipyretic drug. It is a derivative of phenacetin and thus has the same mechanism of action (COX-2 inhibition). It used to control inflammation in such diseases as gout, influenza, malaria, rheumatism and pleuritis.
Click to view ethotoin Ethotoin is a hydantoin derivative and anticonvulsant. Ethotoin exerts an antiepileptic effect without causing general central nervous system depression. The mechanism of action is probably very similar to that of phenytoin. The latter drug appears to stabilize rather than to raise the normal seizure threshold, and to prevent the spread of seizure activity rather than to abolish the primary focus of seizure discharges. It is indicated for the control of tonic-clonic (grand mal) and complex partial (psychomotor) seizures. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1957-04-22 FDA
Click to view aminoacridine Trypanothione reductase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P28593, gene: TPR, swissprot: TYTR_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10639286) Aminoacridine is a highly fluorescent anti-infective dye used experimentally as a mutagen, due to its interaction with DNA. It is also used as an intracellular pH indicator. It is used in combination with lidocaine for the quick, effective relief from the pain of common mouth ulcers and denture rubbing. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Coloring Agents (Code: D004396) Fluorescent Dyes (Code: D005456) Indicators and Reagents (Code: D007202) Luminescent Agents (Code: D049408) Mutagens (Code: D009153) Noxae (Code: D009676) 1988-09-08 New Zealand Medicines and Medical Devices Safety Authority AA
Click to view hexylresorcinol Polyphenol oxidase 2 (Organism: Agaricus bisporus, class: Enzyme, accessions: O42713, gene: PPO2, swissprot: PPO2_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19054671) Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23871907) Hexylresorcinol is a local anaesthetic for topical use on the mucous membranes of the mouth and throat. Mild antiseptic activity has also been demonstrated. Hexylresorcinol is used as an antiseptic and local anaesthetic for the relief of sore throat and its associated pain. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) FDA
Click to view salamidacetic acid salamidacetic acid (salicylamide O-acetic acid) is a nonsteroidal anti-inflammatory drug.
Click to view buramate Buramate is a member of benzenes. Buramate was used for the treatment of epilepsy, espesially in Petit Mal.
Click to view phenallymal Phenallymal (alphenal) is a barbiturate derivative. It has primarily anticonvulsant properties, and was used occasionally for the treatment of epilepsy or convulsions.
Click to view metirosine Metirosine is an antihypertensive drug. Metyrosine inhibits tyrosine hydroxylase, which catalyzes the first transformation in catecholamine biosynthesis, i.e., the conversion of tyrosine to dihydroxyphenylalanine (DOPA). Metirosine is used for the treatment of patients with pheochromocytoma, for preoperative preparation of patients for surgery, management of patients when surgery is contraindicated, and chronic treatment of patients with malignant pheochromocytoma. antihypertensive agent (Code: CHEBI:35674) Catecholamine Synthesis Inhibitor (Code: N0000175569) Catecholamine Synthesis Inhibitors (Code: N0000175361) 1979-10-03 FDA
Click to view amisometradine Amisometradine is a pyrimidinedione-based diuretic and isomer of aminometradine with less toxicity. Amisometradine produces diuresis by a mechanism similar to that of the xanthines. Amisometradine causes inhibition of reabsorption of sodium by the proximal tubules. Amisometradine was used to for treatment of mild edema in patients with congestive heart failure. Amisometradine was voluntarly withdrawn from market. 1956 YEAR INTRODUCED
Click to view aminometradine Aminometradine is a pyrimidinedione-based diuretic. Aminometradine appears to inhibit the reabsorption of sodium ions by the renal tubules and is a relatively weak diuretic. It was used to for treatment of congestive heart failure. It was withdrawn from the market due to its unsatisfactory results and replaced by amisometradine. 1954 YEAR INTRODUCED
Click to view pimeclone Pimeclone is a respiratory stimulant. It is no longer available.
Click to view flurbiprofen Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10377455) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10091674) Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22877157) Aldo-keto reductase family 1 member C2 (Organism: Homo sapiens, class: Enzyme, accessions: P52895, gene: AKR1C2, swissprot: AK1C2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22877157) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018766s020lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018766s020lbl.pdf) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991954) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-6 (Organism: Homo sapiens, class: Enzyme, accessions: P19224, gene: UGT1A6, swissprot: UD16_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW9, gene: UGT1A8, swissprot: UD18_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 2B4 (Organism: Homo sapiens, class: Enzyme, accessions: P06133, gene: UGT2B4, swissprot: UD2B4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) UDP-glucuronosyltransferase 1-10 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW8, gene: UGT1A10, swissprot: UD110_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843492) Flurbiprofen is a derivative of propionic acid, and a phenylalkanoic acid derivative of non-steroidal antiinflammatory drugs (NSAIDs) with analgesic, antiinflammatory and antipyretic effects. Flurbiprofen non-selectively binds to and inhibits cyclooxygenase (COX). This results in a reduction of arachidonic acid conversion into prostaglandins that are involved in the regulation of pain, inflammation and fever. This NSAID also inhibits carbonic anhydrase, thereby reducing the production of hydrogen and bicarbonate ions. Upon ocular administration, flurbiprofen may reduce bicarbonate ion concentrations leading to a decrease in the production of aqueous humor, thereby lowering intraocular pressure. Esflurbiprofen (S-enantiomer of flurbiprofen) was approved by PMDA on Sep 28, 2015. Flurbiprofen is used for the treatment of intraoperative miosis, rheumatoid arthritis, osteorarthritis and anklosing spondylitis. Esflurbiprofen is indicated for the treatment of osteoarthritis pain and inflammation. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) antipyretic (Code: CHEBI:35493) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Central Nervous System Agents (Code: D002491) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1986-12-31 FDA FLP
FLR
Click to view gluconic acid Gluconic Acid is the carboxylic acid formed by the oxidation of the first carbon of glucose with antiseptic and chelating properties. Gluconic acid, found abundantly in plant, honey and wine, can be prepared by fungal fermentation process commercially. This agent and its derivatives can used in formulation of pharmaceuticals, cosmetics and food products as additive or buffer salts. Aqueous gluconic acid solution contains cyclic ester glucono delta lactone structure, which chelates metal ions and forms very stable complexes. In alkaline solution, this agent exhibits strong chelating activities towards anions, i.e. calcium, iron, aluminium, copper, and other heavy metals. 1975-08-13 FDA GCO
Click to view bismuth camphocarbonate
Click to view creatinolfosfate Creatinolphosphate is an anti-ischemic and an antiarrhythmic agent. It is used for the treatment of conditions involving a hypoxic damage of the heart muscle. 1968 Italian Medicines Agency (AIFA)
Click to view levodopa D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9633680) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9633680) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16730978) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16730978) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16730978) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17174092) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17174092) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17499996) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18627905) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18627905) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/19464888) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Unclassified, accessions: P40881, gene: None, swissprot: CAH_METTE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20061162) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Unclassified, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20061162) The naturally occurring form of dihydroxyphenylalanine and the immediate precursor of dopamine. Unlike dopamine itself, it can be taken orally and crosses the blood-brain barrier. It is rapidly taken up by dopaminergic neurons and converted to dopamine. It is used for the treatment of parkinsonian disorders and is usually given with agents that inhibit its conversion to dopamine outside of the central nervous system. antidyskinesia agent (Code: CHEBI:66956) dopaminergic agent (Code: CHEBI:48560) antiparkinson drug (Code: CHEBI:48407) prodrug (Code: CHEBI:50266) Aromatic Amino Acid Decarboxylation Inhibitor (Code: N0000175754) DOPA Decarboxylase Inhibitors (Code: N0000175755) Aromatic Amino Acid (Code: N0000193220) Amino Acids, Aromatic (Code: N0000011248) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Neurotransmitter Agents (Code: D018377) 1970-06-04 FDA DAH
Click to view ethylnorepinephrine Ethylnorepinephrine is a sympathomimetic with beta-adrenoceptor agonist activity. Ethylnorepinephrine is used as a bronchodilator
Click to view pildralazine Pildralazine is a tertiary amino compound and a dialkylarylamine. Pildralazine is antihypertensive vasodilator which is containing a free hydrazine group. It was used for the treatment of hypertension.
Click to view beclamide Beclamide (N-benzyl-B-chloropropionamide) is an acetylurea derivative with anticonvulsant properties. Beclamide has been used for over three decades with little knowledge of how it acts in the CNS. It was as a sedative and as an anticonvulsant for the treatment of epilepsy and behavioral disorders associated with epilepsy. It was studied in the 1950s for generalised tonic-clonic seizures but was not effective for absence seizures. It was withdrawn from the market. 1952 FDA
Click to view nitrofurazone Nitrofurazone is a topical anti-infective agent effective against gram-negative and gram-positive bacteria. It is used for superficial wounds and injuries and skin infections. Nitrofurazone has also been administered orally in the treatment of trypanosomiasis. antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) 1945-10-04 FDA NFZ
Click to view mimosine Polyphenol oxidase 2 (Organism: Agaricus bisporus, class: Enzyme, accessions: O42713, gene: PPO2, swissprot: PPO2_AGABI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16750372) Mimosine is an antineoplastic alanine-substituted pyridine derivative isolated from Leucena glauca. Major effects of mimosine is to stop hair growth. Mimosine is an effective inhibitor of DNA replication in mammalian cells. It blocks entry into S phase (late G1 phase), and suppress elongation of DNA replication (S phase). The chelation of iron seems to be one of the main modes of action of mimosine for cell cycle arrest. As an iron-chelating and cell cycle stopping agent, mimosine was tested in preclinical models of cancer, pulmonary fibrosis and iron overload. MMS
Click to view guaifenesin Guaifenesin is an expectorant the action of which promotes or facilitates the removal of secretions from the respiratory tract. The precise mechanism of action of guaifenesin is not known; however, it is thought to act as an expectorant by increasing the volume and reducing the viscosity of secretions in the trachea and bronchi. Guaifenesin isused for the treatment of cough and common cold. Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) 2002-07-12 FDA
Click to view metharbital Metharbital is a barbiturate anticonvulsant, similar to phenobarbital. Metharbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. Metharbital is used in the treatment of epilepsy. It was withdrawn from the market. 1952 FDA
Click to view tacrine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18479118) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18479118) Amine oxidase [flavin-containing] A (Organism: Rattus norvegicus, class: Enzyme, accessions: P21396, gene: Maoa, swissprot: AOFA_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22503231) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21599003) Tacrine is a parasympathomimetic, a reversible cholinesterase inhibitor. Tacrine is postulated to exert its therapeutic effect by enhancing cholinergic function. Tacrine is indicated for the treatment of mild to moderate dementia of the Alzheimer's type. Because of its liver toxicity and attendant requirement for monitoring liver function, tacrine prescriptions dropped after other acetylcholinesterase inhibitors were introduced, and its use has been largely discontinued. Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Nootropic Agents (Code: D018697) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) Cholinesterase Inhibitor (Code: N0000175723) 1993-09-09 FDA THA
Click to view guanethidine Guanethidine is an antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. Guanethidine is used for the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension. antihypertensive agent (Code: CHEBI:35674) adrenergic antagonist (Code: CHEBI:37887) sympatholytic agent (Code: CHEBI:66991) Adrenergic Agents (Code: D018663) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1960-07-05 FDA
Click to view oxophenarsine Oxophenarsine is a partial oxidation product of arsphenamine and has the same therapeutic uses. Oxophenarsine causes a rapid disappearance of the spirochetes, healing of the lesions and areversal of a positive Wassermann's reaction in most cases. Oxophenarsine an arsenical formerly used in the form of its hydrochloride to treat syphilis. Oxophenarsine is no longer available.
Click to view diethylcarbamazine Diethylcarbamazine is an anthelmintic used primarily as the citrate in the treatment of filariasis, particularly infestations with Wucheria bancrofti or Loa loa. The exact mechanism of its action is unknown, however some studies showed the involvment of inducible nitric-oxide synthase and the cyclooxygenase pathway. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Enzyme Inhibitors (Code: D004791) Filaricides (Code: D005369) Lipoxygenase Inhibitors (Code: D016859) Antihelminthic (Code: N0000175481) 1950-11-13 FDA
Click to view cevimeline Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24980056) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24980056) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24980056) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24980056) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/020989s008lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/020989s008lbl.pdf) Dimethylaniline monooxygenase [N-oxide-forming] 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q01740, gene: FMO1 swissprot: FMO1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11725960) Cevimeline is a cholinergic agonist which binds to muscarinic receptors. Muscarinic agonists in sufficient dosage can increase secretion of exocrine glands, such as salivary and sweat glands and increase tone of the smooth muscle in the gastrointestinal and urinary tracts. Cevimeline is indicated for the treatment of symptoms of dry mouth in patients with Sj?gren’s Syndrome. muscarinic agonist (Code: CHEBI:38325) Cholinergic Muscarinic Agonists (Code: N0000000104) Cholinergic Receptor Agonist (Code: N0000175884) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Muscarinic Agonists (Code: D018721) Neurotransmitter Agents (Code: D018377) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) 2000-01-11 FDA
Click to view octamylamine Octamylamine is a secondary amino compound. It was used as an antispasmodic.
Click to view sevoflurane Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8214760) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7879937) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7879937) Sevoflurane is an inhalational anesthetic agent for use in induction and maintenance of general anesthesia. Although the mechanism of action has not been fully elucidated, sevoflurane may act by interfering with the release and re-uptake of neurotransmitters at post-synaptic terminals, and/or alter ionic conductance following receptor activation by a neurotransmitter. Sevoflurane may also interact directly with lipid matrix of neuronal membranes, thereby affecting gating properties of ion channels. In addition, this agent may activate gamma-aminobutyric acid (GABA) receptors hyperpolarizing cell membranes. inhalation anaesthetic (Code: CHEBI:38870) platelet aggregation inhibitor (Code: CHEBI:50427) central nervous system depressant (Code: CHEBI:35488) General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) 1995-06-07 FDA
Click to view pyrovalerone Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16480278) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16480278) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16480278) Pyrovalerone is a psychostimulant. It has a central action. Pyrovalerone inhibits the dopamine transporter and the norepinephrine transporter, and is a weak inhibitor of the serotonin transporter. Pyrovalerone was demonstrated to reduce symptoms of chronic fatigue in humans. It was used for the treatment of chronic fatigue or lethargy. Pyrovalerone was withdrawn from the market. Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) 1973 YEAR INTRODUCED
Click to view monobenzone Monobenzone is the monobenzyl ether of hydroquinone. Its mechanism of action is not fully understood. The topical application of monobenzone increases the excretion of melanin from the melanocytes. Monobenzone may cause destruction of melanocytes and permanent depigmentation. Monobenzone is indicated for final depigmentation in extensive Vitiligo. dermatologic drug (Code: CHEBI:50177) melanin synthesis inhibitor (Code: CHEBI:64933) Depigmenting Activity (Code: N0000175851) Depigmenting Agent (Code: N0000175853) Melanin Synthesis Inhibitors (Code: N0000175850) 1952-11-10 FDA
Click to view tetryzoline Tetryzoline is an imidazole derivative with sympathomimetic activity. Applied locally to the eye or nose, tetrahydrozoline binds to and activates alpha-adrenergic receptors, resulting in vasoconstriction and decreased nasal and ophthalmic congestion. nasal decongestant (Code: CHEBI:77715) sympathomimetic agent (Code: CHEBI:35524) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Nasal Decongestants (Code: D014663) Ophthalmic Solutions (Code: D009883) Peripheral Nervous System Agents (Code: D018373) Pharmaceutical Solutions (Code: D019999) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1979-11-30 FDA
Click to view medetomidine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021038s027lbl.pdf) Medetomidine is a relatively selective alpha2-adrenergic agonist with sedative properties. Medetomidine is a racemic mixture of the active R and inactive L isomers. Dexmedetomidine is a pure preparation of the R-isomer and produces physiologic and analgesic effects similar to medetomidine at approximately half the dose. Dexmedetomidine is indicated for sedation of initially intubated and mechanically ventilated or non-intubated patients during treatment in an intensive care setting, prior to and/or during surgical and other procedures. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-2 Receptor Agonists (Code: D058647) Adrenergic alpha-Agonists (Code: D000316) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1999-12-17 FDA
Click to view thiabendazole Methionine aminopeptidase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P50579, gene: METAP2, swissprot: MAP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621724) Methionine aminopeptidase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P53582, gene: METAP1, swissprot: MAP11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621724) Methionine aminopeptidase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AE18, gene: map, swissprot: MAP1_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621724) Thiabendazole is a 2-substituted benzimidazole. The precise mode of action of thiabendazole on the parasite is unknown, but it may inhibit the helminth specific enzyme fumarate reductase. Thiabendazole is vermicidal andr vermifugal against Ascaris lumbricoides, Strongyloides stercoralis, Necator americanus, and Ancylostoma duodenale, Trichuris trichiura, Ancylostoma braziliense, Toxocara canis and Toxocara cati, and Enterobius vermicularis. Its effect on larvae of Trichinella spiralis that have migrated to muscle is questionable. Thiabendazole also suppresses egg and/or larval production and may inhibit the subsequent development of those eggs or larvae which are passed in the feces. Thiabendazole is indicated for the treatment of Strongyloidiasis (threadworm), Cutaneous larva migrans (creeping eruption), Visceral larva migrans, trichinosis. Thiabendazole is usually inappropriate as first line therapy for enterobiasis (pinworm). antifungal agrochemical (Code: CHEBI:86328) antinematodal drug (Code: CHEBI:35444) Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antihelminthic (Code: N0000175481) 1967-04-07 FDA TMG
Click to view indanazoline Indanazoline is an imidazoline related to naphazoline. It is sympathomimetic with vasoconstrictir properties. Indanazoline stimulates the alpha 1-adrenergic receptors. It causes vasoconstriction, reduces swelling of the nasal mucosa and nasopharynx, nasal breathing easier by reducing the blood flow to the venous sinuses. It is formerly used as a nasal decongestant.
Click to view spizofurone Spizofurone is a spirobenzofuranone derivative. In preclinical models Spizofurone dose-dependently increase in gastric mucosal blood flow. It was studied as the anti-ulcer agent.
Click to view carbromal Carbromal is a brominated monoureide. Carbromal is a mild hypnotic. Carbromal is structurally similar to bromisoval. Carbromal is in a list of drugs capable of causing purpura. Now carbromal is used in combination with aminophenazone as analgesic and anti-inflammatory. 1994-02-04 Hungary National Institute of Pharmacy and Nutrition
Click to view amezinium metilsulfate Amine oxidase [flavin-containing] A (Organism: Canis lupus familiaris, class: Enzyme, accessions: P58027, gene: MAOA, swissprot: AOFA_CANLF) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/6873182) Amine oxidase [flavin-containing] B (Organism: Canis lupus familiaris, class: Enzyme, accessions: Q7YRB7, gene: MAOB, swissprot: AOFB_CANLF) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/6873182) Amezinium metilsulfate is a sympathomimetic agent. Amezinium metilsulfate inhibited monoamine oxidase activity. Amezinium metilsulfate antagonized the response to tyramine and blocked neuronal uptake of noradrenaline. It is used for in the treatment of hypotensive states: essential hypotension, orthostatic hypotension, blood pressure decrease during dialysis. Autonomic Agents (Code: D001337) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1999-07-01 PMDA
Click to view acetylcarnitine Solute carrier family 22 member 5 (Organism: Mus musculus, class: Transporter, accessions: Q9Z0E8, gene: Slc22a5, swissprot: S22A5_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17965255) Solute carrier family 22 member 21 (Organism: Mus musculus, class: Transporter, accessions: Q9WTN6, gene: Slc22a21, swissprot: S22AL_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17965255) Acetylcarnitine, a compound, naturally produced by the body, is necessary for fatty-acid metabolism and energy production. The mechanisms of action of acetylcarnitine have not been fully elucidated, but it seems that the main role of acetylcarnitine is to donate an acetyl group during fatty acid metabolism to help transport fatty acids, such as acetyl CoA, into the mitochondrial matrix where fatty acid metabolism occurs. It is often taken as a dietary supplement. Also it is used for the treatment of diabetic neuropathy in some countries. Central Nervous System Agents (Code: D002491) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Nootropic Agents (Code: D018697) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) 1984-06-01 Italian Medicines Agency (AIFA)
Click to view chloramphenicol palmitate 2014 China Food and Drug Administration (CFDA)
Click to view methsuximide N-desmethylmethsuximide: Voltage-gated T-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: O43497|O95180|Q9P0X4, gene: CACNA1G|CACNA1H|CACNA1I, swissprot: CAC1G_HUMAN|CAC1H_HUMAN|CAC1I_HUMAN) blocker (Source: https://pubmed.ncbi.nlm.nih.gov/11641441/) Methsuximide is a succinimide with anticonvulsant properties. Although the exact mechanism of action of methsuximide is unclear, it is thought to increase the seizure threshold and suppress the paroxysmal three-cycle-per-second spike-and-wave pattern seen with absence (petit mal) seizures. The frequency of attacks is reduced by depression of nerve transmission in the motor cortex and elevation of the threshold of the CNS to convulsive stimuli, probably due to direct modification of membrane function in excitable cells and/or alteration of chemically mediated neurotransmission. Methsuximide is indicated for the control of absence (petit mal) seizures that are refractory to other drugs. Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1957-02-08 FDA
Click to view crotamiton antiscabies, antipruritic drug; active ingredient in Eurax Cream & Lotion (Geigy); request from searcher 3/76; structure scabicide (Code: CHEBI:73333) antipruritic drug (Code: CHEBI:59683) Pesticides (Code: D010575) 1949-07-06 FDA
Click to view tretamine Triethylenemelamine is a trisaziridine alkylating agent with antineoplastic and carcinogenic properties. Used to induce cancer in experimental animal models, triethylenemelamine ethylates DNA, resulting in inhibition of DNA replication, unscheduled DNA synthesis, chromosomal aberrations, and sister chromatid exchanges. This agent also exhibits reproductive toxicities. insect sterilant (Code: CHEBI:67105) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676)
Click to view levamisole Alkaline phosphatase, tissue-nonspecific isozyme (Organism: Homo sapiens, class: Enzyme, accessions: P05186, gene: ALPL, swissprot: PPBT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15476587) Intestinal-type alkaline phosphatase (Organism: Bos taurus, class: Unclassified, accessions: P19111, gene: ALPI, swissprot: PPBI_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25865133) Alkaline phosphatase, tissue-nonspecific isozyme (Organism: Bos taurus, class: Unclassified, accessions: P09487, gene: ALPL, swissprot: PPBT_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25865133) Acetylcholine receptor subunit alpha-type unc-63 (Organism: Caenorhabditis elegans, class: Ion channel, accessions: Q9N587, gene: unc-63, swissprot: ACH6_CAEEL) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17314321) An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6) antinematodal drug (Code: CHEBI:35444) antirheumatic drug (Code: CHEBI:35842) immunomodulator (Code: CHEBI:50846) immunological adjuvant (Code: CHEBI:50847) Adjuvants, Immunologic (Code: D000276) Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Antirheumatic Agents (Code: D018501) Immunologic Factors (Code: D007155) 1990-06-18 FDA
Click to view ethambutol Probable arabinosyltransferase B (Organism: Mycobacterium tuberculosis (strain CDC 1551 / Oshkosh), class: Enzyme, accessions: P9WNL6, gene: embB, swissprot: EMBB_MYCTO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19596878) Probable arabinosyltransferase C (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WNL5, gene: embC, swissprot: EMBC_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19596878) Probable arabinosyltransferase A (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WNL9, gene: embA, swissprot: EMBA_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19596878) Ethambutol is an oral chemotherapeutic agent which is specifically effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Ethambutol inhibits the transfer of mycolic acids into the cell wall of the tubercle bacillus. It may also inhibit the synthesis of spermidine in mycobacteria. The action is usually bactericidal, and the drug can penetrate human cell membranes to exert its lethal effect. (From Smith and Reynard, Textbook of Pharmacology, 1992, p863) antitubercular agent (Code: CHEBI:33231) Antimycobacterial (Code: N0000175483) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antitubercular Agents (Code: D000995) 1967-11-06 FDA 95E
Click to view guanoxan was MH 1976-92 (see under GUANIDINES 1976-90); use GUANIDINES to search GUANOXAN 1976-92; antihypertensive agent similar in its mechanism of action to guanethidine; may cause liver damage 2015 China Food and Drug Administration (CFDA)
Click to view etifelmine Etifelmine is a diphenylmethylenebutylamine derivative. It is a sympathomimetic and a central nervous system stimulant. It was used for the treatment of hypotensive circulatory disorders.
Click to view telmesteine Telmesteine is an organonitrogen compound. elmesteine. Telmesteine decreases LPS-induced NO production. Also telmeteine can inhibit activation of nuclear factor kappa-kB (NF-kB) by blocking phosphoinositide 3-kinase/protein kinase B (PI3K/Akt)/IkB kinase (IKK) activities. Telmesteine is used as mucolytic for the treatment of respiratory tract disorders and is an active ingredient in topical compositions for dermatitis. Italian Medicines Agency (AIFA)
Click to view dexpanthenol Panthenol is an alcohol derivative of pantothenic acid, a component of the B complex vitamins and an essential component of a normally functioning epithelium. Only D-panthenol (dexpanthenol) is biologically active, however both forms have moisturizing properties. Dexpanthenol, the active form of panthenol, is enzymatically cleaved to form pantothenic acid (Vitamin B5), which is an essential component of Coenzyme A that acts as a cofactor in many enzymatic reactions that are important for protein metabolism in the epithelium. Dermatological effects of the topical use of dexpanthenol include increased fibroblast proliferation and accelerated re-epithelialization in wound healing. Furthermore, it acts as a topical protectant, moisturizer, and has demonstrated anti-inflammatory properties. cholinergic drug (Code: CHEBI:38323) 1947-07-08 FDA MV2
Click to view trapidil A coronary vasodilator agent. Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Phosphodiesterase Inhibitors (Code: D010726) Platelet Aggregation Inhibitors (Code: D010975) Vasodilator Agents (Code: D014665)
Click to view phenformin Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12240953) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12240953) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12502361) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24307270) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24307270) Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/20188727) Sulfonylurea receptor 2, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: O60706|Q14654, gene: ABCC9|KCNJ11, swissprot: ABCC9_HUMAN|KCJ11_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/20188727) Solute carrier family 22 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9R0W2, gene: Slc22a2, swissprot: S22A2_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130709) Phenformin is a biguanide hypoglycemic agent with actions and uses similar to those of metformin. It is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal. Phenformin is used in combination with chlorpropamide for the treatment of diabetes mellitus type 2. antineoplastic agent (Code: CHEBI:35610) Hypoglycemic Agents (Code: D007004) 1962-03-24 Italian Medicines Agency (AIFA) 8CV
Click to view pheneturide product of ring hydrolysis of phenobarbital; structure; RN given refers to parent cpd without isomeric designation Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491)
Click to view diethylpropion Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: ) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: ) A appetite depressant considered to produce less central nervous system disturbance than most drugs in this therapeutic category. It is also considered to be among the safest for patients with hypertension. (From AMA Drug Evaluations Annual, 1994, p2290) appetite depressant (Code: CHEBI:50507) Anti-Obesity Agents (Code: D019440) Appetite Depressants (Code: D001067) Central Nervous System Agents (Code: D002491) Appetite Suppression (Code: N0000175372) Increased Sympathetic Activity (Code: N0000175651) Sympathomimetic Amine Anorectic (Code: N0000175423) 1959-08-06 FDA
Click to view tosylchloramide sodium Cytochrome P450 2E1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P05182, gene: Cyp2e1, swissprot: CP2E1_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/28499825) Cytochrome P450 1A1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P00185, gene: Cyp1a1, swissprot: CP1A1_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/28499825) Cytochrome P450 1A2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P04799, gene: Cyp1a2, swissprot: CP1A2_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/28499825) Cytochrome P450 1B1 (Organism: Rattus norvegicus, class: Enzyme, accessions: Q64678, gene: Cyp1b1, swissprot: CP1B1_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/28499825) Cytochrome P450 2B1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P00176, gene: Cyp2b1, swissprot: CP2B1_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/28499825) Cytochrome P450 4A2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P20816, gene: Cyp4a2, swissprot: CP4A2_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/28499825) Tosylchloramide sodium (Chloramine-T) is an organic sodium salt derivative of toluene-4-sulfonamide with a chloro substituent in place of an amino hydrogen. Tosylchloramide sodium is used for disinfection in saunas, solariums, gyms, sport centres, kitchens, sanitary facilities, and air conditioning units. As an anti-microbial agent, tosylchloramide sodium it has had widespread use in a broad range of practices, including medical, dental, verterinary food processing and agricultural. It also has been used in direct contact with tissues because it has a low degree of cytotoxicity. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Disinfectants (Code: D004202) Indicators and Reagents (Code: D007202) Noxae (Code: D009676) Oxidants (Code: D016877) 1957 Italian Medicines Agency (AIFA)
Click to view etidronic acid Etidronic acid is a diphosphonate which affects calcium metabolism. Although the mechanism of action of non-nitrogenous bisphosphonates has not been fully elucidated, available data suggest that etidronic acid can inhibit the formation, growth, and dissolution of hydroxyapatite crystals and their amorphous precursors by chemisorption to calcium phosphate surfaces. Inhibition of crystal resorption occurs at lower doses than are required to inhibit crystal growth. Etidronic acid is indicated for the treatment of symptomatic Paget’s disease of bone and in the prevention and treatment of heterotopic ossification following total hip replacement or due to spinal cord injury. antineoplastic agent (Code: CHEBI:35610) bone density conservation agent (Code: CHEBI:50646) Bisphosphonate (Code: N0000175579) Diphosphonates (Code: N0000007707) Bone Density Conservation Agents (Code: D050071) 1977-09-01 FDA 911
Click to view caroxazone Caroxazone is a psychotropic agent with antidepressant activity. Caroxazone is a reversible MAO-inhibitor. It was used for the treatment of depression. It has been withdrawn from the market. 1975 Italian Medicines Agency (AIFA)
Click to view ciclopirox trivalent metal (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21022s004lbl.pdf) Ciclopirox is a hydroxypyridone antifungal agent that acts by chelation of polyvalent cations (Fe3+ or Al3+), resulting in the inhibition of the metal-dependent enzymes that are responsible for the degradation of peroxides within the fungal cell. Ciclopirox is indicated for the topical treatment of the following dermal infections: tinea pedis, tinea cruris, and tinea corporis due to Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis; candidiasis (moniliasis) due to Candida albicans; and tinea (pityriasis) versicolor due to Malassezia furfur. antiseborrheic (Code: CHEBI:59010) Decreased DNA Replication (Code: N0000008577) Decreased Protein Synthesis (Code: N0000008841) Decreased RNA Replication (Code: N0000008853) Protein Synthesis Inhibitors (Code: N0000000150) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 1982-12-30 FDA B4O
Click to view pivhydrazine Pivhydrazine (pivazide) is a member of the hydrazine family with irreversible and non-selective inhibitory activity against monoamine oxidases. In 1960, it was widely used as an antidepressant agent but it is now discontinued.
Click to view pyrantel Pyrantel is an anthelmintic which acts as an agonist of nicotinic receptors of nematodes. Pyrantel exerts its therapeutic effects by depolarizing their muscle membranes. However, pyrantel acts as a weak agonist of mouse AChRs because of reduced channel opening coupled with high-affinity open channel block. Pyrantel is used for the treatment of parasitic worm infections (ascariasis, hookworm infections, enterobiasis (pinworm infection), trichostrongyliasis and trichinellosis). antinematodal drug (Code: CHEBI:35444) Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Depolarizing Agents (Code: D009467) Peripheral Nervous System Agents (Code: D018373) 1970-05-01 CDSCO (INDIA)
Click to view miglitol Lysosomal alpha-glucosidase (Organism: Homo sapiens, class: Enzyme, accessions: P10253, gene: GAA, swissprot: LYAG_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020682s010lbl.pdf) Lactase-phlorizin hydrolase (Organism: Homo sapiens, class: Enzyme, accessions: P09848, gene: LCT, swissprot: LPH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020682s010lbl.pdf) Glucosylceramidase (Organism: Homo sapiens, class: Enzyme, accessions: P04062, gene: GBA, swissprot: GLCM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20000679) Non-lysosomal glucosylceramidase (Organism: Homo sapiens, class: Enzyme, accessions: Q9HCG7, gene: GBA2, swissprot: GBA2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20000679) Maltase-glucoamylase, intestinal (Organism: Homo sapiens, class: Enzyme, accessions: O43451, gene: MGAM, swissprot: MGA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21669536) Sucrase-isomaltase, intestinal (Organism: Homo sapiens, class: Enzyme, accessions: P14410, gene: SI, swissprot: SUIS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21669536) Miglitol is a desoxynojirimycin derivative that delays the digestion of ingested carbohydrates, thereby resulting in a smaller rise in blood glucose concentration following meals. As a consequence of plasma glucose reduction, miglitol reduce levels of glycosylated hemoglobin in patients with Type II (non-insulin-dependent) diabetes mellitus. alpha Glucosidase Inhibitors (Code: N0000000166) alpha-Glucosidase Inhibitor (Code: N0000175559) Enzyme Inhibitors (Code: D004791) Glycoside Hydrolase Inhibitors (Code: D065089) Hypoglycemic Agents (Code: D007004) 1996-12-18 FDA MIG
Click to view minoxidil Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/9008235) Sulfonylurea receptor 2, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: O60706|Q14654, gene: ABCC9|KCNJ11, swissprot: ABCC9_HUMAN|KCJ11_HUMAN) opener (Source: https://www.ncbi.nlm.nih.gov/pubmed/11886528) Minoxidil is a potent direct-acting peripheral vasodilator that is used largely for patients with severe and refractory hypertension not responding to conventional therapies. Minoxidil is also used topically to treat male pattern baldness. vasodilator agent (Code: CHEBI:35620) antihypertensive agent (Code: CHEBI:35674) Arteriolar Vasodilation (Code: N0000175379) Arteriolar Vasodilator (Code: N0000175564) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1979-10-18 FDA MXD
Click to view thurfyl nicotinate Thurfyl nicotinate is a member of pyridines and an aromatic carboxylic acid. It was investigated as a local antirheumatic agent but was withdrawn because of erythema induced by this agent.
Click to view toloxatone Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24115740) Toloxatone is an antidepressant. It is a selective reversible inhibitor of MAO-A. It was used for the treatment of major depressive disorder. It is no longer available. Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) 1977-09-13 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view guabenxan combination of bemetizid diuretic & guabenxan antihypertensive agent
Click to view butacetin Butacetin is an anilide derivative with potent analgesic and antipyretic activity.
Click to view meobentine Meobentine is an antiarrhythmic agent. Meobentine may prevent induction of ventricular tachycardia or fibrillation, or reduce frequency of complex ventricular ectopy.
Click to view orciprenaline Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://pdf.hres.ca/dpd_pm/00024794.PDF) Orciprenaline is a bronchodilating agent. Orciprenaline is a beta-2 adrenergic agonist. Following oral administration, the effect is usually noted within 30 minutes. Orciprenaline is used for the treatment of bronchial asthma, chronic bronchitis, pulmonary emphysema. Orciprenaline is also useful in sarcoidosis, silicosis, carcinoma of the lung and tuberculosis when bronchospasm contributes to the disability. bronchodilator agent (Code: CHEBI:35523) beta-adrenergic agonist (Code: CHEBI:35522) anti-asthmatic drug (Code: CHEBI:49167) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Reproductive Control Agents (Code: D012102) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Tocolytic Agents (Code: D015149) Adrenergic beta2-Agonists (Code: N0000009922) beta2-Adrenergic Agonist (Code: N0000175779) 1973-07-31 FDA
Click to view allobarbital Allobarbital (diallylbarbituric acid) is an intermediate barbiturate. It was used as a sedative in combination with acetaminophen in patients experiencing pain and discomfort . It was withdrawm from the market.
Click to view pilocarpine Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18824613) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18824613) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18824613) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18824613) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18824613) Pilocarpine is a natural alkaloid extracted from plants of the genus Pilocarpus with cholinergic agonist activity. As a cholinergic parasympathomimetic agent, pilocarpine predominantly binds to muscarinic receptors, thereby inducing exocrine gland secretion and stimulating smooth muscle in the bronchi, urinary tract, biliary tract, and intestinal tract. Pilocarpine is used as a miotic and in the treatment of glaucoma. antiglaucoma drug (Code: CHEBI:39456) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Miotics (Code: D008916) Muscarinic Agonists (Code: D018721) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Cholinergic Muscarinic Agonists (Code: N0000000104) Cholinergic Receptor Agonist (Code: N0000175884) 1974-07-29 FDA 9PL
Click to view chlormidazole Chlormidazole is the first azole introduced the treatment of topical mycosis. It demonstrated inhibitory activity against many fungi and some gram-positive cocci. It was used for the treatment of fungal and bacterial infections of nails and skin, including interdigital and periungual mycoses. 1984-06-15 The Office for Registration of Medicinal Products, Medical Devices and Biocidal Products (Poland)
Click to view bendazol Bendazol is a spasmolytic myotropic agent, has antispasmodic effect on all smooth muscle organs, dilates blood vessels. Bendazol is used for spasms of smooth muscles of internal organs (peptic ulcer, spasms of the gatekeeper and intestines), hypertensive crises and advanced arterial hypertension. 1964-04-30 Ministry of Health of the Russian Federation
Click to view oxyfenamate Oxyfenamate (hydroxyphenamate) is an open-ring analogue of phenobarbital. Oxyfenamate was used as an adjunct in the treatment of anxiety, tension, and musculoskeletal disorders. 1961 YEAR INTRODUCED
Click to view isoprenaline Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19362005) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19362005) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19362005) Isoprenaline is a non-selective beta-adrenoreceptor agonist that is the isopropylaminomethyl analog of epinephrine. Isoprenaline's effects on the cardiovascular system (non-selective) relate to its actions on cardiac beta-1 receptors and beta-2 receptors on smooth muscle within the tunica media of arterioles. Isoprenaline has positive inotropic and chronotropic effects on the heart. Isoproterenol is a racemic compound. L-isoprenaline (levisoprenaline) is an optically active isomer. Isoproterenol is indicated for mild or transient episodes of heart block that do not require electric shock or pacemaker therapy, for serious episodes of heart block and Adams-Stokes attacks, for use in cardiac arrest until electric shock or pacemaker therapy, for bronchospasm occurring during anesthesia, as an adjunct to fluid and electrolyte replacement therapy and the use of other drugs and procedures in the treatment of hypovolemic and septic shock, low cardiac output (hypoperfusion) states, congestive heart failure, and cardiogenic shock. beta-adrenergic agonist (Code: CHEBI:35522) bronchodilator agent (Code: CHEBI:35523) cardiotonic drug (Code: CHEBI:38147) sympathomimetic agent (Code: CHEBI:35524) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) 1956-03-09 FDA 5FW
Click to view proflavine Topical antiseptic used mainly in wound dressings. antiseptic drug (Code: CHEBI:48218) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) FDA PRL
Click to view fepradinol Fepradinol is a non-steroidal anti-inflammatory agent. It was used for the topical treatment of pain due to osteoarthritis, bursitis, etc. Topical application of fepradinol caused allergic contact dermatitis. It is no longer available. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1988-11-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view bamethan Bamethan is an adrenaline derivativ. Bamethan produces vasodilatation through adrenergic beta-receptor activation. Bamethan was used in the treatment of certain peripheral vascular and circulatory disturbances. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view talipexole D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10455328) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10455328) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10455328) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Talipexole is an an azepine derivative and a D2 receptor agonist with no D1 receptor activity. Also talipexole has aplha2-adrenoceptor agonist activity. It is used for the treatment of Parkinson's disease. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) 1996-04-16 PMDA
Click to view tolonidine Tolonidine (2-(2-chloro-p-toluidino)-2-imidazoline-nitrate) is an antihypertensive agent structurally related to clonidine. It was used as a tolonidine nitrate for the treatment of hypertension. It is no longer available. 1986-12-01 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view milrinone cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Organism: Homo sapiens, class: Enzyme, accessions: Q14432, gene: PDE3A, swissprot: PDE3A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12181427) cGMP-inhibited 3',5'-cyclic phosphodiesterase B (Organism: Homo sapiens, class: Enzyme, accessions: Q13370, gene: PDE3B, swissprot: PDE3B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10644042) Milrinone is a member of a new class of bipyridine inotropic/vasodilator agents with phosphodiesterase inhibitor activity, distinct from digitalis glycosides or catecholamines. Milrinone is a selective inhibitor of peak III cAMP phosphodiesterase isozyme in cardiac and vascular muscle. This inhibitory action is consistent with cAMP mediated increases in intracellular ionized calcium and contractile force in cardiac muscle, as well as with cAMP dependent contractile protein phosphorylation and relaxation in vascular muscle. Milrinone is indicated for the short-term intravenous treatment of patients with acute decompensated heart failure. platelet aggregation inhibitor (Code: CHEBI:50427) vasodilator agent (Code: CHEBI:35620) cardiotonic drug (Code: CHEBI:38147) Phosphodiesterase 3 Inhibitor (Code: N0000175598) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Phosphodiesterase 3 Inhibitors (Code: D058987) Phosphodiesterase Inhibitors (Code: D010726) Platelet Aggregation Inhibitors (Code: D010975) Protective Agents (Code: D020011) Vasodilator Agents (Code: D014665) 1987-12-31 FDA MIL
Click to view phanquinone Phanquinone is an orthoquinone. Phanquinone is an anti-mycotic drug with anti-protozoal activity. It is active against a wide range of Gram-positive and Gram-negative organisms. It partically inhibited oxygen consumption by Escherichia coli and Staphylococcus aureus. Phanquinone was used for the treatment of amoebiasis and other protozoal diseases.
Click to view aprobarbital Aprobarbital is a barbiturate derivative. Aprobarbital have been used for the short-term treatment of insomnia and for routine sedation to relieve anxiety, tension, and apprehension however, barbiturates generally have been replaced by benzodiazepines. Aprobarbital was never as widely used as more common barbiturate derivatives such as phenobarbital and is now rarely prescribed.
Click to view naphazoline Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9605427) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9605427) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9605427) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11597419) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11597419) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11597419) Nischarin (Organism: Homo sapiens, class: Cytosolic other, accessions: Q9Y2I1, gene: NISCH, swissprot: NISCH_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18621536) Trace amine-associated receptor 4 (Organism: Mus musculus, class: GPCR, accessions: Q5QD15, gene: Taar4, swissprot: TAAR4_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20559446) Naphazoline is an imidazole derivative with vasoconstrictive activity. Upon ocular administration, naphazoline exerts its effect by acting on alpha-adrenergic receptors in the arterioles of the conjunctiva to produce vasoconstriction, resulting in decreased conjunctival congestion and diminished itching, irritation and redness. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Cardiovascular Agents (Code: D002317) Nasal Decongestants (Code: D014663) Neurotransmitter Agents (Code: D018377) Respiratory System Agents (Code: D019141) Vasoconstrictor Agents (Code: D014662) 1971-06-07 FDA
Click to view xenbucin Xenbucin is a non-steroidal analgesic drug and antihypercholesterolemic. It has anti-inflammatory properties.
Click to view altretamine Altretamine is an alkylating agent, formerly known as hexamethylmelamine. The precise mechanism by which altretamine exerts its cytotoxic effect is unknown, although a number of theoretical possibilities have been studied. Structurally, altretamine resembles the alkylating agent triethylenemelamine, yet in vitro tests for alkylating activity of altretamine and its metabolites have been negative. Altretamine has been demonstrated to be efficacious for certain ovarian tumors resistant to classical alkylating agents. Metabolism of altretamine is a requirement for cytotoxicity. Synthetic monohydroxymethylmelamines, and products of altretamine metabolism, in vitro and in vivo, can form covalent adducts with tissue macromolecules including DNA, but the relevance of these reactions to antitumor activity is unknown. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) 1990-12-26 FDA
Click to view phosphocreatine Creatine kinase B-type (Organism: Homo sapiens, class: Kinase, accessions: P12277, gene: CKB, swissprot: KCRB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/1731757) Creatine kinase U-type, mitochondrial (Organism: Homo sapiens, class: Kinase, accessions: P12532, gene: CKMT1A, swissprot: KCRU_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/1731757) Creatine kinase M-type (Organism: Homo sapiens, class: Kinase, accessions: P06732, gene: CKM, swissprot: KCRM_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/1731757) Creatine kinase S-type, mitochondrial (Organism: Homo sapiens, class: Kinase, accessions: P17540, gene: CKMT2, swissprot: KCRS_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/1731757) Phosphocreatine - or creatine phosphate - is the phosphorylated form of creatine. It is primarily found endogenously in the skeletal muscles of vertebrates where it serves a critical role as a rapidly acting energy buffer for muscle cell actions like contractions via its ability to regenerate adenosine triphosphate (ATP) from adenosine diphosphate (ADP). Phosphocreatine undergoes irreversible cyclization and dehydration to form creatinine at a fractional rate of 0. 026 per day, thus forming approximately 2 g creatinine/day in an adult male. This is the amount of creatine that must be provided either from dietary sources or by endogenous synthesis to maintain the body pool of (creatine and) phosphocreatine. Phosphocreatine is used for involve conditions caused by energy shortage or by increased energy requirements - such as in ischemic stroke and other cerebrovascular diseases. Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Protective Agents (Code: D020011) 1965-04-05 Italian Medicines Agency (AIFA)
Click to view nicorandil ATP-binding cassette sub-family C member 9 (Organism: Homo sapiens, class: Ion channel, accessions: O60706, gene: ABCC9, swissprot: ABCC9_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12770942) Sodium/calcium exchanger 1 (Organism: Canis lupus familiaris, class: Ion channel, accessions: P23685, gene: SLC8A1, swissprot: NAC1_CANLF) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/26631169) Nicorandil is a niacinamide derivative, a plasma membrane adenosine triphosphate (ATP)-sensitive potassium (K+) (KATP) channel activator and a nitric oxide (NO) donor, with vasodilatory, antihypertensive and potential cardio- and lung-protective activities. Nicorandil is indicated in adults for the symptomatic treatment of patients with stable angina pectoris who are inadequately controlled or have a contraindication or intolerance to first-line antianginal therapies. vasodilator agent (Code: CHEBI:35620) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) Vasodilator Agents (Code: D014665) Vitamin B Complex (Code: D014803) 1992-08-12 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view methyldopa Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10052994) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14557373) An alpha-2 adrenergic agonist that has both central and peripheral nervous system effects. Its primary clinical use is as an antihypertensive agent. sympatholytic agent (Code: CHEBI:66991) antihypertensive agent (Code: CHEBI:35674) alpha-adrenergic agonist (Code: CHEBI:35569) peripheral nervous system drug (Code: CHEBI:49110) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-2 Receptor Agonists (Code: D058647) Adrenergic alpha-Agonists (Code: D000316) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1962-12-20 FDA
Click to view melevodopa Melevodopa is the methyl ester of levodopa. Melevodopa is a prodrug of levodopa. After oral administration melevodopa is hydrolyzed by intestinal esterases. Melevodopa is used alone or in combination with decarboxylase inhibitors for the treatment of Parkinson’s disease. (See: levodopa) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) 1999-07-02 Italian Medicines Agency (AIFA)
Click to view zalcitabine dideoxycytidine 5'-triphosphate: Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s16lbl.pdf) DNA polymerase subunit gamma-1 (Organism: Homo sapiens, class: Enzyme, accessions: P54098, gene: POLG, swissprot: DPOG1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s16lbl.pdf) DNA polymerase beta (Organism: Homo sapiens, class: Enzyme, accessions: P06746, gene: POLB, swissprot: DPOLB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/20199s16lbl.pdf) zalcitabine: Solute carrier family 22 member 7 (Organism: Mus musculus, class: Transporter, accessions: Q91WU2, gene: Slc22a7, swissprot: S22A7_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11504818) Equilibrative nucleoside transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q99808, gene: SLC29A1, swissprot: S29A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11463208) Zalcitabine is a synthetic nucleoside analogue of the naturally occurring nucleoside deoxycytidine, in which the 3'-hydroxyl group is replaced by hydrogen. Within cells, zalcitabine is converted to the active metabolite, dideoxycytidine 5'-triphosphate (ddCTP), by the sequential action of cellular enzymes. Dideoxycytidine 5'-triphosphate inhibits the activity of the HIV-reverse transcriptase both by competing for utilization of the natural substrate, deoxycytidine 5'-triphosphate (dCTP), and by its incorporation into viral DNA. The lack of a 3'- OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation and, therefore, the viral DNA growth is terminated. The active metabolite, ddCTP, is also an inhibitor of cellular DNA polymerasebeta and mitochondrial DNA polymerase-gamma and has been reported to be incorporated into the DNA of cells in culture. Zalcitabine was used in combination with antiretroviral agents for the treatment of HIV infection. Zalcitabine was discontinued on December 31, 2006 due to the availability of newer HIV medicines. antiviral drug (Code: CHEBI:36044) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antimetabolites (Code: D000963) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Noxae (Code: D009676) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 1992-06-19 FDA DCT
Click to view methoxamine Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10433504) Methoxamine is a potent sympathomimetic amine that increases both systolic and diastolic blood pressure. Methoxamine acts through peripheral vasoconstriction by acting as a pure alpha-1 adrenergic receptor agonist, consequently increasing systemic blood pressure (both systolic and diastolic). Methoxamine is indicated for prevention and treatment of the acute hypotensive state occurring with spinal anesthesia. It is also indicated as adjunctive treatment of hypotension due to hemorrhage, reactions to medications, surgical complications, and shock associated with brain damage due to trauma or tumor. antihypotensive agent (Code: CHEBI:137431) alpha-adrenergic agonist (Code: CHEBI:35569) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-1 Receptor Agonists (Code: D058646) Adrenergic alpha-Agonists (Code: D000316) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1950-12-31 Health Canada
Click to view dioxethedrin Dioxethedrin is the ephedrine derivative. It is the beta-adrenergic agonist. Dioxethedrin was used as a bronchodilator and sympathomimetic agent.
Click to view varenicline Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P17787|P43681, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021928s048lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021928s048lbl.pdf) Acetylcholine receptor; alpha1/beta1/delta/gamma (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P07510|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND|CHRNG, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN|ACHG_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021928s048lbl.pdf) Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Rattus norvegicus, class: Ion channel, accessions: P04757|P12392, gene: Chrna3|Chrnb4, swissprot: ACHA3_RAT|ACHB4_RAT) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021928s048lbl.pdf) Neuronal acetylcholine receptor subunit alpha-7 (Organism: Rattus norvegicus, class: Ion channel, accessions: Q05941, gene: Chrna7, swissprot: ACHA7_RAT) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021928s048lbl.pdf) Varenicline is a partial nicotinic agonist selective for ?4?2 nicotinic acetylcholine receptor subtypes. Electrophysiology studies in vitro and neurochemical studies in vivo have shown that varenicline binds to ?4?2 neuronal nicotinic acetylcholine receptors and stimulates receptor-mediated activity, but at a significantly lower level than nicotine. Varenicline blocks the ability of nicotine to activate ?4?2 receptors and thus to stimulate the central nervous mesolimbic dopamine system, believed to be the neuronal mechanism underlying reinforcement and reward experienced upon smoking. Varenicline is highly selective and binds more potently to ?4?2 receptors than to other common nicotinic receptors (>500-fold ?3?4, >3,500-fold ?7, >20,000-fold ?1???), or to nonnicotinic receptors and transporters (>2,000-fold). Varenicline also binds with moderate affinity (Ki = 350 nM) to the 5-HT3 receptor. Varenicline indicated for use as an aid to smoking cessation treatment. nicotinic acetylcholine receptor agonist (Code: CHEBI:47958) serotonergic agonist (Code: CHEBI:35941) Partial Cholinergic Nicotinic Agonist (Code: N0000175705) Partial Cholinergic Nicotinic Agonists (Code: N0000175702) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Neurotransmitter Agents (Code: D018377) Nicotinic Agonists (Code: D018722) 2006-05-10 FDA QMR
Click to view pramipexole D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020667s036lbl.pdf) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020667s036lbl.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020667s036lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020667s036lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388667) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20496886) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20496886) Pramipexole is a dopamine agonist that binds with high selectivity and specificity to the D2 subfamily of dopamine receptors of which it has a preferential affinity to D3 receptors, and has full intrinsic activity. Pramipexole alleviates parkinsonian motor deficits by stimulation of dopamine receptors in the striatum. Animal studies have shown that pramipexole inhibits dopamine synthesis, release, and turnover. Pramipexole is indicated for the symptomatic treatment of Parkinson’s disease and primary Restless Legs Syndrome (RLS). antiparkinson drug (Code: CHEBI:48407) dopamine agonist (Code: CHEBI:51065) antidyskinesia agent (Code: CHEBI:66956) Nonergot Dopamine Agonist (Code: N0000175768) Anti-Dyskinesia Agents (Code: D018726) Antioxidants (Code: D000975) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1997-07-01 FDA
Click to view chlorthenoxazine Chlorthenoxazine is a benzoxazinone. It has anti-inflammatory, antipyretic, analgesic activities.
Click to view kainic acid Glutamate receptor ionotropic, kainate 1 (Organism: Homo sapiens, class: Ion channel, accessions: P39086, gene: GRIK1, swissprot: GRIK1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10969973) Glutamate receptor ionotropic, kainate 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q13002, gene: GRIK2, swissprot: GRIK2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10969973) Glutamate receptor ionotropic, kainate 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q13003, gene: GRIK3, swissprot: GRIK3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16475972) Glutamate receptor ionotropic, kainate 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q16099, gene: GRIK4, swissprot: GRIK4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16475972) Glutamate receptor ionotropic, kainate 5 (Organism: Rattus norvegicus, class: Ion channel, accessions: Q63273, gene: Grik5, swissprot: GRIK5_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18811139) Kainic acid is a cyclic analog of l-glutamate and a potent agonist for kainate receptors that can lead to status epilepticus in animals. Kainic acid is an ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. antinematodal drug (Code: CHEBI:35444) excitatory amino acid agonist (Code: CHEBI:50103) Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Agonists (Code: D018690) Neurotransmitter Agents (Code: D018377) PMDA KAI
Click to view mefenorex Mefenorex is a anti-obesity drug with little CNS stimulant activity. It was withdrawn due to unfavourable benefit/risk balance. Autonomic Agents (Code: D001337) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1987-06-17 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view zonisamide Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020789s034lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020789s034lbl.pdf) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23965175) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23965175) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23965175) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23965175) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23965175) Amine oxidase [flavin-containing] B (Organism: Mus musculus, class: Enzyme, accessions: Q8BW75, gene: Maob, swissprot: AOFB_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19948168) Zonisamide is an antiseizure drug chemically classified as a sulfonamide and unrelated to other antiseizure agents. The precise mechanism by which zonisamide exerts its antiseizure effect is unknown, although it is believed that the drug blocks sodium and calcium channels, which leads to the suppression of neuronal hypersynchronization (i.e. convulsions). Zonisamide has also been found to potentiate dopaminergic and serotonergic neurotransmission but does not appear to potentiate syanptic activity by GABA (gamma amino butyric acid). Zonisamide binds to sodium channels and voltage sensitive calcium channels, which suppresses neuronal depolarization and hypersynchronization. Zonisamide also inhibits carbonic anhydrase to a weaker extent, but such an effect is not thought to contribute substantially to the drug's anticonvulsant activity. Zonisamide is used for adjunctive treatment of partial seizures in patients with epilepsy. anticonvulsant (Code: CHEBI:35623) central nervous system drug (Code: CHEBI:35470) protective agent (Code: CHEBI:50267) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Sulfonamides (Code: N0000008048) Carbonic Anhydrase Inhibitors (Code: N0000000235) P-Glycoprotein Inhibitors (Code: N0000185503) Anticonvulsants (Code: D000927) Antioxidants (Code: D000975) Central Nervous System Agents (Code: D002491) Protective Agents (Code: D020011) 2000-03-27 FDA ZON
Click to view felbinac Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: http://www.kegg.jp/entry/D01675) an anti-inflammatory/analgesic agent which has been developed into a topical gel for local treatment and pain and inflammation associated with conditions of the musculo-skeletal system non-steroidal anti-inflammatory drug (Code: CHEBI:35475) 2013-07-18 China Food and Drug Administration (CFDA)
Click to view benzyl benzoate Benzyl benzoate is the ester of benzyl alcohol and benzoic acid. It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system. Benzyl benzoate is one of the older preparations used to treat scabies caused by the mite sarcoptes scabiei. Benzyl benzoate exerts toxic effects on the nervous system of the parasite, resulting in its death. It is also toxic to mite ova, though its exact mechanism of action is unknown. scabicide (Code: CHEBI:73333) acaricide (Code: CHEBI:22153) Insecticides (Code: D007306) Pesticides (Code: D010575) 1976-09-02 FDA BZM
Click to view butobarbital Butobarbital should be distinguished from Butabarbital (a synonym for Secbutabarbital) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1969-12-31 New Zealand Medicines and Medical Devices Safety Authority
Click to view secbutabarbital GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator Butabarbital (a synonym for Secbutabarbital) should be distinguished from Butobarbital Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1939-06-05 FDA
Click to view albutoin Albutoin has anticonvulsant activity.
Click to view inaperisone Inaperisone is a pyrrolidinopropiophenone derivative. It was developed as a muscle-relaxant and antispasmodic agent for reducing symptoms of pelvic floor.
Click to view troxacitabine Troxacitabine is a synthetic nucleoside analogue. It is a poor substrate for nucleoside transporters and gains entry into cells by passive diffusion. Troxacitabine is activated by cellular kinases and incorporated into DNA, inhibiting its replication. In contrast to other cytosine nucleoside analogs, troxacitabine is resistant to inactivation by cytidine deaminase. It is the first nucleoside analog with anticancer activity that has an unnatural stereochemical configuration. Troxacitabine is investigated for the treatment in myeloid leukemia. Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antineoplastic Agents (Code: D000970) Antiviral Agents (Code: D000998) LTT
Click to view salicylanilide Salicylanilide is an anilide of salicylic acid with antifungal properties. It is used for the treatment of tinea capitis. 2015-05-28 China Food and Drug Administration (CFDA) SLI
Click to view benzyl nicotinate Benzyl nicotinate is a benzyl ester resulting from the formal condensation of the carboxy group of nicotinic acid with benzyl alcohol. It has been used as a rubefacient. It has a role as a vasodilator agent. It derives from a nicotinic acid. vasodilator agent (Code: CHEBI:35620) 2005-12-16 Ministry of Health of the Russian Federation 0OM
Click to view phenazopyridine Phenazopyridine is a synthetic pyridine derivative anesthetic. Phenazopyridine is indicated for the symptomatic relief of pain, burning, urgency, frequency, and other discomforts arising from irritation of the lower urinary tract mucosa caused by infection. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity.Phenazopyridine is compatible with antibacterial therapy and can help to relieve pain and discomfort during the interval before antibacterial therapy controls the infection. local anaesthetic (Code: CHEBI:36333) non-narcotic analgesic (Code: CHEBI:35481) 1965-04-08 FDA
Click to view ketamine Glutamate receptor ionotropic, NMDA 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q05586, gene: GRIN1, swissprot: NMDZ1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/016812s040lbl.pdf) Glutamate receptor ionotropic, NMDA 2A (Organism: Homo sapiens, class: Ion channel, accessions: Q12879, gene: GRIN2A, swissprot: NMDE1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/016812s040lbl.pdf) Glutamate receptor ionotropic, NMDA 2B (Organism: Homo sapiens, class: Ion channel, accessions: Q13224, gene: GRIN2B, swissprot: NMDE2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/016812s040lbl.pdf) Glutamate receptor ionotropic, NMDA 2C (Organism: Homo sapiens, class: Ion channel, accessions: Q14957, gene: GRIN2C, swissprot: NMDE3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/016812s040lbl.pdf) Glutamate receptor ionotropic, NMDA 2D (Organism: Homo sapiens, class: Ion channel, accessions: O15399, gene: GRIN2D, swissprot: NMDE4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/016812s040lbl.pdf) Glutamate receptor ionotropic, NMDA 3A (Organism: Homo sapiens, class: Ion channel, accessions: Q8TCU5, gene: GRIN3A, swissprot: NMD3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/016812s040lbl.pdf) Glutamate receptor ionotropic, NMDA 3B (Organism: Homo sapiens, class: Ion channel, accessions: O60391, gene: GRIN3B, swissprot: NMD3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/016812s040lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211243lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211243lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211243lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211243lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211243lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211243lbl.pdf) Ketamine is a cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors. Esketamine is the S- (more active) enantiomer of ketamine. Ketamine is used as the sole anesthetic agent for diagnostic and surgical procedures that do not require skeletal muscle relaxation; also, it is indicated for the induction of anesthesia prior to the administration of other general anesthetic agents. Esketamine is used for the treatment of treatment-resistant depression. General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) Analgesics (Code: D000700) Anesthetics (Code: D000777) Anesthetics, Dissociative (Code: D000778) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) intravenous anaesthetic (Code: CHEBI:38877) analgesic (Code: CHEBI:35480) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1970-02-19 FDA RKE
Click to view guanadrel Guanadrel is a postganglionic adrenergic blocking agent. Guanadrel slowly displaces norepinephrine from its storage in nerve endings and thereby blocks the release of norepinephrine normally produced by nerve stimulation. The reduction in neurotransmitter release in response to sympathetic nerve stimulation, as a result of catecholamine depletion, leads to reduced arteriolar vasoconstriction, especially the reflex increase in sympathetic tone that occurs with a change in position. Guanadrel is used to treat and control hypertension. antihypertensive agent (Code: CHEBI:35674) adrenergic antagonist (Code: CHEBI:37887) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) 1982-12-29 FDA
Click to view baclofen GABA-B receptor (Organism: Homo sapiens, class: GPCR, accessions: O75899|Q9UBS5, gene: GABBR1|GABBR2, swissprot: GABR1_HUMAN|GABR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7650684) Baclofen is a gamma-aminobutyric acid (GABA-ergic) agonist. Baclofen inhibits both monosynaptic and polysynaptic reflexes at the spinal level, possibly by decreasing excitatory neurotransmitter release from afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect. Baclofen is indicated for the treatment of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. Baclofen may also be of some value in patients with spinal cord injuries and other spinal cord diseases. muscle relaxant (Code: CHEBI:51371) central nervous system depressant (Code: CHEBI:35488) GABA agonist (Code: CHEBI:51373) GABA A Agonists (Code: N0000000196) GABA B Agonists (Code: N0000000116) gamma-Aminobutyric Acid-ergic Agonist (Code: N0000175759) Central Nervous System Agents (Code: D002491) GABA Agents (Code: D018682) GABA Agonists (Code: D018755) GABA-B Receptor Agonists (Code: D058786) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) 1977-11-22 FDA 2C0
Click to view clorprenaline Clorprenaline is a bronchodilator. Itis used to prevent bronchospasm and relieve acute attacks in bronchitis and bronchial asthma. Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) 1970 PMDA
Click to view chloroxine Arachidonate 5-lipoxygenase (Organism: Mus musculus, class: Enzyme, accessions: P48999, gene: Alox5, swissprot: LOX5_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21739938) Arachidonate 12-lipoxygenase, 12R-type (Organism: Mus musculus, class: Enzyme, accessions: O70582, gene: Alox12b, swissprot: LX12B_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21739938) Arachidonate 15-lipoxygenase (Organism: Mus musculus, class: Enzyme, accessions: P39654, gene: Alox15, swissprot: LOX15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21739938) Botulinum neurotoxin type A (Organism: Clostridium botulinum, class: Enzyme, accessions: P10845, gene: botA, swissprot: BXA1_CLOBO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24387280) Chloroxine (dichloroquinolinol) is an antibacterial drug. Although the mechanism of action is not understood, chloroxine may slow down mitotic activity in the epidermis, thereby reducing excessive scaling associated with dandruff or seborrheic dermatitis of the scalp. Chloroxine induces SOS-DNA repair in E. coli, so chloroxine may be genotoxic to bacteria. Chloroxine is incorporated into shampoos to treat dandruff and seborrheic dermatitis. Also it was used as an antidiarrheal and in the lab as an analytical reagent. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 1976-10-19 FDA
Click to view cinametic acid used in liver function tests; relaxes sphincter of Oddi; regulates hepato-biliary function; structure Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765) 2015 China Food and Drug Administration (CFDA)
Click to view carmustine DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) alkylating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020637s026lbl.pdf) RNA (Organism: None, class: RNA, accessions: None, gene: None, swissprot: None) alkylating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020637s026lbl.pdf) Glutathione reductase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P00390, gene: GSR, swissprot: GSHR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15321730) Carmustine is a parenterally administered alkylating agent used alone and in combination with other antineoplastic agents in the treatment of several forms of cancer including leukemias, lymphomas, and breast, testicular, ovarian, gastric and pancreatic cancer. antineoplastic agent (Code: CHEBI:35610) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) 1977-03-07 FDA
Click to view niridazole Niridazole is a nitro heterocyclic compound with antischistosomal properties. The mode of action of niridazole is not fully understood. The major action of niridazole seems to be on the glycogen metabolism of the helminths. The drug also case structural damage to the reproductive system of female schistosomes. Another possible mechanism of action of niridazole involves the inhibition of DNA synthesis in schistosomes. Niridazole is used for the treatment of schistosomiasis, dracunculiasis and tungiasis, but in some countries it is no longer availabale due to its toxicity. Amebicides (Code: D000563) Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Antiprotozoal Agents (Code: D000981) Schistosomicides (Code: D012556)
Click to view phenyl salicylate Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22197706) Phenyl salicylate is a 2-hydroxybenzoic acid phenyl ester. It is utilized in some manufacturing processes of polymers, lacquers, adhesives, waxes, as well as polishes. It is an active ingredient in some pharmaceutical products as a mild analgesic for pain relief by releasing salicylate. Phenyl salicylate may also be found in some antiseptic agents. 1964-04-30 Ministry of Health of the Russian Federation
Click to view amifostine Alkaline phosphatase, tissue-nonspecific isozyme (Organism: Homo sapiens, class: Enzyme, accessions: P05186, gene: ALPL, swissprot: PPBT_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020221s036lbl.pdf) Amifostine is an organic thiophosphate cytoprotective agent. Amifostine is a prodrug that is dephosphorylated by alkaline phosphatase in tissues to a pharmacologically active free thiol metabolite (2-((3-Aminopropyl)amino)ethanethiol). This metabolite is believed to be responsible for the reduction of the cumulative renal toxicity of cisplatin and for the reduction of the toxic effects of radiation on normal oral tissues. The ability of amifostine to differentially protect normal tissues is attributed to the higher capillary alkaline phosphatase activity, higher pH and better vascularity of normal tissues relative to tumor tissue, which results in a more rapid generation of the active thiol metabolite as well as a higher rate constant for uptake into cells. The higher concentration of the thiol metabolite in normal tissues is available to bind to, and thereby detoxify, reactive metabolites of cisplatin. This thiol metabolite can also scavenge reactive oxygen species generated by exposure to either cisplatin or radiation. Amifostine is indicated to reduce the cumulative renal toxicity associated with repeated administration of cisplatin in patients with advanced ovarian cancer and to reduce the incidence of moderate to severe xerostomia in patients undergoing post-operative radiation treatment for head and neck cancer, where the radiation port includes a substantial portion of the parotid glands. prodrug (Code: CHEBI:50266) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) 1995-12-08 FDA
Click to view salbutamol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020983s032lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) weak inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Salbutamol is a short acting beta2-adrenergic receptor agonist. The pharmacologic effects of salbutamol are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate to cyclic-3',5'- adenosine monophosphate. Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. Salbutamol is a chiral drug with R (levosalbutamol) and S-isomers. The commonly used formulation is a racemic mixture. Levosalbutamol is the therapeutically active isomer and has all the beta 2 agonist activity. Salbutamol is indicated for the symptomatic relief and prevention of bronchospasm due to bronchial asthma, chronic bronchitis, reversible obstructive airway disease, and other chronic bronchopulmonary disorders in which bronchospasm is a complicating factor, and/or the acute prophylaxis against exercise-induced bronchospasm and other stimuli known to induce bronchospasm. Adrenergic beta2-Agonists (Code: N0000009922) beta2-Adrenergic Agonist (Code: N0000175779) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) beta-adrenergic agonist (Code: CHEBI:35522) bronchodilator agent (Code: CHEBI:35523) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Reproductive Control Agents (Code: D012102) Respiratory System Agents (Code: D019141) Tocolytic Agents (Code: D015149) salbutamol: 1981-05-01 FDA levosalbutamol: 1999-03-25 FDA 68H
Click to view sulfacetamide Dihydropteroate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AC13, gene: folP, swissprot: DHPS_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/13873645) Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20350811) Dihydrofolate reductase (Organism: Bos taurus, class: Unclassified, accessions: P00376, gene: DHFR, swissprot: DYR_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20350811) Sulfacetamide is a synthetic sulfanylacetamide derivative with bacteriostatic activity. Sulfacetamide inhibits bacterial folic acid synthesis by competing with para amino benzoic acid. With a broad spectrum of action, it is used as an anti-infective topical agent to treat skin infections and as an oral agent for urinary tract infections. antibacterial drug (Code: CHEBI:36047) antiinfective agent (Code: CHEBI:35441) Sulfonamide Antibacterial (Code: N0000175503) Sulfonamides (Code: N0000008048) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076) 1945-09-12 FDA
Click to view sulfaguanidine Prothrombin (Organism: Homo sapiens, class: Enzyme, accessions: P00734, gene: F2, swissprot: THRB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10794696) Trypsin-1 (Organism: Homo sapiens, class: Enzyme, accessions: P07477, gene: PRSS1, swissprot: TRY1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10794696) Trypsin-2 (Organism: Homo sapiens, class: Enzyme, accessions: P07478, gene: PRSS2, swissprot: TRY2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10794696) Trypsin-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35030, gene: PRSS3, swissprot: TRY3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10794696) Sulfaguanidine is a guanidine derivative of sulfanilamide. Sulfaguanidine blocks the synthesis of dihydrofolic acid by inhibiting the enzyme dihydropteroate synthase in bacteria. Sulfaguanidine also has selective thrombin inhibitory properties. Sulfaguanidine is used to treat the gastrointestinal infections particularly bacillary dysentery. Anti-Infective Agents (Code: D000890) 1964-04-30 Ministry of Health of the Russian Federation
Click to view velnacrine Acetylcholinesterase (Organism: Rattus norvegicus, class: Enzyme, accessions: P37136, gene: Ache, swissprot: ACES_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2385001) Velnacrine (9-amino-1,2,3,4-tetrahydroacridin-1-ol) is an inhibitor of acetylcholinesterase. It was studied for the treatment of Alzheimer's disease however development was discontinued. Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377)
Click to view fenyramidol considered as a drug that possibly causes hepatotoxicity
Click to view clofibric acid Peroxisome proliferator-activated receptor alpha (Organism: Mus musculus, class: Transcription factor, accessions: P23204, gene: Ppara, swissprot: PPARA_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16107150) Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16107150) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16107150) Clofibric acid is a monocarboxylic acid that is an active metabolite of the drug clofibrate. Clofibric acid is an agonist of the PPAR-alpha receptor in muscle, liver, and other tissues. This agonism ultimately leads to modification in gene expression resulting in increased beta-oxidation, decreased triglyceride secretion, increased HDL, and increased lipoprotein lipase activity. Clofibrate was used for the treatment of hyperlipoproteinemias. Clofibrate was discontinued in 2002 due to adverse effects. anticholesteremic drug (Code: CHEBI:35821) antilipemic drug (Code: CHEBI:35679) antineoplastic agent (Code: CHEBI:35610) herbicide (Code: CHEBI:24527) Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) 1967-02-08 FDA
Click to view phenaglycodol Phenaglycodol is a weak inhibitor of monamine oxidase. It was used for the treatment of nervous conditions and tensions including anxiety and depression. It can lead to gynecomastia and urinary steroid excretion. It was withdrawn from the market.
Click to view glutethimide GABA-A receptor alpha-1/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P28472, gene: GABRA1|GABRB3|GABRG2, swissprot: GBRA1_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive modulator A hypnotic and sedative. Its use has been largely superseded by other drugs. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1976-10-28 FDA
Click to view naftazone Naftazone is a naphtoquinone derivative. Naftazone has venoconstrictive properties. Its venotonic mechanism of action remains unknown, but the drug has anti?inflammatory effects and inhibits platelet aggregation. It is used for the treatment of varicose veins and venous insufficiency. Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) 1996-11-14 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view ciclobendazole Ciclobendazole is a benzimidazole derivative. It is used in the treatment of Ascaris and Hookworm infestations.
Click to view kinetin Endochitinase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P29029, gene: CTS1, swissprot: CHIT_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17524989) Kinetin (6-furfuryladenine) is a biologically active natural phytochemical. Kinetin is a cytokinin which are plant hormones promotes cell division and plant growth. It was shown to naturally exist in DNA of organisms including humans and various plants. While kinetin is used in tissue cultures to produce new plants, it is also found in cosmetic products as an anti-aging agents. Growth Substances (Code: D006133) Plant Growth Regulators (Code: D010937) H35
Click to view sulfacarbamide Sulfacaramide is a sulfonamide anti-infective agent. Sulfacaramide has a bacteriostatic effect due to competitive antagonism with para-aminobenzoic acid, preventing its inclusion in dihydrofolic acid, which leads to a violation of the synthesis of tetrahydrofolic acid. Thus, the synthesis of nucleic acids is broken, as a result of which the growth and multiplication of microorganisms are suppressed. It was used for the treatment of bacterial urinary infections. Sulfacaramide are known to cause renal toxicity, erythema multiforma, agranulocytosis, haemolytic and aplastic anemia. Sulfacaramide was withdrawn due to its adverse effects profile.
Click to view 5-aminolevulinic acid hexyl ester 5-aminolevulinic acid hexyl ester is an ester of the heme precursor, aminolevulinic acid. After bladder instillation, 5-aminolevulinic acid hexyl ester enters the bladder mucosa and is proposed to enter the intracellular space of mucosal cells where it is used as a precursor in the formation of the photoactive intermediate protoporphyrin IX (PpIX) and other photoactive porphyrins (PAPs). 5-aminolevulinic acid hexyl ester is indicated for use in the cystoscopic detection of carcinoma of the bladder, including carcinoma in situ (CIS), among patients suspected or known to have lesion(s) on the basis of a prior cystoscopy, or in patients undergoing surveillance cystoscopy for carcinoma of the bladder. 2010-05-28 FDA
Click to view ibuproxam Ibuproxam is a prodrug which metabolizes into ibuprofen and is therefore indicated for the treatment of pain and inflammation. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1978 Italian Medicines Agency (AIFA)
Click to view nadoxolol Nadoxolol is a beta-adrenergic blocking agent. It has antihypertensive properties.
Click to view tramazoline Tramazoline is an ?-adrenergic receptor agonist. Tramazoline is used in nasal decongestant preparations. Autonomic Agents (Code: D001337) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1994-10-31 Italian Medicines Agency (AIFA)
Click to view butoctamide stimulates serotonin release from rat peritoneal mast cells
Click to view fencamfamin Fencamfamin is a stimulant which was developed in the 1960s as an appetite suppressant, but was later withdrawn for this application due to problems with dependence and abuse. Fencamfamine acts as an indirect dopamine agonist. It releases dopamine by a similar mechanism to amphetamines, but is 10x less potent than dexamphetamine at producing this effect. The drug seems to inhibit the dopamine transporter (DAT) that removes dopamine from the synapses. This inhibition of DAT blocks the reuptake of dopamine and norepinephrine into the presynaptic neuron, increasing the amount of dopamine in the synapse. It also stimulates the release of dopamine and norepinephrine into the synapse. Fencamfamin also was used for treating depressive day-time fatigue, lack of concentration and lethargy. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Central Nervous System Stimulants (Code: D000697) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view tiamenidine Tiamenidine is a centrally-acting antihypertensive structurally related to clonidine. It was used for the treatment of mild to moderate hypertension.
Click to view cicletanine a diuretic, developed for the treatment of hypertension Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Natriuretic Agents (Code: D045283) ANSM (French National Agency for Medicines and Health Products Safety)
Click to view bergapten Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/31920428) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/31920428) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/31920428) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/31920428) Oligo-1,6-glucosidase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Unclassified, accessions: P53051, gene: IMA1, swissprot: MALX3_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/29233045) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22155270) Amine oxidase [flavin-containing] B (Organism: Mus musculus, class: Enzyme, accessions: Q8BW75, gene: Maob, swissprot: AOFB_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10403141) Bergapten (5-methoxypsoralen) is a cumarine-derivate compound and presents in many fruits and vegetables. It has shown antitumor effects in a variety of cell types. The key target of bergapten action in breast cancer cells was identified the oncosuppressor gene PTEN (phosphatase tensin homolog deleted from chromosome 10); bergapten by inducing PTEN expression, produces autophagy in breast cancer cells. It is used in combination with psoralen for the treatment of vitiligo,alopecia, fungal mycosis, psoriasis. hepatoprotective agent (Code: CHEBI:62868) Dermatologic Agents (Code: D003879) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) 1993-04-21 Ministry of Health of the Russian Federation
Click to view methoxsalen DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) cross-linking agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/09048slr037_methoxsalen_lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11353760) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23746477) Cytochrome P450 2A13 (Organism: Homo sapiens, class: Enzyme, accessions: Q16696, gene: CYP2A13, swissprot: CP2AD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22696418) Methoxsalen is a furocoumarin referred to collectively as psoralen that have photosensitizing activity and is used orally and topically in conjunction with ultraviolet irradiation for the therapy of psoriasis and vitiligo. dermatologic drug (Code: CHEBI:50177) antineoplastic agent (Code: CHEBI:35610) photosensitizing agent (Code: CHEBI:47868) cross-linking reagent (Code: CHEBI:50684) Cross-Linking Reagents (Code: D003432) Dermatologic Agents (Code: D003879) Indicators and Reagents (Code: D007202) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) Photoabsorption (Code: N0000010217) Photoactivated Radical Generator (Code: N0000175984) Photosensitizing Activity (Code: N0000009801) Psoralen (Code: N0000175879) Psoralens (Code: N0000007909) 1954-12-03 FDA 8MO
Click to view bisorcic -
Click to view arsanilic acid Arsanilic acid is an organoarsenic compound. Its sodium salt was used by injection in the early 20th century as the first organic arsenical drug, but it was soon found prohibitively toxic for human use. Arsanilic acid saw long use as a veterinary feed additive promoting growth and to prevent or treat dysentery in poultry and swine. It causes blindness and is ototoxic and nephrotoxic in animals. ASR
Click to view fosfosal Fosfosal (2-phosphonoxybenzoic acid) is a O-phosphorylated derivative of salicylic acid with analgesic, antipyrelic and anti-inflammatory properties. Fosfosal is used as a nutrition supplement for phosphorus, selenium, magnesium, copper and potassium deficiencies.
Click to view tetrabarbital Tetrabarbital is a barbituric acid derivative. It was used as a central nervous system depressant.
Click to view captopril Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/018343s087lbl.pdf) 72 kDa type IV collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P08253, gene: MMP2, swissprot: MMP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20184869) Matrix metalloproteinase-9 (Organism: Homo sapiens, class: Enzyme, accessions: P14780, gene: MMP9, swissprot: MMP9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501888) Leukotriene A-4 hydrolase (Organism: Homo sapiens, class: Enzyme, accessions: P09960, gene: LTA4H, swissprot: LKHA4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12207002) Succinyl-diaminopimelate desuccinylase (Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd), class: Enzyme, accessions: P44514, gene: dapE, swissprot: DAPE_HAEIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19822427) A potent and specific inhibitor of peptidyl-dipeptidase A. It blocks the conversion of angiotensin i to angiotensin ii, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the renin-angiotensin system and inhibits pressure responses to exogenous angiotensin. It is used in the therapy of hypertension and heart failure. EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor (Code: CHEBI:35457) antihypertensive agent (Code: CHEBI:35674) Angiotensin Converting Enzyme Inhibitor (Code: N0000175562) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 1981-04-06 FDA X8Z
Click to view tinazoline Nasal decongestant- Acute cold vasomotor rhinitis to facilitate rhinoscopy and to aid drainage of secretions in affectious of the paranasal sinuses. 1985-08 CDSCO (INDIA)
Click to view prolintane Prolintane is a sympathomimetic amine with pharmacologic properties similar to d-amphetamine. Prolintane is a mild central stimulant. It acts indirectly as a sympathomimetic. It was used for the treatment of narcolepsy and attention deficit hyperactivity disorder. Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) 1994-11-14 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view salicylsulfuric acid Salicylsulfuric acid is a derivative of salicylic acid. It is said to possess the analgesic and antirheumatic effects of acetylsalicylic acid with fewer side reactions.
Click to view triacetin A triglyceride that is used as an antifungal agent. solvent (Code: CHEBI:46787) adjuvant (Code: CHEBI:60809) antifungal drug (Code: CHEBI:86327) food additive carrier (Code: CHEBI:78059) food emulsifier (Code: CHEBI:63047) food humectant (Code: CHEBI:77969) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Solvents (Code: D012997)
Click to view heptobarbital 72 kDa type IV collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P08253, gene: MMP2, swissprot: MMP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11327602) Matrix metalloproteinase-9 (Organism: Homo sapiens, class: Enzyme, accessions: P14780, gene: MMP9, swissprot: MMP9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11327602) Heptobarbital (phenylmethylbarbituric acid) is a barbiturate derivative. It has anticonvulsant, antispasmodic and sedative action. It was used in epilepsy.
Click to view meprobamate GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47870|P18507, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19244096) Meprobamate is a carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate's mechanism of action is not fully understood; in animal studies, meprobamate is reported to act at multiple sites in the central nervous system, such as the thalamus and limbic system. It binds to the GABAA receptors, leading to inhibitory effects on the neurons transmitting signals in the reticular formation and spinal cord. Meprobamate is used for the management of anxiety disorders or for the short-term relief of the symptoms of anxiety. Anti-Anxiety Agents (Code: D014151) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1955-04-28 FDA
Click to view primidone Primidone is an antiepileptic agent related to the barbiturates. Although the mechanism of action has not been fully elucidated, primidone probably exerts its actions, in a manner similar to phenobarbital, via activation of gamma-aminobutyric acid (GABA)-A receptor/chloride ionophore complex, which leads to prolonged and increased frequency of opening of the chloride channel within the receptor complex. This results in an alteration in the electrical activity of the nerve cell membrane, causing hyperpolarization and prevention of partial and tonic-clonic seizures. In addition, this agent is partially metabolized to phenobarbital and phenylethylmalonamide (PEMA), which may also contribute to its anti-seizure properties. Primidone is indicated for the control of grand mal and psychomotor seizure. anticonvulsant (Code: CHEBI:35623) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1954-03-08 FDA
Click to view mephenytoin Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) agonist (Source: https://pubmed.ncbi.nlm.nih.gov/15039302/) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/10417492/) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/10417492/) Mephenytoin is a heterocyclic organic compound with anticonvulsant property. Although the mechanism of action is not well established, mephenytoin potentially promotes sodium efflux from neurons in motor cortex, and stabilizes the threshold against hyperexcitability caused by excessive stimulation. Thus this agent reduces the membrane sodium gradient and prevents cortical seizure signal spreading. It may cause blood dyscrasias, therefore, this agent was only used after other less toxic anticonvulsants had failed. Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1946-10-23 FDA
Click to view levocarnitine propionate Levocarnitine propionate (Propionyl L-carnitine) is the propionyl ester of L-carnitine. Propionyl-L-carnitine stimulates energy production in ischaemic muscles by increasing citric acid cycle flux and stimulating pyruvate dehydrogenase activity.Levocarnitine propionate improves coagulative fibrinolytic homeostasis in vasal endothelium and positively affects blood viscosity. It exhibits a high affinity for carnitine acyl transferase and as such readily converts into propionyl-CoA and free carnitine. Levocarnitine propionate is indicated for patients with peripheral arterial occlusive disorders and for exercise intolerance enhancement in patients with chronic congestive heart failure. Carnitine (Code: N0000006688) Carnitine Analog (Code: N0000175903) 1994-11-01 Italian Medicines Agency (AIFA)
Click to view aclatonium Aclatonium is a cholinergic agonist. It is used as (also known as aclatonium napadisilate for the treatment of gastrointestinal dysfunction (nausea, vomiting, anorexia) in the chronic gastritis, biliary dyskinesia, after gastrointestinal surgerys. 1981-09-01 PMDA
Click to view benzylthiouracil Benzylthiouracil is a pyrimidone. Benzylthiouracil has anti-thyroid activity. It is used for the treatment of hyperthyroidism. 1997-01-23 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view malotilate Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2537738) Malotilate is a sulphur-containing compound with antifibrotic and hepatoprotective properties. Malotilate selectively inhibits the 5-lipoxygenase. Malotilate prevented increases in serum markers of type III and IV collagen synthesis as well as accumulation of the collagens, laminin and fibronectin in the liver. It is used for the improvement of liver function in the liver cirrhosis. 2008-12-01 PMDA
Click to view fenoxazoline Fenoxazoline is a vasoconstrictor. It is used for nasal congestion.
Click to view uredepa Uredepa is an aziridine alkylating agent that cross-links with DNA, causing inhibition of DNA synthesis. It has been used as a chemosterilant.
Click to view calcium pantothenate A butyryl-beta-alanine that can also be viewed as pantoic acid complexed with BETA ALANINE. It is incorporated into COENZYME A and protects cells against peroxidative damage by increasing the level of GLUTATHIONE. Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) Vitamin B Complex (Code: D014803) 1993-12-29 FDA PAU
Click to view aniracetam Aniracetam is a positive modulator of AMPA-sensitive glutamate receptors and a nootropic drug. It is used in patients with mild to moderate senile dementia of the Alzheimer type. Also aniracetam is used for the treatment of emotional disturbances, such as depressed mood and anxiety/agitation. Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Nootropic Agents (Code: D018697) Psychotropic Drugs (Code: D011619) FDA 4MP
Click to view dacisteine -
Click to view pirbuterol Pirbuterol is a short-acting beta2 adrenoreceptor agonist with bronchodilating action. Pirbuterol selectively binds to beta-2 adrenergic receptors in bronchial smooth muscle, thereby activating intracellular adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels cause relaxation of bronchial smooth muscle, relieve bronchospasms, improve mucociliary clearance and inhibit the release of mediators of immediate hypersensitivity from cells, especially from mast cells. Pirbuterol is used in asthma for reversal of acute bronchospasm, and also as a maintenance medication to prevent future attacks. Adrenergic beta2-Agonists (Code: N0000009922) beta2-Adrenergic Agonist (Code: N0000175779) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Respiratory System Agents (Code: D019141) 1986-12-30 FDA
Click to view miglustat Ceramide glucosyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: Q16739, gene: UGCG, swissprot: CEGT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021348s010lbl.pdf) Lysosomal alpha-glucosidase (Organism: Rattus norvegicus, class: Enzyme, accessions: Q6P7A9, gene: Gaa, swissprot: LYAG_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7608901) Sucrase-isomaltase, intestinal (Organism: Rattus norvegicus, class: Enzyme, accessions: P23739, gene: Si, swissprot: SUIS_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7608901) Trehalase (Organism: Rattus norvegicus, class: Unclassified, accessions: O70282, gene: Treh, swissprot: O70282_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7608901) Lysosomal alpha-glucosidase (Organism: Homo sapiens, class: Enzyme, accessions: P10253, gene: GAA, swissprot: LYAG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19853441) Non-lysosomal glucosylceramidase (Organism: Homo sapiens, class: Enzyme, accessions: Q9HCG7, gene: GBA2, swissprot: GBA2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19853441) Maltase-glucoamylase, intestinal (Organism: Homo sapiens, class: Enzyme, accessions: O43451, gene: MGAM, swissprot: MGA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20000679) Miglustat is an oral inhibitor of glucosylceramide synthase which is used in the therapy of type 1 Gaucher disease. Miglustat can be used in substrate reduction therapy in diseases in which the enzyme glucocerebrosidase, that is responsible for the breakdown of GSL, is deficient. Glucosylceramide Synthase Inhibitor (Code: N0000175783) Glucosylceramide Synthase Inhibitors (Code: N0000020019) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Glycoside Hydrolase Inhibitors (Code: D065089) Hypoglycemic Agents (Code: D007004) 2002-11-20 EMA NBV
Click to view alminoprofen a nonsteroidal anti-inflammatory drug (NSAID) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antirheumatic drug (Code: CHEBI:35842) antipyretic (Code: CHEBI:35493) non-narcotic analgesic (Code: CHEBI:35481) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view carbidopa Aromatic-L-amino-acid decarboxylase (Organism: Homo sapiens, class: Enzyme, accessions: P20711, gene: DDC, swissprot: DDC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11106255) An inhibitor of dopa decarboxylase, preventing conversion of levodopa to dopamine. It is used in parkinson disease to reduce peripheral adverse effects of levodopa. It has no antiparkinson actions by itself. antidyskinesia agent (Code: CHEBI:66956) antiparkinson drug (Code: CHEBI:48407) dopaminergic agent (Code: CHEBI:48560) Aromatic Amino Acid Decarboxylation Inhibitor (Code: N0000175754) DOPA Decarboxylase Inhibitors (Code: N0000175755) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Aromatic Amino Acid Decarboxylase Inhibitors (Code: D065105) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) 1975-05-02 FDA 142
Click to view ornidazole Ornidazole is a nitroimidazole antiprotozoal agent used in the treatment of susceptible protozoal infections, such as ameba and trichomonas infections, and for the treatment of anaerobic bacterial infections. It is partially plasma-bound and also has radiation-sensitizing action. Ornidazole is a nitroimidazole derivative, which is mediated through the reduction in anaerobic environment into amino or the formation of free radicals from the nitro, interacting with celluar components, results in the death of microorganisms. Ornidazole is the mixture of its levo- and dextro-isomers. Levornidazole has been found to have lower central nervous system toxicity as compared with D- and racemic omidazole. antiprotozoal drug (Code: CHEBI:35820) antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) antitrichomonal drug (Code: CHEBI:50685) Amebicides (Code: D000563) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Antitrichomonal Agents (Code: D000994) Radiation-Sensitizing Agents (Code: D011838) ornidazole: 1997-01-13 CDSCO (INDIA) levornidazole: 2009-08-13 China Food and Drug Administration (CFDA)
Click to view oxitriptan 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/26227779) Proton-coupled amino acid transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q7Z2H8, gene: SLC36A1, swissprot: S36A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16126914) Indoleamine 2,3-dioxygenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P14902, gene: IDO1, swissprot: I23O1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/25815143) Oxitriptan (5-Hydroxytryptophan, 5-HTP) is a chemical by-product of the protein building block L-tryptophan. It is also produced commercially from the seeds of an African plant known as Griffonia simplicifolia. Oxitriptan is indicated for the treatment of post-anoxic myoclonus (Lance and Adams syndrome). Also 5-HTP is used for sleep disorders such as insomnia, depression, anxiety, migraine and tension-type headaches, fibromyalgia, obesity, premenstrual syndrome, premenstrual dysphoric disorder, attention deficit-hyperactivity disorder, seizure disorder, and Parkinson's disease. Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1980-06-10 Italian Medicines Agency (AIFA) 4PQ
Click to view cicloxilic acid Cicloxilic acid is a choleretic agent. Cicloxilic acid feeding lowered bile saturation (though bile tended to remain more saturated than normal) without affecting total bile acid pool size. It was used in gallstone disease either in association with the litholytic bile acids or in prevention of stone formation in high-risk populations (diabetics, obese, hyperlipidemic, etc.). 1975 Italian Medicines Agency (AIFA)
Click to view fadrozole Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1825337) Cytochrome P450 11B1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P15538, gene: CYP11B1, swissprot: C11B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19622340) Cytochrome P450 11B2, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P19099, gene: CYP11B2, swissprot: C11B2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19622340) Fadrozole is a selective aromatase inhibitor. It was used in the treatment of estrogen-dependent disease including breast cancer. Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Aromatase Inhibitors (Code: D047072) Enzyme Inhibitors (Code: D004791) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Steroid Synthesis Inhibitors (Code: D065088) 0T3
JD7
Click to view lidamidine Lidamidine is an alpha2-adrenergic receptor agonist that inhibits intestinal secretion, reduces intestinal transit, and inhibits smooth muscle contraction. Lidamidine hydrochloride is used to treat diarrhoea and other gastrointestinal disorders.. Lidamidine crosses the blood brain barrier poorly and is therefore devoid of the centrally mediated alpha-2 effects. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Antidiarrheals (Code: D000930) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377)
Click to view butibufen Butibufen is a non-steroidal anti-inflammatory cyclooxygenase inhibitor with analgesic and antipyretic properties. The drug was used for the treatment of osteoarthritis, rheumatoid artritis, and other arthroses. It was withdrawn from the market. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view prilocaine Prilocaine is a local anesthetic that is similar pharmacologically to lidocaine. Prilocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action. It is used most often for infiltration anesthesia in dentistry. Local anaesthetic (Code: CHEBI:36333) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Amide Local Anesthetic (Code: N0000175682) Amides (Code: N0000007681) Local Anesthesia (Code: N0000175976) 1965-11-18 FDA
Click to view metaxalone The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system depression. Metaxalone has no direct action on the contractile mechanism of striated muscle, the motor end plate, or the nerve fiber. Centrally-mediated Muscle Relaxation (Code: N0000175730) Muscle Relaxant (Code: N0000175737) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 1962-08-13 FDA
Click to view phenamacide Phenamacide was used as a spasmolytic.
Click to view exalamide an antifungal agent PMDA
Click to view procarbazine DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) alkylation agent (Source: https://www.ncbi.nlm.nih.gov/pubmed/2908840) Amine oxidase [flavin-containing] A (Organism: Rattus norvegicus, class: Enzyme, accessions: P21396, gene: Maoa, swissprot: AOFA_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1359073) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1359073) Membrane primary amine oxidase (Organism: Rattus norvegicus, class: Enzyme, accessions: O08590, gene: Aoc3, swissprot: AOC3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1359073) Procarbazine is an antineoplastic agent used primarily in combination with mechlorethamine, vincristine, and prednisone in the treatment of Hodgkin's disease. Procarbazine inhibits DNA, RNA, and protein synthesis by inhibiting transmethylation of methionine into tRNA and may also damage DNA directly through alkylation. antineoplastic agent (Code: CHEBI:35610) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Antineoplastic Agents (Code: D000970) 1969-07-22 FDA
Click to view mecloralurea Mecloralurea (trichloroethylolmethylureaa) is an anxiolytic.
Click to view chlorazanil Chlorazanil is a triazine derivative and diuretic agent. Chlorazanil appears to prevent the absorption of sodium and chloride in the distal convoluted tubule.
Click to view methiodal Methiodal is an iodinated X-ray contrast media for myelographies. It is used since 1931. Myelography with methiodal a low incidence of complications is stated, and in particular only very few eases of serious neurologie complications are mentioned.
Click to view dimecrotic acid Dimecrotic acid is a choleretic agent with spasmolytic properties. It is indicated for the treatment of hepato-digestive insufficiency and its manifestations. It shouldn’t be used in case of blockage of bile ducts, severe liver failure and severe renal impairment. 1984-02-21 National Authority of Medicines and Health Products (Portugal)
Click to view phenindione Vitamin K epoxide reductase complex subunit 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BQB6, gene: VKORC1, swissprot: VKOR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3781349) Arachidonate 5-lipoxygenase (Organism: Rattus norvegicus, class: Enzyme, accessions: P12527, gene: Alox5, swissprot: LOX5_RAT) (Source: https://www.sciencedirect.com/science/article/pii/S0960894X0080236X) Phenindione is an indandione that has been used as an anticoagulant. Phenindione inhibits vitamin K reductase, resulting in depletion of the reduced form of vitamin K (vitamin KH2). Phenindione has actions similar to warfarin, but it is now rarely employed because of its higher incidence of severe adverse effects. anticoagulant (Code: CHEBI:50249) Anticoagulants (Code: D000925) Hematologic Agents (Code: D006401) FDA
Click to view morinamide Morinamide is a second line anti-tuberculous agent. The anti-mycobacterial effect of morinamide is the same as pyrazinamide. It is used for the treatment of tuberculosis.
Click to view acetazolamide Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18167490) Carbonic anhydrase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P53615, gene: NCE103, swissprot: CAN_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase 2 (Organism: Cryptococcus neoformans var. grubii, class: Unclassified, accessions: Q3I4V7, gene: CAN2, swissprot: Q3I4V7_CRYNV) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase 13 (Organism: Homo sapiens, class: Enzyme, accessions: Q8N1Q1, gene: CA13, swissprot: CAH13_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21515057) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Enzyme, accessions: P40881, gene: None, swissprot: CAH_METTE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15546717) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18572406) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991988) Acetazolamide is an inhibitor of the enzyme carbonic anhydrase. In the eye, inhibitory action of acetazolamide decreases the secretion of aqueous humor and results in a drop in intraocular pressure, a reaction considered desirable in cases of glaucoma and even in certain non-glaucomatous conditions. Also inhibition of carbonic anhydrase appears to retard abnormal, paroxysmal, excessive discharge from central nervous system neurons. The diuretic effect of acetazolamide is due to its action in the kidney on the reversible reaction involving hydration of carbon dioxide and dehydration of carbonic acid. Acetazolamide is indicated for adjunctive treatment of chronic simple (open-angle) glaucoma, secondary glaucoma, and preoperatively in acute angle-closure glaucoma where delay of surgery is desired in order to lower intraocular pressure. Acetazolamide is also indicated for the prevention or amelioration of symptoms associated with acute mountain sickness despite gradual ascent. Anticonvulsants (Code: D000927) Carbonic Anhydrase Inhibitors (Code: D002257) Central Nervous System Agents (Code: D002491) Diuretics (Code: D004232) Enzyme Inhibitors (Code: D004791) Natriuretic Agents (Code: D045283) Carbonic Anhydrase Inhibitor (Code: N0000175517) Sulfonamides (Code: N0000008048) 1953-07-27 FDA AZM
Click to view nimorazole Nimorazole is an antitrichomonal agent which is effective either topically or orally and whose urinary metabolites are also trichomonicidal. It is also being investigated for the treatment of head and neck cancer. Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Antitrichomonal Agents (Code: D000994) 1977-10-01 CDSCO (INDIA)
Click to view nicametate Nicametate is a vasodilator. It is no longer available. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view bromisoval Bromisoval is a hypnotic and sedative compound of the bromoureide group.Bromisoval can suppress expression of many kinds of pro- and anti-inflammatory mediators in LPS- or interferon-gamma activated alveolar and peritoneal macrophages. Bromisoval was found to ameliorate sepsis in rats. It also prevents elevated serum-IL-6 level as well as IL-6 mRNA expression in septic rats. Bromisoval was also found useful for inflammatory skin disorders. The compound is able to suppress the Toll-like recptor ligands-induced proinflammatory response without the side effects often associated with the steroid usage. It was formerly used for its sedative and hypnotic properties. sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 2010-08-03 Ministry of Health of the Russian Federation
Click to view mephenoxalone Mephenoxalone is a mild tranquiliser used in the treatment of anxiety and muscular spasm.
Click to view nifenalol Nifenalol is the beta-receptor antagonist. The levo-isomer are active in antagonizing beta-receptors, the dextro-isomer is inactive. Nifenalolhas little local anesthetic properties in contrast to procaine, propranolol, and butidrine. Nifenalol has been studied against coronary artery disease. Nifenalol protects against angina and ischemic changes in the EKG. It was further noted that nifenalol had no antiarrhythmic action and that it was devoid of evident side effects.
Click to view pentobarbital GABA-A receptor; anion channel alpha-1/beta-3/delta (Organism: Rattus norvegicus, class: Ion channel, accessions: P62813|P63079|P18506, gene: Gabra1|Gabrb3|Gabrd, swissprot: GBRA1_RAT|GBRB3_RAT|GBRD_RAT) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15247320) GABA-A receptor; anion channel alpha-1/beta-3/gamma-2 (Organism: Rattus norvegicus, class: Ion channel, accessions: P62813|P63079|P18508, gene: Gabra1|Gabrb3|Gabrg2, swissprot: GBRA1_RAT|GBRB3_RAT|GBRG2_RAT) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15247320) Pentobarbital is a short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It was used for sleep induction than for sedation. Also it is used for humane, painless and rapid euthanasia in dogs and cats. GABAA receptor agonist (Code: CHEBI:91016) Adjuvants, Anesthesia (Code: D000759) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) 1973-09-19 FDA RAV
Click to view bufexamac Histone deacetylase 10 (Organism: Homo sapiens, class: Enzyme, accessions: Q969S8, gene: HDAC10, swissprot: HDA10_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21258344) Histone deacetylase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBN7, gene: HDAC6, swissprot: HDAC6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21258344) Bufexamac is a nonsteroidal antiinflammatory drug. The phenolic bufexamac decomposition products could be the reason for its eczema-provoking properties frequently described in the literature. Bufexamac is a class IIb histone deacetylase inhibitor. Bufexamac is used in topical formulations to treat dermatological diseases (eczema and dermatitis) and proctological conditions (haemorrhoids and anal fissure). non-narcotic analgesic (Code: CHEBI:35481) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antipyretic (Code: CHEBI:35493) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Italian Medicines Agency (AIFA) A4Z
Click to view rimiterol Rimiterol1 is a catecholamine and a selective beta2-adrenoreceptor agonist, but is not effective as a bronchodilator by the oral route of administration. It is used in the management of bronchial asthma. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Neurotransmitter Agents (Code: D018377)
Click to view etamivan Etamivan is phenol substituted at C-2 and C-4 by a methoxy group and an N,N-diethylaminocarbonyl group respectively. Etamvin is a respiratory stimulant drug similar to nikethamide. Etamivan was used in pulmonary emphysema, but the risk of toxicity associated with effective doses is now considered to be unacceptable. It is available in oral preparations for use in cerebrovascular and circulatory disorders and hypotension, but it is no longer recommended. 2DL
Click to view cerulenin Fatty acid synthase (Organism: Homo sapiens, class: Enzyme, accessions: P49327, gene: FASN, swissprot: FAS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16870425) Coagulation factor XIII A chain (Organism: Homo sapiens, class: Enzyme, accessions: P00488, gene: F13A1, swissprot: F13A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26005023) Cerulenin is an antifungal antibiotic isolated from Cephalosporium caerulens. It inhibits eukaryotic lipid and sterol synthesis and blocks lipid modification of proteins. Cerulenin is a potent inhibitor of fatty acid synthase (FAS). Cerulenin has activity against yeast-like fungi, such as Candida, Saccharomyces, and Cryptococcus. Cerulenin is commercially available as a biochemical tool. antiinfective agent (Code: CHEBI:35441) antilipemic drug (Code: CHEBI:35679) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antimetabolites (Code: D000963) Fatty Acid Synthesis Inhibitors (Code: D054872) Hypolipidemic Agents (Code: D000960) 1X9
Click to view benmoxin Benmoxin is an irreversible and nonselective monoamine oxidase inhibitor (MAOI) of the hydrazine class. It was synthesized in 1967 and was subsequently used as an antidepressant in Europe, but is now no longer marketed.
Click to view bucetin Bucetin is an analgesic and antipyretic medication which was withdrawn from the market in 1986 due to its renal toxicity.
Click to view neostigmine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/203629s000lbl.pdf) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24675179) Neostigmine is a cholinesterase inhibitor used in the treatment of myasthenia gravis. Its indication is for the reversal of the effects of non-depolarizing neuromuscular blocking agents after surgery. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier. Cholinesterase Inhibitor (Code: N0000175723) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) 2013-05-31 FDA
Click to view toliprolol Beta-1 adrenergic receptor (Organism: Cavia porcellus, class: GPCR, accessions: B0FL73, gene: ADRB1, swissprot: B0FL73_CAVPO) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2903245) Beta-2 adrenergic receptor (Organism: Cavia porcellus, class: GPCR, accessions: Q8K4Z4, gene: Adrb2, swissprot: ADRB2_CAVPO) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2903245) Toliprolol is beta-adrenergic blocker. It was developed as antianginal and antihypertensive agent.
Click to view tigloidine Tigloyltropeine is an alkaloid from Physalis alkekengi (winter cherry) roots. Tigloidine was used in the treatment of Parkinsonism, Huntington’s Chorea and spastic paraplegia.
Click to view bucillamine Bucillamine is a synthetic SH compound developed from tiopronin. Activity is mediated by the two thiol groups that the molecule contains. Bucillamine is a more potent thiol donor than other cysteine derivatives: approximately 16-fold more potent than N-acetylcysteine in vivo. Bucillamine is a potent antioxidant which exerts its beneficial therapeutic activities in RA patients by metal chelation rather than by scavenging free radical species. It is used for the treatment of rheumatoid arthritis. In addition bucillamine appears to have additional anti-inflammatory effects unrelated to its antioxidant effect. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antioxidants (Code: D000975) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sensory System Agents (Code: D018689) 1998-10-01 PMDA
Click to view ciramadol Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/2572952) benzylamine analgesics; structure given in fourth source Analgesics (Code: D000700) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view vinylbital Vinylbital is a barbiturate derivative. It was used as a sedative and in the treatment of insomnia.
Click to view nifuradene Nifuradene is a nitrofurantoin analogue. Nifuradene was used for the treatment of urinary tract infection.
Click to view stavudine Stavudine is a nucleoside analogue of thymidine, is phosphorylated by cellular kinases to the active metabolite stavudine triphosphate. Stavudine triphosphate inhibits the activity of HIV-1 reverse transcriptase by competing with the natural substrate thymidine triphosphate and by causing DNA chain termination following its incorporation into viral DNA. Stavudine triphosphate inhibits cellular DNA polymerases and markedly reduces the synthesis of mitochondrial DNA. Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175462) Nucleoside Analog (Code: N0000175459) Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009947) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antimetabolites (Code: D000963) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Noxae (Code: D009676) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 1994-06-24 FDA
Click to view etofylline Etofylline is a derivative of theophylline, a smooth muscle relaxant. It may act as a phosphodiesterase inhibitor and adenosine receptor antagonist. Etofylline is used to relieve bronchoconstriction. Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1993-06-14 CDSCO (INDIA)
Click to view vinbarbital Vinbarbital is a barbiturate derivative and a hypnotic drug. It is no longer available.
Click to view enallylpropymal Enallylpropymal is a rapidly acting member of barbiturates.
Click to view butalbital GABA-A receptor alpha-1/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P28472, gene: GABRA1|GABRB3|GABRG2, swissprot: GBRA1_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator Butalbital, a barbiturate, is a GABAA receptor agonist and may inhibit excitatory AMPA receptors. Management of butalbital withdrawal can be simplified by using a phenobarbital-loading protocol; RN given refers to parent cpd sedative (Code: CHEBI:35717) analgesic (Code: CHEBI:35480) Barbiturate (Code: N0000175693) Barbiturates (Code: N0000008016) 1976-05-04 FDA
Click to view febuprol Febuprol is a choleretic which is used in the treatment of biliary tract disorders. Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765) 1989-04-26 National Authority of Medicines and Health Products (Infarmed)
Click to view furazolidone Furazolidone is a nitrofuran derivative with antiprotozoal and antibacterial activity. Furazolidone has been shown to exhibit antibiotic and anti-microbial functions. Furazolidone is also used as a poultry food additive. Furoxone has a broad antibacterial spectrum covering the majority of gastrointestinal tract pathogens including E. coli, staphylococci, Salmonella, Shigella, Proteus, Aerobacter aerogenes, Vibrio cholerae and Giardia lamblia. Its bactericidal activity is based upon its interference with DNA replication and protein production. Furazolidone binds bacterial DNA which leads to the gradual inhibition of monoamine oxidase. antitrichomonal drug (Code: CHEBI:50685) antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Anti-Infective Agents, Urinary (Code: D000892) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Antitrichomonal Agents (Code: D000994) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Renal Agents (Code: D012076) 1958-01-20 FDA FUR
Click to view ancitabine Congener of CYTARABINE that is metabolized to cytarabine and thereby maintains a more constant antineoplastic action. prodrug (Code: CHEBI:50266) antineoplastic agent (Code: CHEBI:35610) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Noxae (Code: D009676) 1975 PMDA
Click to view aciclovir Aciclovir: Thymidine kinase (Organism: Human herpesvirus 1, class: Kinase, accessions: Q9QNF7, gene: TK, swissprot: KITH_HHV1) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/018828s031lbl.pdf) Thymidine kinase (Organism: Human herpesvirus 2 (strain 333), class: Kinase, accessions: P04407, gene: TK, swissprot: KITH_HHV23) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/018828s031lbl.pdf) Thymidine kinase (Organism: Varicella-zoster virus (strain Dumas), class: Kinase, accessions: P09250, gene: None, swissprot: KITH_VZVD) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/018828s031lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11861798) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11861798) Ileal sodium/bile acid cotransporter (Organism: Homo sapiens, class: Transporter, accessions: Q12908, gene: SLC10A2, swissprot: NTCP2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15832499) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Aciclovir triphosphate: DNA polymerase catalytic subunit (Organism: Human herpesvirus 1 (strain 17), class: Enzyme, accessions: P04293, gene: None, swissprot: DPOL_HHV11) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/018828s031lbl.pdf) DNA polymerase catalytic subunit (Organism: Varicella-zoster virus (strain Dumas), class: Enzyme, accessions: P09252, gene: None, swissprot: DPOL_VZVD) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/018828s031lbl.pdf) Acyclovir is a synthetic purine nucleoside analogue active against herpes simplex virus types 1 (HSV-1), 2 (HSV-2), and varicella-zoster virus (VZV). Acyclovir is phosphorylated intracellularly by the viral encoded thymidine kinase (TK) of HSV into acyclovir monophosphate, a nucleotide analogue. The monophosphate is further converted into diphosphate by cellular guanylate kinase and into triphosphate by a number of cellular enzymes. In a biochemical reaction, acyclovir triphosphate inhibits replication of herpes viral DNA by competing with nucleotides for binding to the viral DNA polymerase and by incorporation into and termination of the growing viral DNA chain. The cellular thymidine kinase of normal, uninfected cells does not use acyclovir effectively as a substrate, hence toxicity to mammalian host cells is low. Acyclovir is indicated for the treatment of recurrent herpes labialis (cold sores), herpes zoster (shingles), genital herpes, chickenpox (varicella). antiviral drug (Code: CHEBI:36044) DNA Polymerase Inhibitors (Code: N0000020060) Herpes Simplex Virus Nucleoside Analog DNA Polymerase Inhibitor (Code: N0000180187) Herpes Zoster Virus Nucleoside Analog DNA Polymerase Inhibitor (Code: N0000180188) Herpesvirus Nucleoside Analog DNA Polymerase Inhibitor (Code: N0000175468) Nucleoside Analog (Code: N0000175459) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 1982-03-29 FDA AC2
Click to view mephenesin carbamate Mephenesin carbamate is a mephenesin derivative. It was used for the treatment of skeletal muscle spasm associated with neurologic disorders. Also it was used as a diagnostic agent in neurologic disorders. 1970 FDA
Click to view drometrizole Drometrizole is a benzotriazole derivative. It is used as an ultraviolet light absorber and stabilizer in cosmetics, plastics, polyesters, celluloses, acrylates, dyes, rubber, synthetic and natural fibers, waxes, detergent solutions, and orthodontic adhesives. It is similarly used in agricultural products and insecticides.
Click to view amobarbital A barbiturate with hypnotic and sedative properties (but not antianxiety). Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high. (From Martindale, The Extra Pharmacopoeia, 30th ed, p565) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) FDA
Click to view terbutaline Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21652207) Terbutaline is a beta-adrenergic agonist bronchodilator. In vitro and in vivo pharmacologic studies have demonstrated that terbutaline exerts a preferential effect on beta 2-adrenergic receptors. Terbutaline is indicated for the prevention and reversal of bronchospasm in patients with asthma and reversible bronchospasm associated with bronchitis and emphysema. hypoglycemic agent (Code: CHEBI:35526) beta-adrenergic agonist (Code: CHEBI:35522) anti-asthmatic drug (Code: CHEBI:49167) bronchodilator agent (Code: CHEBI:35523) sympathomimetic agent (Code: CHEBI:35524) tocolytic agent (Code: CHEBI:66993) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Reproductive Control Agents (Code: D012102) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Tocolytic Agents (Code: D015149) 1974-03-25 FDA
Click to view prenalterol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10531390) Prenalterol is a selective beta-1 adrenergic receptor agonist used clinically for the treatment of hypotension, acute heart failure and shock. Prenalterol was withdrawn because of side effects in animals. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-1 Receptor Agonists (Code: D058665) Adrenergic beta-Agonists (Code: D000318) Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sympathomimetics (Code: D013566) 1980-01-01 YEAR INTRODUCED
Click to view lefetamine Lefetamine is an opioid analgesic. Since withdrawal symptoms were observed during treatment, it became a controlled substance.
Click to view dithranol 5-lipoxygenase (Organism: Bos taurus, class: Enzyme, accessions: Q9BEG3, gene: None, swissprot: Q9BEG3_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8201600) Dithranol (anthralin) is a hydroxyanthrone, anthracene derivative. It works by slowing the reproduction of skin cells, precise mechanism of anti-psoriatic action is not yet fully understood. The anti-proliferative effects of anthralin appear to result from both an inhibition of DNA synthesis as well as from its strong reducing properties. It is used for the treatment of psoriasis. antipsoriatic (Code: CHEBI:50748) Dermatologic Agents (Code: D003879) 1994-04-21 Ministry of Health of the Russian Federation
Click to view proxibarbal Proxibarbal is a non-sedative barbiturate with a specific anti-serotonin and anti-histamine effect, due to enzyme induction of serotoninase and histaminase. Proxibarbal was used for the treatment of migraine. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993)
Click to view methallatal Methallatal is a member of class thiobarbiturates. It was used for the prevention and treatment of nausea caused by motion sickness.
Click to view crotetamide same pharmacological action as prethcamide; component of prethcamide
Click to view clopirac Clopirac is a non-steroidal anti-inflammatory drug. It is a weak inhibitor of prostaglandin synthetase and has standard anti-inflammatory and analgesic activity. Clopirac was used in rheumatoid arthritis, trauma conditions, osteoarthritis and pain.
Click to view pirlindole Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9368911) Amine oxidase [flavin-containing] A (Organism: Rattus norvegicus, class: Enzyme, accessions: P21396, gene: Maoa, swissprot: AOFA_RAT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9368911) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9368911) Pirlindole is a reversible inhibitor of monoamine oxidase A. Its chemical structure is similar to metralindole. It is used for the treatment of major depression in several European and non-European countries. Antidepressive Agents (Code: D000928) Antineoplastic Agents (Code: D000970) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) 1975-07-25 Ministry of Health of the Russian Federation
Click to view alclofenac Alclofenac is a non-steroidal anti-inflammatory agent. Aceclofenac has little pharmacological activity itself; its main mode of action is through its metabolites which include diclofenac and 4’-hydroxy diclofenac. It was used in rheumatoid arthritis, degenerative joint disease and ankylosing spondylitis. It was withdrawn from the market after a review by European regulators concluded that the risk of arterial thrombotic events (myocardial infarction; stroke) with diclofenac is greater than with other non-selective NSAIDs and similar to the COX-2 inhibitors. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1969-01-01 YEAR INTRODUCED
Click to view methocarbamol Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: ) A centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1206) muscle relaxant (Code: CHEBI:51371) Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) Centrally-mediated Muscle Relaxation (Code: N0000175730) 1957-07-16 FDA
Click to view glyceryl trinitrate Aldehyde dehydrogenase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P05091, gene: ALDH2, swissprot: ALDH2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12048254) Glyceryl trinitrate (nitroglycerin) is an organic nitrate with vasodilator activity. Nitroglycerin forms free radical nitric oxide (NO), which activates guanylate cyclase, resulting in an increase of guanosine 3',5'-monophosphate (cyclic GMP) in smooth muscle and other tissues. This eventually leads to dephosphorylation of myosin light chains, which regulates the contractile state in smooth muscle and results in vasodilatation. Glyceryl trinitrate is indicated for acute relief of an attack or prophylaxis of angina pectoris due to coronary artery disease. vasodilator agent (Code: CHEBI:35620) tocolytic agent (Code: CHEBI:66993) muscle relaxant (Code: CHEBI:51371) prodrug (Code: CHEBI:50266) Cardiovascular Agents (Code: D002317) Explosive Agents (Code: D053834) Vasodilator Agents (Code: D014665) Nitrate Vasodilator (Code: N0000175415) Nitrates (Code: N0000007647) Vasodilation (Code: N0000009909) 1981-05-28 FDA TNG
Click to view decitabine DNA (cytosine-5)-methyltransferase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P26358, gene: DNMT1, swissprot: DNMT1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021790s021lbl.pdf) DNA (cytosine-5)-methyltransferase 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y6K1, gene: DNMT3A, swissprot: DNM3A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021790s021lbl.pdf) DNA (cytosine-5)-methyltransferase 3B (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBC3, gene: DNMT3B, swissprot: DNM3B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021790s021lbl.pdf) Equilibrative nucleoside transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q99808, gene: SLC29A1, swissprot: S29A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/29174536) Deoxycytidine kinase (Organism: Homo sapiens, class: Kinase, accessions: P27707, gene: DCK, swissprot: DCK_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/29174536) Decitabine (5-aza-2’-deoxycitidine) is an analogue of the natural nucleoside 2’-deoxycytidine. Decitabine is believed to exert its antineoplastic effects after phosphorylation and direct incorporation into DNA and inhibition of DNA methyltransferase, causing hypomethylation of DNA and cellular differentiation or apoptosis. Decitabine inhibits DNA methylation in vitro, which is achieved at concentrations that do not cause major suppression of DNA synthesis. Decitabine-induced hypomethylation in neoplastic cells may restore normal function to genes that are critical for the control of cellular differentiation and proliferation. In rapidly dividing cells, the cytotoxicity of decitabine may also be attributed to the formation of covalent adducts between DNA methyltransferase and decitabine incorporated into DNA. Non-proliferating cells are relatively insensitive to decitabine. Decitabine is indicated for treatment of adult patients with myelodysplastic syndromes (MDS) including previously treated and untreated, de novo and secondary MDS of all French-American-British subtypes (refractory anemia, refractory anemia with ringed sideroblasts, refractory anemia with excess blasts, refractory anemia with excess blasts in transformation, and chronic myelomonocytic leukemia) and intermediate-1, intermediate-2, and high-risk International Prognostic Scoring System groups. Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Noxae (Code: D009676) Teratogens (Code: D013723) 2006-05-02 FDA
Click to view diphenan Diphenan is p-benzyl-phenyl-carbamate. It was used for the treatment of enterobiasis, but diphenan was found to have no detectable anthelmintic effect and was not effective.
Click to view salinazid Salinazid is an antibacterial agent. It has tuberculostatic activity.
Click to view dextrofemine Dextrofemine is a member of amphetamines. Dextrofemine is the (+)-form of racefemine. It is antispasmodic agent. Dextrofemine was used as utrine spasmolytic or muscle relaxant.
Click to view cyprodenate Cyprodenate is a stimulant drug. Upon administration, cyprodenate is hydrolyzed to produce dimethylethanolamine (deanol), which is a precursor of choline, and may enhance central acetylcholine formation. It was used for counteracting the effects of benzodiazepine tranquillizer drugs. It was removed from the market by newer antidotes such as flumazenil.
Click to view buclosamide Buclosamide is a member of salicylamides and a topical antimycotic agent. It was used for the treatment of dermatomycoses.
Click to view tulobuterol Tulobuterol is a long-acting beta2-adrenergic receptor agonist. It is used as a patch for treatment of patients with asthma and chronic obstructive pulmonary disease without co-morbidity. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1981 PMDA
Click to view pamidronic acid Farnesyl pyrophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P14324, gene: FDPS, swissprot: FPPS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10620343) Farnesyl pyrophosphate synthase (Organism: Leishmania major class: Enzyme, accessions: Q4QBL1, gene: FPPS, swissprot: Q4QBL1_LEIMA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15828834) Pamidronic Acid is an amino- bisphosphonate with anti-resorptive and anti-hypercalcemic activities. Pamidronic acid binds to and adsorbs onto hydroxyapatite crystals in the bone matrix, thereby preventing osteoclast resorption. This agent also binds to and inhibits farnesyl pyrophosphate synthase, an enzyme that plays an important role in the mevalonate pathway. Pamidronate disodium is indicated for the treatment of moderate or severe hypercalcemia associated with malignancy, with or without bone metastases, for the treatment of patients with moderate to severe Paget’s disease of bone, for the treatment of osteolytic bone metastases of breast cancer and osteolytic lesions of multiple myeloma. Bisphosphonate (Code: N0000175579) Diphosphonates (Code: N0000007707) Bone Density Conservation Agents (Code: D050071) 1991-10-31 FDA 210
Click to view chlorquinaldol Botulinum neurotoxin type A (Organism: Clostridium botulinum, class: Enzyme, accessions: P10845, gene: botA, swissprot: BXA1_CLOBO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24387280) Chlorquinaldol is a halogenated hydroxyquinoline with properties similar to those of clioquinol. It is mainly applied topically in infected skin conditions and in vaginal infections. Also it is used as antiseptic, fungistat, or deodorant. antibacterial drug (Code: CHEBI:36047) antiseptic drug (Code: CHEBI:48218) antiprotozoal drug (Code: CHEBI:35820) Anti-Infective Agents (Code: D000890) Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) 1981-04-22 Italian Medicines Agency (AIFA)
Click to view pemirolast a mast cell stabilizer that inhibits the in vivo Type I immediate hypersensitivity reaction Decreased Histamine Release (Code: N0000175628) Mast Cell Stabilizer (Code: N0000175630) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Neurotransmitter Agents (Code: D018377) 1999-09-24 FDA
Click to view guaiacol benzoate Guaiacol benzoate is a benzoic acid ester of guaiacol. Guaiacol benzoate is decomposed slowly in the intestinal tract into guaiacol and benzoic acid. (See: guaiacol) (See: benzoic acid) 1894 YEAR INTRODUCED
Click to view oxybenzone Hormone-sensitive lipase (Organism: Rattus norvegicus, class: Enzyme, accessions: P15304, gene: Lipe, swissprot: LIPS_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18808096) Oxybenzone is a benzophenone derivative used as a sunscreen agent. Oxybenzone absorbs UVB and UVA II rays, resulting in a photochemical excitation and absorption of energy. Upon return to ground state, the absorbed energy results in emission of longer wavelength radiation and decreased skin penetration of radiation which reduces the risk of DNA damage. dermatologic drug (Code: CHEBI:50177) protective agent (Code: CHEBI:50267) Cosmetics (Code: D003358) Dermatologic Agents (Code: D003879) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) Sunscreening Agents (Code: D013473) 1992-12-07 FDA
Click to view ozagrel Thromboxane-A synthase (Organism: Homo sapiens, class: Enzyme, accessions: P24557, gene: TBXAS1, swissprot: THAS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11992782) Ozagrel is a thromboxane A2 synthesis inhibitor. It is used for the treatment of cerebral vasospasm after subarachnoid hemorrhage. Also ozagrel is used for the treatment asthma and for the prevention of thrombosis. Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Fibrin Modulating Agents (Code: D050299) Fibrinolytic Agents (Code: D005343) Hematologic Agents (Code: D006401) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Neurotransmitter Agents (Code: D018377) 2004-09-01 PMDA
Click to view nabumetone Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: ) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) a non-steroidal anti-inflammatory drug non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) prodrug (Code: CHEBI:50266) Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase 2 Inhibitors (Code: D052246) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1991-12-24 FDA NBO
Click to view indalpine Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT) selective 5-hydroxytryptamine uptake inhibitor Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367)
Click to view fenpentadiol Fenpentadiol is a psychotropic drug that was used as a tranquilizer and antidepressant.
Click to view sapropterin Phenylalanine-4-hydroxylase (Organism: Homo sapiens, class: Enzyme, accessions: P00439, gene: PAH, swissprot: PH4H_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022181s019,205065s005lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022181s019,205065s005lbl.pdf) Sapropterin is a synthetic form of tetrahydrobiopterin (BH4), phenylalanine hydroxylase activator indicated to reduce blood phenylalanine (Phe) levels in patients with hyperphenylalaninemia (HPA) due to tetrahydrobiopterin- (BH4-) responsive Phenylketonuria (PKU). Phenylalanine Hydroxylase Activator (Code: N0000190483) Phenylalanine Hydroxylase Activators (Code: N0000190482) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) P-Glycoprotein Inhibitors (Code: N0000185503) diagnostic agent (Code: CHEBI:33295) 2007-12-13 FDA
Click to view fenamisal Fenamisal (phenyl aminosalicylate) is the phenyl ester of para-aminosalicylic acid, reported to have less side effects than simple salts of para-aminosalicylic acid. It was used as a second-line antituberculosis drug with a high incidence of hypersensitivity reactions and gastrointestinal upset. 1959 FDA
Click to view osalmid Osalmid is a choleretic drug which is used as a choleretic in the convalescent stage of infectious hepatitis. 1971-07-14 Ministry of Health of the Russian Federation
Click to view amiloride Amiloride-sensitive sodium channel subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P37088, gene: SCNN1A, swissprot: SCNNA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12928313) Solute carrier family 22 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63089, gene: Slc22a1, swissprot: S22A1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11758759) Solute carrier family 22 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9R0W2, gene: Slc22a2, swissprot: S22A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11758759) Urokinase-type plasminogen activator (Organism: Homo sapiens, class: Enzyme, accessions: P00749, gene: PLAU, swissprot: UROK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26575094) Acid-sensing ion channel 3 (Organism: Rattus norvegicus, class: Ion channel, accessions: O35240, gene: Asic3, swissprot: ASIC3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19339181) Sodium/hydrogen exchanger 2 (Organism: Oryctolagus cuniculus, class: Transporter, accessions: P50482, gene: SLC9A2, swissprot: SL9A2_RABIT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7685025) Sodium/hydrogen exchanger 5 (Organism: Homo sapiens, class: Unclassified, accessions: Q14940, gene: SLC9A5, swissprot: SL9A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10692428) Short transient receptor potential channel 6 (Organism: Mus musculus, class: Ion channel, accessions: Q61143, gene: Trpc6, swissprot: TRPC6_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11179201) Transient receptor potential cation channel subfamily A member 1 (Organism: Rattus norvegicus, class: Ion channel, accessions: Q6RI86, gene: Trpa1, swissprot: TRPA1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843607) Amiloride is a potassium-conserving (antikaliuretic) drug that possesses weak (compared with thiazide diuretics) natriuretic, diuretic, and antihypertensive activity. Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. Amiloride is indicated as adjunctive treatment with thiazide diuretics or other kaliureticdiuretic agents in congestive heart failure or hypertension to help restore normal serum potassium levels in patients who develop hypokalemia on the kaliuretic diuretic and to prevent development of hypokalemia in patients who would be exposed to particular risk if hypokalemia were to develop, e.g., digitalized patients or patients with significant cardiac arrhythmias. diuretic (Code: CHEBI:35498) Acid Sensing Ion Channel Blockers (Code: D062646) Diuretics (Code: D004232) Epithelial Sodium Channel Blockers (Code: D062686) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Channel Blockers (Code: D026941) Decreased Renal K+ Excretion (Code: N0000008859) Increased Diuresis (Code: N0000175359) Potassium-sparing Diuretic (Code: N0000175418) 1981-10-05 FDA AMR
Click to view furonazide Furonazide has been used in the treatment of tuberculosis.
Click to view enfenamic acid inhibits platelet aggregation Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Hematologic Agents (Code: D006401) Peripheral Nervous System Agents (Code: D018373) Platelet Aggregation Inhibitors (Code: D010975) Sensory System Agents (Code: D018689)
Click to view lamivudine Lamivudine is a synthetic nucleoside analogue with activity against HIV-1 and HBV. Intracellularly, lamivudine is phosphorylated to its active 5’-triphosphate metabolite, lamivudine triphosphate (3TC-TP). The principal mode of action of 3TC-TP is inhibition of HIV-1 reverse transcriptase via DNA chain termination after incorporation of the nucleotide analogue. antiviral drug (Code: CHEBI:36044) prodrug (Code: CHEBI:50266) Hepatitis B Virus Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175656) Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175462) Nucleoside Analog (Code: N0000175459) Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009947) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 1995-11-17 FDA 3TC
Click to view furfenorex Furfenorex is a member of amphetamines. Furfenorex was used against obesity as an appetite suppressant. It is no longer available because one of its metabolite is metamphetamine.
Click to view pronetalol Pronetalol is a nonselective beta-adrenoceptor antagonist that is structurally related to propranolol. Pronetalol was the first beta-adrenoceptor antagonist used for the treatment of coronary heart disease and cardiac arrhythmias. It was found to produce thymic tumors in mice. It is no longer available.
Click to view triclofos trichloroethanol: GABA-A receptor alpha-2/beta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P18505, gene: GABRA2|GABRB1, swissprot: GBRA1_HUMAN|GBRB1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) Triclofos (2,2,2-trichloroethyl phosphate) is a monoalkyl phosphate. Triclofos is converted to Trichloroethanol in the body. Trichloroethanol acts on GABAa receptors. Triclofos is primarily indicated in conditions like Insomnia, and can also be given in adjunctive therapy as an alternative drug of choice in Nausea, vertigo, labyrinthine disorders. 1964-12-01 CDSCO (INDIA)
Click to view bifemelane Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/3335842/) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/3335842/) Bifemelane is a psychotropic drug, was found to inhibit monoamine oxidase (MAO). It inhibited type A MAO (MAO-A) competitively and type B (MAO-B) noncompetitively and it was a more potent inhibitor of MAO-A than of MAO-B. Bifemelane was used for the treatment of cerebral infarction patients with depressive symptoms, and in the treatment of senile dementia as well. Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619)
Click to view indeloxazine Monoamine oxidase (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643|P21396, gene: Maoa|Maob, swissprot: AOFA_RAT|AOFB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/518676) Indeloxazine is a neuroleptic. It is used to allay autonomic hyperactivity following cerebral infarction/haemorrhage or atherosclerosis. Anticonvulsants (Code: D000927) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1988 PMDA
Click to view clonidine Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022331s013lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022331s013lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022331s013lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11082457) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11082457) Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7969082) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Organism: Mus musculus, class:Ion channel, accessions: O70507, gene: Hcn4, swissprot: HCN4_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17261653) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 (Organism: Mus musculus, class: Ion channel, accessions: O88703, gene: Hcn2, swissprot: HCN2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17261653) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 (Organism: Mus musculus, class: Ion channel, accessions: O88704, gene: Hcn1, swissprot: HCN1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17261653) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9655880) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10966924) Nischarin (Organism: Homo sapiens, class: Cytosolic other, accessions: Q9Y2I1, gene: NISCH, swissprot: NISCH_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18621536) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24900506) Clonidine is a centrally active alpha-adrenergic agonist used predominantly as an antihypertensive agent, usually in combination with other agents. sympatholytic agent (Code: CHEBI:66991) antihypertensive agent (Code: CHEBI:35674) non-narcotic analgesic (Code: CHEBI:35481) alpha-adrenergic agonist (Code: CHEBI:35569) Adrenergic alpha2-Agonists (Code: N0000009918) Central alpha-2 Adrenergic Agonist (Code: N0000175554) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-2 Receptor Agonists (Code: D058647) Adrenergic alpha-Agonists (Code: D000316) Analgesics (Code: D000700) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Sympatholytics (Code: D013565) 1974-09-03 FDA
Click to view naproxen Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/017581s113,018164s063,020067s020lbl.pdf) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/017581s113,018164s063,020067s020lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9248768) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9248768) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9248768) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991954) Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16183274) Aldo-keto reductase family 1 member C2 (Organism: Homo sapiens, class: Enzyme, accessions: P52895, gene: AKR1C2, swissprot: AK1C2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22877157) Hormone-sensitive lipase (Organism: Rattus norvegicus, class: Enzyme, accessions: P15304, gene: Lipe, swissprot: LIPS_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18808096) Naproxen is an anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Gout Suppressants (Code: D006074) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1976-03-11 FDA NPS
Click to view propyphenazone Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/25765567) Propyphenazone is a pyrazolone derivative with anti-inflammatory, analgesic and antipyretic activity. It is used to reduce fever and pain in conditions like headache. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) peripheral nervous system drug (Code: CHEBI:49110) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1980-02-01 CDSCO (INDIA)
Click to view mefenamic acid Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) Aldo-keto reductase family 1 member C2 (Organism: Homo sapiens, class: Enzyme, accessions: P52895, gene: AKR1C2, swissprot: AK1C2_HUMAN) Acetylcholinesterase (Organism: Torpedo californica, class: Enzyme, accessions: P04058, gene: ache, swissprot: ACES_TORCA) Aldo-keto reductase family 1 member C1 (Organism: Homo sapiens, class: Enzyme, accessions: Q04828, gene: AKR1C1, swissprot: AK1C1_HUMAN) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: ) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: ) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Aldo-keto reductase family 1 member B10 (Organism: Homo sapiens, class: Enzyme, accessions: O60218, gene: AKR1B10, swissprot: AK1BA_HUMAN) Aldose reductase (Organism: Homo sapiens, class: Enzyme, accessions: P15121, gene: AKR1B1, swissprot: ALDR_HUMAN) A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) analgesic (Code: CHEBI:35480) antirheumatic drug (Code: CHEBI:35842) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antipyretic (Code: CHEBI:35493) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1967-03-28 FDA ID8
Click to view ibudilast cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18686943) cAMP-specific 3',5'-cyclic phosphodiesterase 4B (Organism: Homo sapiens, class: Enzyme, accessions: Q07343, gene: PDE4B, swissprot: PDE4B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18686943) cAMP-specific 3',5'-cyclic phosphodiesterase 4C (Organism: Homo sapiens, class: Enzyme, accessions: Q08493, gene: PDE4C, swissprot: PDE4C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18686943) cAMP-specific 3',5'-cyclic phosphodiesterase 4D (Organism: Homo sapiens, class: Enzyme, accessions: Q08499, gene: PDE4D, swissprot: PDE4D_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18686943) Ibudilast is an orally bioavailable inhibitor of cyclic nucleotide phosphodiesterase (PDE), mainly PDE-3, -4, -10, and -11, with anti-(neuro)inflammatory, vasorelaxant, bronchodilator, analgesic, neuroprotective and potential anti-tumor activities. Ibudilast is able to cross the blood-brain barrier. Ibudilast is used for improving prognosis and relieving symptoms in patients suffering from ischemic stroke and for the treatment of bronchial asthma. Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Peripheral Nervous System Agents (Code: D018373) Phosphodiesterase Inhibitors (Code: D010726) Platelet Aggregation Inhibitors (Code: D010975) Respiratory System Agents (Code: D019141) Vasodilator Agents (Code: D014665) 1989-05-01 PMDA AVL
Click to view diazoxide Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12270187) Diazoxide is a benzothiadiazine derivative that is a peripheral vasodilator. Diazoxide administered orally produces a prompt dose-related increase in blood glucose level, due primarily to an inhibition of insulin release from the pancreas, and also to an extrapancreatic effect. Diazoxide is useful in the management of hypoglycemia due to hyperinsulinism. antihypertensive agent (Code: CHEBI:35674) sympathomimetic agent (Code: CHEBI:35524) cardiotonic drug (Code: CHEBI:38147) bronchodilator agent (Code: CHEBI:35523) beta-adrenergic agonist (Code: CHEBI:35522) diuretic (Code: CHEBI:35498) vasodilator agent (Code: CHEBI:35620) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1973-01-22 FDA 20J
Click to view guanabenz Trace amine-associated receptor 1 (Organism: Mus musculus, class: GPCR, accessions: Q923Y8, gene: Taar1, swissprot: TAAR1_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19725810) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9351903) Guanabenz is an aminoguanidine derivative, 2,'6-dichlorobenzylideneamina-guanidine acetate. Guanabenz is an active central alpha-2 adrenergic agonist. Its antihypertensive action appears to be mediated via stimulation of central alpha-adrenergic receptors, resulting in a decrease of sympathetic outflow from the brain at the bulbar level to the peripheral circulatory system. Guanabenz is indicated for treatment of hypertension. Adrenergic alpha2-Agonists (Code: N0000009918) Central alpha-2 Adrenergic Agonist (Code: N0000175554) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-2 Receptor Agonists (Code: D058647) Adrenergic alpha-Agonists (Code: D000316) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 1982-09-07 FDA
Click to view methaniazide Methaniazide is a derivative of isoniazid, a synthetic derivative of nicotinic acid, with antituberculosis properties. It is used for the treatment of pulmonary tuberculosis due to Micobacterium tuberculosis. 2009-09-25 PMDA
Click to view fenfluramine Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14675103) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9825834) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9825834) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9690701) Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8643547) Chromaffin granule amine transporter (Organism: Homo sapiens, class: Transporter, accessions: P54219, gene: SLC18A1, swissprot: VMAT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8643547) Fenfluramine is an anorectic that is no longer marketed. Fenfluramine is a centrally active drug that apparently both blocks serotonin uptake and provokes transport-mediated serotonin release. It is the racemic mixture of two enantiomers, dexfenfluramine, and levofenfluramine. Dexfenfluramine is the S-isomer offenfluramine. It is used as an anorectic. Unlike fenfluramine, it does not possess any catecholamine agonist activity. In combination with phentermine, it was part of the anti-obesity medication. Fenfluramine was withdrawn in 1997. serotonin uptake inhibitor (Code: CHEBI:50949) serotonergic agonist (Code: CHEBI:35941) appetite depressant (Code: CHEBI:50507) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) 1987-07-01 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view aminophenazone Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10784435) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10784435) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10784435) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10784435) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10784435) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10784435) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10220563) Aminophenazone is a pyrazolone with analgesic, anti-inflammatory, and antipyretic properties that carries a risk of agranulocytosis. It is used for symptomatic treatment of influenza and common cold (fever, headache, myalgia). In biomedical applications, radiolabelled (13C-labeled) aminophenazone has been used in breath tests to measure the cytochrome P-450 metabolic activity in liver function tests. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) 1941-07-27 Hungary National Institute of Pharmacy and Nutrition
Click to view sulfathiourea Sulfathiourea is a short-acting sulfonamide antibiotic. Sulfathiourea has been show active against tuberculosis. It was used for the treatment of pneumonia. antibacterial drug (Code: CHEBI:36047)
Click to view eptazocine an opioid analgesic 1987 PMDA
Click to view taurosteine Taurosteine (N-2-thenoyltaurine) is a mucolytic agent.
Click to view nifurprazine Nifurprazine is a derivative of nitrofuran and an antibacterial agent. It has high activity against Clostridia and Pseudomonas aeruginosa in comparison with other nitrofurans.
Click to view phenobarbital GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47869|P34903|P48169|P31644|Q16445|P18505|P47870|P28472|O14764|P78334|Q8N1C3|P18507|Q99928|O00591|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16981722) Acetylcholine receptor; alpha2/beta/gamma/delta (Organism: Mus musculus, class: Ion channel, accessions: Q91X60|P09690|P04760|P02716, gene: Chrna2|Chrnb1|Chrng|Chrnd, swissprot: ACHA2_MOUSE|ACHB_MOUSE|ACHG_MOUSE|ACHD_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9089445) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642468) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642468) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642468) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642468) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642468) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642468) UDP-glucuronosyltransferase 1-6 (Organism: Homo sapiens, class: Enzyme, accessions: P19224, gene: UGT1A6, swissprot: UD16_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/26684499) UDP-glucuronosyltransferase 1-7 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW7, gene: UGT1A7, swissprot: UD17_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/26684499) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18824002) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/9738950) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/9738950) Solute carrier organic anion transporter family member 1A4 (Organism: Rattus norvegicus, class: Transporter, accessions: O35913, gene: Slco1a4, swissprot: SO1A4_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/11451172) Phenobarbital is a long-acting barbituric acid derivative with antipsychotic property. Phenobarbital binds to and activates the gamma-aminobutyric acid (GABA)-A receptor, thereby mimicking the inhibitory actions of GABA in the brain. The activation effects of the phenobarbital-receptor-ionophore complex include increased frequency of chloride channel openings, membrane hyperpolarization and ultimately synaptic inhibition and decreased neuronal excitability. In addition, this agent inhibits glutamate induced depolarization. Phenobarbital is used for the treatment of all types of seizures except absence seizures. anticonvulsant (Code: CHEBI:35623) sedative (Code: CHEBI:35717) drug allergen (Code: CHEBI:88188) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Cytochrome P-450 CYP2B6 Inducers (Code: D065695) Cytochrome P-450 CYP3A Inducers (Code: D065701) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Metabolic Side Effects of Drugs and Substances (Code: D065606) Neurotransmitter Agents (Code: D018377) 1912-01-01 YEAR INTRODUCED
Click to view nalidixic acid DNA gyrase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES4|P0AES6, gene: gyrA|gyrB, swissprot: GYRA_ECOLI|GYRB_ECOLI) inhibitor (http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/014214s060lbl.pdf) Nalidixic Acid is a synthetic quinolone and antibacterial agent with urinary tract antiseptic activity. Nalidixic acid blocks DNA replication in susceptible bacteria by inhibiting a subunit of DNA gyrase. Nalidixic acid is active against most gram-negative organisms that cause urinary tract infections. antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1964-03-06 FDA NIX
Click to view todralazine An antihypertensive agent with both central and peripheral action; it has some central nervous system depressant effects. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317)
Click to view mebutamate Mebutamate is a biscarbamate drug that has anxiolytic, sedative, and antihypertensive effects. Its effects comparable to those of other barbiturates but is only around 1/3rd the potency of secobarbital as a sedative. Mebutamate acts via allosteric agonism of the GABAA receptor at the beta-subreceptor. It was used for the treatment of hypertension. 1975 FDA
Click to view isonixin Isonixin is a non-steroidal anti-inflammatory agent. It was used for the treatment of rheumatoid arthritis, gout. 1978-04-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view mofebutazone Mofebutazone is a pyrazolone. Mofebutazone has anti-inflammatory, analgetic and antipyretic activities. It was used for the treatment of rheumatic disorders. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1962 YEAR INTRODUCED
Click to view melatonin Melatonin receptor type 1B (Organism: Homo sapiens, class: GPCR, accessions: P49286, gene: MTNR1B, swissprot: MTR1B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20674373) Melatonin receptor type 1A (Organism: Homo sapiens, class: GPCR, accessions: P48039, gene: MTNR1A, swissprot: MTR1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20674373) Eosinophil peroxidase (Organism: Homo sapiens, class: Enzyme, accessions: P11678, gene: EPX, swissprot: PERE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18516076) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19919601) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19919601) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19919601) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12358729) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12750432) Ribosyldihydronicotinamide dehydrogenase [quinone] (Organism: Homo sapiens, class: Enzyme, accessions: P16083, gene: NQO2, swissprot: NQO2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18400335) Melatonin is a hormone produced by the pineal gland that has multiple effects including somnolence, and is believed to play a role in regulation of the sleep-wake cycle. Melatonin is available over-the-counter and is reported to have beneficial effects on wellbeing and sleep. Melatonin is also an effective antioxidant. anticonvulsant (Code: CHEBI:35623) central nervous system depressant (Code: CHEBI:35488) immunological adjuvant (Code: CHEBI:50847) Antioxidants (Code: D000975) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Protective Agents (Code: D020011) FDA ML1
Click to view aminoglutethimide Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26689671) Aminoglutethimide is an aromatase inhibitor. Aminoglutethimide inhibits the enzymatic conversion of cholesterol to D5-pregnenolone, resulting in a decrease in the production of adrenal glucocorticoids, mineralocorticoids, estrogens, and androgens. It is used in the treatment of advanced breast cancer. Adrenal Steroid Synthesis Inhibitor (Code: N0000175928) Adrenal Steroid Synthesis Inhibitors (Code: N0000175921) antineoplastic agent (Code: CHEBI:35610) adrenergic agent (Code: CHEBI:37962) anticonvulsant (Code: CHEBI:35623) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Aromatase Inhibitors (Code: D047072) Enzyme Inhibitors (Code: D004791) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Steroid Synthesis Inhibitors (Code: D065088) 1980-10-29 FDA
Click to view pyrrocaine Pyrrocaine is the amide local anesthetics. Pyrrocaine provided to be somewhat less toxic than lidocaine. It has been classified as unsafe for use in acute porphyria. It was used as an infiltration and nerve block dental anesthetic in the 1960s and favored due to its rapid onset. It is no longer available.
Click to view lomustine DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) alkylation (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/017588s040lbl.pdf) Lomustine is an orally administered alkylating agent used alone and in combination with other antineoplastic agents in the treatment of several malignancies including Hodgkin disease, lymphoma, and brain cancer. Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) 1976-08-04 FDA
Click to view tymazoline Tymazoline is a nasal preparation. Tymazoline is a drug with antihistaminic and sympathomimetic properties. It locally reduces swelling, inflammation and mucosal secretions of the nasal passages. Tymazoline is used for the treatment of Inflammation of the lining of the nose and paranasal sinuses and allergic inflammation of nasopharyngeal.
Click to view symclosene Symclosene (trichloroisocyanuric acid) is an N-halo compound. It has been used primarily as a disinfectant in swimming pools and water treatment as bleaching agent and bactericide. And is also used as a bleaching agent in the textile industry. 1977-12-31 Health Canada
Click to view acitazanolast Acitazanolast is a leukotriene D4 antagonist. 2000 PMDA
Click to view sulbactam Beta-lactamase SHV-1 (Organism: Klebsiella pneumoniae, class: Enzyme, accessions: P0AD64, gene: bla, swissprot: BLA1_KLEPN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22974281) Beta-lactamase TEM (Organism: Escherichia coli, class: Enzyme, accessions: P62593, gene: bla, swissprot: BLAT_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10230627) Beta-lactamase (Organism: Serratia marcescens, class: Enzyme, accessions: P18539, gene: ampC, swissprot: AMPC_SERMA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10230627) Beta-lactamase (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: Q3SAW3, gene: bla(BEL1), swissprot: Q3SAW3_PSEAI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19884378) Sulbactam is a beta-lactamase inhibitor with very weak antibacterial action. The compound prevents antibiotic destruction of beta-lactam antibiotics by inhibiting beta-lactamases, thus extending their spectrum activity. Combinations of sulbactam with beta-lactam antibiotics have been used successfully for the therapy of infections caused by organisms resistant to the antibiotic alone. beta Lactamase Inhibitor (Code: N0000175930) beta Lactamase Inhibitors (Code: N0000000202) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) beta-Lactamase Inhibitors (Code: D065093) Enzyme Inhibitors (Code: D004791) 1986-12-31 FDA 0RN
Click to view hexobarbital Gamma-aminobutyric acid receptor subunit rho-1 (Organism: Homo sapiens, class: Ion channel, accessions: P24046, gene: GABRR1, swissprot: GBRR1_HUMAN)activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/7965056) Gamma-aminobutyric acid receptor subunit rho-2 (Organism: Homo sapiens, class: Ion channel, accessions: P28476, gene: GABRR2, swissprot: GBRR2_HUMAN)activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/7965056) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17487889) Hexobarbital is a barbiturate derivative having hypnotic and sedative effects. It was used in the 1940s-1950s as an agent for inducing anesthesia for surgery. Hexobarbital binds at a distinct binding site associated with a Cl- ionophore at the GABA-A receptor, increasing the duration of time for which the Cl- ionophore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) 1932-01-01 YEAR INTRODUCED
Click to view hopantenic acid Hopantenic acid is a central nervous system depressant. Hopantenic acid has a unique spectrum of pharmacological effects (nootropic, anticonvulsant, mild activating) in the absence of addiction, hyperstimulation or withdrawal syndrome 1979-11-12 Ministry of Health of the Russian Federation
Click to view riluzole Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020599s017lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020599s017lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19146924) Sodium channel protein type 2 subunit alpha (Organism: Rattus norvegicus, class: Ion channel, accessions: P04775, gene: Scn2a, swissprot: SCN2A_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/9703475) Intermediate conductance calcium-activated potassium channel protein 4 (Organism: Homo sapiens, class: Ion channel, accessions: O15554, gene: KCNN4, swissprot: KCNN4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18955585) Small conductance calcium-activated potassium channel protein 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UGI6, gene: KCNN3, swissprot: KCNN3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18955585) Small conductance calcium-activated potassium channel protein 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P70604, gene: Kcnn2, swissprot: KCNN2_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18955585) Small conductance calcium-activated potassium channel protein 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q92952, gene: KCNN1, swissprot: KCNN1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18955585) Short transient receptor potential channel 5 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UL62, gene: TRPC5, swissprot: TRPC5_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/24117252) Pteridine reductase 1 (Organism: Leishmania major, class: Enzyme, accessions: Q01782, gene: PTR1, swissprot: PTR1_LEIMA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21126022) Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21126022) Riluzole is a benzothiazole derivative with neuroprotective and potential anti-depressant and anxiolytic activities. While the mechanism of action of riluzole is unknown, its pharmacological activities in motor neurons include the following, some of which may be related to its effect: 1) an inhibitory effect on glutamate release, 2) inactivation of voltage-dependent sodium channels, and 3) interference with intracellular events that follow transmitter binding at excitatory amino acid receptors. Riluzole is used for therapy of amyotrophic lateral sclerosis. Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Neuroprotective Agents (Code: D018696) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) Benzothiazole (Code: N0000175740) Benzothiazoles (Code: N0000167094) 1995-12-12 FDA 657
Click to view cyclopentobarbital Cyclopentobarbital is a member of barbiturates. Cyclopentobarbital was used as a sedative and a hypnotic.
Click to view epirizole 4-Methoxy-2-(5-methoxy-3-methylpyrazol-1-yl)-6-methylpyrimidine. A pyrimidinyl pyrazole with antipyretic, analgesic, and anti-inflammatory activity. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view metisazone An antiviral agent effective against pox viruses. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998)
Click to view thiopental GABA-A receptor; anion channel (Organism: Rattus norvegicus, class: Ion channel, accessions: P62813|P23576|P20236|P28471|P19969|P30191|P15431|P63138|P63079|P18506|P23574|P18508|P28473|Q9ES14|O09028|Q91ZM7, gene: Gabra1|Gabra2|Gabra3|Gabra4|Gabra5|Gabra6|Gabrb1|Gabrb2|Gabrb3|Gabrd|Gabrg1|Gabrg2|Gabrg3|Gabre|Gabrp|Gabrq, swissprot: GBRA1_RAT|GBRA2_RAT|GBRA3_RAT|GBRA4_RAT|GBRA5_RAT|GBRA6_RAT|GBRB1_RAT|GBRB2_RAT|GBRB3_RAT|GBRD_RAT|GBRG1_RAT|GBRG2_RAT|GBRG3_RAT|GBRE_RAT|GBRP_RAT|Q91ZM7_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18619475) Thiopental is a barbiturate that is administered intravenously for the induction of general anesthesia or for the production of complete anesthesia of short duration. Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) drug allergen (Code: CHEBI:88188) anticonvulsant (Code: CHEBI:35623) sedative (Code: CHEBI:35717) intravenous anaesthetic (Code: CHEBI:38877) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) FDA EDP
Click to view cyclobarbital Cyclobarbital is a short-acting barbiturate exerting sedative-hypnotic properties. Cyclobarbital is metabolized to inactive ketocyclobarbital. Ccyclobarbital is regulated as a schedule III barbiturate. Cyclobarbital was used in combination with diazepam tranquilizer.
Click to view monoctanoin dissolution agent for retained cholesterol bile duct stones; RN in Chemline for octanoic acid, ester with 1,2,3-propanetriol, MF unknown: 11140-04-8; RN for octanoic acid, 2,3-dihydroxypropyl ester (1-monooctanoin): 502-54-5; RN in 9th CI Form Index for (+-)-1-monooctanoin: 19670-49-6 1985-10-29 FDA 480
Click to view stiripentol Sodium- and chloride-dependent GABA transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P30531, gene: SLC6A1, swissprot: SC6A1_HUMAN) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) In animal models, stiripentol antagonizes seizures induced by electric shock, pentetrazole and bicuculline. In rodent models, stiripentol appears to increase brain levels of gamma-aminobutyric acid (GABA) - the major inhibitory neurotransmitter in mammalian brain. This could occur by inhibition of synaptosomal uptake of GABA and/or inhibition of GABA transaminase. Stiripentol has also been shown to enhance GABAA receptor-mediated transmission in the immature rat hippocampus and increase the mean open-duration (but not the frequency) of GABAA receptor chloride channels by a barbiturate-like mechanism. Stiripentol potentiates the efficacy of other anticonvulsants, such as carbamazepine, sodium valproate, phenytoin, phenobarbital and many benzodiazepines, as the result of pharmacokinetic interactions. The second effect of stiripentol is mainly based on metabolic inhibition of several isoenzymes, in particular CYP450 3A4 and 2C19, involved in the hepatic metabolism of other anti-epileptic medicines. Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 2007-01-04 EMA
Click to view octacaine Octacaine is a para-amino-benzoic ester. Octacaine has anesthetic effect. It was synthesised in 1943 and was used as a surface anaesthetic.
Click to view meprylcaine Meprylcaine is a local anesthetic with stimulant properties that is structurally related to dimethocaine. Meprylcaine has a relatively potent inhibitory action on the monoamine transporter and inhibits the reuptake of dopamine, norepinephrine and serotonin. Meprylcaine was used as the hydrochloride salt by the dental profession and in dermatologic surgery for local anesthesia.
Click to view amylocaine Amylocaine is a first synthetic and non-addictive local anesthetic. Like all other local anesthetics, amylocaine acts as a membrane stabilizing drug that reversibly decreases the rate of depolarization and depolarization of excitable membranes. It was widely used for spinal anesthesia in Caesarean section. Now it is used for the topical pain relief in painful tooth eruption. 1981-02-09 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view carbamazepine Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/20526191) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/17045309) Sodium channel protein type 9 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q15858, gene: SCN9A, swissprot: SCN9A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/15285907) Carbamazepine is an anticonvulsant and specific analgesic used to control grand mal and psychomotor or focal seizures Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Mood Stabilizer (Code: N0000175751) Cytochrome P450 3A4 Inducers (Code: N0000185506) Cytochrome P450 1A2 Inducers (Code: N0000191266) Cytochrome P450 2B6 Inducers (Code: N0000187064) Cytochrome P450 2C9 Inducers (Code: N0000185507) Cytochrome P450 2C19 Inducers (Code: N0000185607) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) drug allergen (Code: CHEBI:88188) non-narcotic analgesic (Code: CHEBI:35481) analgesic (Code: CHEBI:35480) antimanic drug (Code: CHEBI:35477) anticonvulsant (Code: CHEBI:35623) glutamate transporter activator (Code: CHEBI:64370) Anticonvulsants (Code: D000927) Antimanic Agents (Code: D018692) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Cytochrome P-450 CYP3A Inducers (Code: D065701) Metabolic Side Effects of Drugs and Substances (Code: D065606) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) Tranquilizing Agents (Code: D014149) 1968-03-11 FDA
Click to view azapetine Azapetine is a benzazepine derivative. It is an alpha-1 adrenoceptor antagonist. It is a potent arterial vasodilator in the treatment of peripheral vascular diseases. It was used as an azapetine phosphate.
Click to view procainamide Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10192412) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634131) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10966924) Solute carrier family 22 member 4 (Organism: Homo sapiens, class: Transporter, accessions: Q9H015, gene: SLC22A4, swissprot: S22A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215651) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Solute carrier family 22 member 1 (Organism: Mus musculus, class: Unclassified, accessions: O08966, gene: Slc22a1, swissprot: S22A1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12176030) Procainamide is an oral antiarrhythmic agent that has been in wide use for more than 60 years for the medical treatment of cardiac arrhythmias. Long term procainamide therapy is known to induce hypersensitivity reactions, autoantibody formation and a lupus-like syndrome but is a rare cause of clinically apparent acute liver injury. Anti-Arrhythmia Agents (Code: D000889) anti-arrhythmia drug (Code: CHEBI:38070) platelet aggregation inhibitor (Code: CHEBI:50427) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) Antiarrhythmic (Code: N0000175426) 1950-06-02 FDA
Click to view carbocloral Carbocloral is a carbamate ester and is used as sedative and hypnotic drug.
Click to view picilorex Picilorex is an anorexic agent. It is no longer available.
Click to view isosorbide dinitrate Isosorbide dinitrate (ISDN) is an organic nitrate. Isosorbide dinitrate is converted to nitric oxide (NO), an active intermediate compound that activates the enzyme guanylate cyclase (atrial natriuretic peptide receptor A). The principal pharmacological action of isosorbide dinitrate is relaxation of vascular smooth muscle and consequent dilatation of peripheral arteries and veins, especially the latter. Dilatation of the veins promotes peripheral pooling of blood and decreases venous return to the heart, thereby reducing left ventricular end-diastolic pressure and pulmonary capillary wedge pressure (preload). Arteriolar relaxation reduces systemic vascular resistance, systolic arterial pressure, and mean arterial pressure (afterload). Dilatation of the coronary arteries also occurs. The relative importance of preload reduction, afterload reduction, and coronary dilatation remains undefined. Both metabolites of isosorbide dinitrate have biological activity. Isosorbide dinitrate is indicated for the prevention and for the treatment of angina pectoris due to coronary artery disease. (See: isosorbide mononitrate) vasodilator agent (Code: CHEBI:35620) Cardiovascular Agents (Code: D002317) Nitric Oxide Donors (Code: D020030) Vasodilator Agents (Code: D014665) Nitrate Vasodilator (Code: N0000175415) Nitrates (Code: N0000007647) Vasodilation (Code: N0000009909) 1959-11-09 FDA
Click to view didanosine Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72549, gene: pol, swissprot: Q72549_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021183s029lbl.pdf) A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. Didanosine is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA by binding to reverse transcriptase; ddI is then metabolized to dideoxyadenosine triphosphate, its putative active metabolite. antiviral drug (Code: CHEBI:36044) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antimetabolites (Code: D000963) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Noxae (Code: D009676) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175462) Nucleoside Analog (Code: N0000175459) Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009947) 1991-10-09 FDA 2DI
Click to view zileuton Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020471s017lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020471s017lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020471s017lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020471s017lbl.pdf) Zileuton is a specific inhibitor of 5-lipoxygenase and thus inhibits leukotriene (LTB4, LTC4, LTD4, and LTE4) formation. Both the R(+) and S(-) enantiomers are pharmacologically active as 5-lipoxygenase inhibitors in in vitro systems. Zileuton inhibits leukotriene-dependent smooth muscle contractions in vitro in human airways. In humans, pretreatment with zileuton attenuated bronchoconstriction caused by cold air challenge in patients with asthma. Zileuton is indicated for the prophylaxis and chronic treatment of asthma. 5-Lipoxygenase Inhibitor (Code: N0000175956) 5-Lipoxygenase Inhibitors (Code: N0000175955) Decreased Leukotriene Production (Code: N0000008683) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) leukotriene antagonist (Code: CHEBI:49159) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) anti-asthmatic drug (Code: CHEBI:49167) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Leukotriene Antagonists (Code: D020024) Lipoxygenase Inhibitors (Code: D016859) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1996-12-09 FDA
Click to view thioacetazone Thioacetazone is an oral antibiotic, which is used in the treatment of tuberculosis. Possible mechanism action of thioacetazone is interference with the metabolism of methionine of susceptible tubercle bacilli, which utilize methionine for nucleic acid synthesis. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antitubercular Agents (Code: D000995) 1971-12-31 Ministry of Health of the Russian Federation
Click to view butethamine Butethamine is an ester of the para-aminobenzoic acid. It is a local anesthetic formerly used in dentistry. Butethamine is probably a mild vasoconstrictor. It has diminished toxicity and increased the speed of action as compared with procaine.
Click to view procaine 5-hydroxytryptamine receptor 3A (Organism: Rattus norvegicus, class: Ion channel, accessions: P35563, gene: Htr3a, swissprot: 5HT3A_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7539114) Sodium channel protein type 10 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y5Y9, gene: SCN10A, swissprot: SCNAA_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/2167458) Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. Procaine is indicated for production of local or regional anesthesia, particularly for oral surgery. Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) local anaesthetic (Code: CHEBI:36333) central nervous system depressant (Code: CHEBI:35488) peripheral nervous system drug (Code: CHEBI:49110) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1954-07-01 FDA
Click to view dropropizine a peripheral antitussive Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141) Ministry of Health of the Russian Federation
Click to view agomelatine Melatonin receptor type 1A (Organism: Homo sapiens, class: GPCR, accessions: P48039, gene: MTNR1A, swissprot: MTR1A_HUMAN) agonist (Source: https://www.ema.europa.eu/documents/product-information/thymanax-epar-product-information_en.pdf) Melatonin receptor type 1B (Organism: Homo sapiens, class: GPCR, accessions: P49286, gene: MTNR1B, swissprot: MTR1B_HUMAN) agonist (Source: https://www.ema.europa.eu/documents/product-information/thymanax-epar-product-information_en.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.ema.europa.eu/documents/product-information/thymanax-epar-product-information_en.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/thymanax-epar-product-information_en.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/thymanax-epar-product-information_en.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/thymanax-epar-product-information_en.pdf) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12750432) Agomelatine is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors. Agomelatine is indicated for the treatment of major depressive episodes in adults. 2009-02-19 EMA AWY
Click to view tilbroquinol Tilbroquinol is a 8-hydroxyquinoline compound exerting antiprotozoal actions. The mechanism of action remains unknown. Tilbroquinol in combination with tiliquinol is indicated for the treatment of intestinal amebiasis. Some countries have withdrawn from the market products containing tilbroquinol because of the hepatoxicity. 1997-06-30 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view nitrofurantoin Nitrofurantoin is an oral antibiotic. Nitrofurantoin is reduced by a wide range of enzymes including bacterial flavoproteins to reactive intermediates which are damaging to macromolecules such as DNA and proteins. Nitrofurantoin is indicated for the treatment of urinary tract infections when due to susceptible strains of Escherichia coli, enterococci, Staphylococcus aureus, and certain susceptible strains of Klebsiella and Enterobacter species. Nitrofuran Antibacterial (Code: N0000175494) Nitrofurans (Code: N0000007658) antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076) 1953-02-06 FDA
Click to view rufinamide Sodium channel protein type 9 subunit alpha (Organism: Mus musculus, class: Unclassified, accessions: Q62205, gene: Scn9a, swissprot: SCN9A_MOUSE) modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/23221868) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) weak inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf) Rufinamide is a triazole derivative and an anticonvulsant medication to treat seizure disorders like Lennox-Gastuat syndrome, a form of childhood epilepsy. The results of in vitro studies suggest that the principal mechanism of action of rufinamide is modulation of the activity of sodium channels and, in particular, prolongation of the inactive state of the channel. Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 2007-01-16 EMA
Click to view dipyrocetyl Dipyrocetyl (2,3-diacetyloxybenzoic acid) is an analgesics and antipyretics. Dipyrocetyl possesses the anticoagulation properties, which may contribute directly to improve tissue integrity as well as indirectly by the prevention of activation of pro-inflammatory cytokines.
Click to view acefylline Acefylline is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. The mechanism of action is still not clear. Acefylline inhibits phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism and effects on intracellular calcium. It is used as acefylline piperazine for the treatment of bronchospasm caused by chronic bronchitis, asthma, emphysema.
Click to view pronilide Pronilide (acetylaminonitropropoxybenzene) is an anesthetic for topical use. Pronilide is used in the occurrence of inflammatory processes of the upper respiratory tract - tonsillitis, pharyngitis and laryngitis. 2007-04-20 Ministry of Health of the Russian Federation
Click to view felbamate Glutamate [NMDA] receptor (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q12879|Q13224|Q14957|O15399|Q8TCU5|O60391, gene: GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B, swissprot: NMDZ1_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMDE4_HUMAN|NMD3A_HUMAN|NMD3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020189s027lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/9314612/) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/9314612/) Felbamate is an antiepileptic. The mechanism by which felbamate exerts its anticonvulsant activity is unknown, but in animal test systems designed to detect anticonvulsant activity, felbamate has properties in common with other marketed anticonvulsants. Receptor-binding studies in vitro indicate that felbamate has weak inhibitory effects on GABA-receptor binding, benzodiazepine receptor binding, and is devoid of activity at the MK-801 receptor binding site of the NMDA receptor-ionophore complex. However, felbamate does interact as an antagonist at the strychnine-insensitive glycine recognition site of the NMDA receptor-ionophore complex. Felbamate is not indicated as a first line antiepileptic treatment. Felbamate is recommended for use only in those patients who respond inadequately to alternative treatments and whose epilepsy is so severe that a substantial risk of aplastic anemia and/or liver failure is deemed acceptable in light of the benefits conferred by its use. Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) neuroprotective agent (Code: CHEBI:63726) anticonvulsant (Code: CHEBI:35623) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1993-07-29 FDA
Click to view protheobromine Protheobromine is a derivative of the xanthine alkaloid theobromine. It was used as diuretic and vasodilator agent.
Click to view proxyphylline Proxyphylline is a xanthine derivative that acts as a cardiac stimulant, vasodilator and bronchodilator. Proxyphylline inhibits the cyclic nucleotide phosphodiesterases. In combination with ephedrine it is used for relief of acute bronchial asthma and for reversible bronchospasm associated with chronic bronchitis and emphysema. Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1994-09-01 PMDA
Click to view frovatriptan 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021006s022lbl.pdf) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021006s022lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021006s022lbl.pdf) Frovatriptan is a is a second generation triptan drug developed for the treatment of migraine headaches, in particular those associated with menstruation. Frovatriptan causes vasoconstriction of arteries and veins that supply blood to the head. The therapeutic activity of frovatriptan is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. Serotonin 1b Receptor Agonists (Code: N0000175763) Serotonin 1d Receptor Agonists (Code: N0000175764) Serotonin-1b and Serotonin-1d Receptor Agonist (Code: N0000175765) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) 2001-11-08 FDA
Click to view nealbarbital Nealbarbital. is a barbiturate derivative It is an effective sedative with only slight hypnotic action. It is no longer available. Nealbarbital is a schedule III drug in USA.
Click to view secobarbital Secobarbital is a barbituric acid derivative. Secobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. Secobarbital is used as a hypnotic (for the short-term treatment of insomnia, since it appears to lose its effectiveness for sleep induction and sleep maintenance after 2 weeks) and as a preanesthetic. Adjuvants, Anesthesia (Code: D000759) anaesthesia adjuvant (Code: CHEBI:60807) GABA modulator (Code: CHEBI:50268) sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) 1950-07-19 FDA
Click to view nomifensine Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT) Transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q63380, gene: NET, swissprot: Q63380_RAT) Transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q9WTR4, gene: Slc6a2, swissprot: Q9WTR4_RAT) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Hemoglobin HbA (Organism: Homo sapiens, class: Enzyme, accessions: P68871|P69905, gene: HBA1|HBB, swissprot: HBA_HUMAN|HBB_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: ) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: ) Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266) dopamine uptake inhibitor (Code: CHEBI:51039) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179)
Click to view metapramine Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q9R1M7|Q8VHN2, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3A_RAT|NMD3B_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9076749) Metapramine is a tetracyclic antidepressant. Metapramine is a low-affinity antagonist of the NMDA receptor complex channel. Its acting as a norepinephrine reuptake inhibitor without affecting the reuptake of serotonin and dopamine. Metapramine was used for the treatment of depression. It was withdrawn from market. Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1983 YEAR INTRODUCED
Click to view flosequinan an antihypertensive (vasodilator) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view phencyclidine Glutamate receptor ionotropic, NMDA 1 (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439, gene: Grin1, swissprot: NMDZ1_RAT Lysosomal Pro-X carboxypeptidase (Organism: Homo sapiens, class: Enzyme, accessions: P42785, gene: PRCP, swissprot: PCP_HUMAN Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN Muscarinic acetylcholine receptor (Organism: Mus musculus, class: GPCR, accessions: P12657|P32211|Q920H4|Q9ERZ3|Q9ERZ4, gene: Chrm1|Chrm2|Chrm3|Chrm4|Chrm5, swissprot: ACM1_MOUSE|ACM2_MOUSE|ACM3_MOUSE|ACM4_MOUSE|ACM5_MOUSE Glutamate receptor ionotropic, NMDA 2C (Organism: Rattus norvegicus, class: Ion channel, accessions: Q00961, gene: Grin2c, swissprot: NMDE3_RAT Cholinesterase (Organism: Mus musculus, class: Enzyme, accessions: Q03311, gene: Bche, swissprot: CHLE_MOUSE Glutamate NMDA receptor; GRIN1/GRIN2B (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q13224, gene: GRIN1|GRIN2B, swissprot: NMDE2_HUMAN|NMDZ1_HUMAN Glutamate NMDA receptor; GRIN1/GRIN2A (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q12879, gene: GRIN1|GRIN2A, swissprot: NMDE1_HUMAN|NMDZ1_HUMAN Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q8VHN2|Q9R1M7, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMD3A_RAT|NMD3B_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMDZ1_RAT Acetylcholine receptor subunit alpha (Organism: Torpedo californica, class: Ion channel, accessions: P02710, gene: CHRNA1, swissprot: ACHA_TORCA Glutamate [NMDA] receptor (Organism: Homo sapiens, class: Ion channel, accessions: O15399|O60391|Q05586|Q12879|Q13224|Q14957|Q8TCU5, gene: GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B, swissprot: NMD3A_HUMAN|NMD3B_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMDE4_HUMAN|NMDZ1_HUMAN Sigma non-opioid intracellular receptor 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: Q9R0C9, gene: Sigmar1, swissprot: SGMR1_RAT A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust. psychotropic drug (Code: CHEBI:35471) anaesthetic (Code: CHEBI:38867) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Hallucinogens (Code: D006213) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) 1PC
Click to view emorfazone Emorfazone is a pyridazinone NSAID with antipyretic, analgesic, anti-inflammatory properties. PMDA
Click to view moprolol Moprolol is a non-selective beta-blocker effective in reducing both blood and intraocular pressure. Levomoprolol is a active enantiomer. It was used for the treatment of hypertension and open-angle glaucoma.
Click to view isoetarine Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: ) Adrenergic beta-2 agonist used as bronchodilator for emphysema, bronchitis and asthma. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1979-10-23 FDA
Click to view iproclozide Iproclozide is an irreversible and selective hydrazine class based monoamine oxidase inhibitor. It was used as an antidepressant. It was withdrawn from the market. It is capable of causing fulminant hepatitis and its use has been documented as the cause for at least three reported fatalities.
Click to view benzphetamine Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) releasing agent Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) inhibitor Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) a sympathomimetic amine with pharmacologic activity similar to the prototype drugs of this class used in obesity, the amphetamines. Actions include central nervous system stimulation and elevation of blood pressure. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) sympathomimetic agent (Code: CHEBI:35524) dopamine uptake inhibitor (Code: CHEBI:51039) appetite depressant (Code: CHEBI:50507) adrenergic uptake inhibitor (Code: CHEBI:35640) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Appetite Suppression (Code: N0000175372) Increased Sympathetic Activity (Code: N0000175651) Sympathomimetic Amine Anorectic (Code: N0000175423) 1960-10-26 FDA
Click to view bupropion Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022108s014lbl.pdf) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022108s014lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022108s014lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022108s014lbl.pdf) Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991997) Neuronal acetylcholine receptor; alpha3/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P17787|P32297, gene: CHRNA3|CHRNB2, swissprot: ACHA3_HUMAN|ACHB2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991997) Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P30926|P32297, gene: CHRNA3|CHRNB4, swissprot: ACHA3_HUMAN|ACHB4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991997) 5-hydroxytryptamine receptor 3A (Organism: Mus musculus, class: Ion channel, accessions: P23979, gene: Htr3a, swissprot: 5HT3A_MOUSE) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27671323) Bupropion, an antidepressant of the aminoketone class, is chemically unrelated to tricyclic, tetracyclic, selective serotonin reuptake inhibitor, or other known antidepressant agents. Its structure closely resembles that of diethylpropion; it is related to phenylethylamines. The mechanism of action of bupropion is unknown, as is the case with other antidepressants. However, it is presumed that this action is mediated by noradrenergic and/or dopaminergic mechanisms. Bupropion is a relatively weak inhibitor of the neuronal uptake of norepinephrine and dopamine and does not inhibit monoamine oxidase or the reuptake of serotonin. Bupropion is indicated for the treatment of major depressive disorder (MDD) and seasonal affective disorder (SAD) and as an aid to smoking cessation. Aminoketone (Code: N0000180855) Increased Dopamine Activity (Code: N0000009282) Increased Norepinephrine Activity (Code: N0000009456) Norepinephrine Uptake Inhibitors (Code: N0000000102) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Cytochrome P-450 CYP2D6 Inhibitors (Code: D065690) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Enzyme Inhibitors (Code: D004791) Membrane Transport Modulators (Code: D049990) Metabolic Side Effects of Drugs and Substances (Code: D065606) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) 1985-12-30 FDA
Click to view dantron mild purgative anthraquinone derivative chemically related to emodin, the active principle of cascara and other naturally occurring products such as senna, aloes and rhubarb, it acts on the nerve endings of the myenteric plexus and stimulates the muscles of the large intestine Cathartics (Code: D002400) Gastrointestinal Agents (Code: D005765) Mutagens (Code: D009153) Noxae (Code: D009676) 1994-10-19 UK Medicines and Healthcare Products Regulatory Agency (MHRA) CHZ
Click to view fluindione Arachidonate 5-lipoxygenase (Organism: Rattus norvegicus, class: Enzyme, accessions: P12527, gene: Alox5, swissprot: LOX5_RAT) inhibitor (Source: https://www.sciencedirect.com/science/article/pii/S0960894X0080236X) Fluindione is an oral anticoagulant, belongs to the vitamin K antagonist class. It is indicated to treat the thromboembolic diseases, the deep venous thrombosis, and pulmonary embolism. Anticoagulants (Code: D000925) Hematologic Agents (Code: D006401) 1988-10-12 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view imiquimod Toll-like receptor 7 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q9NYK1, gene: TLR7, swissprot: TLR7_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14616353) Toll-like receptor 8 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q9NR97, gene: TLR8, swissprot: TLR8_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14616353) Imiquimod is a topically-applied aminoquinoline immune modulator that induces interferon production. It is used in the treatment of external genital and perianal warts, superficial carcinoma, basal cell; and actinic keratosis. Increased Cytokine Activity (Code: N0000009267) Increased Cytokine Production (Code: N0000009269) Adjuvants, Immunologic (Code: D000276) antineoplastic agent (Code: CHEBI:35610) interferon inducer (Code: CHEBI:36710) Antineoplastic Agents (Code: D000970) Immunologic Factors (Code: D007155) Interferon Inducers (Code: D007369) 1997-02-27 FDA 6T0
Click to view budralazine Budralazine is a vasodilator. Budralazine is a direct-acting vasodilator that does not produce marked tachycardia. It was used as an antihypertensive drug. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view buthalital Buthalital is a barbiturate derivative. It was under development as a short-acting anesthetic. Development was discontinued.
Click to view cropropamide component of prethcamide; same pharmacological activity as prethacamide
Click to view pheniramine Pheniramine is the histamine H1 antagonist with little sedative action. The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.It It is used in treatment of hay fever, rhinitis, allergic dermatoses, and pruritus. Anti-Allergic Agents (Code: D018926) Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1994-06-08 FDA
Click to view anethole trithione Choleretic used to allay dry mouth and constipation due to tranquilizers.
Click to view thiram Gamma-butyrobetaine dioxygenase (Organism: Homo sapiens, class: Enzyme, accessions: O75936, gene: BBOX1, swissprot: BODG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25266780) Monoglyceride lipase (Organism: Homo sapiens, class: Enzyme, accessions: Q99685, gene: MGLL, swissprot: MGLL_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19883085) Fatty-acid amide hydrolase 1 (Organism: Homo sapiens, class: Enzyme, accessions: O00519, gene: FAAH, swissprot: FAAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19883085) Thiram is tetramethylthiuram disulfide. Thiram belongs to the ethylene bisdithiocarbamate (EBDC) chemical class. In vivo studies indicate that it inactivates the enzyme glutathione reductase. It has mutagenic activity and may induce chromosomal aberrations. Thiram is used as a fungicide to prevent crop damage in the field and to prevent crops from deterioration in storage or transport. Thiram is also used as a seed, nut, fruit, and mushroom disinfectant from a variety of fungal diseases. In addition, it is used as an animal repellent to protect fruit trees and ornamentals from damage by rabbits, rodents, and deer. Thiram has been used in the treatment of human scabies, as a sun screen, and as a bactericide applied directly to the skin or incorporated into soap. antifungal agrochemical (Code: CHEBI:86328) antibacterial drug (Code: CHEBI:36047) antiseptic drug (Code: CHEBI:48218) Fungicides, Industrial (Code: D005659) Mutagens (Code: D009153) Noxae (Code: D009676) Pesticides (Code: D010575) Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131)
Click to view moxonidine Nischarin (Organism: Homo sapiens, class: Cytosolic other, accessions: Q9Y2I1, gene: NISCH, swissprot: NISCH_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15028616) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15028616) Moxonidine is a new-generation centrally acting antihypertensive drug approved for the treatment of mild to moderate essential hypertension. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) 2002-03-27 Italian Medicines Agency (AIFA)
Click to view nidroxyzone Nidroxyzone is a furan derivative and is a close relative of nitrofurazone. It is active against a number of other trypanosome infections, but it is inactive against T.cruzi.
Click to view benzoyl peroxide Benzoyl peroxide is an oxidizing agent with bactericidal and keratolytic effects, but the precise mechanism of action is unknown. In medicine, benzoyl peroxide is used as a topical treatment for acne, either in combination with antibiotics or as a single agent. Benzoyl peroxide is also used for bleaching flour or hair, teeth whitening, for cross-linking polyester resins, and many other chemical uses. It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system. Dermatologic Agents (Code: D003879) 1984-10-26 FDA
Click to view mexenone Mexenone is a benzophenone derivative. It was used as a sunscreen agent. It can cause contact and photocontact dermatitis.
Click to view fenoprofen Cyclooxygenase (Organism: Bos taurus, class: Enzyme, accessions: O62664|O62698, gene: PTGS1|PTGS2, swissprot: PGH1_BOVIN|PGH2_BOVIN) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: ) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: ) Sodium-coupled monocarboxylate transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q8N695, gene: SLC5A8, swissprot: SC5A8_HUMAN) inhibitor (Source: ) A propionic acid derivative that is used as a non-steroidal anti-inflammatory agent. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antipyretic (Code: CHEBI:35493) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1976-03-16 FDA PFN
Click to view myrtecaine Myrtecaine is an ester series local anasthetic. Myrtecain has a muscle relaxant effect. It is used by topical application for local pain relief. Also it is used in its lauryl sulfate form in combination with other active ingredients in the management of gastric pain and burning. 1976-09-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view methylsulfonal Methylsulfonal (trional) is chemically dietbylsulphomethylethylmethane. Methylsulfonal is a hypnotic which acts on the cortex of the brain. It was used for the treatment of insomnia in the end of XIX centry.
Click to view dixanthogen Dixanthogen is the oxidized product of xanthate. Dixanthogen is sulpfur containing drug wich was used against scabies, lice and other ectoparasites.
Click to view clofibrate clofibrate is a prodrug of clofibric acid which acts as an agonist of the PPAR-alpha receptor in muscle, liver, and other tissues. This agonism ultimately leads to modification in gene expression resulting in increased beta-oxidation, decreased triglyceride secretion, increased HDL, and increased lipoprotein lipase activity. Clofibrate was used for the treatment of hyperlipoproteinemias. Clofibrate was discontinued in 2002 due to adverse effects. (See: clofibric acid) anticholesteremic drug (Code: CHEBI:35821) antilipemic drug (Code: CHEBI:35679) Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) 1967-02-08 FDA
Click to view cytarabine DNA polymerase (alpha/delta/epsilon) (Organism: Homo sapiens, class: Enzyme, accessions: P09884|P28340|Q07864, gene: POLA1|POLD1|POLE, swissprot: DPOLA_HUMAN|DPOD1_HUMAN|DPOE1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209401s000lbl.pdf) Cytidine deaminase (Organism: Homo sapiens, class: Enzyme, accessions: P32320, gene: CDA, swissprot: CDD_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209401s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15204103) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitir (Source: https://www.ncbi.nlm.nih.gov/pubmed/15204103) Multidrug resistance-associated protein 7 (Organism: Homo sapiens, class: Transporter, accessions: Q5T3U5, gene: ABCC10, swissprot: MRP7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19118001) A pyrimidine nucleoside analog that is used mainly in the treatment of leukemia, especially acute non-lymphoblastic leukemia. Cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. Its actions are specific for the S phase of the cell cycle. It also has antiviral and immunosuppressant properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p472) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) Anti-Infective Agents (Code: D000890) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Antiviral Agents (Code: D000998) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Noxae (Code: D009676) Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) 1969-06-17 FDA AR3
Click to view taribavirin Taribavirin is an orally available prodrug of ribavirin, a synthetic nucleoside analog of ribofuranose with activity against a wide range of DNA and RNA viruses, especially the hepatitis C virus and influenza virus. Taribavirin is converted into ribavirin, which is incorporated into viral nucleic acid, thereby inhibiting viral RNA synthesis, inducing viral genome mutations, and inhibiting normal viral replication. (See: ribavirin)
Click to view molsidomine Guanylate cyclase soluble subunit alpha-2 (Organism: Homo sapiens, class: Enzyme, accessions: P33402, gene: GUCY1A2, swissprot: GCYA2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2983523) Molsidomine is an orally active, long-acting vasodilator, which belongs to the class of medications known as syndnones. It acts as nitric oxide donors and is a vasodilator that has been used in angina pectoris. Cardiovascular Agents (Code: D002317) Nitric Oxide Donors (Code: D020030) Vasodilator Agents (Code: D014665) 2005-12-16 Ministry of Health of the Russian Federation
Click to view tolperisone Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12695352) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12695352) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12695352) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12695352) Tolperisone is a centrally acting muscle relaxant. The precise mechanism of action is not known. Due to its membrane stabilising and local anaesthetic effects tolperisone inhibits conductance of the primary afferent nerve fibres, therefore inhibits spinal mono- and polysynaptic reflexes. Tolperisone inhibits reticulospinal reflex facilitation in the brain stem. In animal models tolperisone reduces decerebration muscle tone elevation and rigidity. Tolperisone increases peripheral blood circulation. Tolperisone is used for the treatment of spasticity and muscle spasms. Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 2004-07-05 Ministry of Health of the Russian Federation
Click to view pidotimod Toll-like receptor 2 (Organism: Homo sapiens, class: Membrane receptor, accessions: O60603, gene: TLR2, swissprot: TLR2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/23663325) Pidotimod is a synthetic dipeptide with immunomodulatory properties. Pidotimod is used in patients with cell-mediated immunodepression during respiratory and urinary tract infections. Adjuvants, Immunologic (Code: D000276) Immunologic Factors (Code: D007155) 1993-01-16 Italian Medicines Agency (AIFA)
Click to view etomidate Cytochrome P450 11B1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P15538, gene: CYP11B1, swissprot: C11B1_HUMAN) Cytochrome P450 11B2, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P19099, gene: CYP11B2, swissprot: C11B2_HUMAN) Acetylcholine receptor subunit delta (Organism: Torpedo californica, class: Ion channel, accessions: P02718, gene: chrnd, swissprot: ACHD_TORCA) GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive modulator (Source: ) GABA A receptor alpha-2/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P47869|P47870, gene: GABRA2|GABRB2|GABRG2, swissprot: GBRA2_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) Gamma-aminobutyric acid receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P14867, gene: GABRA1, swissprot: GBRA1_HUMAN) a general anesthetic without analgesic activity; imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic. General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) intravenous anaesthetic (Code: CHEBI:38877) sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1982-09-07 FDA
Click to view biotin Sodium-dependent multivitamin transporter (Organism: Homo sapiens, class: Transporter, accessions: Q9Y289, gene: SLC5A6, swissprot: SC5A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20980265) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/15333708) Biotin (vitamin H or B7 or coenzyme R) is an enzyme co-factor present in minute amounts in every living cell. It occurs mainly bound to proteins or polypeptides and is abundant in liver, kidney, pancreas, yeast, and milk. Biotin deficiency is associated with neurological manifestations, skin rash, hair loss and metabolic disturbances that are thought to relate to the various carboxylase deficiencies (metabolic ketoacidosis with lactic acidosis). Biotin acts as a carboxyl carrier in carboxylation reactions. Human cells accumulate biotin by using both the sodium-dependent multivitamin transporter and monocarboxylate transporter 1. These transporters and other biotin-binding proteins partition biotin to compartments involved in biotin signaling: cytoplasm, mitochondria, and nuclei. The activity of cell signals such as biotinyl-AMP, Sp1 and Sp3, nuclear factor (NF)-kappaB, and receptor tyrosine kinases depends on biotin supply. Consistent with a role for biotin and its catabolites in modulating these cell signals, greater than 2000 biotin-dependent genes have been identified in various human tissues. B vitamin (Code: CHEBI:75769) nutraceutical (Code: CHEBI:50733) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) 1953-02-20 FDA BTN
Click to view amidefrine Amidephrine is an alpha-sympathomimetic that causes vasoconstriction. It reduces swelling and congestion when applied to mucous membrane. Amidephrine is used in mesilate form for the treatment of ccute and chronic rhinitis, vasomotor and allergic rhinitis. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Neurotransmitter Agents (Code: D018377) 1969-02-06 Austrian Medicines and Medical Devices Agency
Click to view xylometazoline Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9632357) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9632357) A nasal vasoconstricting decongestant drug which acts by binding to the same receptors as adrenaline. It is applied as a spray or as drops into the nose to ease inflammation and congestion of the nasal passageways. Cardiovascular Agents (Code: D002317) Nasal Decongestants (Code: D014663) Respiratory System Agents (Code: D019141) Vasoconstrictor Agents (Code: D014662) FDA
Click to view isoaminile Isoaminile is a cough suppressant that acts by influencing the cough centre. It is no longer available. Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141) Italian Medicines Agency (AIFA)
Click to view clodronic acid Solute carrier family 17 member 9 (Organism: Homo sapiens, class: Transporter, accessions: Q9BYT1, gene: SLC17A9, swissprot: S17A9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28720702) Clodronic Acid is a first-generation bisphosphonate with anti-resorptive and anti-hypercalcemic activities. Clodronic acid adsorbs onto the surface of the hydroxyapatite crystals in bone matrix. Although the exact mechanism through which clodronic acid exerts its cytotoxic effect on osteoclasts has yet to be fully elucidated, this agent is metabolized intracellularly to a toxic beta-gamma-methylene analog of adenosine triphosphate (ATP), AppCCl2p. The ATP analog AppCCl2p competitively inhibits ADP/ATP translocase, thereby interfering with mitochondrial membrane potential and cellular energy metabolism. This may cause osteoclast apoptosis and, eventually, inhibiting osteoclast-mediated bone resorption. Clodronic acid is indicated in the management of osteolytic lesions, hypercalcemia and bone pain associated with skeletal metastases in patients with carcinoma of the breast or multiple myeloma. Clodronic acid is also indicated for the maintenance of clinically acceptable serum calcium levels in patients with hypercalcemia of malignancy initially treated with an intravenous bisphosphonate. bone density conservation agent (Code: CHEBI:50646) antineoplastic agent (Code: CHEBI:35610) Bone Density Conservation Agents (Code: D050071) 1986-01-01 YEAR INTRODUCED
Click to view apraclonidine Adrenergic receptor alpha-1 (Organism: Homo sapiens, class: GPCR, accessions: P35348|P35368|P25100, gene: ADRA1A|ADRA1B|ADRA1D, swissprot: ADA1A_HUMAN|ADA1B_HUMAN|ADA1D_HUMAN) partial agonist (Source: https://pdf.hres.ca/dpd_pm/00044397.PDF) Adrenergic receptor alpha-2 (Organism: Homo sapiens, class: GPCR, accessions: P08913|P18089|P18825, gene: ADRA2A|ADRA2B|ADRA2C, swissprot: ADA2A_HUMAN|ADA2B_HUMAN|ADA2C_HUMAN) partial agonist (Source: https://pdf.hres.ca/dpd_pm/00044397.PDF) Apraclonidine is an alpha adrenergic agonist. Apraclonidine is a relatively selective, alpha adrenergic agonist and does not have significant membrane stabilizing (local anesthetic) activity. Apraclonidine is indicated to control or prevent post-surgical elevations in intraocular pressure that occur in patients after pphthalmic laser therapy. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-2 Receptor Agonists (Code: D058647) Adrenergic alpha-Agonists (Code: D000316) ophthalmology drug (Code: CHEBI:66981) beta-adrenergic agonist (Code: CHEBI:35522) diagnostic agent (Code: CHEBI:33295) alpha-adrenergic agonist (Code: CHEBI:35569) antiglaucoma drug (Code: CHEBI:39456) Neurotransmitter Agents (Code: D018377) 1987-12-31 FDA
Click to view menadoxime Menadoxime has antihemorrhagic activity.
Click to view ramifenazone Ramifenazone is an analgesic, antipyretic, and anti-inflammatory agent.
Click to view dezocine Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) antagonist (Source: ) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) partial agonist (Source: ) potent analgesic Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) opioid analgesic (Code: CHEBI:35482) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) FDA
Click to view oxolamine Oxolamine has antitussive, anti-inflammatory and spasmolytic action. Oxolamine is used as a cough suppressant for the treatment of pharyngitis, tracheitis, bronchitis, bronchiectasis, pertussis. Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141) 1962 Italian Medicines Agency (AIFA)
Click to view pinacidil Sulfonylurea receptor 2, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: O60706|Q14654, gene: ABCC9|KCNJ11, swissprot: ABCC9_HUMAN|KCJ11_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/9692785) Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) agonist (Source: https://link.springer.com/article/10.1007/s11434-012-5035-0) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11851418) Pinacidil is a cyanoguanidine drug that acts by opening ATP-sensitive potassium channels, leading to peripheral vasodilatation of arterioles and decreasing peripheral vascular resistance. The above processes result in reduced blood pressure. It was used for the treatment of hypertension. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) 1989-12-28 FDA
Click to view guanfacine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022037s018lbl.pdf) Guanfacine is a central alpha2A-adrenergic receptor agonist. Guanfacine is not a central nervous system (CNS) stimulant. Guanfacine is indicated for the management of hypertension. Guanfacine is indicated for the threatment of Attention Deficit Hyperactivity Disorder but the mechanism of action of guanfacine in this disorder is not known. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-2 Receptor Agonists (Code: D058647) Adrenergic alpha-Agonists (Code: D000316) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Adrenergic alpha2-Agonists (Code: N0000009918) Central alpha-2 Adrenergic Agonist (Code: N0000175554) 1986-10-27 FDA
Click to view floxuridine Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18652477) Thymidine phosphorylase (Organism: Homo sapiens, class: Enzyme, accessions: P19971, gene: TYMP, swissprot: TYPH_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18652477) Floxuridine is an antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract. (See: fluorouracil) radiosensitizing agent (Code: CHEBI:132992) antineoplastic agent (Code: CHEBI:35610) antiviral drug (Code: CHEBI:36044) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Noxae (Code: D009676) Antimetabolite (Code: N0000180853) Deoxyuridine (Code: N0000007770) 1970-12-18 FDA
Click to view doxifluridine Doxifluridine is a 5-fluorouracil (5-FU) prodrug. After oral administration it is metabolised to 5-FU by intestinal pyrimidine nucleoside phosphorylase. Doxifluridine is used for the treatment of gastric cancer. (See: fluorouracil) antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Appetite Stimulants (Code: D019167) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Noxae (Code: D009676) 1987-01-01 YEAR INTRODUCED
Click to view nifurpirinol Nifurpirinol is an antibacterial agent. It is active against many species of bacteria, including Vibrio anguilIarum, Aeromonas salmonicida, and Aeromonas liquefaciens. It is used in veterinary.
Click to view pethidine Mu-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P97266, gene: OPRM1, swissprot: OPRM_CAVPO) Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT) Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: ) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Opioid receptor (Organism: Mus musculus, class: GPCR, accessions: O55242|P32300|P33534|P42866, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_MOUSE|OPRK_MOUSE|OPRM_MOUSE|SGMR1_MOUSE) Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT) Glutamate receptor ionotropic, NMDA 3A (Organism: Homo sapiens, class: Ion channel, accessions: Q8TCU5, gene: GRIN3A, swissprot: NMD3A_HUMAN Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) A narcotic analgesic that can be used for the relief of most types of moderate to severe pain, including postoperative pain and the pain of labor. Prolonged use may lead to dependence of the morphine type; withdrawal symptoms appear more rapidly than with morphine and are of shorter duration. Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) Adjuvants, Anesthesia (Code: D000759) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1942-11-10 FDA
Click to view azanidazole Azanidazole is a nitroimidazole derivative. It has trichomonicidal activity. Azanidazole appears to act on bacterial cellular metabolism. It is used both topically and systemicall for the treatment of Trichomonas vaginalis. 1977-07-01 Italian Medicines Agency (AIFA)
Click to view methylphenobarbital Methylphenobarbital is a barbiturate derivative used primary as an anticonvulsant in combination with phenytoin, but also as a sedative and anxiolytic. Methylphenobarbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. Marketing of methylphenobarbital was discontinued in 2012. anticonvulsant (Code: CHEBI:35623) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) 1952-06-23 Italian Medicines Agency (AIFA)
Click to view busulfan DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) other (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020954s014lbl.pdf) Glutathione S-transferase A1 (Organism: Homo sapiens, class: Enzyme, accessions: P08263, gene: GSTA1, swissprot: GSTA1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8886613) Glutathione S-transferase P (Organism: Homo sapiens, class: Enzyme, accessions: P09211, gene: GSTP1, swissprot: GSTP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8886613) Busulfan is a bifunctional alkylating agent. Busulfan is known chemically as 1,4-butanediol dimethanesulfonate. Busulfan is not a structural analog of the nitrogen mustards. Busulfan is indicated for the palliative treatment of chronic myelogenous (myeloid, myelocytic, granulocytic) leukemia. Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) insect sterilant (Code: CHEBI:67105) antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Myeloablative Agonists (Code: D019653) Noxae (Code: D009676) 1954-06-26 FDA
Click to view parsalmide anti-inflammatory analgesic with possible antianxiety action
Click to view nefiracetam antagonizes amnestic effects of picrotoxin or bicuculline; structure given in first source Central Nervous System Agents (Code: D002491) Neuroprotective Agents (Code: D018696) Nootropic Agents (Code: D018697) Protective Agents (Code: D020011) Psychotropic Drugs (Code: D011619)
Click to view milnacipran Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022256s023lbl.pdf) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022256s023lbl.pdf) Milnacipran is a selective serotonin and norepinephrine reuptake inhibitor. Milnacipran was originally developed for and continues to be approved and indicated for the treatment of depression. Furthermore, the US FDA approved milnacipran for the additional indication of treating fibromyalgia. Norepinephrine Uptake Inhibitors (Code: N0000000102) Serotonin and Norepinephrine Reuptake Inhibitor (Code: N0000175749) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) 2009-01-14 FDA
Click to view mepivacaine Sodium channel protein type 10 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y5Y9, gene: SCN10A, swissprot: SCNAA_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/20044988) Potassium channel subfamily K member 3 (Organism: Homo sapiens, class: Ion channel, accessions: O14649, gene: KCNK3, swissprot: KCNK3_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/10201682) Mepivacaine is an amide-type local anesthetic agent. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168) Amide Local Anesthetic (Code: N0000175682) Amides (Code: N0000007681) Local Anesthesia (Code: N0000175976) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) local anaesthetic (Code: CHEBI:36333) drug allergen (Code: CHEBI:88188) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1960-01-06 FDA
Click to view guanoxabenz Guanoxabenz is a metabolite of guanabenz. It was used for the treatment of hypertension.
Click to view pyridoxal phosphate P2X purinoceptor 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P49653, gene: P2rx2, swissprot: P2RX2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) Low molecular weight phosphotyrosine protein phosphatase (Organism: Homo sapiens, class: Enzyme, accessions: P24666, gene: ACP1, swissprot: PPAC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24035092) Pyridoxal Phosphate is the active form of vitamin B6 and a coenzyme for many pyridoxal phosphate (PLP)-dependent enzymes and for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. Pyridoxal Phosphate can be used as a dietary supplement in cases of vitamin B6 deficiency. Reduced levels of pyridoxal phosphate in the brain can cause neurological dysfunction. Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) 1968-12-01 PMDA PLP
Click to view emtricitabine Emtricitabine 5'-triphosphate: Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021500s029lbl.pdf) Emtricitabine: Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17172311) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17172311) Canalicular multispecific organic anion transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: O15438, gene: ABCC3, swissprot: MRP3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17172311) Emtricitabine is a synthetic fluoro derivative of thiacytidine with potent antiviral activity. The chemical classification of emtricitabine is Nucleoside Analog. Emtricitabine is phosphorylated to form emtricitabine 5'-triphosphate within the cell. This metabolite inhibits the activity of human immunodeficiency virus (HIV) reverse transcriptase both by competing with the natural substrate deoxycytidine 5'-triphosphate and by incorporation into viral DNA causing a termination of DNA chain elongation (due to the lack of the essential 3'-OH group). Emtricitabine is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175462) Nucleoside Analog (Code: N0000175459) Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009947) antiviral drug (Code: CHEBI:36044) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 2003-07-02 FDA ETV
Click to view tinidazole Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021618s006lbl.pdf) Tinidazole is a 5-nitroimidazole derivative, broad spectrum antimicrobial agent used in the treatment of bacterial, protozoal and parasitic infections. Chemically reduced tinidazole was shown to release nitrites and cause damage to purified bacterial DNA in vitro. Nitroimidazole Antimicrobial (Code: N0000175435) Nitroimidazoles (Code: N0000007663) Alkylating Agents (Code: D000477) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Antitrichomonal Agents (Code: D000994) Noxae (Code: D009676) 2004-05-17 FDA
Click to view ciclonicate antilipolytic & myolytic; RN given refers to trans-isomer 1978 YEAR INTRODUCED
Click to view ketobemidone Opioid receptor (Organism: Mus musculus, class: GPCR, accessions: O55242|P32300|P33534|P42866, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_MOUSE|OPRK_MOUSE|OPRM_MOUSE|SGMR1_MOUSE) Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) Glutamate receptor ionotropic, NMDA 3A (Organism: Homo sapiens, class: Ion channel, accessions: Q8TCU5, gene: GRIN3A, swissprot: NMD3A_HUMAN) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) Opioid Analgesics Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Narcotics (Code: D009294) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1947-01-01 YEAR INTRODUCED
Click to view butidrine Butidrine is naphthalenemethanol devivative with beta-adrenolytic, antiarrhythmic, and local anesthetic properties having sympatholytic and antiarrhythmic effects.
Click to view triflusal inhibits platelet aggregation similarly to aspirin Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) 2001-01-07 CDSCO (INDIA)
Click to view amoscanate Indicated in treatment of adult hookworm infestation only. Anthelmintics (Code: D000871) schistosomicide drug (Code: CHEBI:38941) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Filaricides (Code: D005369) Schistosomicides (Code: D012556) 1985-11-01 CDSCO (INDIA)
Click to view enoximone Phosphodiesterase 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q14432|Q13370, gene: PDE3A|PDE3B, swissprot: PDE3A_HUMAN|PDE3B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1386515) Phosphodiesterase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27815|Q07343|Q08493|Q08499, gene: PDE4A|PDE4B|PDE4C|PDE4D, swissprot: PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1386515) Enoximone is a selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with congestive heart failure. Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Phosphodiesterase 3 Inhibitors (Code: D058987) Phosphodiesterase Inhibitors (Code: D010726) Protective Agents (Code: D020011) Vasodilator Agents (Code: D014665) 1987-10-27 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view dapsone 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23787290) Dapsone is a sulfone active against a wide range of bacteria but mainly employed for its actions against Mycobacterium Leprae. Its mechanism of action is probably similar to that of the sulfonamides which involves inhibition of folic acid synthesis in susceptible organisms. It is also used with pyrimethamine in the treatment of malaria. Sulfone (Code: N0000175881) Sulfones (Code: N0000008053) antimalarial (Code: CHEBI:38068) leprostatic drug (Code: CHEBI:35816) antiinfective agent (Code: CHEBI:35441) anti-inflammatory drug (Code: CHEBI:35472) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) Leprostatic Agents (Code: D007917) 1979-07-03 FDA
Click to view piridocaine Piridocaine is a piperidyl propanol ester of orthoaminobenzoic acid. The toxicity of this drug resembles that of procaine. It differs from procaine in that the minimum anesthetic dose is smaller, the minimal lethal dose larger, and duration of anesthesia longer. It was used as an local anesthetic.
Click to view pindolol Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) partial agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/018285s034lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) partial agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/018285s034lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) partial agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/018285s034lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9550290) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12606755) Pindolol is a non-selective beta-adrenergic antagonist (beta-blocker) which possesses intrinsic sympathomimetic activity. In addition, this agent blocks serotonin (5-HT) 1A receptors, thereby increasing the available serotonin in the brain. Pindolol is used for the therapy of hypertension and angina pectoris. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) serotonergic antagonist (Code: CHEBI:48279) beta-adrenergic antagonist (Code: CHEBI:35530) antiglaucoma drug (Code: CHEBI:39456) antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Vasodilator Agents (Code: D014665) 1982-09-03 FDA
Click to view bunitrolol Bunitrolol is a non-cardioselective beta-blocker with sympathomimetic action.
Click to view pirprofen Pirprofen is a non-steroidal anti-inflammatory drug. Pirprofen was was used for the treatment for rheumatic diseases. In 1990 due to adverse effects, including some cases of fatal liver toxicity the manufacturers decided to discontinue marketing it worldwide. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1982-01-01 YEAR INTRODUCED
Click to view trimecaine Trimecaine is an organic compound used as a local anesthetic and cardial antiarrhythmic. Trimecaine decreases the cell membrane permeability, causes depolarization and shortens the action potential. Trimecaine is used for the local anesthesia and for the treatment of ventriculous arrhytmia on myocardial infarction. Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1964-04-30 Ministry of Health of the Russian Federation
Click to view pyrimethamine Bifunctional dihydrofolate reductase-thymidylate synthase (Organism: Plasmodium falciparum, class: Enzyme, accessions: P13922, gene: None, swissprot: DRTS_PLAFK) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23035243) Bifunctional dihydrofolate reductase-thymidylate synthase (Organism: Toxoplasma gondii, class: Enzyme, accessions: Q07422, gene: None, swissprot: DRTS_TOXGO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27994750) Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27994750) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20065018) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20065018) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20065018) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20065018) Pyrimethamine is an antiparasitic agent. Pyrimethamine is a folic acid antagonist and the rationale for its therapeutic action is based on the differential requirement between host and parasite for nucleic acid precursors involved in growth. This activity is highly selective against Toxoplasma gondii. The action of pyrimethamine against Toxoplasma gondii is greatly enhanced when used in conjunction with sulfonamides. Pyrimethamine is indicated for the treatment of toxoplasmosis when used conjointly with a sulfonamide. Also pyrimethamine is indicated in combination with sulfadoxine for the treatment and prevention of malaria. Dihydrofolate Reductase Inhibitor Antimalarial (Code: N0000175934) Dihydrofolate Reductase Inhibitors (Code: N0000000191) antimalarial (Code: CHEBI:38068) antiprotozoal drug (Code: CHEBI:35820) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) 1953-01-23 FDA CP6
Click to view alprenolol 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Beta-2 adrenergic receptor (Organism: Bos taurus, class: GPCR, accessions: Q28044, gene: ADRB2, swissprot: ADRB2_BOVIN) Squalene synthase (Organism: Rattus norvegicus, class: Enzyme, accessions: Q02769, gene: Fdft1, swissprot: FDFT_RAT) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/12388666) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/12388666) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT) One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) anti-arrhythmia drug (Code: CHEBI:38070) antihypertensive agent (Code: CHEBI:35674) beta-adrenergic antagonist (Code: CHEBI:35530) sympatholytic agent (Code: CHEBI:66991) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1966-01-01 YEAR INTRODUCED JTZ
Click to view alendronic acid Farnesyl pyrophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P14324, gene: FDPS, swissprot: FPPS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10620343) Receptor-type tyrosine-protein phosphatase epsilon (Organism: Mus musculus, class: Enzyme, accessions: P49446, gene: Ptpre, swissprot: PTPRE_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8610169) Tyrosine-protein phosphatase non-receptor type 4 (Organism: Homo sapiens, class: Enzyme, accessions: P29074, gene: PTPN4, swissprot: PTN4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9310349) Alendronic acid is a synthetic analog of pyrophosphate that bind to the hydroxyapatite found in bone. Alendronic acid acts as a specific inhibitor of osteoclast-mediated bone resorption. Alendronic acid is indicated for the treatment of osteoporosis in postmenopausal women and for the treatment to increase bone mass in men with osteoporosis. bone density conservation agent (Code: CHEBI:50646) Bone Density Conservation Agents (Code: D050071) Bisphosphonate (Code: N0000175579) Diphosphonates (Code: N0000007707) 1995-09-29 FDA 212
Click to view cinchophen Proto-oncogene c-Fos (Organism: Rattus norvegicus, class: Unclassified protein, accessions: P12841, gene: Fos, swissprot: FOS_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/8981440) Cinchophen is a phenylcinchoninic acid. It was used fir the treatment of gout as well as for other forms of arthritis and for the relief of pain of all types. It was withdrawn due to the discovery that it can cause serious liver damage. 1908 YEAR INTRODUCED
Click to view flunoxaprofen Flunoxaprofen is a nonsteroidal anti-inflammatory drug (NSAID). It is an arylalkanoic acid derivative. Flunoxaprofen inhibits leukotriene rather than prostaglandin synthesis. It was used for the treatment of rheumatoid arthritis and osteoarthritis. Flunoxaprofen was withdrawn from clinical use because of concerns of potential hepatotoxicity. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) antirheumatic drug (Code: CHEBI:35842) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Italian Medicines Agency (AIFA)
Click to view sulfapyridine Sulfapyridine is a sulfonamide antibiotic. Sulfapyridine is a competitive inhibitor of the bacterial enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid by means of processing the substrate para-aminobenzoic acid (PABA). It was used to treat of infections in humans in particular, dermatitis herpetiformis (Duhring's disease), a skin problem, but that usage was discontinued by manufacturer. It is also known, that sulfapyridine is one of the two primary metabolite of the anti-inflammatory drug salicylazosulfapyridine. antiinfective agent (Code: CHEBI:35441) dermatologic drug (Code: CHEBI:50177) Anti-Infective Agents (Code: D000890) Dermatologic Agents (Code: D003879) 1939-03-09 FDA SFY
Click to view erdosteine Erdosteine is an antioxidant compound. Erdosteine acts as a free radicals scavenger (through the formation of the active metabolite I, N-thiodiglycolylhomocysteine). Also the drug effect may be due to the inhibition of the activity of elastase enzyme and its interaction with mucosa. It is used as a nexpectorant for the treatment of chronic bronchitis and chronic obstructuve pulmonary disease. Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) 1993-08-24 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view epinastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: ) Histamine H1 receptor (Organism: Cavia porcellus, class: GPCR, accessions: P31389, gene: HRH1, swissprot: HRH1_CAVPO) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell, indicated for the prevention of itching associated with allergic conjunctivitis anti-allergic agent (Code: CHEBI:50857) histamine antagonist (Code: CHEBI:37956) ophthalmology drug (Code: CHEBI:66981) H1-receptor antagonist (Code: CHEBI:37955) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) Adrenergic Agonists (Code: N0000000122) Adrenergic Receptor Agonist (Code: N0000175883) Decreased Histamine Release (Code: N0000175628) Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Inhibitor (Code: N0000175519) 2003-10-16 FDA
Click to view mabuprofen Mabuprofen is an amide prodrug of ibuprofen. It is used for topical treatment of various painful processes that occur with inflammation. (See: ibuprofen) 1989-04-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view benzoctamine Benzoctamine is a tetracyclic compound and is very closely related structurally to the maprotiline, differing only in the length of their side chain. Benzoctamine can be used as a sedative which does not depress the respiratory system, but rather stimulates it. It can also be used as an anxiolytic with the same efficacy as chlordiazepoxide for treating anxiety neurosis.
Click to view diflunisal Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/018445s058lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/018445s058lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991954) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18819808) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18819808) UDP-glucuronosyltransferase 1-8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW9, gene: UGT1A8, swissprot: UD18_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10497143) Diflunisal is a non-steroidal drug with analgesic, anti-inflammatory and antipyretic properties. Diflunisal is a difluorophenyl derivative of salicylic acid. It is a peripherally-acting non-narcotic analgesic drug. Diflunisal is a prostaglandin synthetase inhibitor. The precise mechanism of the analgesic and anti-inflammatory actions of diflunisal is not known. Diflunisal is indicated for acute or long-term use for symptomatic treatment of mild to moderate pain, osteoarthritis and rheumatoid arthritis. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) 1982-04-19 FDA 1FL
Click to view nefopam Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22711801) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22711801) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22711801) Sodium-dependent noradrenaline transporter (Organism: Mus musculus, class: Transporter, accessions: O55192, gene: Slc6a2, swissprot: SC6A2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7507578) Sodium-dependent serotonin transporter (Organism: Mus musculus, class: Transporter, accessions: Q60857, gene: Slc6a4, swissprot: SC6A4_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7507578) Nefopam is a centrally acting analgesic with a rapid onset of action. The main site of action appears to be in the central nervous system both at the brain and spinal levels. Unlike the narcotic agents, Nefopam has been shown not to cause respiratory depression. It is indicated for the relief of acute and chronic pain, including post-operative pain, dental pain, musculo-skeletal pain, acute traumatic pain and cancer pain. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) adrenergic uptake inhibitor (Code: CHEBI:35640) dopamine uptake inhibitor (Code: CHEBI:51039) non-narcotic analgesic (Code: CHEBI:35481) serotonin uptake inhibitor (Code: CHEBI:50949) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1980-05-15 New Zealand Medicines and Medical Devices Safety Authority
Click to view metesculetol Metesculetol is a vitamin P derivative. It increases capillary resistance and reduces membrane permeability. Permethol is for damaged gums and helps to stop gum bleeding, relieves inflammation and nourishes the gum tissues. It is used as a component of products for oral cavity care.
Click to view olprinone Olprinone is a cardiotonic agent. Mechanism of action of olprinone is selective inhibition of PDE III specific to cAMP. Olprinone is used for treatment acute heart failure. Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Phosphodiesterase 3 Inhibitors (Code: D058987) Phosphodiesterase Inhibitors (Code: D010726) Protective Agents (Code: D020011) 1996-04-01 PMDA
Click to view sulfadiazine Dihydrofolate synthetase (Organism: Arabidopsis thaliana, class: Enzyme, accessions: F4JYE9, gene: DHFS, swissprot: DHFS_ARATH) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9127492) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843491) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843491) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15843491) Sulfadiazine is a synthetic pyrimidinyl sulfonamide derivative, short-acting bacteriostatic Sulfadiazine inhibits bacterial folic acid synthesis by competing with para amino benzoic acid. It is used in combination with pyrimethamine to treat toxoplasmosis in patients with acquired immunodeficiency syndrome and in newborns with congenital infections. Sulfonamide Antibacterial (Code: N0000175503) Sulfonamides (Code: N0000008048) coccidiostat (Code: CHEBI:35818) antiinfective agent (Code: CHEBI:35441) antiprotozoal drug (Code: CHEBI:35820) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Coccidiostats (Code: D003049) 1941-08-11 FDA
Click to view heptabarb It was used for the treatment of insomnia, discontinued
Click to view methaqualone GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26056160) GABA-A receptor alpha-1/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P28472, gene: GABRA1|GABRB3|GABRG2, swissprot: GBRA1_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26056160) GABA A receptor alpha-2/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P47869|P47870, gene: GABRA2|GABRB2|GABRG2, swissprot: GBRA2_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26056160) GABA A receptor alpha-3/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P34903|P47870, gene: GABRA3|GABRB2|GABRG2, swissprot: GBRA3_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26056160) GABA A receptor alpha-4/beta-2/delta (Organism: Homo sapiens, class: Ion channel, accessions: O14764|P47870|P48169, gene: GABRA4|GABRB2|GABRD, swissprot: GBRA4_HUMAN|GBRB2_HUMAN|GBRD_HUMAN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26056160) GABA A receptor alpha-4/beta-3/delta (Organism: Homo sapiens, class: Ion channel, accessions: O14764|P28472|P48169, gene: GABRA4|GABRB3|GABRD, swissprot: GBRA4_HUMAN|GBRB3_HUMAN|GBRD_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/26056160) GABA A receptor alpha-5/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P31644|P47870, gene: GABRA5|GABRB2|GABRG2, swissprot: GBRA5_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26056160) GABA-A receptor alpha-6/beta-2 (Organism: Homo sapiens, class: Ion channel, accessions: P47870|Q16445, gene: GABRA6|GABRB2, swissprot: GBRA6_HUMAN|GBRB2_HUMAN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26056160) GABA-A receptor alpha-6/beta-2/delta (Organism: Homo sapiens, class: Ion channel, accessions: O14764|P47870|Q16445, gene: GABRA6|GABRB2|GABRD, swissprot: GBRA6_HUMAN|GBRB2_HUMAN|GBRD_HUMAN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26056160) GABA-A receptor alpha-6/beta-3/delta (Organism: Homo sapiens, class: Ion channel, accessions: O14764|P28472|Q16445, gene: GABRA6|GABRB3|GABRD, swissprot: GBRA6_HUMAN|GBRB3_HUMAN|GBRD_HUMAN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/26056160) A quinazoline derivative with hypnotic and sedative properties. It has been withdrawn from the market in many countries because of problems with abuse. (From Martindale, The Extra Pharmacopoeia, 30th ed, p604) GABA agonist (Code: CHEBI:51373) sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1965-01-01 YEAR INTRODUCED
Click to view xibenolol Xibenolol a selective beta-adrenergic blocker. It has been developing for the treatment of hypertension.
Click to view butazolamide Butazolamide containis thiadiazole nucleus. Butazolamide was used as a diuretic.
Click to view gemfibrozil Fatty acid-binding protein, liver (Organism: Rattus norvegicus, class: Unclassified, accessions: P02692, gene: Fabp1, swissprot: FABPL_RAT) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) Lipoprotein lipase (Organism: Homo sapiens, class: Enzyme, accessions: P06858, gene: LPL, swissprot: LIPL_HUMAN) Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) agonist (Source: ) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Transthyretin (Organism: Homo sapiens, class: Secreted, accessions: P02766, gene: TTR, swissprot: TTHY_HUMAN) A lipid-regulating agent that lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total cholesterol. Peroxisome Proliferator Receptor alpha Agonist (Code: N0000175596) Peroxisome Proliferator-activated Receptor alpha Agonists (Code: N0000175375) PPAR alpha (Code: N0000170118) antilipemic drug (Code: CHEBI:35679) Antimetabolites (Code: D000963) Cytochrome P-450 CYP2C8 Inhibitors (Code: D065687) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Metabolic Side Effects of Drugs and Substances (Code: D065606) 1981-12-21 FDA 4TX
Click to view naepaine Naepaine is a local anesthetic. It was used for the local anesthesia during the eye procedure.
Click to view rivastigmine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1558065937482.pdf) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1558065937482.pdf) Acetylcholinesterase (Organism: Rattus norvegicus, class: Enzyme, accessions: P37136, gene: Ache, swissprot: ACES_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15993600) Butyrylcholinesterase; Protein Bche (Organism: Rattus norvegicus, class: Enzyme, accessions: Q9JKC1, gene: Bche, swissprot: Q9JKC1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15993600) Rivastigmine is an acetyl- and butyrylcholinesterase inhibitor of the carbamate type, thought to facilitate cholinergic neurotransmission by slowing the degradation of acetylcholine released by functionally intact cholinergic neurones. Thus, rivastigmine may have an ameliorative effect on cholinergic-mediated cognitive deficits in dementia associated with Alzheimer’s disease and Parkinson’s disease. Cholinesterase Inhibitor (Code: N0000175723) neuroprotective agent (Code: CHEBI:63726) cholinergic drug (Code: CHEBI:38323) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neuroprotective Agents (Code: D018696) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1998-05-12 EMA
Click to view amfetaminil a supposedly insoluble amphetamine complex that may release amphetamine; proposed as central nervous system stimulant; withdrawn
Click to view alibendol is an antispasmodic, choleretic, and cholekinetic 1981 YEAR INTRODUCED
Click to view dimethazan Dimethazan is a caffeine derivative. Dimethazan possesses antidepressant and diuretic properties. Dimethazan was used as a psychostimulant and antidepressant. Recent abuse through overuse has caused it to be withdrawn.
Click to view rimazolium Rimazolium is a non-narcotic analgesic. 1975 YEAR INTRODUCED
Click to view uracil mustard DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) alkylating agent (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/1999/012892Orig1s015s016lbl.pdf) Uracil mustard is an alkylating agent belonging to the class nitrogen mustards. Uracil mustard alkylates and damages DNA by binding to the guanine and cytosine moieties of DNA. This leads to cross-linking of DNA, which inhibits DNA synthesis and promotes cell death in rapidly metabolizing cells, such as cancer cells. It is used for the palliative treatment of chronic lymphocytic leukemia, Non-Hodgkin's lymphomas, chronic myelogenous leukemia, early stages of polycythemia vera and mycosis fungoides. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) 1962-09-13 FDA
Click to view anisindione Vitamin K-dependent gamma-carboxylase (Organism: Homo sapiens, class: Enzyme, accessions: P38435, gene: GGCX, swissprot: VKGC_HUMAN) inhibitor (Source: ) Arachidonate 5-lipoxygenase (Organism: Rattus norvegicus, class: Enzyme, accessions: P12527, gene: Alox5, swissprot: LOX5_RAT) a synthetic anticoagulant it exercises its therapeutic action by reducing the prothrombin activity of the blood by inhibiting the vitamin K-mediated gamma-carboxylation of precursor proteins anticoagulant (Code: CHEBI:50249) 1957-04-05 FDA
Click to view phenytoin Sodium channel protein type 2 subunit alpha (Organism: Rattus norvegicus, class: Ion channel, accessions: P04775, gene: Scn2a, swissprot: SCN2A_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19388676) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/008762s063lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/008762s063lbl.pdf) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23812503) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11038165) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.fda.gov/media/99941/download) Cytochrome P450 11B1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P15538, gene: CYP11B1, swissprot: C11B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2519258) UDP-glucuronosyltransferase 1-6 (Organism: Homo sapiens, class: Enzyme, accessions: P19224, gene: UGT1A6, swissprot: UD16_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15933229) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15933229) UDP-glucuronosyltransferase 2B15 (Organism: Homo sapiens, class: Enzyme, accessions: P54855, gene: UGT2B15, swissprot: UDB15_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15933229) Solute carrier organic anion transporter family member 1C1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9EPZ7, gene: Slco1c1, swissprot: SO1C1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18845642) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18824002) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17045309) Phenytoin is an anticonvulsant that is used to treat a wide variety of seizures. It is also an anti-arrhythmic and a muscle relaxant. The precise mechanism by which phenytoin exerts its therapeutic effect has not been established but is thought to involve the voltage-dependent blockade of membrane sodium channels resulting in a reduction in sustained high-frequency neuronal discharges. The mechanism of its muscle relaxant effect appears to involve a reduction in the sensitivity of muscle spindles to stretch. Phenytoin has been proposed for several other therapeutic uses, but its use has been limited by its many adverse effects and interactions with other drugs. Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Cytochrome P450 1A2 Inducers (Code: N0000191266) Cytochrome P450 2B6 Inducers (Code: N0000187064) Cytochrome P450 2C8 Inducers (Code: N0000187063) Cytochrome P450 2C19 Inducers (Code: N0000185607) Cytochrome P450 2D6 Inducers (Code: N0000191267) Cytochrome P450 3A Inducers (Code: N0000190118) Cytochrome P450 2C9 Inducers (Code: N0000185507) drug allergen (Code: CHEBI:88188) anticonvulsant (Code: CHEBI:35623) Anticonvulsants (Code: D000927) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Cytochrome P-450 CYP1A2 Inducers (Code: D065694) Membrane Transport Modulators (Code: D049990) Metabolic Side Effects of Drugs and Substances (Code: D065606) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1953-01-06 FDA
Click to view oxcarbazepine Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021014s043lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021014s043lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021014s043lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021014s043lbl.pdf) Oxcarbazepine is an antiepileptic drug. As a prodrug, oxcarbazepine is converted to its active metabolite, 10-monohydroxy. Although the mechanism of action has not been fully elucidated. Oxcarbazepine is indicated for monotherapy or adjunctive therapy in the treatment of partial-onset seizures. Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) anticonvulsant (Code: CHEBI:35623) Anticonvulsants (Code: D000927) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Cytochrome P-450 CYP3A Inducers (Code: D065701) Membrane Transport Modulators (Code: D049990) Metabolic Side Effects of Drugs and Substances (Code: D065606) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 2000-01-14 FDA
Click to view cimetidine Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) antagonist (Source: https://pdf.hres.ca/dpd_pm/00049348.PDF) Dimethylaniline monooxygenase [N-oxide-forming] 3 (Organism: Homo sapiens, class: Enzyme, accessions: P31513, gene: FMO3, swissprot: FMO3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7720103) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15496291) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15496291) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15496291) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15496291) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/25034211) Solute carrier family 22 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63089, gene: Slc22a1, swissprot: S22A1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9195965) Solute carrier family 22 member 3 (Organism: Mus musculus, class: Transporter, accessions: Q9WTW5, gene: Slc22a3, swissprot: S22A3_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10966924) Solute carrier family 22 member 3 (Organism: Rattus norvegicus, class: Transporter, accessions: O88446, gene: Slc22a3, swissprot: S22A3_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10385678) Solute carrier family 22 member 9 (Organism: Homo sapiens, class: Transporter, accessions: Q8IVM8, gene: SLC22A9, swissprot: S22A9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14978359) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: www.ncbi.nlm.nih.gov/pubmed/17509534) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28971610) Solute carrier family 22 member 4 (Organism: Homo sapiens, class: Transporter, accessions: Q9H015, gene: SLC22A4, swissprot: S22A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215651) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10223772) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10223772) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10223772) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11334262) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11334262) Cimetidine is a histamine H2 - receptor antagonists. Cimetidine inhibits both daytime and nocturnal basal gastric acid secretion. Cimetidine also inhibits gastric acid secretion stimulated by food, histamine, pentagastrin, caffeine and insulin. Cimetidine also has cytoprotective properties. Cimetidine is primary therapy for conditions where the inhibition of gastric acid secretion is likely to be beneficial such as Duodenal ulcer therapy, Non-malignant gastric ulcer therapy, Prophylaxis of recurrent duodenal or gastric ulcer, Gastroesophageal reflux disease, Pathological hypersecretion associated with Zollinger-Ellison Syndrome, systemic mastocytosis and multiple endocrine adenomas, Adjunctive therapy in the management of cystic fibrosis in children, Treatment of NSAID-induced lesions and gastrointestinal symptoms and prevention of their recurrence. Histamine H2 Receptor Antagonists (Code: N0000000151) Histamine-2 Receptor Antagonist (Code: N0000175784) H2-receptor antagonist (Code: CHEBI:37961) analgesic (Code: CHEBI:35480) adjuvant (Code: CHEBI:60809) anti-ulcer drug (Code: CHEBI:49201) Anti-Ulcer Agents (Code: D000897) Cytochrome P-450 CYP1A2 Inhibitors (Code: D065609) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H2 Antagonists (Code: D006635) Metabolic Side Effects of Drugs and Substances (Code: D065606) Neurotransmitter Agents (Code: D018377) 1977-08-16 FDA
Click to view cioteronel Cioteronel is an antiandrogen agent. It was developed for androgenetic alopecia (male pattern baldness), and acne. It was also under development for the oral treatment of benign prostatic hyperplasia, but it was discontinued due to poor efficacy. The antineoplastic action of cioteronel appears to be the inhibition of RNA synthesis, but it has no detectable untoward effects on nonneoplastic cells, in vitro. Although it blocks competitively the binding of dihydrotestosterone (DHT) to its protein receptor, it has no significant effects on either estrogen or progesterone receptors.
Click to view cinoxacin Cinoxacin is a synthetic antibacterial quinolone. Cinoxacin has in vitro activity against many gram-negative aerobic bacteria, particularly strains of Enterobacteriaceae. Cinoxacin inhibits bacterial deoxyribonucleic acid synthesis, is bactericidal, and is active over the entire urinary pH range. Cross-resistance with nalidixic acid has been demonstrated. Cinoxacin has been shown to be active against Enterobacter species, Escherichia coli, Klebsiella species, Proteus mirabilis, Proteus vulgaris. Cinobac is indicated for the treatment and prevention of initial and recurrent urinary tract infections caused by the following susceptible microorganisms. antibacterial drug (Code: CHEBI:36047) antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1980-06-13 FDA
Click to view pyricarbate A drug that has been given by mouth in the treatment of atherosclerosis and other vascular disorders, hyperlipidemias, and thrombo-embolic disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1408) Ministry of Health of the Russian Federation
Click to view penciclovir Thymidine kinase (Organism: Human herpesvirus 1, class: Kinase, accessions: Q9QNF7, gene: TK, swissprot: KITH_HHV1) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020629s019lbl.pdf) Thymidine kinase (Organism: Human herpesvirus 2 (strain 333), class: Kinase, accessions: P04407, gene: TK, swissprot: KITH_HHV23) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020629s019lbl.pdf) Penciclovir is a nucleoside analogue. It has inhibitory activity against herpes simplex virus types 1 (HSV-1) and 2 (HSV-2). In cells infected with HSV, the viral thymidine kinase phosphorylates penciclovir to a monophosphate form that, in turn, is converted by cellular kinases to the active form penciclovir triphosphate. Biochemical studies demonstrate that penciclovir triphosphate inhibits HSV DNA polymerase competitively with deoxyguanosine triphosphate. Penciclovir is used for the treatment recurrent cold sores on the lips and face from various herpes virus infections. DNA Polymerase Inhibitors (Code: N0000020060) Herpesvirus Nucleoside Analog DNA Polymerase Inhibitor (Code: N0000175468) Nucleoside Analog (Code: N0000175459) antiviral drug (Code: CHEBI:36044) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 1996-09-24 FDA PE2
Click to view triamterene Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16035375) Triamterene is a potassium-conserving (antikaliuretic) diuretic with relatively weak natriuretic properties. It exerts its diuretic effect on the distal renal tubule to inhibit the reabsorption of sodium in exchange for potassium and hydrogen. With this action, triamterene increases sodium excretion and reduces the excessive loss of potassium and hydrogen associated with hydrochlorothiazide. Triamterene is indicated alone or in combination with hydrochlorothiazide for the treatment of hypertension or edema. Decreased Renal K+ Excretion (Code: N0000008859) Increased Diuresis (Code: N0000175359) Potassium-sparing Diuretic (Code: N0000175418) diuretic (Code: CHEBI:35498) Diuretics (Code: D004232) Epithelial Sodium Channel Blockers (Code: D062686) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Channel Blockers (Code: D026941) 1964-08-10 FDA DX2
Click to view actinoquinol radiation protectant, a chemical compound that absorbs UVB light (from "Central corneal thickness considered an index of corneal hydration of the UVB irradiated rabbit cornea as influenced by UVB absorber". Physiol Res. 61 (3): 299–306. July 2012. )
Click to view sulfamethoxazole Dihydropteroate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AC13, gene: folP, swissprot: DHPS_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/017376s061lbl.pdf) Dihydropteroate synthase (Organism: Streptococcus pneumoniae (strain ATCC BAA-255 / R6), class: Enzyme, accessions: P59655, gene: sulA, swissprot: DHPS_STRR6) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/017376s061lbl.pdf) Dihydropteroate synthase (Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd), class: Enzyme, accessions: P43776, gene: folP, swissprot: DHPS_HAEIN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/017376s061lbl.pdf) Dihydropteroate synthase (Organism: Shigella flexneri, class: Enzyme, accessions: P0AC15, gene: folP, swissprot: DHPS_SHIFL) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/017376s061lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/017376s061lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/017376s061lbl.pdf) Endothelin-1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P26684, gene: Ednra, swissprot: EDNRA_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7731020) Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic that is most commonly used in combination with trimethoprim. Sulfamethoxazole competitively inhibits dihydropteroate synthase preventing the formation of dihydropteroic acid, a precursor of folic acid which is required for bacterial growth. It is used for the treatment of Urinary Tract Infections, Acute Otitis Media, Acute Exacerbations of Chronic Bronchitis, Travelers’ Diarrhea, Shigellosis and Pneumocystis jiroveci Pneumonia. Sulfonamide Antimicrobial (Code: N0000175504) Sulfonamides (Code: N0000008048) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) drug allergen (Code: CHEBI:88188) antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) 1961 FDA 08D
Click to view ethacridine Telomerase reverse transcriptase (Organism: Homo sapiens, class: Enzyme, accessions: O14746, gene: TERT, swissprot: TERT_HUMAN) Reverse transcriptase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q9WKE8, gene: reverse transcriptas, swissprot: Q9WKE8_9HIV1) A topically applied anti-infective agent. It is effective against mostly Gram-positive bacteria, such as Streptococci and Staphylococci Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Ministry of Health of the Russian Federation
Click to view nepafenac Nepafenac is a prodrug for amfenac, used in eye drops to treat pain and inflammation following cataract surgery. Nepafenac penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, a nonsteroidal anti-inflammatory drug, amfenac is thought to inhibit the action of prostaglandin H synthase (cyclooxygenase), an enzyme required for prostaglandin production. Cyclooxygenase Inhibitors (Code: N0000000160) Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) prodrug (Code: CHEBI:50266) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2005-08-19 FDA
Click to view vanitiolide Vanitiolide is a member of methoxybenzenes and a member of phenols. Vanitiolide is a choleretic agent.
Click to view meladrazine an antispasmodic, used in urology
Click to view tolpropamine Tolpropamine is an alkylamine H1-antihistamine.Tolpropamine is an antihistamine and anticholinergic used as an antipruritic.
Click to view tizanidine Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021447s011_020397s026lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021447s011_020397s026lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021447s011_020397s026lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021447s011_020397s026lbl.pdf) Tizanidine is an agonist at alpha2-adrenergic receptor sites and presumably reduces spasticity by increasing presynaptic inhibition of motor neurons. Tizanidine is indicated for the relief of muscle spasticity, which can interfere with daily activities. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-2 Receptor Agonists (Code: D058647) Adrenergic alpha-Agonists (Code: D000316) Analgesics (Code: D000700) alpha-adrenergic agonist (Code: CHEBI:35569) muscle relaxant (Code: CHEBI:51371) Anticonvulsants (Code: D000927) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Adrenergic alpha2-Agonists (Code: N0000009918) Central alpha-2 Adrenergic Agonist (Code: N0000175554) 1996-11-27 FDA
Click to view proguanil Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021078s023lbl.pdf) Proguanil primarily exerts its effect by means of the metabolite cycloguanil, a dihydrofolate reductase inhibitor. Inhibition of dihydrofolate reductase in the Plasmodium parasite disrupts deoxythymidylate synthesis. Proguanil is used in combination with atovaquone for prophylaxis of Plasmodium falciparum malaria, including in areas where chloroquine resistance has been reported. and for treatment of acute, uncomplicated P. falciparum malaria. (See: cycloguanil) Dihydrofolate Reductase Inhibitors (Code: N0000000191) antimalarial (Code: CHEBI:38068) antiprotozoal drug (Code: CHEBI:35820) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antimetabolites (Code: D000963) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Noxae (Code: D009676) 2000-07-14 FDA
Click to view dichlorophenarsine Dichlorophenarsine is an arsenic-containing agent formerly used in the treatment of syphilis.
Click to view iodothiouracil Iodothiouracil is a combination of iodine and thiouracil. Iodothiouracil is a goitrogenic agent, but it is less effective than thiouracil.
Click to view cinromide Cinromide was an experimental anticonvulsant agent. It was withdrawn because of its very limited clinical usefulness in humans.
Click to view diprophylline Dyphylline is a xanthine derivative. Dyphilline exerts bronchodilator effects and to a lesser extent vasodilator and diuretic properties. Dyphilline probably acts as a competitive inhibitor of phosphodiesterase which leads to an increase in intracellular cAMP. This results in relaxation of bronchial smooth muscle and other smooth muscles. Dyphylline may also antagonize adenosine receptors. Dyphylline is used in the treatment of acute bronchial asthma, chronic bronchitis and emphysema. bronchodilator agent (Code: CHEBI:35523) vasodilator agent (Code: CHEBI:35620) muscle relaxant (Code: CHEBI:51371) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Phosphodiesterase Inhibitors (Code: D010726) Respiratory System Agents (Code: D019141) Vasodilator Agents (Code: D014665) 1951-03-07 FDA X0T
Click to view menadione sodium bisulfite Aldose reductase (Organism: Gallus gallus, class: Enzyme, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3927923) Menadione sodium sulfonate is a synthetic naphthoquinone without the isoprenoid side chain and biological activity, but can be converted into active vitamin K2, menaquinone, after alkylation in vivo. 2005-01-27 Ministry of Health of the Russian Federation 2L3
2LB
Click to view ketoprofen Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14987823 Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14987823) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515014) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26721703) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Ketoprofen is an ibuprofen-type anti-inflammatory analgesic and antipyretic. Ketoprofen exists in two enantiomeric forms, S-ketoprofen (dexketoprofen) and R-ketoprofen (levoketoprofen). It has been reported that dexketoprofen is the active optical isomer (eutomer) of ketoprofen. It is used in the treatment of rheumatoid arthritis and osteoarthritis. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antipyretic (Code: CHEBI:35493) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) ketoprofen: 1986-01-09 FDA dexketoprofen: 1998-01-14 UK Medicines and Helthcare Products Regulatory Agency (MHRA) JGE
Click to view fenbufen Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: ) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: ) an orally active nonsteroidal anti-inflammatory drug with analgesic and antipyretic activity Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Italian Medicines Agency (AIFA)
Click to view midodrine Midodrine is a direct-acting prodrug and sympathomimetic agent with antihypotensive properties. Midodrine is converted to its active metabolite, desglymidodrine by deglycination reaction. Desglymidodrine selectively binds to and activates alpha-1-adrenergic receptors of the arteriolar and venous vasculature. This causes smooth muscle contraction and leads to an elevation of blood pressure. Desglymidodrine diffuses poorly across the blood-brain barrier, and is therefore not associated with effects on the central nervous system. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-1 Receptor Agonists (Code: D058646) Adrenergic alpha-Agonists (Code: D000316) prodrug (Code: CHEBI:50266) alpha-adrenergic agonist (Code: CHEBI:35569) sympathomimetic agent (Code: CHEBI:35524) vasoconstrictor agent (Code: CHEBI:50514) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1996-09-06 FDA
Click to view levorphanol Acetylcholinesterase (Organism: Electrophorus electricus, class: Enzyme, accessions: O42275, gene: ache, swissprot: ACES_ELEEL Mu-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P42866, gene: Oprm1, swissprot: OPRM_MOUSE Kappa-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P33534, gene: Oprk1, swissprot: OPRK_MOUSE Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist Kappa-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P41144, gene: OPRK1, swissprot: OPRK_CAVPO Sigma non-opioid intracellular receptor 1 (Organism: Mus musculus, class: Membrane receptor, accessions: O55242, gene: Sigmar1, swissprot: SGMR1_MOUSE Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q8VHN2|Q9R1M7, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMD3A_RAT|NMD3B_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMDZ1_RAT Mu-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P97266, gene: OPRM1, swissprot: OPRM_CAVPO Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Glutamate [NMDA] receptor (Organism: Homo sapiens, class: Ion channel, accessions: O15399|O60391|Q05586|Q12879|Q13224|Q14957|Q8TCU5, gene: GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B, swissprot: NMD3A_HUMAN|NMD3B_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMDE4_HUMAN|NMDZ1_HUMAN Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection. Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1953-01-08 FDA
Click to view sulfadicramide Sulfadicramide is a sulfonamide anti-infective agent. It was used for the treatment of bacterial infections. Also it was used as ointment for application to the eye. It was replacenet from market by less toxic and more active antibiotics.
Click to view thiamylal Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/10960410/) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/10960410/) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/10960410/) Thiamylal is a barbiturate. Thiamylal binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. It was used for the production of complete anesthesia of short duration, for the induction of general anesthesia, or for inducing a hypnotic state. Thiamylal also was used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) 1957-12-01 PMDA
Click to view bucricaine Bucricaine is tetrahydroaminoacridine derivative. It that has been studied as acetylcholinesterase and monoamine oxidase inhibitor. Bucricaine has analgesic, local anesthetic, analeptic, and respiratory stimulant activities.
Click to view phenbenzamine Phenbenzamine belongs to the phenylbenzamines class. Phenbenzamine is an antihistamine with anticholinergic properties. It is no longer available.
Click to view tripelennamine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: ) A histamine H1 antagonist with low sedative action but frequent gastrointestinal irritation. It is used to treat ASTHMA; HAY FEVER; URTICARIA; and RHINITIS; and also in veterinary applications. Tripelennamine is administered by various routes, including topically. Anti-Allergic Agents (Code: D018926) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1948-02-19 FDA
Click to view pilsicainide Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12960687) Sodium channel protein type 4 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35499, gene: SCN4A, swissprot: SCN4A_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/20590641) Pilsicainide is a lidocaine derivative. Pilsicainide has a sodium channel-blocking activity. Pilsicainide is indicated for the emergency treatment of tachyarrhythmia (supraventricular and ventricular) in patients, who can not use or do not response to other antiarrhythmic agents. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) 2008 PMDA
Click to view butanilicaine Butanilicaine is an amino acid amide amide in which N-butylglycine and 2-chloro-6-methylaniline have combined to form the amide bond. Butanilicaine was used as a local anaesthetic. local anaesthetic (Code: CHEBI:36333)
Click to view ganciclovir Ganciclovir: Protein UL27 (Organism: Human cytomegalovirus, class: Enzyme, accessions: Q6SWA4, gene: UL27, swissprot: UL27_HCMVM) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019661s037lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11861798) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11861798) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Ganciclovir-triphosphate: DNA polymerase catalytic subunit (Organism: Human cytomegalovirus, class: Enzyme, accessions: Q6SW77, gene: UL54, swissprot: DPOL_HCMVM) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019661s037lbl.pdf) Ganciclovir is a synthetic guanine derivative active against cytomegalovirus (CMV). Ganciclovir is a synthetic analogue of 2'-deoxyguanosine, which inhibits replication of human CMV in cell culture and in vivo. In CMV-infected cells, ganciclovir is initially phosphorylated to ganciclovir monophosphate by the viral protein kinase, pUL97. Further phosphorylation occurs by cellular kinases to produce ganciclovir triphosphate, which is then slowly metabolized intracellularly. As the phosphorylation is largely dependent on the viral kinase, phosphorylation of ganciclovir occurs preferentially in virus-infected cells. The virustatic activity of ganciclovir is due to inhibition of the viral DNA polymerase, pUL54, by ganciclovir triphosphate. Ganciclovir is indicated for the treatment and prevention of CMV disease in adult transplant recipients at risk for CMV disease. antiviral drug (Code: CHEBI:36044) antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Cytomegalovirus Nucleoside Analog DNA Polymerase Inhibitor (Code: N0000175461) DNA Polymerase Inhibitors (Code: N0000020060) Nucleoside Analog (Code: N0000175459) Nucleoside Analog Antiviral (Code: N0000175466) 1989-06-23 FDA GA2
Click to view pranoprofen Prostaglandin G/H synthase 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: Q63921, gene: Ptgs1, swissprot: PGH1_RAT) inhibitor (Source: https://www.sciencedirect.com/science/article/pii/0960894X9500141F) Pranoprofen is a non steroidal anti-inflammatory drug (NSAID). Its mechanism of action is the inhibition of inflammatory prostaglandin synthesis. Pranoprofen is used for the treatment of pain and inflammation in rheumatoid arthritis, osteoarthritis, acute gout, acute upper respiratory inflammation (bronchitis) and as analgetic after trauma, minor surgery and tooth extraction. 1988-09-01 PMDA
Click to view ketorolac Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12446609) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11695255) A pyrrolizine carboxylic acid derivative structurally related to indomethacin. It is a non-steroidal anti-inflammatory agent used for analgesia for postoperative pain and inhibits cyclooxygenase activity. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) analgesic (Code: CHEBI:35480) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Cyclooxygenase Inhibitor (Code: N0000175939) 1989-11-30 FDA KTR
Click to view tenonitrozole Tenonitrozole is an antiprotozoal. It is used for the treatment of Urogenital Trichomoniasis caused by Trichomonas vaginalis. 1997-02-11 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view cetoxime Cetoxime is an antihistamine which is used for the treatment of allergic disorders without unwanted sedation. It is no longer available. 1961-04-22 YEAR INTRODUCED
Click to view metralindole Metralindole used as an antidepressant Ministry of Health of the Russian Federation
Click to view thiazosulfone Thiazosulfone is an aniline derivative and a hemolytic drug. It was used for the treatment of tuberculosis and leprosy.
Click to view sulfathiazole Dihydropteroate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AC13, gene: folP, swissprot: DHPS_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3906132) Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/20630653) Sulfathiazole is a short-acting sulfonamide antibiotic. Its use has been largely replaced with less toxic alternatives but is still used in combination with sulfacetamide and sulfabenzamide for the treatment of vaginal infections and for disinfecting home aquariums. antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) 1945-09-12 FDA YTZ
Click to view tofenacin an antidepressant Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neurotransmitter Agents (Code: D018377) UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view phenyltoloxamine D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/28684) an H1 blocking agent which interferes with the action of histamine primarily in capillaries surrounding mucous tissues and sensory nerves of the nasal and adjacent areas. It has the ability to interfere with certain areas of acetylcholine-inhibiting secretions in the nose, mouth and pharynx. It commonly causes CNS depression.
Click to view diphenhydramine Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08485, gene: Chrm4, swissprot: ACM4_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16453179) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions:P10980, gene: Chrm2, swissprot: ACM2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16453179) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16453179) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2878016) A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects. Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Antagonist (Code: N0000175587) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Anti-Allergic Agents (Code: D018926) H1-receptor antagonist (Code: CHEBI:37955) antiemetic (Code: CHEBI:50919) sedative (Code: CHEBI:35717) anti-allergic agent (Code: CHEBI:50857) muscarinic antagonist (Code: CHEBI:48876) antiparkinson drug (Code: CHEBI:48407) antipruritic drug (Code: CHEBI:59683) local anaesthetic (Code: CHEBI:36333) antidyskinesia agent (Code: CHEBI:66956) antitussive (Code: CHEBI:51177) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Sleep Aids, Pharmaceutical (Code: D000068776) 1946-03-04 FDA 2PM
Click to view atomoxetine Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021411s048lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021411s048lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021411s048lbl.pdf) Glutamate receptor ionotropic, NMDA 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q05586, gene: GRIN1, swissprot: NMDZ1_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/20423340) Glutamate receptor ionotropic, NMDA 2A (Organism: Homo sapiens, class: Ion channel, accessions: Q12879, gene: GRIN2A, swissprot: NMDE1_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/20423340) G protein-activated inward rectifier potassium channel 2 (Organism: Homo sapiens, class: Ion channel, accessions: P48051, gene: KCNJ6, swissprot: KCNJ6_HUMAN) inhibitor (Source: l) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871604) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871604) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18954038) Atomoxetine is a propylamine derivative and a selective norepinephrine reuptake inhibitor. The precise mechanism by which atomoxetine produces its therapeutic effects is unknown, but is thought to be related to selective inhibition of the pre-synaptic norepinephrine transporter. Atomoxetine is indicated for the treatment of Attention-Deficit/Hyperactivity Disorder. Norepinephrine Reuptake Inhibitor (Code: N0000175695) Norepinephrine Uptake Inhibitors (Code: N0000000102) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) adrenergic uptake inhibitor (Code: CHEBI:35640) antidepressant (Code: CHEBI:35469) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) 2002-11-26 FDA
Click to view dimemorfan a antitussive drug Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141) PMDA
Click to view clobutinol a cough suppressant. It is used for the short-term treatment of irritable, non-productive cough (a ‘dry’ cough where the patient does not cough up any phlegm or mucus) Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141)
Click to view anagrelide cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2846839) cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Organism: Homo sapiens, class: Enzyme, accessions: Q14432, gene: PDE3A, swissprot: PDE3A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1311763) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020333s025lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020333s025lbl.pdf) Anagrelide is a platelet-reducing agent. The precise mechanism by which anagrelide reduces blood platelet count is unknown. In cell culture studies, anagrelide suppressed expression of transcription factors including GATA-1 and FOG-1 required for megakaryocytopoiesis, ultimately leading to reduced platelet production. Anagrelide is indicated for the treatment of thrombocythemia, secondary to myeloproliferative neoplasms, to reduce the elevated platelet count and the risk of thrombosis and to ameliorate associated symptoms including thrombo-hemorrhagic events. anticoagulant (Code: CHEBI:50249) platelet aggregation inhibitor (Code: CHEBI:50427) antifibrinolytic drug (Code: CHEBI:48675) cardiovascular drug (Code: CHEBI:35554) Cardiovascular Agents (Code: D002317) Fibrin Modulating Agents (Code: D050299) Fibrinolytic Agents (Code: D005343) Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) Decreased Platelet Production (Code: N0000175972) Platelet-reducing Agent (Code: N0000175638) Phosphodiesterase 3 Inhibitors (Code: N0000175086) 1997-03-14 FDA
Click to view lamotrigine Sodium channel protein type 4 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35499, gene: SCN4A, swissprot: SCN4A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14998340) Sodium channel protein type 2 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q99250, gene: SCN2A, swissprot: SCN2A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501613) Sodium channel protein type X alpha subunit (Organism: Rattus norvegicus, class: Unclassified, accessions: Q62968, gene: Scn10a, swissprot: SCNAA_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18501613) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020241s056,020764s049,022251s020lbl.pdf) Lamotrigine is an anti-epileptic agent and mood stabilizer. The physiologic effect of lamotrigine is by means of decreased central nervous system disorganized electrical activity. anticonvulsant (Code: CHEBI:35623) antimanic drug (Code: CHEBI:35477) antidepressant (Code: CHEBI:35469) non-narcotic analgesic (Code: CHEBI:35481) Anticonvulsants (Code: D000927) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Mood Stabilizer (Code: N0000175751) 1994-12-27 FDA
Click to view tiaprofenic acid Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor a non-steroidal, anti-inflammatory, analgesic compound, which nonselectively inhibits cyclooxygenase protein Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Ministry of Health of the Russian Federation
Click to view irsogladine Irsogladine is a mucosal protective drug for the treatment of peptic ulcer disease and acute gastritis. Anti-Ulcer Agents (Code: D000897) Anticarcinogenic Agents (Code: D016588) Antineoplastic Agents (Code: D000970) Gastrointestinal Agents (Code: D005765) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) PMDA
Click to view phenyl acetylsalicylate Phenyl acetylsalicylate is a nonsteroidal anti-inflammatory drug. Phenyl acetylsalicylate was used as an analgesic and antipyretic.
Click to view edoxudine Edoxudine is a deoxythymidine analog with activity against herpes simplex virus. Edoxudine is activated by viral thymidine kinase to the 5'-monophosphate which is further phosphorylated by cellular enzymes to the 5'-triphosphate, a competitive inhibitor of the viral-coded DNA polymerase. Edoxudine was for the treatment of human herpes keratitis. Edoxudine also indicated for the treatment of dermal herpes simplex virus. This medication was discontinued from the market. 1992-12-31 Health Canada
Click to view phenosulfazole Phenosulfazole is a sulfonamide compound. It was introduced for the treatment of poliomyelitis during the 1948 epidemic. Later, it was found to be of no value in the treatment of poliomyelitis.
Click to view etoxazene Etoxazene is a phenazopyridine analogue and a NSAID analgesic. Etoxazene is excreted in water-soluble form giving a red colour to the urine. Etoxazene was used as a urinary analgesic. FDA
Click to view phenbutamide Phenbutamide is a sulfonamide and a hypoglycemic agent.
Click to view echothiophate Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/011963s034lbl.pdf) Echothiophate is a potent, long-acting cholinesterase inhibitor used as a miotic in the treatment of glaucoma. miotic (Code: CHEBI:51068) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Miotics (Code: D008916) Neurotransmitter Agents (Code: D018377) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) Cholinesterase Inhibitor (Code: N0000175723) Iodine (Code: N0000007196) 1960-06-27 FDA
Click to view bephenium Bephenium is a member of the quaternary ammonium drug class. Bephenium exhibits antihelmintic action by acting as a cholinergic agonist, causing paralysis of the parasite musculature. It was used for treating ascariasis, ankylostomiasis, enterobiasis, trichostrongyliasis, and tricocefalosis. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977)
Click to view hexyldecanoic acid viscous oil
Click to view pyrrolnitrin 3-Chloro-4-(3-chloro-2-nitrophenyl)pyrrole. Antifungal antibiotic isolated from Pseudomonas pyrrocinia. It is effective mainly against Trichophyton, Microsporium, Epidermophyton, and Penicillium. antifungal drug (Code: CHEBI:86327) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935)
Click to view benzamidosalicylate Benzamidosalicylate (benzoylpas) is a benzoic acid-modified form of para-aminosalicylate. This analog of aminobenzoic acid was used to treat tuberculosis. 1956 FDA
Click to view benserazide Aromatic-L-amino-acid decarboxylase (Organism: Homo sapiens, class: Enzyme, accessions: P20711, gene: DDC, swissprot: DDC_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00052550.PDF) Benserazide is an inhibitor of dopa decarboxylase that does not enter the central nervous system. It is often given with levodopa in the treatment of parkinsonism to prevent the conversion of levodopa to dopamine in the periphery, thereby increasing the amount that reaches the central nervous system and reducing the required dose. It has no antiparkinson actions when given alone. antiparkinson drug (Code: CHEBI:48407) dopaminergic agent (Code: CHEBI:48560) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) 1974-02-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view carmofur Acid ceramidase (Organism: Rattus norvegicus, class: Enzyme, accessions: Q6P7S1, gene: Asah1, swissprot: ASAH1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23301156) Carmofur is a derivative of fluorouracil and is a pyrimidine analogue which acts as an antineoplastic agent through inhibition of thymidylate synthase. It is used in the treatment of breast and colorectal cancer. Carmofur has been known to induce leukoencephalopathy. Antineoplastic Agents (Code: D000970) China Food and Drug Administration (CFDA)
Click to view tolmetin Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/018084s052,017628s068lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/018084s052,017628s068lbl.pdf) Tryptophan 2,3-dioxygenase (Organism: Rattus norvegicus, class: Enzyme, accessions: P21643, gene: Tdo2, swissprot: T23O_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16952380) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10220563) Aldose reductase (Organism: Homo sapiens, class: Enzyme, accessions: P15121, gene: AKR1B1, swissprot: ALDR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22155003) Tolmetin is a nonselective nonsteroidal anti-inflammatory agent. The mode of action of tolmetin is not known. Tolmetin inhibits prostaglandin synthetase in vitro and lowers the plasma level of prostaglandin E in man. This reduction in prostaglandin synthesis may be responsible for the anti-inflammatory action. Tolmetin does not appear to alter the course of the underlying disease in man.Tolmetin is effective in treating both the acute flares and in the long-term management of the symptoms of rheumatoid arthritis, osteoarthritis and juvenile rheumatoid arthritis. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1976-03-24 FDA TLT
Click to view etebenecid Etebenecid is a uricosuric agent, lower uric acid levels in the body by increasing the elimination of uric acid by the kidneys, also inhibits penicillin tubular secretion. It was used for the treatment of gout.
Click to view medifoxamine Medifoxamine is an atypical antidepressant, with anxiolyitc properties. It was withdrawn from the market due to it causing cases of hepatotoxicity.
Click to view suprofen Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14570769) Suprofen is an ibuprofen-type anti-inflammatory analgesic and antipyretic. It binds to the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) isoenzymes, preventing the synthesis of prostaglandins and reducing the inflammatory response. It was used for the inhibition of intraoperative miosis. Today it is used for the treatment of eczema, contact dermatitis, atopic dermatitis, chronic eczema, rosace, herpes zoster. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antirheumatic drug (Code: CHEBI:35842) peripheral nervous system drug (Code: CHEBI:49110) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1988-12-23 FDA
Click to view metrifonate Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12794390) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12794390) Metrifonate (trichlorfon) is an organophosphorus compound originally used as an insecticide. It has selective and variable schistosomicidal activity against S. haematobium that results from its partial metabolism to a highly active anti-cholinesterase, dichlorvos. Metrifonate can be used for the treatment of urinary schistosomiasis, but is no longer commercially available. Metrifonate was withdrawn due to adverse effects. Now it is used as an insecticide in some countries. Anthelmintics (Code: D000871) insecticide (Code: CHEBI:24852) agrochemical (Code: CHEBI:33286) anthelminthic drug (Code: CHEBI:35443) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Insecticides (Code: D007306) Neurotransmitter Agents (Code: D018377) Pesticides (Code: D010575)
Click to view meclofenoxate Meclofenoxate is a cholinergic nootropic used as a dietary supplement and drug in the treatment of symptoms of senile dementia and Alzheimer's disease. Central Nervous System Agents (Code: D002491) Neuroprotective Agents (Code: D018696) Nootropic Agents (Code: D018697) Protective Agents (Code: D020011) 2010-08-12 Ministry of Health of the Russian Federation
Click to view iodinated glycerol Iodinated glycerol, a methyl derivative of domiodol, is an isomeric mixture of iodinated dimers of glycerol. It has been used as an expectorant. Prolonged use of iodinated glycerol has been associated with thyroid dysfunction and severe skin eruptions; gastrointestinal disturbances and hypersensitivity reactions have also occurred. Malignant neoplasms have developed in animals given iodinated glycerol. Iodinated glycerol was found to have carcinogenic potential. All drugs containing iodinated glycerol was removed from the market. 1956-05-01 PMDA
Click to view aceglatone an antineoplastic drug
Click to view salsalate a nonsteroidal anti-inflammatory agent Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antirheumatic drug (Code: CHEBI:35842) hypoglycemic agent (Code: CHEBI:35526) antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) FDA
Click to view glycerylphosphorylcholine Glycerylphosphorylcholine is a component of phosphatidylcholines or lecthins, in which the two hydroxy groups of GLYCEROL are esterified with fatty acids. (From Stedman, 26th ed)
Click to view choline alfoscerate Choline alfoscerate is a nootropic choline-containing phospholipid. Choline alphoscerate increases the release of acetylcholine in rat hippocampus, facilitates learning and memory in experimental animals, improves brain transduction mechanisms and decreases age-dependent structural changes occurring in rat brain areas involved in learning and memory. The compound exerts neuroprotective effects in models of altered cholinergic neurotransmission and of brain vascular injury. In clinical studies choline alphoscerate improved memory and attention impairment, as well as affective and somatic symptoms in dementia disorders. It is used for the treatment of Alzheimer's disease, various kinds of dementia, stroke, and transient ischemic attack. It is also used for improving memory, thinking skills, and learning. parasympatholytic (Code: CHEBI:50370) neuroprotective agent (Code: CHEBI:63726) 1987-07-27 Italian Medicines Agency (AIFA) CH5
Click to view thalidomide Protein cereblon (Organism: Homo sapiens, class: Cytosolic other, accessions: Q96SW2, gene: CRBN, swissprot: CRBN_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020785s068lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12060642) Thalidomide (alpha-(N-phthalimido) glutarimide) is an immunomodulatory agent. The mechanism of action of thalidomide is not fully understood. Cellular activities of thalidomide are mediated through its target cereblon, a component of a cullin ring E3 ubiquitin ligase enzyme complex. Thalidomide possesses immunomodulatory, anti-inflammatory and antiangiogenic properties. Available data from in vitro studies and clinical trials suggest that the immunologic effects of this compound can vary substantially under different conditions, but may be related to suppression of excessive tumor necrosis factor-alpha production and down-modulation of selected cell surface adhesion molecules involved in leukocyte migration. Thalidomide in combination with dexamethasone is indicated for the treatment of patients with newly diagnosed multiple myeloma, for the acute treatment and maintenance therapy for prevention of the cutaneous manifestations of moderate to severe erythema nodosum leprosum. Angiogenesis Inhibitors (Code: D020533) Angiogenesis Modulating Agents (Code: D043924) immunosuppressive agent (Code: CHEBI:35705) leprostatic drug (Code: CHEBI:35816) angiogenesis inhibitor (Code: CHEBI:48422) anticonvulsant (Code: CHEBI:35623) antiemetic (Code: CHEBI:50919) sedative (Code: CHEBI:35717) anti-inflammatory drug (Code: CHEBI:35472) antineoplastic agent (Code: CHEBI:35610) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Growth Inhibitors (Code: D006131) Growth Substances (Code: D006133) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Leprostatic Agents (Code: D007917) Noxae (Code: D009676) Teratogens (Code: D013723) Decreased Immunologically Active Molecule Activity (Code: N0000008663) 1998-07-16 FDA 6EL
EF2
Click to view acadesine Acadesine is a 5-aminoimidazole-4-carboxamide (AICA) riboside, a ribnucleoside analog, and a nucleotide biosynthesis precursor with B cell pro-apoptotic activity. The exact mechanism of acadesine-induced apoptosis is unknown. Following cellular uptake, acadesine is phosphorylated to AICA ribotide (ZMP or AICAR), which mimics 5'-adenosine monophosphate (AMP). Both AMP-activated protein kinase and AMPK kinase are activated by ZMP, which appears to be necessary for the induction of apoptosis. Acadesine is used for the treatment of acute lymphoblastic leukemia and may have applications in treating other disorders such as mantle cell lymphoma. platelet aggregation inhibitor (Code: CHEBI:50427) antineoplastic agent (Code: CHEBI:35610) AICA
Click to view menbutone Menbutone is a choleretic. Menbutone stimulates the digestive tract by increasing excretion of bile, gastric acid, and pancreatic juices by two to five times baseline. Now it is used in veterinary medicine in bovine, ovine, caprine, porcine, and equine species. 1977 YEAR INTRODUCED
Click to view phethenylate Phethenylate is an antiepileptic drug. It was withdrawn from the market in 1966 because it was producing hepatic necrosis. 1950 FDA
Click to view lenalidomide Protein cereblon (Organism: Homo sapiens, class: Cytosolic other, accessions: Q96SW2, gene: CRBN, swissprot: CRBN_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22966948) Lenalidomide is an analogue of thalidomide with immunomodulatory, antiangiogenic, and antineoplastic properties. Lenalidomide inhibits proliferation and induces apoptosis of certain hematopoietic tumor cells including multiple myeloma, mantle cell lymphoma, and del (5q) myelodysplastic syndromes in vitro. Lenalidomide causes a delay in tumor growth in some in vivo nonclinical hematopoietic tumor models including multiple myeloma. Immunomodulatory properties of lenalidomide include activation of T cells and natural killer (NK) cells, increased numbers of NKT cells, and inhibition of pro-inflammatory cytokines (e.g., TNF-alpha and IL-6) by monocytes. In multiple myeloma cells, the combination of lenalidomide and dexamethasone synergizes the inhibition of cell proliferation and the induction of apoptosis. Thalidomide Analog (Code: N0000184014) Angiogenesis Inhibitors (Code: D020533) Angiogenesis Modulating Agents (Code: D043924) angiogenesis inhibitor (Code: CHEBI:48422) antineoplastic agent (Code: CHEBI:35610) immunomodulator (Code: CHEBI:50846) Antineoplastic Agents (Code: D000970) Growth Inhibitors (Code: D006131) Growth Substances (Code: D006133) Immunologic Factors (Code: D007155) 2005-12-27 FDA LVY
Click to view ethoxzolamide Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18359629) Carbonic anhydrase (Organism: Methanothermobacter thermautotrophicus (strain ATCC 29096 / DSM 1053 / JCM 10044 / NBRC 100330 / Delta H), class: Enzyme, accessions: Q50565, gene: None, swissprot: Q50565_METTH) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15546717) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Enzyme, accessions: P40881, gene: None, swissprot: CAH_METTE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15546717) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P53615, gene: NCE103, swissprot: CAN_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18993072) Carbonic anhydrase (Organism: Helicobacter pylori (strain ATCC 700392 / 26695), class: Enzyme, accessions: O24855, gene: cynT, swissprot: CYNT_HELPY) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16539401) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Delta carbonic anhydrase (Organism: Thalassiosira weissflogii, class: Unclassified, accessions: Q5U9J1, gene: ca1, swissprot: Q5U9J1_THAWE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24314394) Ethoxzolamide is a sulfonamide and carbonic anhydrase (CA) inhibitor with diuretic and anti-glaucoma activity. In the eye, ethoxzolamide inhibits CA, thereby decreasing the secretion of aqueous humor. This may relieve intraocular pressure. Also, this agent prevents reabsorption of bicarbonate and sodium in the proximal convoluted tubule thereby producing a mild diuresis. It was used for the treatment of glaucoma. Also it was used as an diuretic. diuretic (Code: CHEBI:35498) antiglaucoma drug (Code: CHEBI:39456) Carbonic Anhydrase Inhibitors (Code: D002257) Diuretics (Code: D004232) Enzyme Inhibitors (Code: D004791) Natriuretic Agents (Code: D045283) 1966-10-12 FDA EZL
Click to view xibornol antibacterial drug (Code: CHEBI:36047)
Click to view cloridarol Cloridarol is a vasodilator. It was used for the treatment of coronary insufficiency. Italian Medicines Agency (AIFA)
Click to view pamabrom Pamabrom is a mixture containing 2-amino-2-methyl-1-propanol and 8-bromotheophylline (a methylxanthine) in a 1:1 ratio, with mild diuretic activity. Pamabrom reduces salt and water reabsorption in the proximal tubule and increase renal blood flow, yet its diuretic effect is modest. It is indicated as over-the-counter remedies to relief fluid retention and bloating associated with menstration. 1962-04-01 CDSCO (INDIA)
Click to view lofexidine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209229s000lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209229s000lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22341244) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209229s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209229s000lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209229s000lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209229s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/PsychopharmacologicDrugsAdvisoryCommittee/UCM602419.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/PsychopharmacologicDrugsAdvisoryCommittee/UCM602419.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/PsychopharmacologicDrugsAdvisoryCommittee/UCM602419.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.fda.gov/downloads/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/PsychopharmacologicDrugsAdvisoryCommittee/UCM602419.pdf) Lofexidine is a central alpha-2 adrenergic agonist that binds to receptors on adrenergic neurons. This reduces the release of norepinephrine and decreases sympathetic tone. Lofexidine is indicated for mitigation of opioid withdrawal symptoms to facilitate abrupt opioid discontinuation. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-2 Receptor Agonists (Code: D058647) Adrenergic alpha-Agonists (Code: D000316) alpha-adrenergic agonist (Code: CHEBI:35569) antihypertensive agent (Code: CHEBI:35674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Narcotic Antagonists (Code: D009292) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2018-05-16 FDA
Click to view mizoribine imidazole nucleoside with immunosuppressive activity isolated from culture filtrate of Eupenicillium brefeldianum; structure Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antibiotics, Antineoplastic (Code: D000903) Antimalarials (Code: D000962) Antineoplastic Agents (Code: D000970) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Antirheumatic Agents (Code: D018501) Enzyme Inhibitors (Code: D004791) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2010 PMDA MZR
Click to view ramelteon Melatonin receptor type 1B (Organism: Homo sapiens, class: GPCR, accessions: P49286, gene: MTNR1B, swissprot: MTR1B_HUMAN) agonist Melatonin receptor type 1A (Organism: Homo sapiens, class: GPCR, accessions: P48039, gene: MTNR1A, swissprot: MTR1A_HUMAN) agonist Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors and selectivity over the MT3 receptor. Ramelteon demonstrates full agonist activity in vitro in cells expressing human MT1 or MT2 receptors. The activity of ramelteon at the MT1 and MT2 receptors is believed to contribute to its sleep-promoting properties, as these receptors, acted upon by endogenous melatonin, are thought to be involved in the maintenance of the circadian rhythm underlying the normal sleep-wake cycle. Melatonin Receptor Agonist (Code: N0000175743) Melatonin Receptor Agonists (Code: N0000000250) 2005-07-22 FDA
Click to view propranolol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021438s016lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021438s016lbl.pdf) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021438s016lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021438s016lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021438s016lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021438s016lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021438s016lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10960071) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Cavia porcellus, class: Ion channel, accessions: O35505, gene: CACNA1C, swissprot: CAC1C_CAVPO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/26565745) 5-hydroxytryptamine receptor 2C (Organism: Rattus norvegicus, class: GPCR, accessions: P08909, gene: Htr2c, swissprot: 5HT2C_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3139864) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6146381) Propranolol is a synthetic, nonselective beta-adrenergic receptor blocker with antianginal, antiarrhythmic, antihypertensive properties. Propranolol competitively antagonizes beta-adrenergic receptors, thereby causing negative chronotropic and inotropic effects leading to a reduction in cardiac output. Propranolol has been used for myocardial infarction, arrhythmia, angina pectoris, hypertension, hyperthyroidism, migraine, pheochromocytoma, and anxiety but adverse effects instigate replacement by newer drugs. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) antihypertensive agent (Code: CHEBI:35674) beta-adrenergic antagonist (Code: CHEBI:35530) anxiolytic drug (Code: CHEBI:35474) anti-arrhythmia drug (Code: CHEBI:38070) vasodilator agent (Code: CHEBI:35620) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) 1967-11-13 FDA SNP
Click to view flumequine a synthetic antibiotic Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Renal Agents (Code: D012076) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003)
Click to view primaquine Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) Chloroquine resistance transporter (Organism: Plasmodium falciparum, class: Unclassified, accessions: Q9N623, gene: CRT, swissprot: CRT_PLAFA) Ribosyldihydronicotinamide dehydrogenase [quinone] (Organism: Homo sapiens, class: Enzyme, accessions: P16083, gene: NQO2, swissprot: NQO2_HUMAN) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) Heat shock protein HSP 90-alpha (Organism: Homo sapiens, class: Cytosolic other, accessions: P07900, gene: HSP90AA1, swissprot: HS90A_HUMAN) Hemoglobin subunit alpha (Organism: Homo sapiens, class: Secreted, accessions: P69905, gene: HBA1, swissprot: HBA_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Aryl hydrocarbon receptor (Organism: Homo sapiens, class: Transcription factor, accessions: P35869, gene: AHR, swissprot: AHR_HUMAN) Glucose-6-phosphate 1-dehydrogenase (Organism: Homo sapiens, class: Enzyme, accessions: P11413, gene: G6PD, swissprot: G6PD_HUMAN) An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404) antimalarial (Code: CHEBI:38068) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) 1952-01-23 FDA 1PQ
Click to view eperisone Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Eperisone is an antispasmodic drug which relaxes both skeletal muscles and vascular smooth muscles, and demonstrates a variety of effects such as reduction of myotonia, improvement of circulation, and suppression of the pain reflex. muscle relaxant (Code: CHEBI:51371) Anticonvulsants (Code: D000927) Autonomic Agents (Code: D001337) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Vasodilator Agents (Code: D014665) 2011-06-24 CDSCO (INDIA)
Click to view azintamide Azintamide is a potent choleretic agent. Azintamide exerts also a moderate cholepoietic action. Azintamide can reduce the serum cholestrol, non-esterified fatty acid and free glycerol. It is used in fatty indigestion, cholangitis, cholecystitis, icteric and posticteric cases, liver protection in condition of cholecystopathy, meteorism and hepatogenic dermatosis. Azintamide is also used in hypercholesterolemia. 2014-09-11 China Food and Drug Administration (CFDA)
Click to view clobenzorex is a central stimulant and sympathomimetic used as an anti-obesity drug
Click to view carbarsone Carbarsone is an arsenic-based antiprotozoal drug. It was used for the treatment of amebiasis and trichomonas vaginalis vaginitis. Now carbarsone is used only as a veterinary drug in controlling and preventing blackhead disease in turkeys.
Click to view glucose-1-phosphate Phosphoglucomutase-2 (Organism: Homo sapiens, class: Enzyme, accessions: Q96G03, gene: PGM2, swissprot: PGM2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17804405) Glucose 1-phosphate (G1P) is a monosaccharide phosphate. Glucose-1-phosphate is an important carbohydrate intermediate in glucose metabolism and storage. Glucose 1-phosphate exists in all living species, ranging from bacteria to humans. Within humans, glucose 1-phosphate can be converted into D-glucose through its interaction with the enzyme glucose-6-phosphatase. Glucose 1-phosphate is a potentially toxic compound. Glucose-1-phosphate is subsequently converted to Glucose-6-phosphate by phosphoglucomutase and enters glycolysis. Measurement of intracellular G1P levels is crucial for analyzing the carbohydrate metabolic pathways and their kinetic properties. In medicine G1P is used as infusion solution in phosphate deficiency. 1994-02-09 State Institute for Drug Control (SUKL) G1P
Click to view khellin A vasodilator that also has bronchodilatory action. It has been employed in the treatment of angina pectoris, in the treatment of asthma, and in conjunction with ultraviolet light A, has been tried in the treatment of vitiligo. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1024) vasodilator agent (Code: CHEBI:35620) bronchodilator agent (Code: CHEBI:35523) anti-asthmatic agent (Code: CHEBI:65023) cardiovascular drug (Code: CHEBI:35554) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiovascular Agents (Code: D002317) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Vasodilator Agents (Code: D014665) 2005-09-16 Ministry of Health of the Russian Federation
Click to view tiazofurine a synthetic nucleoside analogue with antineoplastic activity. Tiazofurin (TR) is anabolized intracellularly to an analogue of NAD, tiazole-4-carboxamide adenine dinucleotide (TAD), a potent inhibitor of IMP dehydrogenase (IMPDH); IMPDH is the rate-limiting enzyme for de novo purine synthesis. Inhibition of IMPDH results in reduced levels of guanylates, resulting in the inhibition tumor cell growth in vitro and in vivo. prodrug (Code: CHEBI:50266) antineoplastic agent (Code: CHEBI:35610) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Noxae (Code: D009676) TIZ
Click to view phetharbital Phetharbital is a short-acting barbiturate derivative without hypnotic properties, Phetharbital (N-phenylbarbital) can be used as a sedative and anticonvulsant agent due to its mechanism of enhancing GABA (Gamma Amino Butyric Acid) transmission and inhibition of synaptic excitation. Phetharbital has generally been withdrawn from clinical use. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377)
Click to view carisoprodol A centrally acting skeletal muscle relaxant whose mechanism of action is not completely understood but may be related to its sedative actions. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1202) Centrally-mediated Muscle Relaxation (Code: N0000175730) muscle relaxant (Code: CHEBI:51371) Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 1959-04-09 FDA
Click to view fenspiride Phosphodiesterase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27815|Q07343|Q08493|Q08499, gene: PDE4A|PDE4B|PDE4C|PDE4D, swissprot: PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9489859) cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9489859) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_000049_024429_RCP.pdf&retry=0&sys=m0b1l3) Fenspiride is an oxazolidinone spiro compound used as a drug in the treatment of certain respiratory diseases. It is used for the treatment of acute and chronic inflammatory diseases of the respiratory tract (like rhinopharyngitis, laryngitis, tracheobronchitis, otitis and sinusitis), as well as for maintenance treatment of asthma. Several countries withdrew fenspiride-based drugs from the market due to the risk of QT prolongation and torsades de pointes. Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1996-06-22 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view imolamine Imolamine is indicated for the treatment of angina pectoris. The hydrochloride form is used as a local anesthetic. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view ropinirole D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020658s034lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020658s034lbl.pdf) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18691132) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18691132) Ropinirole is a non-ergoline dopamine agonist. The precise mechanism of action of ropinirole as a treatment for Parkinson's disease is unknown, although it is thought to be related to its ability to stimulate dopamine D2 receptors within the caudate-putamen in the brain. Ropinirole is indicated for the treatment of Parkinson’s disease and moderate-to-severe primary Restless Legs Syndrome. Nonergot Dopamine Agonist (Code: N0000175768) dopamine agonist (Code: CHEBI:51065) central nervous system drug (Code: CHEBI:35470) antidyskinesia agent (Code: CHEBI:66956) antiparkinson drug (Code: CHEBI:48407) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) 1997-09-19 FDA
Click to view oxymetazoline Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20030735) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9632357) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9632357) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10217294) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10217294) Oxymetazoline is an alpha1A adrenoceptor agonist. Oxymetazoline acts as a vasoconstrictor. Oxymetazoline elicits relief of conjunctival hyperemia by causing vasoconstriction of superficial conjunctival blood vessels. Oxymetazoline is used for the treatment of acute allergic conjunctivitis and in chemical (chloride) conjunctivitis. Vasoconstrictor (Code: N0000192562) Vasoconstriction (Code: N0000009908) Increased Sympathetic Activity (Code: N0000175651) Imidazolines (Code: N0000011304) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) alpha-adrenergic agonist (Code: CHEBI:35569) sympathomimetic agent (Code: CHEBI:35524) nasal decongestant (Code: CHEBI:77715) vasoconstrictor agent (Code: CHEBI:50514) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Nasal Decongestants (Code: D014663) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Vasoconstrictor Agents (Code: D014662) 1986-05-30 FDA
Click to view methaphenilene an antihistamine and anticholinergic
Click to view ifosfamide Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019763s020lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019763s020lbl.pdf) Ifosfamide is a chemotherapeutic agent chemically related to the nitrogen mustards and a synthetic analog of cyclophosphamide. Ifosfamide is a prodrug that requires metabolic activation by hepatic cytochrome P450 isoenzymes to exert its cytotoxic activity. Activation occurs by hydroxylation at the ring carbon atom forming the unstable intermediate 4-hydroxyifosfamide and its ring-opened aldo tautomer, which decomposes to yield the cytotoxic and urotoxic compound acrolein and an alkylating isophosphoramide mustard. Its cytotoxic action is primarily through DNA crosslinks caused by alkylation by the isophosphoramide mustard at guanine N-7 positions. The formation of inter-and intra-strand cross-links in the DNA results in cell death. Ifosfamide is indicated for use in combination with certain other approved antineoplastic agents for third-line chemotherapy of germ cell testicular cancer. It should be used in combination with mesna for prophylaxis of hemorrhagic cystitis. Alkylating Agents (Code: D000477) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) 1987-08-14 FDA
Click to view trimetazidine 3-ketoacyl-CoA thiolase B, peroxisomal (Organism: Rattus norvegicus, class: Enzyme, accessions: P07871, gene: Acaa1b, swissprot: THIKB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10720420) Carnitine O-palmitoyltransferase 1, muscle isoform (Organism: Rattus norvegicus, class: Enzyme, accessions: Q63704, gene: Cpt1b, swissprot: CPT1B_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21504156) Trimetazidine is an orally available small molecule compound with anti-ischemic, and potential immunomodulating and antineoplastic properties. Although its exact mechanism is not yet fully elucidated, it is postulated that upon administration, trimetazidine selectively inhibits long-chain 3-ketoacyl coenzyme A thiolase (LC 3-KAT), the final enzyme in the free fatty acid (FFA) beta-oxidation pathway. Trimetazidine also increases pyruvate dehydrogenase activity, binds to the mitochondrial membrane, directly inhibits cardiac fibrosis and improves mechanical resistance of the sarcolemma. Trimetazidine is used for the treatment of angina pectoris. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1986-12-01 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view cyclophosphamide Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012141s090,012142s112lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012141s090,012142s112lbl.pdf) Cytochrome P450 2C18 (Organism: Homo sapiens, class: Enzyme, accessions: P33260, gene: CYP2C18, swissprot: CP2CI_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012141s090,012142s112lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012141s090,012142s112lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012141s090,012142s112lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012141s090,012142s112lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/012141s090,012142s112lbl.pdf) Cyclophosphamide is a prodrug and synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities. In the liver, cyclophosphamide is converted to the active metabolites aldophosphamide and phosphoramide mustard, which bind to DNA, thereby inhibiting DNA replication and initiating cell death. Cyclophosphamide may also cause sterility, birth defects, mutations, and cancer.Cyclophosphamide is indicated for the treatment of: malignant lymphomas, Hodgkin’s disease, lymphocytic lymphoma, mixed-cell type lymphoma, histiocytic lymphoma, Burkitt’s lymphoma, multiple myeloma, leukemias (chronic lymphocytic leukemia, chronic granulocytic leukemia, acute myelogenous and monocytic leukemia, acute lymphoblastic leukemia), mycosis fungoides, neuroblastoma, adenocarcinoma of the ovary, retinoblastoma, carcinoma of the breast and nephrotic syndrome. Alkylating Agents (Code: D000477) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Antirheumatic Agents (Code: D018501) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Mutagens (Code: D009153) Myeloablative Agonists (Code: D019653) Noxae (Code: D009676) 1959-11-16 FDA
Click to view oxolinic acid Synthetic antimicrobial related to NALIDIXIC ACID and used in URINARY TRACT INFECTIONS. antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Renal Agents (Code: D012076) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) Ministry of Health of the Russian Federation OXI
Click to view benznidazole Benznidazole inhibits the synthesis of DNA, RNA, and proteins within the T. cruzi parasite. Studies suggest that benznidazole is reduced by a Type I nitroreductase (NTR) enzyme of T. cruzi producing a series of short-lived intermediates that may promote damage to several macromolecules including DNA. In mammalian cells, however, benznidazole is metabolized by reduction of the nitro group to an amino group by a Type II NTR enzyme. The precise mechanism of action is not known. Benznidazole is active against all three stages, trypomastigotes, amastigotes, and epimastigotes, of T. cruzi. However, the sensitivity of T. cruzi strains to benznidazole, from different geographic regions, may vary. antiprotozoal drug (Code: CHEBI:35820) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Mutagens (Code: D009153) Noxae (Code: D009676) Trypanocidal Agents (Code: D014344) 2017-08-29 FDA
Click to view etoxadrol Etoxadrol is a ketal. Etoxadrol is an NMDA receptor antagonist. It exerts phencyclidine-like properties. Etoxadrol has anticonvulsant and anesthetic activity. Etoxadrol was developed as an anesthetic but later was discontinued due to its side effects.
Click to view hexylcaine Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN) blocker (Source:) a benzoic acid ester, is a local anaesthetic that has been used for surface anaesthesia of mucous membranes. Local anesthetics produce a transient block of nerve conduction by interfering with sodium channels. This effect of the anesthetic interferes with the development of an action potential across the nerve. FDA
Click to view ethoheptazine an opioid analgesic from the phenazepine family. It was invented in the 1950s and is related to other drugs such as proheptazine. Ethoheptazine is no longer marketed in the United States. FDA
Click to view bufuralol Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7935340) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7935340) Bufuralol is a non-cardioselective beta-adrenergic blocker with high intrinsic sympathomimetic activity. It has affinity for both beta1 and beta2-adrenergic receptors. It acts as a potent beta-adrenoceptor antagonist with partial agonist activity. Bufuralol was developed for the treatment of hypertension. However, this research has been discontinued. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Neurotransmitter Agents (Code: D018377)
Click to view etoglucid Alkylating antineoplastic agent used especially in bladder neoplasms. It is toxic to hair follicles, gastro-intestinal tract, and vasculature. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676)
Click to view dimethylthiambutene an opioid analgesic drug opioid analgesic (Code: CHEBI:35482)
Click to view alphaprodine An opioid analgesic chemically related to and with an action resembling that of MEPERIDINE, but more rapid in onset and of shorter duration. It has been used in obstetrics, as pre-operative medication, for minor surgical procedures, and for dental procedures. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1067) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view setiptiline a tetracyclic antidepressant which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA) 1998 PMDA
Click to view phenindamine Histamine H1 receptor (Organism: Cavia porcellus, class: GPCR, accessions: P31389, gene: HRH1, swissprot: HRH1_CAVPO a pyridindene derivative was used to treat sneezing, runny nose, itching, watery eyes, hives, rashes, itching Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377)
Click to view methapyrilene Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Histamine H1 antagonist with sedative action used as a hypnotic and in allergies. Anti-Allergic Agents (Code: D018926) anti-allergic agent (Code: CHEBI:50857) sedative (Code: CHEBI:35717) H1-receptor antagonist (Code: CHEBI:37955) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377)
Click to view amixetrine - 1972 YEAR INTRODUCED
Click to view tolfenamic acid Aldo-keto reductase family 1 member A1 (Organism: Homo sapiens, class: Enzyme, accessions: P14550, gene: AKR1A1, swissprot: AK1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21187079) Aldo-keto reductase family 1 member C1 (Organism: Homo sapiens, class: Enzyme, accessions: Q04828, gene: AKR1C1, swissprot: AK1C1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21187079) Aldo-keto reductase family 1 member C2 (Organism: Homo sapiens, class: Enzyme, accessions: P52895, gene: AKR1C2, swissprot: AK1C2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21187079) Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21187079) Aldo-keto reductase family 1 member C4 (Organism: Homo sapiens, class: Enzyme, accessions: P17516, gene: AKR1C4, swissprot: AK1C4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21187079) Tolfenamic acid is a NSAID with anti-inflammatory, analgesic, and antipyretic effects. Tolfenamic acid acts as a prostaglandin synthesis inhibitor and a leukotriene synthesis inhibitor. It is used for the treatment of acute migraine. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Prostaglandin Antagonists (Code: D011448) Sensory System Agents (Code: D018689) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) 1997-04-25 UK Medicines and Healthcare Products Regulatory Agency (MHRA) TLF
Click to view reposal Reposal is a barbiturate derivative invented in the 1960s in Denmark. It has sedative, hypnotic and anticonvulsant properties, and was used primarily for the treatment of insomnia.
Click to view methohexital GABA-A receptor alpha-1/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P28472, gene: GABRA1|GABRB3|GABRG2, swissprot: GBRA1_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1842156) Methohexital is an intravenous anesthetic with a short duration of action that may be used for induction of anesthesia. Barbiturate (Code: N0000175693) Barbiturates (Code: N0000008016) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) intravenous anaesthetic (Code: CHEBI:38877) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) 1960-06-27 FDA
Click to view benzylsulfamide Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26803577) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26803577) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26803577) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26803577) Benzylsulfamide (4-(Benzylamino)benzenesulfonamide) is an aromatic amine.
Click to view fencibutirol Fencibutirol is alpha-cyclohexylbutyric acid derivative. It exerts choleretic activity. It was used in the treatment of constipation and biliary-tract disorders.
Click to view homosalate cpd not photoallergenic Cosmetics (Code: D003358) Dermatologic Agents (Code: D003879) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) Sunscreening Agents (Code: D013473) 1991 FDA
Click to view mepindolol a non-selective beta blocker; it is used to treat glaucoma Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Neurotransmitter Agents (Code: D018377) Italian Medicines Agency (AIFA)
Click to view cibenzoline Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y3Q4, gene: HCN4, swissprot: HCN4_HUMAN) ATP-sensitive inward rectifier potassium channel 11 (Organism: Homo sapiens, class: Ion channel, accessions: Q14654, gene: KCNJ11, swissprot: KCJ11_HUMAN) a class I sodium channel blocker antiarrhythmic drug Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) 1978-01-01 YEAR INTRODUCED
Click to view clonixin a anti-inflammatory analgesic. Clonixin is indicated for the relief of headaches, muscle aches, joint, dental, ear, dysmenorrhea, post-traumatic, post-surgical, gynecological. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) platelet aggregation inhibitor (Code: CHEBI:50427) vasodilator agent (Code: CHEBI:35620) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 6J3
Click to view ticlopidine Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10233213) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14563790) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14563790) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10759690) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515014) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515014) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515014) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515014) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515014) Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515014) Ticlopidine is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate receptor inhibitor. Ticlopidine is a prodrug that is metabolized to an as yet undetermined metabolite that acts as a platelet aggregation inhibitor. Ticlopidine is approved for the prevention of strokes and, when combined with aspirin, for patients with a new coronary stent to prevent closure. There are also several off-label uses, including acute treatment of myocardial infarction and unstable angina, peripheral vascular disease, prevention of myocardial infarctions, diabetic retinopathy, and sickle cell disease. Decreased Platelet Aggregation (Code: N0000008832) fibrin modulating drug (Code: CHEBI:48676) hematologic agent (Code: CHEBI:50248) platelet aggregation inhibitor (Code: CHEBI:50427) anticoagulant (Code: CHEBI:50249) Cardiovascular Agents (Code: D002317) Cytochrome P-450 CYP2C19 Inhibitors (Code: D065689) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Fibrin Modulating Agents (Code: D050299) Fibrinolytic Agents (Code: D005343) Hematologic Agents (Code: D006401) Metabolic Side Effects of Drugs and Substances (Code: D065606) Neurotransmitter Agents (Code: D018377) Platelet Aggregation Inhibitors (Code: D010975) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P2 Receptor Antagonists (Code: D058919) Purinergic P2Y Receptor Antagonists (Code: D058921) 1978-05-08 ANSM (French National Agency for Medicines and Health Products Safety) TIC
Click to view gemcitabine Gemcitabine: Equilibrative nucleoside transporter 3 (Organism: Homo sapiens, class: Transporter, accessions: Q9BZD2, gene: SLC29A3, swissprot: S29A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19164483) Deoxycytidine kinase (Organism: Homo sapiens, class: Kinase, accessions: P27707, gene: DCK, swissprot: DCK_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17101674) Gemcitabine diphosphate: Ribonucleoside-diphosphate reductase large subunit (Organism: Homo sapiens, class: Enzyme, accessions: P23921, gene: RRM1, swissprot: RIR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020509s082lbl.pdf) Ribonucleoside-diphosphate reductase subunit M2 (Organism: Homo sapiens, class: Enzyme, accessions: P31350, gene: RRM2, swissprot: RIR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020509s082lbl.pdf) Gemcitabine triphosphate: DNA polymerase (alpha/delta/epsilon) (Organism: Homo sapiens, class: Enzyme, accessions: P09884|P28340|Q07864, gene: POLA1|POLD1|POLE, swissprot: DPOD1_HUMAN|DPOE1_HUMAN|DPOLA_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020509s082lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12799644) Gemcitabine is a nucleoside metabolic inhibitor. Gemcitabine is metabolized by nucleoside kinases to diphosphate (dFdCDP) and triphosphate (dFdCTP) nucleosides. Gemcitabine diphosphate inhibits ribonucleotide reductase, an enzyme responsible for catalyzing the reactions that generate deoxynucleoside triphosphates for DNA synthesis, resulting in reductions in deoxynucleotide concentrations, including dCTP. Gemcitabine triphosphate competes with dCTP for incorporation into DNA. The reduction in the intracellular concentration of dCTP by the action of the diphosphate enhances the incorporation of gemcitabine triphosphate into DNA (selfpotentiation). After the gemcitabine nucleotide is incorporated into DNA, only one additional nucleotide is added to the growing DNA strands, which eventually results in the initiation of apoptotic cell death. Gemcitabine is indicated in combination with other drugs for the treatment of advanced ovarian, metastatic breast cancer or non-small cell lung cancer. Gemcitabine is also indicated as a single agent for the treatment of pancreatic cancer. Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) photosensitizing agent (Code: CHEBI:47868) radiosensitizing agent (Code: CHEBI:132992) prodrug (Code: CHEBI:50266) antineoplastic agent (Code: CHEBI:35610) antiviral drug (Code: CHEBI:36044) immunosuppressive agent (Code: CHEBI:35705) Anti-Infective Agents (Code: D000890) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Noxae (Code: D009676) Radiation-Sensitizing Agents (Code: D011838) 1996-05-15 FDA GEO
GCQ
GTF
Click to view miloxacin Miloxacin is an antibacterial agent. Miloxacin is active against a variety of gram-negative bacteria, especially Enterobacteriaceae and Haemophilus. Miloxacin is inactive at the maximum test doses against a Streptococcus pyogenes infection. It was used in veterinary.
Click to view hydroxypethidine Hydroxypethidine is an opioid receptor agonist. It was used as an analgesic. Hydroxypethidine is under international control under the Single Convention on Narcotic Drugs 1961 and therefore controlled like morphine in most countries.
Click to view melperone 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) an atypical antipsychotic of the butyrophenone chemical class. It has been well established in the treatment of confusion, anxiety, restlessness and schizophrenia as It is known to be well-tolerated with an excellent safety profile. 1972-01-01 YEAR INTRODUCED
Click to view tramadol Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022370s016s017lbl.pdf) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022370s016s017lbl.pdf) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022370s016s017lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022370s016s017lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022370s016s017lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022370s016s017lbl.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15105221) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12401609) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11561087) Tramadol is an opioid agonist, and an inhibitor of reuptake of norepinephrine and serotonin. Opioid activity of tramadol is due to both low affinity binding of the parent compound and higher affinity binding of the O-demethylated metabolite M1 to mu-opioid receptors. Tramadol has been shown to inhibit reuptake of norepinephrine and serotonin in vitro, as have some other opioid analgesics. Tramadol indicated for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) adrenergic uptake inhibitor (Code: CHEBI:35640) muscarinic antagonist (Code: CHEBI:48876) opioid analgesic (Code: CHEBI:35482) antitussive (Code: CHEBI:51177) mu-opioid receptor agonist (Code: CHEBI:55322) kappa-opioid receptor agonist (Code: CHEBI:59282) serotonin uptake inhibitor (Code: CHEBI:50949) serotonergic antagonist (Code: CHEBI:48279) nicotinic antagonist (Code: CHEBI:48878) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) 1995-03-03 FDA
Click to view butetamate a cough suppressant
Click to view protriptyline Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Tricyclic antidepressant similar in action and side effects to IMIPRAMINE. It may produce excitation. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Tricyclic Antidepressant (Code: N0000175752) 1967-09-27 FDA
Click to view nortriptyline Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Histamine H1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P31390, gene: Hrh1, swissprot: HRH1_RAT Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) ATP-sensitive inward rectifier potassium channel 10 (Organism: Homo sapiens, class: Ion channel, accessions: P78508, gene: KCNJ10, swissprot: KCJ10_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/17071817) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT A metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions. Tricyclic Antidepressant (Code: N0000175752) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) antidepressant (Code: CHEBI:35469) adrenergic uptake inhibitor (Code: CHEBI:35640) analgesic (Code: CHEBI:35480) antineoplastic agent (Code: CHEBI:35610) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) 1964-11-06 FDA 21B
Click to view sulfamerazine Dihydrofolate reductase (Organism: Pneumocystis carinii, class: Enzyme, accessions: P16184, gene: None, swissprot: DYR_PNECA) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/7486915/) Sulfamerazine is a long-acting sulfanilamide antibacterial agent. Sulfamerazine inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for the binding site on dihydropteroate synthase. Sulfamerazine (in comination with Sulfadiazine and Sulfamethazine) was used for the treatment of bacterial infections. Nowdays, the drugs containing sulfamerazine are no longer available for use in humans and they may be prescribed for veterinary purposes. antiinfective agent (Code: CHEBI:35441) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1949-08-16 FDA
Click to view propacetamol Propacetamol is a water-soluble para-aminophenol derivative and ester prodrug of acetaminophen in which acetaminophen is bound to the carboxylic acid diethylglycine, with analgesic and antipyretic activities. Upon intravenous administration, propacetamol is hydrolyzed by plasma esterases into its active form acetaminophen. Although the exact mechanism of action has yet to be fully elucidated despite its widespread use, acetaminophen enters the central nervous system and acts centrally. This agent binds to cyclooxygenase (COX) and prevents the metabolism of arachidonic acid to prostaglandin. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Ministry of Health of the Russian Federation
Click to view etaqualone an analog of the hypnotic methaqualone, a non-barbiturate sedative Etaqualone was used to treat insomnia.
Click to view pentifylline Pentifylline is an active vasodilating substance which does not affect blood sugar levels.
Click to view thialbarbital Thialbarbital is a barbiturate derivative with sedative effects. Thialbarbital causes marked depression of the activity of the reticular formation and only slight depression of cortical activity. Thialbarbital is short acting and has less of a tendency to induce respiratory depression than other barbiturate derivatives such as pentobarbital. It was used primarily as a surgical anesthesia.
Click to view tetracaine Sodium channel protein type 9 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q15858, gene: SCN9A, swissprot: SCN9A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/21570288) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/22770500) Sodium channel protein type 2 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q99250, gene: SCN2A, swissprot: SCN2A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/22770500) Sodium channel protein type 3 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9NY46, gene: SCN3A, swissprot: SCN3A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/27015369) Sodium channel protein type 8 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9UQD0, gene: SCN8A, swissprot: SCN8A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/27015369) Tetracaine is a benzoate ester with anesthetic properties. Upon administration, tetracaine reversibly binds voltage-gated sodium ion channels in neuronal cell membranes and inhibits sodium influx. This prevents the initiation and conduction of nerve impulses, and stabilizes neuronal membranes. This results in a loss of sensation, and thereby provides analgesia and anesthesia. Ester Local Anesthetic (Code: N0000175683) Esters (Code: N0000166743) Local Anesthesia (Code: N0000175976) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) local anaesthetic (Code: CHEBI:36333) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2005-06-23 FDA TE4
Click to view mianserin Histamine H1 receptor (Organism: Cavia porcellus, class: GPCR, accessions: P31389, gene: HRH1, swissprot: HRH1_CAVPO) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6302549) Histamine H2 receptor (Organism: Cavia porcellus, class: GPCR, accessions: P47747, gene: HRH2, swissprot: HRH2_CAVPO) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6302549) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22708686) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10997731) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8764331) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6142954) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15771415) Synaptic vesicular amine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q01827, gene: Slc18a2, swissprot: VMAT2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/6747993) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12109911) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12109911) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12109911) Mianserin is a tetracyclic antidepressant used for the treatment of depression. Mianserin's mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) antidepressant (Code: CHEBI:35469) sedative (Code: CHEBI:35717) alpha-adrenergic antagonist (Code: CHEBI:37890) adrenergic uptake inhibitor (Code: CHEBI:35640) serotonergic antagonist (Code: CHEBI:48279) histamine agonist (Code: CHEBI:35678) H1-receptor antagonist (Code: CHEBI:37955) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) 1985-08-01 CDSCO (INDIA)
Click to view antazoline Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist An ethylenediamine derivative with histamine H1 antagonistic and sedative properties. Antazoline antagonizes histamine H1 receptor and prevents the typical allergic symptoms caused by histamine activities on capillaries, skin, mucous membranes, and gastrointestinal and bronchial smooth muscles. These histamine activities include vasodilation, bronchoconstriction, increased vascular permeability, pain, itching, and spasmodic contractions of gastrointestinal smooth muscles. Antazoline is used to provide symptomatic relieve of allergic symptoms. Anti-Allergic Agents (Code: D018926) H1-receptor antagonist (Code: CHEBI:37955) cholinergic antagonist (Code: CHEBI:48873) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1990-04-30 FDA
Click to view sulfiram Sulfiram is a sulfide derivative. Sulfiram is a very weak inhibitor of aldehyde dehydrogenase. It is used for the treatment and prevention of scabies and other skin related problems like itching, skin irritation, and inflammation. Sulfiram is usually sold as a solution or medicated soap, sometimes in combination with benzyl benzoate.
Click to view streptozocin Streptozocin inhibits DNA synthesis in bacterial and mammalian cells. In bacterial cells, a specific interaction with cytosine moieties leads to degradation of DNA. The biochemical mechanism leading to mammalian cell death has not been definitely established; streptozocin inhibits cell proliferation at a considerably lower level than that needed to inhibit precursor incorporation into DNA or to inhibit several of the enzymes involved in DNA synthesis. Although streptozocin inhibits the progression of cells into mitosis, no specific phase of the cell cycle is particularly sensitive to its lethal effects. Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) antineoplastic agent (Code: CHEBI:35610) Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) 1982-05-07 FDA STZ
Click to view oxycinchophen cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y233, gene: PDE10A, swissprot: PDE10_HUMAN) Dihydroorotate dehydrogenase (quinone), mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q02127, gene: DHODH, swissprot: PYRD_HUMAN) as antidiuretic and has been specially found useful in cases of diabetes insipidus
Click to view albendazole Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12451431) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12451431) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10759686) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10759686) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10759686) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23959307) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23959307) Albendazole is an anthelmintic drug. Albendazole binds to the colchicine-sensitive site of beta-tubulin inhibiting their polymerization into microtubules. The decrease in microtubules in the intestinal cells of the parasites decreases their absorptive function, especially the uptake of glucose by the adult and larval forms of the parasites, and also depletes glycogen storage. Insufficient glucose results in insufficient energy for the production of adenosine trisphosphate (ATP) and the parasite eventually dies. Albendazole is indicated for the treatment of parenchymal neurocysticercosis due to active lesions caused by larval forms of the pork tapeworm, Taenia solium and for the treatment of cystic hydatid disease of the liver, lung, and peritoneum, caused by the larval form of the dog tapeworm, Echinococcus granulosus. Antihelminthic (Code: N0000175481) Cytochrome P450 1A Inducers (Code: N0000191624) Anthelmintics (Code: D000871) anthelminthic drug (Code: CHEBI:35443) Anti-Infective Agents (Code: D000890) Anticestodal Agents (Code: D000923) Antimitotic Agents (Code: D050256) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Antiprotozoal Agents (Code: D000981) Mitosis Modulators (Code: D050258) Tubulin Modulators (Code: D050257) 1996-06-11 FDA
Click to view parethoxycaine Parethoxycaine is a local anesthetic. It is more potent and more toxic than procaine. It is no longer available.
Click to view oxprenolol Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: ) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT) A beta-adrenergic antagonist used in the treatment of hypertension, angina pectoris, arrhythmias, and anxiety. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Anxiety Agents (Code: D014151) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sympatholytics (Code: D013565) Tranquilizing Agents (Code: D014149) Vasodilator Agents (Code: D014665) FDA
Click to view mirtazapine 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020415s030lbl.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020415s030lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020415s030lbl.pdf) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020415s030lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020415s030lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020415s030lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020415s030lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020415s030lbl.pdf) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020415s030lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020415s030lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/020415s019,021208s010lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/020415s019,021208s010lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/020415s019,021208s010lbl.pdf) Mirtazapine is a synthetic tetracyclic derivative of the piperazino-azepines with antidepressant activity. Mirtazapine is an antagonist at central presynaptic alpha2-adrenergic receptors, antagonist of 5-HT2 and 5-HT3 receptors, antagonist of histamine receptors, antagonist of alpha1-adrenergic receptors and antagonist of muscarinic receptors. Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) alpha-adrenergic antagonist (Code: CHEBI:37890) serotonergic antagonist (Code: CHEBI:48279) histamine antagonist (Code: CHEBI:37956) anxiolytic drug (Code: CHEBI:35474) H1-receptor antagonist (Code: CHEBI:37955) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) 1996-06-14 FDA
Click to view thiamine Thiamine transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: O60779, gene: SLC19A2, swissprot: S19A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10542220) Thiamin pyrophosphokinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q9H3S4, gene: TPK1, swissprot: TPK1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11342111) Thiamine, also known as vitamin B1, is a heat-labile and water-soluble essential vitamin with antioxidant, erythropoietic, mood modulating, and glucose-regulating activities. Thiamine reacts with adenosine triphosphate (ATP) to form an active coenzyme, thiamine pyrophosphate. Thiamine pyrophosphate is necessary for the actions of pyruvate dehydrogenase and alpha-ketoglutarate in carbohydrate metabolism and for the actions of transketolase, an enzyme that plays an important role in the pentose phosphate pathway. Thiamine plays a key role in intracellular glucose metabolism and may inhibit the action of glucose and insulin on arterial smooth muscle cell proliferation. Thiamine may also protect against lead toxicity by inhibiting lead-induced lipid peroxidation. Thiamine is indicated for the treatment of thiamine and niacin deficiency states, Korsakov's alcoholic psychosis, Wernicke-Korsakov syndrome, delirium, and peripheral neuritis. Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) 1947-07-28 FDA VIB
Click to view chloralodol Chlorhexadol is a sedative and hypnotic which is regulated in the United States as a Schedule III controlled substance. It is a derivative of chloral hydrate. Chloral hydrate has sedative/hypnotic activity which has been shown to extend the sleep of normal made adults via a dose-response relationship.
Click to view bropirimine Dihydroneopterin aldolase (Organism: Staphylococcus aureus, class: Enzyme, accessions: P56740, gene: folB, swissprot: FOLB_STAAU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15027862) Xanthine dehydrogenase/oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P47989, gene: XDH, swissprot: XDH_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24508129) Bropirimine is an immunostimulating agent. It acts as a toll-like receptor (TLR7) agonist and has anti-cancer and antiviral properties. Bropirimine may be used in experimental autoimmune encephalomyelitis (EAE) and bladder cancer research. Adjuvants, Immunologic (Code: D000276) Antineoplastic Agents (Code: D000970) Immunologic Factors (Code: D007155) Interferon Inducers (Code: D007369) PMDA
Click to view doxofylline is an oxopurine that is a derivative of xanthine, used in the treatment of asthma. It has a role as a bronchodilator agent, an antitussive and an anti-asthmatic drug. bronchodilator agent (Code: CHEBI:35523) antitussive (Code: CHEBI:51177) anti-asthmatic drug (Code: CHEBI:49167) Anti-Asthmatic Agents (Code: D018927) Antitussive Agents (Code: D000996) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Phosphodiesterase Inhibitors (Code: D010726) Respiratory System Agents (Code: D019141)
Click to view benzarone Solute carrier family 22 member 12 (Organism: Homo sapiens, class: Transporter, accessions: Q96S37, gene: SLC22A12, swissprot: S22AC_HUMAN) a nonpurine xanthine oxidase inhibitor used for the treatment of gout, but never approved for use in the United States because of concerns over reports of acute liver injury and deaths with its use. Cardiovascular Agents (Code: D002317) Fibrin Modulating Agents (Code: D050299) Fibrinolytic Agents (Code: D005343) Hematologic Agents (Code: D006401)
Click to view nevirapine Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020636s050,020933s040lbl.pdf) Gag-Pol polyprotein (Organism: Human immunodeficiency virus type 1 group M subtype B (isolate ARV2/SF2), class: Polyprotein, accessions: P04585, gene: gag-pol, swissprot: POL_HV1H2) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16911530) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020636s050,020933s040lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55| P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020636s050,020933s040lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020636s050,020933s040lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55| P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020636s050,020933s040lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11225565) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11225565) Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1. Nevirapine binds directly to reverse transcriptase (RT) and blocks the RNAdependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site. The activity of nevirapine does not compete with template or nucleoside triphosphates. HIV-2 RT and eukaryotic DNA polymerases are not inhibited by nevirapine. Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175463) Non-Nucleoside Analog (Code: N0000175460) Non-Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009948) Cytochrome P450 3A Inducers (Code: N0000190118) Cytochrome P450 2B6 Inducers (Code: N0000187064) antiviral drug (Code: CHEBI:36044) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Cytochrome P-450 CYP3A Inducers (Code: D065701) Enzyme Inhibitors (Code: D004791) Metabolic Side Effects of Drugs and Substances (Code: D065606) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 1996-06-21 FDA NVP
Click to view dienestrol Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist A synthetic, non-steroidal estrogen structurally related to stilbestrol. It is used, usually as the cream, in the treatment of menopausal and postmenopausal symptoms. xenoestrogen (Code: CHEBI:76988) Estrogens (Code: D004967) Estrogens, Non-Steroidal (Code: D004968) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1947-01-09 FDA
Click to view practolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: ) Beta-2 adrenergic receptor (Organism: Bos taurus, class: GPCR, accessions: Q28044, gene: ADRB2, swissprot: ADRB2_BOVIN) Beta-1 adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18090, gene: Adrb1, swissprot: ADRB1_RAT) Beta-2 adrenergic receptor (Organism: Cavia porcellus, class: GPCR, accessions: Q8K4Z4, gene: Adrb2, swissprot: ADRB2_CAVPO) Beta-1 adrenergic receptor (Organism: Cavia porcellus, class: GPCR, accessions: B0FL73, gene: ADRB1, swissprot: B0FL73_CAVPO) Beta-2 adrenergic receptor (Organism: Mus musculus, class: Unclassified, accessions: P18762, gene: Adrb2, swissprot: ADRB2_MOUSE) A beta-1 adrenergic antagonist that has been used in the emergency treatment of CARDIAC ARRYTHMIAS. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) beta-adrenergic antagonist (Code: CHEBI:35530) anti-arrhythmia drug (Code: CHEBI:38070) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Ministry of Health of the Russian Federation
Click to view atenolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist/antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018760s029lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018760s029lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24014644) Atenolol is a benzeneacetamide, synthetic, beta1-selective (cardioselective) adrenoreceptor blocking agent. Only (S)-atenolol, but not (R)-atenolol, contributes to the beta-blocking effect of currently used racemic atenolol since the same effect can be elicited with the (S)-enantiomer alone. Atenolol is used for the treatment of hypertension, angina pectoris and in the management of hemodynamically stable patients with definite or suspected acute myocardial infarction. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1981-08-19 FDA 2TN
Click to view nordazepam GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) Gamma-aminobutyric acid receptor subunit rho-2 (Organism: Homo sapiens, class: Ion channel, accessions: P28476, gene: GABRR2, swissprot: GBRR2_HUMAN) Gamma-aminobutyric acid type B receptor subunit 2 (Organism: Homo sapiens, class: GPCR, accessions: O75899, gene: GABBR2, swissprot: GABR2_HUMAN) An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam. Anti-Anxiety Agents (Code: D014151) anticonvulsant (Code: CHEBI:35623) sedative (Code: CHEBI:35717) GABA modulator (Code: CHEBI:50268) anxiolytic drug (Code: CHEBI:35474) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1961-01-01 YEAR INTRODUCED
Click to view desipramine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT Transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q63380, gene: NET, swissprot: Q63380_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Sodium-dependent noradrenaline transporter (Organism: Mus musculus, class: Transporter, accessions: O55192, gene: Slc6a2, swissprot: SC6A2_MOUSE Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q9WTR4, gene: Slc6a2, swissprot: Q9WTR4_RAT Sodium-dependent serotonin transporter (Organism: Mus musculus, class: Transporter, accessions: Q60857, gene: Slc6a4, swissprot: SC6A4_MOUSE Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Histamine H1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P31390, gene: Hrh1, swissprot: HRH1_RAT Serotonin (5-HT) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P19327|P28564|P28565|P30940|P30994|P31388|P32305|P35364|P35365|P35563|Q62758|Q9JJ16, gene: Htr1a|Htr1b|Htr1d|Htr1f|Htr2a|Htr2b|Htr2c|Htr3a|Htr3b|Htr4|Htr5a|Htr5b|Htr6|Htr7, swissprot: 5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT|5HT2A_RAT|5HT2B_RAT|5HT2C_RAT|5HT3A_RAT|5HT3B_RAT|5HT4R_RAT|5HT5A_RAT|5HT5B_RAT|5HT6R_RAT|5HT7R_RAT Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Voltage-dependent calcium channel gamma-1 subunit (Organism: Homo sapiens, class: Ion channel, accessions: Q06432, gene: CACNG1, swissprot: CCG1_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) G protein-activated inward rectifier potassium channel 2 (Organism: Mus musculus, class: Ion channel, accessions: P48542, gene: Kcnj6, swissprot: KCNJ6_MOUSE) blocker (Source: ) G protein-activated inward rectifier potassium channel 4 (Organism: Mus musculus, class: Unclassified, accessions: P48545, gene: Kcnj5, swissprot: KCNJ5_MOUSE) blocker (Source: ) Equilibrative nucleoside transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q7RTT9, gene: SLC29A4, swissprot: S29A4_HUMAN) inhibitor (Source: ) A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors. Tricyclic Antidepressant (Code: N0000175752) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) adrenergic uptake inhibitor (Code: CHEBI:35640) serotonin uptake inhibitor (Code: CHEBI:50949) cholinergic antagonist (Code: CHEBI:48873) alpha-adrenergic antagonist (Code: CHEBI:37890) H1-receptor antagonist (Code: CHEBI:37955) antidepressant (Code: CHEBI:35469) drug allergen (Code: CHEBI:88188) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) 1964-11-20 FDA DSM
Click to view cyclizine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) A histamine H1 antagonist given by mouth or parenterally for the control of postoperative and drug-induced vomiting and in motion sickness. (From Martindale, The Extra Pharmacopoeia, 30th ed, p935) antiemetic (Code: CHEBI:50919) cholinergic antagonist (Code: CHEBI:48873) central nervous system depressant (Code: CHEBI:35488) local anaesthetic (Code: CHEBI:36333) H1-receptor antagonist (Code: CHEBI:37955) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) FDA
Click to view propenidazole Propenidazole is an imidazole derivative. It was used as an antiinfective agent for vaginal administration for the treatment of amoebiasis, giardiasis and trichomoniasis.
Click to view zidovudine Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019655s058,019910s045,019951s036lbl.pdf) Telomerase reverse transcriptase (Organism: Homo sapiens, class: Enzyme, accessions: O14746, gene: TERT, swissprot: TERT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23303810) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19953504) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19953504) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19953504) Thymidylate kinase (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Kinase, accessions: P9WKE1, gene: tmk, swissprot: KTHY_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12930144) Thymidine kinase (Organism: Ureaplasma parvum serovar 3 (strain ATCC 700970), class: Unclassified, accessions: Q9PPP5, gene: tdk, swissprot: KITH_UREPA) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20378362) Thymidine kinase (Organism: Homo sapiens, class: Kinase, accessions: P23919, gene: DTYMK, swissprot: KTHY_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20378362) Reverse transcriptase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q9WKE8, gene: reverse transcriptas, swissprot: Q9WKE8_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019655s058,019910s045,019951s036lbl.pdf) A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia. Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175462) Nucleoside Analog (Code: N0000175459) Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009947) antiviral drug (Code: CHEBI:36044) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antimetabolites (Code: D000963) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Noxae (Code: D009676) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 1987-03-19 FDA AZZ
Click to view acetamidoeugenol Acetamidoeugenol is an intravenous anesthetic. Acetamidoeugenol is oxidized very rapidly in vivo into the corresponding aryl-acetic acid. It has been withdrawn because it provokes irritations and lesions of the vascular wall.
Click to view adenosine Adenosine receptor A2b (Organism: Homo sapiens, class: GPCR, accessions: P29275, gene: ADORA2B, swissprot: AA2BR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11226378) Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11226378) Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11226378) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11226378) Phosphatidylinositol 4-kinase type 2-alpha (Organism: Homo sapiens, class: Kinase, accessions: Q9BTU6, gene: PI4K2A, swissprot: P4K2A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21704602) Phosphatidylinositol 4-kinase type 2-beta (Organism: Homo sapiens, class: Kinase, accessions: Q8TCG2, gene: PI4K2B, swissprot: P4K2B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21704602) Adenosine deaminase (Organism: Homo sapiens, class: Enzyme, accessions: P00813, gene: ADA, swissprot: ADA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8452534) Equilibrative nucleoside transporter 3 (Organism: Homo sapiens, class: Transporter, accessions: Q9BZD2, gene: SLC29A3, swissprot: S29A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15701636) Equilibrative nucleoside transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q7RTT9, gene: SLC29A4, swissprot: S29A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20592246) Adenosine is an endogenous nucleoside occurring in all cells of the body. Adenosine may exert its pharmacologic effects by activation of purine (cell surface A1 and A2 adenosine) receptors, as well as relax vascular smooth muscles through the reduction in calcium uptake by inhibition of slow inward calcium current and activation of adenylate cyclase in smooth muscle cells. Adenosine may reduce vascular tone by modulation of sympathetic neurotransmission. The drug also has negative chronotropic, dromotropic, and inotropic effects on the heart by slowing conduction time throught he AV node and interrupting AV nodal reentry pathways. Adenosine is a potent vasodilator in most vascular beds, but vasoconstriction is produced in renal afferent arterioles and hepatic veins. The drug produces a net mild to moderate reduction in systolic, diastolic, and mean arterial blood pressure and a reflex increase in heart rate. Adenosine is used as an initial treatment for the termination of paroxysmal supraventricular tachycardia (PVST), including that associated with accessory bypass tracts, and is a drug of choice for terminating stable, narrow-complex supraventricular tachycardias (SVT). Also used as an adjunct to thallous chloride TI 201 myocardial perfusion scintigraphy (thallium stress test) in patients who are unable to exercise adequately, as well as an adjunct to vagal maneuvers and clinical assessment to establish a specific diagnosis of undefined, stable, narrow-complex SVT. Vidarabine is an analog of adenosine with the D-ribose replaced with D-arabinose. Vidarabine is a synthetic purine nucleoside analog with in vitro and in vivo inhibitory activity against herpes simplex virus types 1 (HSV-1), 2 (HSV-2), and varicella-zoster virus (VZV). The inhibitory activity of Vidarabine is highly selective due to its affinity for the enzyme thymidine kinase (TK) encoded by HSV and VZV. This viral enzyme converts Vidarabine into Vidarabine monophosphate, a nucleotide analog. The monophosphate is further converted into diphosphate by cellular guanylate kinase and into triphosphate by a number of cellular enzymes. in vitro, Vidarabine triphosphate stops replication of herpes viral DNA. When used as a substrate for viral DNA polymerase, Vidarabine triphosphate competitively inhibits dATP leading to the formation of 'faulty' DNA. Vidarabine is used for treatment of chickenpox - varicella, herpes zoster and herpes simplex. Adenosine Receptor Agonist (Code: N0000178375) Adenosine Receptor Agonists (Code: N0000175788) Analgesics (Code: D000700) Anti-Arrhythmia Agents (Code: D000889) anti-arrhythmia drug (Code: CHEBI:38070) vasodilator agent (Code: CHEBI:35620) analgesic (Code: CHEBI:35480) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Purinergic Agents (Code: D058905) Purinergic Agonists (Code: D058913) Purinergic P1 Receptor Agonists (Code: D058906) Sensory System Agents (Code: D018689) Vasodilator Agents (Code: D014665) adenosine: 1989-10-30 FDA vidarabine: 1976-11-26 FDA ADN
RAB
Click to view voglibose Lysosomal alpha-glucosidase (Organism: Homo sapiens, class: Enzyme, accessions: P10253, gene: GAA, swissprot: LYAG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18595718) Lysosomal alpha-glucosidase (Organism: Rattus norvegicus, class: Enzyme, accessions: Q6P7A9, gene: Gaa, swissprot: LYAG_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18595718) Sucrase-isomaltase, intestinal (Organism: Rattus norvegicus, class: Enzyme, accessions: P23739, gene: Si, swissprot: SUIS_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18595718) Voglibose is an alpha-glucosidase inhibitor used for lowering post-prandial blood glucose levels in people with diabetes mellitus. Later on the drug was approved for the prevention of type 2 diabetes. Enzyme Inhibitors (Code: D004791) Glycoside Hydrolase Inhibitors (Code: D065089) Hypoglycemic Agents (Code: D007004) 1994-08-20 PMDA VOG
Click to view cafaminol - 1974 YEAR INTRODUCED
Click to view sulfafurazole Endothelin-1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25101, gene: EDNRA, swissprot: EDNRA_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10969989) Folic acid synthesis protein fol1 (Organism: Pneumocystis carinii, class: Enzyme, accessions: P29251, gene: fol1, swissprot: FOL1_PNECA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7486915) Sulfafurazole (sulfisoxazole) is a broad-spectrum, short-acting sulfanilamide and a synthetic analog of para-aminobenzoic acid (PABA) with antibacterial property. Sulfisoxazole competes with PABA for the bacterial enzyme dihydropteroate synthase, thereby preventing the incorporation of PABA into dihydrofolic acid, the immediate precursor of folic acid. Sulfisoxazole acetyl, the prodrug of sulfafurazole, in combination with erythromycin ethylsuccinate is used for treatment ofacute otitis media caused by susceptible strains of Haemophilus influenzae,Streptococcus pneumoniae, Streptococcus pyogenes or Branhamella catarrhalis. Sulfonamide Antimicrobial (Code: N0000175504) Sulfonamides (Code: N0000008048) antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) 1971-06-07 FDA
Click to view sulfamoxole a sulfonamide antibiotic. It has a role as an antimicrobial agent. Anti-Infective Agents (Code: D000890) 1962-03-01 CDSCO (INDIA)
Click to view apomorphine Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) agonist (Source: ) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: ) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: ) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: ) D(1A) dopamine receptor (Organism: Mus musculus, class: GPCR, accessions: Q61616, gene: Drd1, swissprot: DRD1_MOUSE D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist Dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901|P19020|P25115|P30729|P61169, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_RAT|DRD2_RAT|DRD3_RAT|DRD4_RAT|DRD5_RAT D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P19328|P22086|P22909, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT D(1A) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901, gene: Drd1, swissprot: DRD1_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist Dopamine receptor (Organism: Bos taurus, class: GPCR, accessions: P20288|Q95136, gene: DRD1|DRD2, swissprot: DRD1_BOVIN|DRD2_BOVIN 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT D(4) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30729, gene: Drd4, swissprot: DRD4_RAT 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT D(2) dopamine receptor (Organism: Bos taurus, class: GPCR, accessions: P20288, gene: DRD2, swissprot: DRD2_BOVIN D(3) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19020, gene: Drd3, swissprot: DRD3_RAT Serotonin (5-HT) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P19327|P28564|P28565|P30940|P30994|P31388|P32305|P35364|P35365|P35563|Q62758|Q9JJ16, gene: Htr1a|Htr1b|Htr1d|Htr1f|Htr2a|Htr2b|Htr2c|Htr3a|Htr3b|Htr4|Htr5a|Htr5b|Htr6|Htr7, swissprot: 5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT|5HT2A_RAT|5HT2B_RAT|5HT2C_RAT|5HT3A_RAT|5HT3B_RAT|5HT4R_RAT|5HT5A_RAT|5HT5B_RAT|5HT6R_RAT|5HT7R_RAT Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) activator (Source: ) Mannose-6-phosphate isomerase (Organism: Homo sapiens, class: Enzyme, accessions: P34949, gene: MPI, swissprot: MPI_HUMAN Cytoplasmic zinc-finger protein (Organism: Caenorhabditis elegans, class: Unclassified, accessions: G5EF15, gene: pos-1, swissprot: G5EF15_CAEEL Zinc finger protein mex-5 (Organism: Caenorhabditis elegans, class: Cytosolic other, accessions: Q9XUB2, gene: mex-5, swissprot: MEX5_CAEEL A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. Dopaminergic Agonist (Code: N0000175580) antidyskinesia agent (Code: CHEBI:66956) antiparkinson drug (Code: CHEBI:48407) dopamine agonist (Code: CHEBI:51065) alpha-adrenergic drug (Code: CHEBI:48539) serotonergic drug (Code: CHEBI:48278) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Emetics (Code: D004639) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) 2004-04-20 FDA
Click to view carbuterol sympathomimetric specific for beta2 receptors; proposed bronchodilator agent 1980 YEAR INTRODUCED
Click to view metoprolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12679135) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10960071) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/30248178) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Metoprolol is a cardioselective beta-blocker that is widely used in the treatment of hypertension and angina pectoris. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) beta-adrenergic antagonist (Code: CHEBI:35530) antihypertensive agent (Code: CHEBI:35674) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1978-08-07 FDA
Click to view razoxane iron (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020212s017lbl.pdf) DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7575679) DNA topoisomerase 2-beta (Organism: Homo sapiens, class: Enzyme, accessions: Q02880, gene: TOP2B, swissprot: TOP2B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7575679) Razoxane is an antitu-mor agent. Dexrazoxane is the (+)-(S)-enantiomer of racemic razoxane used to reduce doxorubicin-induced cardiotoxicity. Dexrazoxane likely acts by diffusing into the cell and hydrolyzing to its rings-openedmetal ion binding form, which has a structuresimilar to EDTA. However, the enzyme dihydropyrimidine amidohydrolase in liver and kidney stereoselectively catalyzes the first ring-opening step in dexrazoxane versus levrazoxane, and can subsequently open the second ring only in dexrazoxane, which is required for activity. This form may chelate free iron or displace iron bound to the iron-doxorubicin complex, thus reducing iron-based oxygen radical formation. In vitro, both dexrazoxane and its stereoisomer levrazoxane are equally cytotoxic and inhibitory toward DNA topoisomerase II. At lower doses, corresponding to those used clinically, dexrazoxane improved survival in anthracycline treated animals, and at some doses additionally demonstrated increased cardioprotection and a decrease in immune effector cells. Dexrazoxane is indicated for the treatment of extravasation resulting from intravenous anthracycline chemotherapy. antineoplastic agent (Code: CHEBI:35610) cardiovascular drug (Code: CHEBI:35554) immunosuppressive agent (Code: CHEBI:35705) Antineoplastic Agents (Code: D000970) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protective Agents (Code: D020011) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) Cytoprotective Agent (Code: N0000180854) 1995-05-26 FDA CDX
Click to view azacyclonol Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN an ataractive agent. It was used for treatment of schizophrenia, likely to reduce the psychedelic effects of LSD and mescaline. 1955 YEAR INTRODUCED
Click to view pipradrol an antidepressant. Pipradrol was made illegal in many countries in 1970s because of its potential for abuse. Experimentation with the drug and its derivatives for recreational purposes has led to many cases of acute toxicity and has been linked to three fatalities. It has shown favorable effects in postpartum depressive symptoms
Click to view epervudine a deoxyuridine analogue with antiviral activity against Herpes simplex and Varicella zoster viruses. Ministry of Health of the Russian Federation
Click to view chlornaphazine Chlornaphazine is an alkylating antineoplastic agent. Chlornaphazine was used for the treatment of Hodgkin's disease and polycythemia vera. However this compound caused bladder tumors. It was withdrawn from the market.
Click to view nifurtoinol Nifurtoinol has properties similar to nitrofurantoin. It is bactericidal to most gram positive and gram negative urinary tract pathogens. antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076) Italian Medicines Agency (AIFA)
Click to view inosine A purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It is an intermediate in the degradation of purines and purine nucleosides to uric acid and in pathways of purine salvage. It also occurs in the anticodon of certain transfer RNA molecules. (Dorland, 28th ed) FDA
Click to view isoxepac Non-steroidal arylacetic acid derivative anti-inflammatory with analgesic and antipyretic activity
Click to view pentostatin Adenosine deaminase (Organism: Homo sapiens, class: Enzyme, accessions: P00813, gene: ADA, swissprot: ADA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020122s015lbl.pdf) Pentostatin (2’-deoxycoformycin, DCF), is a potent inhibitor of the enzyme adenosine deaminase (ADA) and is isolated from fermentation cultures of Streptomyces antibioticus. Pentostatin inhibition of ADA, particularly in the presence of adenosine or deoxyadenosine, leads to cytotoxicity, and this is believed to be due to elevated intracellular levels of dATP which can block DNA synthesis through inhibition of ribonucleotide reductase. Pentostatin can also inhibit RNA synthesis as well as cause increased DNA damage. In addition to elevated dATP, these mechanisms may also contribute to the overall cytotoxic effect of pentostatin. The precise mechanism of pentostatin’s antitumor effect, however, in hairy cell leukemia is not known. Pentostatin is indicated as single-agent treatment for both untreated and alpha-interferon-refractory hairy cell leukemia patients with active disease as defined by clinically significant anemia, neutropenia, thrombocytopenia, or disease-related symptoms. Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) Adenosine Deaminase Inhibitors (Code: D058892) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) 1991-10-11 FDA DCF
Click to view ripazepam Ripazepam is a pyrazolodiazepine that has anxiolytic effects.
Click to view diethylstilbestrol Steroid hormone receptor ERR2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O95718, gene: ESRRB, swissprot: ERR2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11297507) Estrogen-related receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P62508, gene: ESRRG, swissprot: ERR3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15161930) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22682699) Steroid hormone receptor ERR1 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11474, gene: ESRRA, swissprot: ERR1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11297507) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: O95718, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: www.ncbi.nlm.nih.gov/pubmed/12533678) A synthetic nonsteroidal estrogen used in the treatment of menopausal and postmenopausal disorders. It was also used formerly as a growth promoter in animals. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), diethylstilbestrol has been listed as a known carcinogen. (Merck, 11th ed) antineoplastic agent (Code: CHEBI:35610) xenoestrogen (Code: CHEBI:76988) Carcinogens (Code: D002273) Estrogens (Code: D004967) Estrogens, Non-Steroidal (Code: D004968) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Noxae (Code: D009676) 1973-05-30 FDA DES
Click to view sulfamethizole Dihydropteroate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AC13, gene: folP, swissprot: DHPS_ECOLI) inhibitor A sulfathiazole antibacterial agent. antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) 1953-10-28 FDA
Click to view moclobemide Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12595913) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12595913) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12595913) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12595913) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12595913) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00035176.PDF) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19091581) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21680183) Moclobemide is a short-acting, Reversible Inhibitor of Monoamine oxidase type A (RIMA). It is a benzamide derivative which inhibits the deamination of serotonin, noradrenaline and dopamine. This action leads to increased concentrations of these neurotransmitters, which may account for the antidepressant activity of moclobemide. antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619) 1991-06-19 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view dichlorophen Dichlorophene is a halogenated phenolic compound that functions as a bacteriocide and fungicide in cosmetics. Dichlorophen was used in the treatment of tapeworm infestation in man and animals and is the basis of a preparation against athlete’s foot. It is often combined with toluene to remove parasites including ascarids, tapeworm, and hookworm from dogs and cats. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Anticestodal Agents (Code: D000923) Antifungal Agents (Code: D000935) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Antiprotozoal Agents (Code: D000981)
Click to view propatylnitrate Propatylnitrate is a coronary vasodilator, which is chemically related to both glyceryl trinitrate and erythrol tetranitrate. Propatylnitrate was more rapid than glyceryl trinitrate in relieving acute attacks of angina. Propatylnitrate is used for the treatment of angina pectoris.
Click to view endralazine Endralazine is a peripheral vasodilator. It acts by direct relaxation of the smooth muscle fibres of the peripheral arterial vessels. Endralazine was used as an antihypertensive agent. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view sulfasomizole Sulfasomizole is a sulfonamide antibiotic with broad-spectrum activity. It was used for the treatment of urinary tract infections.
Click to view sulfamethylthiazole Sulfamethylthiazole is a sulfonamide antibiotic. It is used in combination with tetracycline for the treatment and pre- and post-operative prevention of eye infections caused by bacteria sensitive to Tetracycline and Sulfamethylthiazole such as ulcerative blepharitis, dacryocystitis, conjunctivitis, septic corneal ulcers. Also this combination is used for the adjuvant treatment of trachoma. 2000-06-01 Italian Medicines Agency (AIFA)
Click to view rizatriptan 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) agonist (Source: ) Serotonin 3 (5-HT3) receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35563|Q9JJ16, gene: Htr3a|Htr3b, swissprot: 5HT3A_RAT|5HT3B_RAT) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT) 5-hydroxytryptamine receptor 1D (Organism: Sus scrofa, class: GPCR, accessions: P79400, gene: HTR1D, swissprot: 5HT1D_PIG) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) a selective 5-hydroxytryptamine (5-HT1B/1D) receptor agonist, used in the treatment of migraine headache Serotonin 1b Receptor Agonists (Code: N0000175763) Serotonin 1d Receptor Agonists (Code: N0000175764) Serotonin-1b and Serotonin-1d Receptor Agonist (Code: N0000175765) vasoconstrictor agent (Code: CHEBI:50514) anti-inflammatory drug (Code: CHEBI:35472) serotonergic agonist (Code: CHEBI:35941) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) 1998-06-29 FDA
Click to view orphenadrine Sodium channel protein type 10 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y5Y9, gene: SCN10A, swissprot: SCNAA_HUMAN) blocker Sodium channel protein type 9 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q15858, gene: SCN9A, swissprot: SCN9A_HUMAN) blocker Sodium channel protein type 4 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35499, gene: SCN4A, swissprot: SCN4A_HUMAN) blocker Sodium channel protein type 1 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35498, gene: SCN1A, swissprot: SCN1A_HUMAN) blocker Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Histamine H1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P31390, gene: Hrh1, swissprot: HRH1_RAT Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Glutamate [NMDA] receptor (Organism: Homo sapiens, class: Ion channel, accessions: O15399|O60391|Q05586|Q12879|Q13224|Q14957|Q8TCU5, gene: GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B, swissprot: NMD3A_HUMAN|NMD3B_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMDE4_HUMAN|NMDZ1_HUMAN A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. antidyskinesia agent (Code: CHEBI:66956) H1-receptor antagonist (Code: CHEBI:37955) antiparkinson drug (Code: CHEBI:48407) parasympatholytic (Code: CHEBI:50370) muscle relaxant (Code: CHEBI:51371) muscarinic antagonist (Code: CHEBI:48876) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Cytochrome P-450 CYP2B6 Inhibitors (Code: D065686) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Metabolic Side Effects of Drugs and Substances (Code: D065606) Muscarinic Antagonists (Code: D018727) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Centrally-mediated Muscle Relaxation (Code: N0000175730) 1957-05-10 FDA
Click to view tolbutamide ATP-sensitive inward rectifier potassium channel 11 (Organism: Homo sapiens, class: Ion channel, accessions: Q14654, gene: KCNJ11, swissprot: KCJ11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7502040) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9578596) Solute carrier family 15 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P51574, gene: Slc15a1, swissprot: S15A1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10748266) Solute carrier family 15 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63424, gene: Slc15a2, swissprot: S15A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10748266) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10854830) Tolbutamide is an oral blood-glucose-lowering drug of the sulfonylurea class. Tolbutamide appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which tolbutamide lowers blood glucose during long-term administration has not been clearly established. Tolbutamide is used with diet to lower blood glucose levels in patients with diabetes mellitus type II. Sulfonylurea (Code: N0000175608) Sulfonylurea Compounds (Code: N0000008054) hypoglycemic agent (Code: CHEBI:35526) Hypoglycemic Agents (Code: D007004) 1957-05-31 FDA
Click to view moxastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/13757612) Moxastine is a diarylmethane derivative with an antihistamine and anticholinergic activities. Moxastine is used in combination with caffeine for the prevention and treatment of motion sicknesses. 1969-09-01 State Institute for Drug Control (SUKL) Czech Republic
Click to view pramiracetam a central nervous system stimulant and nootropic agent. Pramiracetam is used for the treatment of concentration and memory disturbances caused by the degeneration of brain cells or to diseases of the blood vessels supplying the brain.
Click to view leflunomide Dihydroorotate dehydrogenase (quinone), mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q02127, gene: DHODH, swissprot: PYRD_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020905s031lbl.pdf) Aryl hydrocarbon receptor (Organism: Homo sapiens, class: Transcription factor, accessions: P35869, gene: AHR, swissprot: AHR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20957046) Leflunomide is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis. Leflunomide therapy is associated with frequent elevations in serum aminotransferase levels and with rare instances of clinically apparent acute liver injury which can be severe and even fatal. Antirheumatic Agent (Code: N0000175713) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antineoplastic agent (Code: CHEBI:35610) antiparasitic agent (Code: CHEBI:35442) prodrug (Code: CHEBI:50266) immunosuppressive agent (Code: CHEBI:35705) Antirheumatic Agents (Code: D018501) Enzyme Inhibitors (Code: D004791) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) 1998-09-10 FDA
Click to view estrone Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Arachidonate 15-lipoxygenase (Organism: Oryctolagus cuniculus, class: Enzyme, accessions: P12530, gene: ALOX15, swissprot: LOX15_RABIT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Steryl-sulfatase (Organism: Homo sapiens, class: Enzyme, accessions: P08842, gene: STS, swissprot: STS_HUMAN Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN Estradiol 17-beta-dehydrogenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P14061, gene: HSD17B1, swissprot: DHB1_HUMAN Corticosteroid-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P08185, gene: SERPINA6, swissprot: CBG_HUMAN An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women. bone density conservation agent (Code: CHEBI:50646) antineoplastic agent (Code: CHEBI:35610) Estrogens (Code: D004967) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1979-02-21 FDA J3Z
Click to view hexestrol Estrogen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P06211, gene: Esr1, swissprot: ESR1_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9048584) Estrogen receptor beta (Organism: Rattus norvegicus, class: Transcription factor, accessions: Q62986, gene: Esr2, swissprot: ESR2_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9048584) Hexestrol is a derivative of alpha,beta-diphenylethane, and it is a synthetic estrogen. Hexestrol is used as a hormonal antineoplastic agent as estrone. It is also used for prostate cancer or its hypertrophy in men. Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Estrogens (Code: D004967) Estrogens, Non-Steroidal (Code: D004968) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1964-04-30 Ministry of Health of the Russian Federation HXS
Click to view doxylamine Histamine H1 antagonist with pronounced sedative properties. It is used in allergies and as an antitussive, antiemetic, and hypnotic. Doxylamine has also been administered in veterinary applications and was formerly used in PARKINSONISM. histamine antagonist (Code: CHEBI:37956) cholinergic antagonist (Code: CHEBI:48873) sedative (Code: CHEBI:35717) H1-receptor antagonist (Code: CHEBI:37955) antitussive (Code: CHEBI:51177) antiemetic (Code: CHEBI:50919) anti-allergic agent (Code: CHEBI:50857) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Antihistamine (Code: N0000175750) Histamine Receptor Antagonists (Code: N0000000207) 1948-04-07 FDA
Click to view tolonium Microtubule-associated protein tau (Organism: Homo sapiens, class: Structural, accessions: P10636, gene: MAPT, swissprot: TAU_HUMAN) Zinc finger protein mex-5 (Organism: Caenorhabditis elegans, class: Cytosolic other, accessions: Q9XUB2, gene: mex-5, swissprot: MEX5_CAEEL) A phenothiazine that has been used as a hemostatic, a biological stain, and a dye for wool and silk. Tolonium chloride has also been used as a diagnostic aid for oral and gastric neoplasms and in the identification of the parathyroid gland in thyroid surgery. fluorochrome (Code: CHEBI:51217) histological dye (Code: CHEBI:77178) diagnostic agent (Code: CHEBI:33295) Coagulants (Code: D003029) Coloring Agents (Code: D004396) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) Heparin Antagonists (Code: D006494)
Click to view fenethazine a first-generation phenothiazine H1-antihistamine.
Click to view mecloqualone a quinazoline-class GABAergic and an analog of methaqualone. It induces sedative, hypnotic and anxiolytic effects.
Click to view clofenamide Clofenamide is a benzenedisulfonamide-based agent and carbonic anhydrase (CA) inhibitor with diuretic activity. Clofenamide inhibits CA, thereby preventing sodium, bicarbonate and thus water reabsorption in the proximal convoluted tubule resulting in diuresis.
Click to view chloroprocaine Chloroprocaine is a non-pyrogenic local anesthetic. It blocks the generation and the conduction of nerve impulses, presumably by increasing the hreshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse and by reducing the rate of rise of the action potential. Chloroprocaine is indicated for the production of local anesthesia by infiltration and peripheral nerve block. Ester Local Anesthetic (Code: N0000175683) Esters (Code: N0000166743) Local Anesthesia (Code: N0000175976) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) local anaesthetic (Code: CHEBI:36333) peripheral nervous system drug (Code: CHEBI:49110) central nervous system depressant (Code: CHEBI:35488) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1955-03-11 FDA
Click to view medazepam A benzodiazepine derivative used in the treatment of anxiety. It has sedative, muscle relaxant, and anticonvulsant properties. Anti-Anxiety Agents (Code: D014151) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 2004-04-12 Ministry of Health of the Russian Federation
Click to view pentrinitrol Pentrinitrol (pentaerythritol trinitrate) is a soluble organic nitrate with hypotensive activity. Pentrinitrol is used as a coronary vasodilator agent.
Click to view delmopinol Delmopinol is a surface-active cationic agent. It was used for the treatment of gingivitis and prevention of periodontitis. The drug interacts with the early acquired pellicle, the thin layer of saliva polymers and proteins covering teeth and gums, and forms a barrier over teeth and gums. This barrier prevents the microbial adhesion and colonisation on the tooth and gum surface. Delmopinol itself has no bactericidal activity. Cosmetics (Code: D003358) Mouthwashes (Code: D009067) Surface-Active Agents (Code: D013501)
Click to view acetaminosalol Acetaminosalol is a salicylic acid derivative. It hasanalgesic, antipyretic and anti-inflammatory properties. It was used as an analgesic. It was also used as a substitute for salicylic acid in acute rheumatism. It is no longer available.
Click to view carbubarb Carbubarb is hydroxyalkylmalonylurea derivative and a member of barbiturates. It was used as a sedatives and hypnotic agent.
Click to view ftivazide Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28197313) Ftivazide is a derivative of isoniazid. It blocks the synthesis of mycolic acids (provide acid resistance of Mycobacterium tuberculosis) and causes cell death. Ftivazide can be used to treat patients with hypersensitivity to isoniazid. Ftivazide is used for treatment of active tuberculosis of all forms and localizations. antitubercular agent (Code: CHEBI:33231) Antitubercular Agents (Code: D000995) 1964-04-30 Ministry of Health of the Russian Federation
Click to view metiazinic acid phenothiazine which acts as an anti-inflammatory agent and has been found in rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis and osteoarthrosis to possess anti-inflammatory activity non-steroidal anti-inflammatory drug (Code: CHEBI:35475)
Click to view carbutamide Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/2445740) A sulfonylurea antidiabetic agent with similar actions and uses to CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p277). Carbutamide was one of the first sulfonylurea compounds used but was withdrawn from the market due to toxic effects on bone marrow (From NCI Thesaurus). Hypoglycemic Agents (Code: D007004) Ministry of Health of the Russian Federation
Click to view desomorphine Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT an informal term for a cheap injectable illicit drug domestically prepared from codeine-containing medication in Russia Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view subathizone Subathizone (p-Ethylsulfonylbenzaldehyde thiosemicarbazone) has antitubercular activity. It was used for the treatment of tuberculosis.
Click to view nepinalone Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) a cough suppressant
Click to view dextromethorphan Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) agonist Glutamate receptor ionotropic, NMDA 3A (Organism: Homo sapiens, class: Ion channel, accessions: Q8TCU5, gene: GRIN3A, swissprot: NMD3A_HUMAN) antagonist Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Rattus norvegicus, class: Ion channel, accessions: P04774|P04775|P08104, gene: Scn1a|Scn2a|Scn3a, swissprot: SCN1A_RAT|SCN2A_RAT|SCN3A_RAT Sigma non-opioid intracellular receptor 1 (Organism: Cavia porcellus, class: Membrane other, accessions: Q60492, gene: SIGMAR1, swissprot: SGMR1_CAVPO Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q8VHN2|Q9R1M7, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMD3A_RAT|NMD3B_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMDZ1_RAT Sigma non-opioid intracellular receptor 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: Q9R0C9, gene: Sigmar1, swissprot: SGMR1_RAT Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Glutamate receptor ionotropic, NMDA 2C (Organism: Homo sapiens, class: Ion channel, accessions: Q14957, gene: GRIN2C, swissprot: NMDE3_HUMAN) blocker (Source: ) Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity. Uncompetitive N-methyl-D-aspartate Receptor Antagonist (Code: N0000181821) Sigma-1 Agonist (Code: N0000182149) Uncompetitive NMDA Receptor Antagonists (Code: N0000181819) Sigma-1 Receptor Agonists (Code: N0000182147) antitussive (Code: CHEBI:51177) Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Neurotransmitter Agents (Code: D018377) Respiratory System Agents (Code: D019141) 1957-12-03 FDA
Click to view bupranolol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: ) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: ) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) antagonist (Source: ) Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Ophthalmic Bupranolol is used for the management of glaucoma and oral Bupranolol is used for the management of cardiovascular disorders. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377)
Click to view zoledronic acid Farnesyl pyrophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P14324, gene: FDPS, swissprot: FPPS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17477829) Geranylgeranyl pyrophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: O95749, gene: GGPS1, swissprot: GGPPS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17535895) Farnesyl pyrophosphate synthase (Organism: Rattus norvegicus, class: Unclassified, accessions: P05369, gene: Fdps, swissprot: FPPS_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18325729) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24650641) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24650641) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24650641) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24650641) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24650641) 72 kDa type IV collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P08253, gene: MMP2, swissprot: MMP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24071448) Neutrophil collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P22894, gene: MMP8, swissprot: MMP8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24071448) Matrix metalloproteinase-14 (Organism: Homo sapiens, class: Enzyme, accessions: P50281, gene: MMP14, swissprot: MMP14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24071448) Matrix metalloproteinase-9 (Organism: Homo sapiens, class: Enzyme, accessions: P14780, gene: MMP9, swissprot: MMP9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24071448) a potent inhibitor of bone resorption. Zoledronic acid inhibits osteoclastic activity and induces osteoclast apoptosis, also blocks the osteoclastic resorption of mineralized bone and cartilage through its binding to bone, inhibits the increased osteoclastic activity and skeletal calcium release induced by various stimulatory factors released by tumors. bone density conservation agent (Code: CHEBI:50646) Bone Density Conservation Agents (Code: D050071) 2001-03-20 EMA ZOL
Click to view muzolimine A pyrazole diuretic with long duration and high capacity of action. It was proposed for kidney failure and hypertension but was withdrawn worldwide because of severe neurological effects. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Natriuretic Agents (Code: D045283)
Click to view zolimidine compound with analgesic, antipyretic & anti-inflammatory action; is used in the treatment of peptic ulcer and gastro-oesophageal reflux disease.
Click to view perisoxal nonsteroidal anti-inflammatory and analgesic drug
Click to view sotalol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019865s021lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019865s021lbl.pdf) Sotalol is an ethanolamine derivative with Class III antiarrhythmic and antihypertensive properties. Sotalol has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. The two isomers of sotalol have similar Class III antiarrhythmic effects, while the l-isomer is responsible for virtually all of the beta-blocking activity. The beta-blocking effect of sotalol is non-cardioselective. Sotalol is indicated for the treatment of life threatening ventricular arrhythmias and for the maintenance of normal sinus rhythm in patients with atrial fibrillation or flutter. Antiarrhythmic (Code: N0000175426) Cardiac Rhythm Alteration (Code: N0000008330) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) beta-adrenergic antagonist (Code: CHEBI:35530) anti-arrhythmia drug (Code: CHEBI:38070) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1992-10-30 FDA
Click to view estradiol Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16309907) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16309907) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16309907) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020472s016lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10471985) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20620155) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15507517) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15507517) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11741520) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11741520) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11741520) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11927002) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15290871) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14681337) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/22815312) Therapeutic Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Typically esterified, estradiol derivatives are formulated for oral or parenteral administration. As the primary, most potent estrogen hormone produced by the ovaries, estradiol binds to and activates specific nuclear receptors. Estradiol exhibits mild anabolic and metabolic properties, and increases blood coagulability. Estradiol is used for the treatment of urogenital symptoms associated with post-menopausal atrophy of the vagina or the lower urinary tract, for the treatment of moderate to severe vasomotor symptoms due to menopause, treatment of symptoms of vulvar and vaginal atrophy due to menopause, treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure and prevention of postmenopausal osteoporosis. Estrogens (Code: D004967) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Estradiol Congeners (Code: N0000011402) Estrogen (Code: N0000175825) Estrogen Receptor Agonists (Code: N0000000100) 1975-07-23 FDA EST
Click to view quinisocaine Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN a topical anesthetic used as an antipruritic. It was shown that dimethisoquin inhibits nicotinic acetylcholine receptors (alpha4/beta4 and alpha4/beta2) with the maximum inhibition potency occurring for the ?4?4 subtype. Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view nimustine Antineoplastic agent especially effective against malignant brain tumors. The resistance which brain tumor cells acquire to the initial effectiveness of this drug can be partially overcome by the simultaneous use of membrane-modifying agents such as reserpine, calcium antagonists such as nicardipine or verapamil, or the calmodulin inhibitor, trifluoperazine. The drug has also been used in combination with other antineoplastic agents or with radiotherapy for the treatment of various neoplasms. antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Ministry of Health of the Russian Federation
Click to view tolcapone Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020697s004lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020697s004lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020697s004lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) Tolcapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT). The precise mechanism of action of tolcapone is unknown, but it is believed to be related to its ability to inhibit COMT and alter the plasma pharmacokinetics of levodopa. It is believed that these sustained plasma levels of levodopa result in more constant dopaminergic stimulation in the brain, leading to greater effects on the signs and symptoms of Parkinson's disease patients. Tolcapone is indicated as an adjunct to levodopa and carbidopa for the treatment of the signs and symptoms of idiopathic Parkinson’s disease. Catechol-O-Methyltransferase Inhibitor (Code: N0000175757) antiparkinson drug (Code: CHEBI:48407) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Catechol O-Methyltransferase Inhibitors (Code: D065098) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) 1998-01-29 FDA TCW
Click to view oxaflozane Oxaflozane is non-tricyclic antidepressant with serotoninergic action. Oxaflozane has anti-cataleptic and anti-aggressive action. It was used for the treatment of depression. The drug was discontinued in 2004. 1977-02-14 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view stepronin Strepronin is a mucolytic drug. A mucolytic agent is any agent which dissolves thick mucus usually used to help relieve respiratory difficulties. The viscosity of mucous secretions in the lungs is dependent upon the concentrations of mucoprotein as well as the presence of disulfide bonds between these macromolecules and DNA. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Expectorants (Code: D005100) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Respiratory System Agents (Code: D019141)
Click to view modafinil Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020717s037s038lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020717s037s038lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020717s037s038lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020717s037s038lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020717s037s038lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020717s037s038lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020717s037s038lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020717s037s038lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020717s037s038lbl.pdf) Modafinil is a wakefulness-promoting agent. Modafinil is a racemic compound. The mechanism through which modafinil promotes wakefulness is unknown. Modafinil has wake-promoting actions similar to sympathomimetic agents including amphetamine and methylphenidate, although the pharmacologic profile is not identical to that of the sympathomimetic amines. In vitro, modafinil binds to the dopamine transporter and inhibits dopamine reuptake. At steady state, total exposure to R-modafinil is approximately three times that for S-modafinil. Modafinil is indicated to improve wakefulness in adult patients with excessive sleepiness associated with obstructive sleep apnea, narcolepsy, or shift work disorder. Central Nervous System Stimulation (Code: N0000175729) Increased Sympathetic Activity (Code: N0000175651) Sympathomimetic-like Agent (Code: N0000175769) central nervous system stimulant (Code: CHEBI:35337) eugeroic (Code: CHEBI:77567) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Cytochrome P-450 CYP3A Inducers (Code: D065701) Metabolic Side Effects of Drugs and Substances (Code: D065606) Wakefulness-Promoting Agents (Code: D064690) modafinil: 1998-12-24 FDA armodafinil: 2007-06-05 FDA
Click to view tilidine Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist An opioid analgesic used similarly to MORPHINE in the control of moderate to severe pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1097) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) opioid analgesic (Code: CHEBI:35482) prodrug (Code: CHEBI:50266) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1970-01-01 YEAR INTRODUCED
Click to view homatropine Homatropine is an anticholinergic drug that acts as an antagonist at muscarinic acetylcholine receptors. It is present in antitussives, under the trade name Hycodan, in combination with hydrocodone (dihydrocodeinone) bitartrate indicated for the symptomatic relief of cough as oral tablets or solutions. Homatropine is included in subtherapeutic amounts as homatropine methylbromide to discourage deliberate overdosage. Homatropine hydrobromide has been administered as ophthalmic solutions as a cycloplegic to temporarily paralyze accomodation, and to induce mydriasis (the dilation of the pupil). Cholinergic Muscarinic Agonist (Code: N0000175840) Cholinergic Muscarinic Agonists (Code: N0000000104) Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) 1953-11-01 Italian Medicines Agency (AIFA) HTQ
Click to view carprofen Fatty-acid amide hydrolase 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P97612, gene: Faah, swissprot: FAAH1_RAT) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: ) Prostaglandin G/H synthase 1 (Organism: Ovis aries, class: Enzyme, accessions: P05979, gene: PTGS1, swissprot: PGH1_SHEEP) anti-inflammatory drug (NSAID) of the propionic acid class with selective inhibition of COX-2 versus COX-1; now it is sold only for veterinary purposes and prescribed for the treatment of postoperative pain and the relief of pain and inflammation associated with osteoarthritis in dogs. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) photosensitizing agent (Code: CHEBI:47868) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Dermatologic Agents (Code: D003879) Peripheral Nervous System Agents (Code: D018373) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) Sensory System Agents (Code: D018689) 1987-12-31 FDA 0LA
Click to view chlormezanone A non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm; Chlormezanone was discontinued worldwide in 1996 by Sanofi due to confirmed serious and rare cutaneous reactions (toxic epidermal necrolysis also known as Stevens-Johnson syndrome). Anti-Anxiety Agents (Code: D014151) antipsychotic agent (Code: CHEBI:35476) anxiolytic drug (Code: CHEBI:35474) muscle relaxant (Code: CHEBI:51371) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1960-05-20 FDA
Click to view tryparsamide Tryparsamide is an organo-arsenic compound with activity against Spirochaetes bacteria. Tryparsamide was used for the treatment of neurosyphilis. Also tryparsamide was the second line drug for treating African trypanosomiasis.
Click to view guaiacol carbonate Guaiacol carbonate is decomposed into guaiacol in the intestine. It is used as an expectorant in combination with camphor and diphenylpyraline. Also it is used as an antiseptic. (See: guaiacol) 1951-12-31 Health Canada
Click to view ensulizole sunscreening agent;a selective UVB filter, allowing almost all UVA transmission. The scope of UVB is 290 to 340 nanometers whereas the UVA range is 320 to 400 nanometers. FDA
Click to view tybamate major descriptor (65-84); on-line search CARBAMATES (65-84); Index Medicus search TYBAMATE (65-84)
Click to view nandrolone Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist (Source: ) Corticosteroid-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P08185, gene: SERPINA6, swissprot: CBG_HUMAN C18 steroid with androgenic and anabolic properties. It is generally prepared from alkyl ethers of ESTRADIOL to resemble TESTOSTERONE but less one carbon at the 19 position. Androgen (Code: N0000175824) Anabolic Agents (Code: D045930) Androgens (Code: D000728) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 2008-12-26 Ministry of Health of the Russian Federation 6VW
Click to view chlorphenamine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12167464) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12873512) Lethal(3)malignant brain tumor-like protein 3 (Organism: Homo sapiens, class: Unclassified, accessions: Q96JM7, gene: L3MBTL3, swissprot: LMBL3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20931980) Lethal(3)malignant brain tumor-like protein 1 (Organism: Homo sapiens, class: Unclassified, accessions: Q9Y468, gene: L3MBTL1, swissprot: LMBL1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20931980) MBT domain-containing protein 1 (Organism: Homo sapiens, class: Unclassified, accessions: Q05BQ5, gene: MBTD1, swissprot: MBTD1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20931980) Solute carrier family 22 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63089, gene: Slc22a1, swissprot: S22A1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11758759) Solute carrier family 22 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9R0W2, gene: Slc22a2, swissprot: S22A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11758759) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9537821) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9537821) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9537821) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11936702) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11994058) Chlorphenamine is a H1-receptor antagonist. Chlorphenamine is usually given as a racemic mixture, the (S)-(+)-enantiomer (dexchlorpheniramine) is approximately 100 times more potent than the R-(-)-enantiomer. It is indicated for use in the common cold and for symptomatic treatment of allergies. Dexchlorpheniramine is used for the treatment of perennial and seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis due to inhalant allergens and foods, mild, uncomplicated allergic skin manifestations of urticaria and angioedema, amelioration of allergic reactions to blood or plasma, dermographism. Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Antagonist (Code: N0000175587) Anti-Allergic Agents (Code: D018926) serotonin uptake inhibitor (Code: CHEBI:50949) antidepressant (Code: CHEBI:35469) H1-receptor antagonist (Code: CHEBI:37955) histamine antagonist (Code: CHEBI:37956) antipruritic drug (Code: CHEBI:59683) anti-allergic agent (Code: CHEBI:50857) Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) chlorphenamine: 1950-08-15 FDA dexchlorpheniramine: 1981-07-14 FDA
Click to view iobenguane (123I) Iobenguane is a synthetic, aralkylguanidine analogue of the adrenergic neurotransmitter norepinephrine (NE) and adrenergic neuron blocking agent with potential diagnostic imaging or antineoplastic activity when radiolabeled. Iobenguane accumulates in adrenergically innervated tissues such as the adrenal medulla, salivary glands, heart, liver, spleen and lungs as well as tumors derived from the neural crest. By labeling iobenguane with the isotope iodine 123, it is possible to obtain scintigraphic images of the organs and tissues in which the radiopharmaceutical accumulates. Iobenguane (123I) is used for gamma-scintigraphy for detection of primary or metastatic pheochromocytoma or neuroblastoma, forscintigraphic assessment of sympathetic innervation of the myocardium. Radioactive Diagnostic Agent (Code: N0000177914) Radiopharmaceutical Activity (Code: N0000000205) 2008-09-19 FDA
Click to view acetarsol Acetarsol is a pentavalent arsenical compound with antiprotozoal and antihelmintic properties. Although its mechanism of action is not fully known, acetarsone may bind to protein-containing sulfhydryl groups located in the parasite, thereby forming lethal As-S bonds. This may prevent their functioning and eventually kill the parasite. It is used for the treatment of urogenital trichomoniasis. Anti-Infective Agents (Code: D000890) 2005-12-09 Ministry of Health of the Russian Federation
Click to view nifuroxazide Signal transducer and activator of transcription 3 (Organism: Homo sapiens, class: Transcription factor, accessions: P40763, gene: STAT3, swissprot: STAT3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22650325) Nifuroxazide is an intestinal antibacterial agent used for the treatment of acute diarrhoea in adults. Nifuroxazide is a potent inhibitor of STAT3 signaling. It exerts antineoplastic potential both in vitro and in vivo. Anti-Infective Agents (Code: D000890) 1980-07-30 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view furalazine Furalazine is an antibiotic agent with activity against drug-resistant strains of cholera bacteria.
Click to view meturedepa Meturedepa is an aziridine alkylating agent that cross-links with DNA, causing inhibition of DNA synthesis. It was studied for use in colon cancer.
Click to view tipepidine a synthetic, non-opioid antitussive and expectorant of the thiambutene class
Click to view meticrane Meticrane is a sulphonamide-derivative with thiazide-like diuretic activity. Meticrane acts in a similar manner as the thiazide diuretics. Meticrane is used to treat essential hypertension. 1977-07-01 PMDA
Click to view physostigmine Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Acetylcholinesterase (Organism: Bos taurus, class: Enzyme, accessions: P23795, gene: ACHE, swissprot: ACES_BOVIN) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: ) Acetylcholinesterase (Organism: Torpedo californica, class: Enzyme, accessions: P04058, gene: ache, swissprot: ACES_TORCA) Acetylcholinesterase (Organism: Electrophorus electricus, class: Enzyme, accessions: O42275, gene: ache, swissprot: ACES_ELEEL) Acetylcholinesterase (Organism: Gallus gallus, class: Unclassified, accessions: P36196, gene: ACHE, swissprot: ACES_CHICK) Acetylcholinesterase (Organism: Rattus norvegicus, class: Enzyme, accessions: P37136, gene: Ache, swissprot: ACES_RAT) Acetylcholinesterase (Organism: Mus musculus, class: Enzyme, accessions: P21836, gene: Ache, swissprot: ACES_MOUSE) Butyrylcholinesterase; Protein Bche (Organism: Rattus norvegicus, class: Enzyme, accessions: Q9JKC1, gene: Bche, swissprot: Q9JKC1_RAT) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) Cholinesterase (Organism: Mus musculus, class: Enzyme, accessions: Q03311, gene: Bche, swissprot: CHLE_MOUSE) Cholinesterase (Organism: Equus caballus, class: Enzyme, accessions: P81908, gene: BCHE, swissprot: CHLE_HORSE) Muscarinic acetylcholine receptor M1 (Organism: Mus musculus, class: GPCR, accessions: P12657, gene: Chrm1, swissprot: ACM1_MOUSE) Butyrylcholinesterase (Organism: Equus caballus, class: Enzyme, accessions: Q9N1N9, gene: BCHE, swissprot: Q9N1N9_HORSE) A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. antidote to curare poisoning (Code: CHEBI:74530) miotic (Code: CHEBI:51068) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Miotics (Code: D008916) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) 1875-01-01 YEAR INTRODUCED
Click to view propipocaine Propipocaine is an aromatic ketone derivative with potent local anaesthetic activity. Propipocaine was used for surface anaesthesia in a concentration of 0.5 to 1 %.
Click to view cyclobenzaprine Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN structurally related to tricyclic antidepressants relieves skeletal muscle spasm of local origin without interfering with muscle function, it is ineffective in muscle spasm due to central nervous system disease muscle relaxant (Code: CHEBI:51371) tranquilizing drug (Code: CHEBI:35473) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) Centrally-mediated Muscle Relaxation (Code: N0000175730) 1977-08-26 FDA
Click to view propiram Propiram is an opioid analgesic with partial morphine-like agonist and weak antagonist properties. Propiram binds with relatively specific affinity to opioid mu-receptors, which modulate supraspinal and spinal analgesia, but is inactive at delta-receptors. Propiram is used for providing relief of acute moderate to severe pain arising from various surgical or gynaecological procedures. 1974 Italian Medicines Agency (AIFA)
Click to view flutamide Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18571420) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9351907) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17403914) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17403914) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17403914) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11160641) Arylacetamide deacetylase (Organism: Homo sapiens, class: Enzyme, accessions: P22760, gene: AADAC, swissprot: AAAD_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22207054) Cocaine esterase (Organism: Homo sapiens, class: Enzyme, accessions: O00748, gene: CES2, swissprot: EST2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22446520) Flutamide is a toluidine derivative and a nonsteroidal antiandrogen that is structurally related to bicalutamide and nilutamide. Flutamide and its more potent active metabolite 2-hydroxyflutamide competitively block dihydrotestosterone binding at androgen receptors, forming inactive complexes which cannot translocate into the cell nucleus. Formation of inactive receptors inhibits androgen-dependent DNA and protein synthesis, resulting in tumor cell growth arrest or transient tumor regression. Flutamide is used for the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate. Androgen Receptor Antagonists (Code: N0000000243) Androgen Receptor Inhibitor (Code: N0000175560) Androgen Antagonists (Code: D000726) antineoplastic agent (Code: CHEBI:35610) androgen antagonist (Code: CHEBI:35497) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1989-01-27 FDA
Click to view oxagrelate Oxagrelate is a member of phthalazines. Oxagrelate is an inhibitor of cAMP phosphodiesterase and lead to the platelet aggregation inhibition. Oxagrelate was studied as a smooth muscle relaxant. Enzyme Inhibitors (Code: D004791) Phosphodiesterase Inhibitors (Code: D010726)
Click to view sulfabenzamide an antibacterial/antimicrobial. Often used in conjunction with sulfathiazole and sulfacetamide (trade name - Sultrin) as a topical, intravaginal antibacterial preparation against Haemophilus (Gardnerella) vaginalis bacteria. 1945-09-12 FDA BS4
Click to view cyclandelate a vasodilator developed for the treatment of cardiovascular diseases; used in for such diseases as intermittent claudication, arteriosclerosis obliterans, thrombophlebitis, nocturnal leg cramps, local frostbite, Raynaud's phenomenon; was withdrawn from the market in the USA for lack of effectiveness. vasodilator agent (Code: CHEBI:35620) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view entecavir Entecavir, a guanosine nucleoside analogue with activity against HBV reverse transcriptase, is efficiently phosphorylated to the active triphosphate form. By competing with the natural substrate deoxyguanosine triphosphate, entecavir triphosphate functionally inhibits all three activities of the HBV reverse transcriptase (base priming, reverse transcription of the negative strand from the pregenomic messenger RNA, and synthesis of the positive strand of HBV DNA). Entecavir triphosphate is a weak inhibitor of cellular DNA polymerases alpha, beta, and delta and mitochondrial DNA polymerase gamma. Entecavir is used for the treatment of chronic hepatitis B virus infection in adults with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease. antiviral drug (Code: CHEBI:36044) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2005-03-29 FDA ET9
Click to view tetraethylphthalamide Tetraethylphthalamide is a member of benzamides. Tetraethylphthalamide was used as a central analeptic. It was withdrawn from the market due to severe poisonings.
Click to view molindone Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: ) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: ) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT) D(1A) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901, gene: Drd1, swissprot: DRD1_RAT) D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT) An indole derivative effective in schizophrenia and other psychoses and possibly useful in the treatment of the aggressive type of undersocialized conduct disorder. Molindone has much lower affinity for D2 receptors than most antipsychotic agents and has a relatively low affinity for D1 receptors. It has only low to moderate affinity for cholinergic and alpha-adrenergic receptors. Some electrophysiologic data from animals indicate that molindone has certain characteristics that resemble those of CLOZAPINE. (From AMA Drug Evaluations Annual, 1994, p283) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) Typical Antipsychotic (Code: N0000180182) 1974-01-18 FDA
Click to view mebhydrolin Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6119605) Mebhydrolin is a histamine H1-receptor antagonist. It is used for symptomatic relief of allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis. 1954-01-01 YEAR INTRODUCED
Click to view bolandiol dipropionate anabolic steroid with androgenic, estrogenic, and progestational activities; an anabolic-androgenic steroid that was never marketed
Click to view etidocaine Sodium channel protein type 4 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35499, gene: SCN4A, swissprot: SCN4A_HUMAN) blocker Sodium channel protein type 2 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q99250, gene: SCN2A, swissprot: SCN2A_HUMAN) blocker Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker Sodium channel protein type 2 subunit alpha (Organism: Rattus norvegicus, class: Ion channel, accessions: P04775, gene: Scn2a, swissprot: SCN2A_RAT) blocker (Source: ) A local anesthetic with rapid onset and long action, similar to BUPIVACAINE. Etidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action. Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) local anaesthetic (Code: CHEBI:36333) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1976-08-30 FDA
Click to view chlorpropamide Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21571536) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15842554) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15842554) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15842554) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15842554) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10748266) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10748266) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10854830) Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22209866) Chlorpropamide is an oral blood-glucose-lowering drug of the sulfonylurea class. Chlorpropamide stimulates the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which chlorpropamide lowers blood glucose during long-term administration has not been clearly established. Extra-pancreatic effects may play a part in the mechanism of action of oral sulfonylurea hypoglycemic drugs. While chlorpropamide is a sulfonamide derivative, it is devoid of antibacterial activity. Chlorpropamide is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Sulfonylurea (Code: N0000175608) Sulfonylurea Compounds (Code: N0000008054) hypoglycemic agent (Code: CHEBI:35526) Hypoglycemic Agents (Code: D007004) 1958-10-28 FDA
Click to view neridronic acid Farnesyl pyrophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P14324, gene: FDPS, swissprot: FPPS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18327899) Farnesyl pyrophosphate synthase (Organism: Leishmania major, class: Enzyme, accessions: Q4QBL1, gene: FPPS, swissprot: Q4QBL1_LEIMA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14613320) Neridronic acid (6-amino-1-idroxyesilidene-1,1-bisphosphonate) is a nitrogen-containing bisphosphonate. It is aminohexane bisphosphonate with anti-resorptive and anti-hypercalcemic activities. The pharmacodynamic profile is similar to that of other nitrogen-containing bisphosphonates and is characterized by its high affinity for bone tissue particularly at sites undergoing a process of remodeling. In growing children affected by osteogenesis imperfect, neridronic acid rapidly increases bone mineral density as measured by dual X-ray absorptiometry and this is associated with a significant decrease in fracture cumulative number. It is used for the treatment of osteogenesis imperfecta and Paget’s disease of bone. 2002-04-01 Italian Medicines Agency (AIFA) NRD
Click to view clenbuterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590599) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590599) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20590599) A substituted phenylaminoethanol that has beta-2 adrenomimetic properties at very low doses. It is used as a bronchodilator in asthma. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) bronchodilator agent (Code: CHEBI:35523) beta-adrenergic agonist (Code: CHEBI:35522) sympathomimetic agent (Code: CHEBI:35524) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) 1980-08-26 Italian Medicines Agency (AIFA)
Click to view azathioprine Protein-arginine deiminase type-4 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UM07, gene: PADI4, swissprot: PADI4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17964793) Azathioprine is an immunosuppressive antimetabolite. It is an imidazolyl derivative of 6-mercaptopurine and many of its biological effects are similar to those of the parent compound. It is a prodrug for mercaptopurine. (See: mercaptopurine) Azathioprine is indicated as an adjunct for the prevention of rejection in renal homotransplantation. It is also indicated for the management of active rheumatoid arthritis to reduce signs and symptoms. Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Analog (Code: N0000175459) Purine Antimetabolite (Code: N0000175712) Purines (Code: N0000008065) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Antirheumatic Agents (Code: D018501) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Noxae (Code: D009676) 1968-03-20 FDA
Click to view folescutol capillary therapeutic agent; vascular protector; structure
Click to view elliptinium Fibroblast growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P22607, gene: FGFR3, swissprot: FGFR3_HUMAN Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN an antineoplastic agent, which was used in the treatment of metastatic breast cancer Antineoplastic Agents (Code: D000970) Indicators and Reagents (Code: D007202) Intercalating Agents (Code: D007364)
Click to view venlafaxine Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020151s031s055s058s060lbl.pdf) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020151s031s055s058s060lbl.pdf) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020151s031s055s058s060lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10192828) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10192828) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12649369) Venlafaxine is an antidepressant. The mechanism of the antidepressant action of venlafaxine in humans is believed to be associated with its potentiation of neurotransmitter activity in the CNS. Preclinical studies have shown that venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), are potent inhibitors of neuronal serotonin and norepinephrine reuptake and weak inhibitors of dopamine reuptake. Venlafaxine and ODV have no significant affinity for muscarinic, histaminergic, or ?-1 adrenergic receptors in vitro. Pharmacologic activity at these receptors is hypothesized to be associated with the various anticholinergic, sedative, and cardiovascular effects seen with other psychotropic drugs. Venlafaxine and ODV do not possess monoamine oxidase (MAO) inhibitory activity. Venlafaxine is indicated for the treatment of major depressive disorder. serotonin uptake inhibitor (Code: CHEBI:50949) adrenergic uptake inhibitor (Code: CHEBI:35640) dopamine uptake inhibitor (Code: CHEBI:51039) analgesic (Code: CHEBI:35480) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin and Noradrenaline Reuptake Inhibitors (Code: D000068760) Norepinephrine Uptake Inhibitors (Code: N0000000102) Serotonin and Norepinephrine Reuptake Inhibitor (Code: N0000175749) Serotonin Uptake Inhibitors (Code: N0000000109) 1993-12-28 FDA
Click to view maprotiline Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20141432) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20141432) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19091563) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19091563) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19091563) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19091563) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19091563) Maprotiline is a tetracyclic antidepressant. Maprotiline inhibits neuronal norepinephrine reuptake and does not affect monoamine oxidase activity. Maprotiline may be used to treat depressive affective disorders, including dysthymic disorder and major depressive disorder. Maprotiline is effective at reducing symptoms of anxiety associated with depression. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) 1980-12-01 FDA
Click to view amitriptyline Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.medsafe.govt.nz/profs/Datasheet/a/ArrowAmitryptylinetab.pdf) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.medsafe.govt.nz/profs/Datasheet/a/ArrowAmitryptylinetab.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.medsafe.govt.nz/profs/Datasheet/a/ArrowAmitryptylinetab.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.medsafe.govt.nz/profs/Datasheet/a/ArrowAmitryptylinetab.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.medsafe.govt.nz/profs/Datasheet/a/ArrowAmitryptylinetab.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.medsafe.govt.nz/profs/Datasheet/a/ArrowAmitryptylinetab.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.medsafe.govt.nz/profs/Datasheet/a/ArrowAmitryptylinetab.pdf) G protein-activated inward rectifier potassium channel 2 (Organism: Mus musculus, class: Ion channel, accessions: P48542, gene: Kcnj6, swissprot: KCNJ6_MOUSE) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/15150531) G protein-activated inward rectifier potassium channel 4 (Organism: Mus musculus, class: Ion channel, accessions: P48545, gene: Kcnj5, swissprot: KCNJ5_MOUSE) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/15150531) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/18448342) Sodium channel protein type 2 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q99250, gene: SCN2A, swissprot: SCN2A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/22770500) Sodium channel protein type 9 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q15858, gene: SCN9A, swissprot: SCN9A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/22770500) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/22770500) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Amitriptyline is a tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines. Amitriptyline is indicated for the treatment of major depressive disorder ,for the management of neuropathic pain, for prophylactic treatment of chronic tension-type headache (CTTH) and of migraine. Tricyclic Antidepressant (Code: N0000175752) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) antidepressant (Code: CHEBI:35469) adrenergic uptake inhibitor (Code: CHEBI:35640) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) 1961-04-07 FDA TP0
Click to view perhexiline Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) Carnitine palmitoyltransferase 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P18886, gene: Cpt2, swissprot: CPT2_RAT Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT Carnitine palmitoyltransferase 1A (Organism: Rattus norvegicus, class: Unclassified, accessions: P32198, gene: Cpt1a, swissprot: CPT1A_RAT Carnitine O-palmitoyltransferase 2, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P23786, gene: CPT2, swissprot: CPT2_HUMAN Carnitine O-palmitoyltransferase 1, liver isoform (Organism: Homo sapiens, class: Enzyme, accessions: P50416, gene: CPT1A, swissprot: CPT1A_HUMAN) Voltage-dependent T-type calcium channel subunit alpha-1I (Organism: Homo sapiens, class: Ion channel, accessions: Q9P0X4, gene: CACNA1I, swissprot: CAC1I_HUMAN) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) Voltage-dependent T-type calcium channel subunit alpha-1G (Organism: Homo sapiens, class: Ion channel, accessions: O43497, gene: CACNA1G, swissprot: CAC1G_HUMAN) 2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis. cardiovascular drug (Code: CHEBI:35554) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) 1976-02-26 New Zealand Medicines and Medical Devices Safety Authority
Click to view treosulfan Treosulfan is a bifunctional alkylating agent which has been shown to possess antineoplastic activity in animal tumour screen and in clinical trials. The activity of treosulfan is due to the formation of epoxide compounds in vivo. Treosulfan is converted under physiological conditions nonenzymatically via a monoepoxide to the diepoxide (diepoxybutane). The epoxides formed can alkylate a nucleophilic centre of the DNA. Treosulfan is indicated for the palliative treatment of epithelial ovarian cancer. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) 1992-01-20 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view lomifylline Lomifylline is a xanthine derivative with peripheral vasodilator action. It is used in combination with dihydroergocristine for the symptomatic treatment of cerebral circulation disorders.
Click to view pentoxifylline cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8496906) cAMP-specific 3',5'-cyclic phosphodiesterase 4B (Organism: Homo sapiens, class: Enzyme, accessions: Q07343, gene: PDE4B, swissprot: PDE4B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8496906) cAMP-specific 3',5'-cyclic phosphodiesterase 4C (Organism: Homo sapiens, class: Enzyme, accessions: Q08493, gene: PDE4C, swissprot: PDE4C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8496906) cAMP-specific 3',5'-cyclic phosphodiesterase 4D (Organism: Homo sapiens, class: Enzyme, accessions: Q08499, gene: PDE4D, swissprot: PDE4D_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8496906) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23791077) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9394024) Pentoxifylline is a methylxanthine derivative with hemorrheologic and immunomodulating properties. Pentoxifylline inhibits phosphodiesterase, resulting in increased levels of cyclic adenosine monophosphate (cAMP) in erythrocytes, endothelium, and the surrounding tissues. This leads to vasodilation, improves erythrocyte flexibility, and enhances blood flow. In addition, the increased level of cAMP in platelets inhibits platelet aggregation, which may contribute to a reduction in blood viscosity. Pentoxil is indicated for the treatment of patients with intermittent claudication based on chronic occlusive arterial disease of the limbs. Antioxidants (Code: D000975) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Free Radical Scavengers (Code: D016166) Hematologic Agents (Code: D006401) Phosphodiesterase Inhibitors (Code: D010726) Platelet Aggregation Inhibitors (Code: D010975) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) Vasodilator Agents (Code: D014665) Blood Viscosity Reducer (Code: N0000175895) Hematologic Activity Alteration (Code: N0000009065) 1984-08-30 FDA PNX
Click to view sulfisomidine A sulfanilamide antibacterial agent. It’s used in the treatment, control, prevention, and improvement of the following conditions and symptoms: Lower urinary tract infections; Meningococcal meningitis; Streptococcal pharyngitis; Gum infection; Bacillary dysentery. antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890)
Click to view sulfadimidine Folic acid synthesis protein fol1 (Organism: Pneumocystis carinii, class: Enzyme, accessions: P29251, gene: fol1, swissprot: FOL1_PNECA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7486915) Dihydropteroate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AC13, gene: folP, swissprot: DHPS_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/4577373) Sulfamethazine is a sulfonamide drug that inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase). It is used for the treatment of bronchitis, prostatitis and urinary tract infections. antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) 1949-08-16 FDA
Click to view tolycaine an amide local anaesthetic included in some preparations to reduce the pain of injection. It can be used for dental injection.
Click to view proquazone Cyclooxygenase (Organism: Bos taurus, class: Enzyme, accessions: O62664|O62698, gene: PTGS1|PTGS2, swissprot: PGH1_BOVIN|PGH2_BOVIN Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) nonsteroid anti-inflammatory agent Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Central Nervous System Agents (Code: D002491) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view demexiptiline Demexiptiline is a tricyclic antidepressant, noradrenergic drug. It is a norepinephrine reuptake inhibitor. Demexiptiline was used for the treatment of depression. It is no longer available.
Click to view sodium gualenate a water-soluble derivative of azulene, a natural product which is an antiinflammatory component of chamomile of the family of Asteraceae; used as a therapeutic agent in the treatment of inflammation of the mouth and throat, for example, pharyngitis as well as other inflammatory diseases such as tonsillitis, stomatitis and conjunctivitis 1986-01-01 YEAR INTRODUCED
Click to view trichloroethylene Trichloroethylene is a highly volatile inhalation anesthetic used mainly in short surgical procedures where light anesthesia with good analgesia is required. It is also used as an industrial solvent. Prolonged exposure to high concentrations of the vapor can lead to cardiotoxicity and neurological impairment. inhalation anaesthetic (Code: CHEBI:38870) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Solvents (Code: D012997)
Click to view egualen a stable azulene derivative, antiulcer agent anti-ulcer drug (Code: CHEBI:49201) 2011 PMDA
Click to view dimethocaine a synthetic derivative of cocaine, is a widely distributed "legal high" consumed as a "new psychoactive substance" (NPS), originally was used in the 1930s as an anesthetic, primarily in dentistry, ophthalmology, and otolaryngology. Dimethocaine is intended for forensic and research purposes. Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view triprolidine Histamine H1 receptor (Organism: Cavia porcellus, class: GPCR, accessions: P31389, gene: HRH1, swissprot: HRH1_CAVPO Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Histamine H1 antagonist used in allergic rhinitis; ASTHMA; and URTICARIA. It is a component of COUGH and COLD medicines. It may cause drowsiness. Anti-Allergic Agents (Code: D018926) H1-receptor antagonist (Code: CHEBI:37955) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1983-05-17 FDA
Click to view gamolenic acid Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN Peroxisome proliferator-activated receptor delta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q03181, gene: PPARD, swissprot: PPARD_HUMAN Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN Tissue factor (Organism: Homo sapiens, class: Membrane receptor, accessions: P13726, gene: F3, swissprot: TF_HUMAN 3-oxo-5-alpha-steroid 4-dehydrogenase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P31213, gene: SRD5A2, swissprot: S5A2_HUMAN An omega-6 fatty acid produced in the body as the delta 6-desaturase metabolite of linoleic acid. It is converted to dihomo-gamma-linolenic acid, a biosynthetic precursor of monoenoic prostaglandins such as PGE1. (From Merck Index, 11th ed); gamolenic acid was used for the treatment of breast painand atopic dermatitis in Europe, although now the drug is withdrawn from the market (there is no safety issue associated with the withdrawal of the licences).
Click to view clidanac an anti-inflammatory agent developed in Japan for the treatment of rheumatoid arthritis
Click to view acecarbromal Acecarbromal is a non-barbiturate sedative-hypnotic with action similar to that of glutethimide. Acecarbromal was used as a sedative and hypnotyc in combination with other drugs. It has been replaced by other more effective and less toxic drugs. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993)
Click to view cidofovir DNA polymerase catalytic subunit (Organism: Human herpesvirus 1 (strain 17), class: Enzyme, accessions: P04293, gene: None, swissprot: DPOL_HHV11) inhibitor potent, selective inhibitor of human cytomegalovirus replication Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 1996-06-26 FDA L8P
Click to view oxamniquine An anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine causes worms to shift from the mesenteric veins to the liver where the male worms are retained; the female worms return to the mesentery, but can no longer release eggs. (From Martindale, The Extra Pharmacopoeia, 31st ed, p121) Anthelmintics (Code: D000871) schistosomicide drug (Code: CHEBI:38941) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Schistosomicides (Code: D012556) Antihelminthic (Code: N0000175481) 1980-07-23 FDA OAQ
OQR
Click to view ramosetron 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist a serotonin 5-HT3 receptor antagonist for the treatment of nausea, vomiting and "diarrhea-predominant irritable bowel syndrome in males" (IBS-D). Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) 1996-07-10 PMDA
Click to view sulfalene Dihydropteroate synthase (Organism: Streptococcus pneumoniae (strain ATCC BAA-255 / R6), class: Enzyme, accessions: P59655, gene: sulA, swissprot: DHPS_STRR6) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25775967) Long-acting plasma-bound sulfonamide used for respiratory and urinary tract infections and also for malaria. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Renal Agents (Code: D012076) 1975-12-16 Ministry of Health of the Russian Federation
Click to view etamiphylline Etamiphylline is a methylxanthine and a theophylline derivative. It is a smooth mascle relaxant. In contrast to theophylline, etamiphylline has only a weak diuretic effect. It was used in both human and veterinary medicine as the camsylate salt. Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141)
Click to view moxisylyte An alpha-adrenergic blocking agent that is used in Raynaud's disease; used in urology for the treatment of erectile dysfunction, also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312); in the spring 2005 the manufacturer of moxisylyte decided to withdraw this drug from Europe market, presumable due to its low market shares. Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Miotics (Code: D008916) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) Vasodilator Agents (Code: D014665)
Click to view letosteine a mucolytic used in the treatment of chronic bronchopneumopathies and related conditions. mucolytic (Code: CHEBI:77034) Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) Italian Medicines Agency (AIFA)
Click to view doxepin Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Serotonin (5-HT) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P19327|P28564|P28565|P30940|P30994|P31388|P32305|P35364|P35365|P35563|Q62758|Q9JJ16, gene: Htr1a|Htr1b|Htr1d|Htr1f|Htr2a|Htr2b|Htr2c|Htr3a|Htr3b|Htr4|Htr5a|Htr5b|Htr6|Htr7, swissprot: 5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT|5HT2A_RAT|5HT2B_RAT|5HT2C_RAT|5HT3A_RAT|5HT3B_RAT|5HT4R_RAT|5HT5A_RAT|5HT5B_RAT|5HT6R_RAT|5HT7R_RAT 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Histamine H4 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9H3N8, gene: HRH4, swissprot: HRH4_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors. Tricyclic Antidepressant (Code: N0000175752) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Sleep Aids, Pharmaceutical (Code: D000068776) 1969-09-23 FDA 5EH
D7V
Click to view bendazac It is applied topically as bendazac lysine 0.5% (wt/vol) aqueous solution for delaying the progression of cataract. Topical application of bendazac is associated with transient burning sensation. It reduces the secretion of the skin ulcer surface, promotes skin formation and accelerates tissue repair. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antimetabolites (Code: D000963) Antirheumatic Agents (Code: D018501) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1981-05-12 Italian Medicines Agency (AIFA)
Click to view fenpiprane
Click to view sibutramine Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020632s034s035lbl.pdf) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020632s034s035lbl.pdf) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020632s034s035lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020632s034s035lbl.pdf) Potassium voltage-gated channel subfamily D member 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UK17, gene: KCND3, swissprot: KCND3_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/17312186) Potassium voltage-gated channel subfamily A member 3 (Organism: Homo sapiens, class: Ion channel, accessions: P22001, gene: KCNA3, swissprot: KCNA3_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/17312186) Potassium voltage-gated channel subfamily C member 1 (Organism: Homo sapiens, class: Ion channel, accessions: P48547, gene: KCNC1, swissprot: KCNC1_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/17312186) Sibutramine is an organochlorine compound and a tertiary amino compound. Sibutramine is indicated for the management of obesity, including weight loss and maintenance of weight loss, and should be used in conjunction with a reduced calorie diet. Sibutramine produces its therapeutic effects by norepinephrine, serotonin and dopamine reuptake inhibition. Sibutramine exerts its pharmacological actions predominantly via its secondary (M1) and primary (M2) amine metabolites. The parent compound, sibutramine, is a potent inhibitor of serotonin (5hydroxytryptamine, 5-HT) and norepinephrine reuptake in vivo, but not in vitro. However, metabolites M1 and M2 inhibit the reuptake of these neurotransmitters both in vitro and in vivo. In human brain tissue, M1 and M2 also inhibit dopamine reuptake in vitro, but with ~3-fold lower potency than for the reuptake inhibition of serotonin or norepinephrine. Appetite Suppression (Code: N0000175372) Dopamine Uptake Inhibitors (Code: N0000000114) Norepinephrine Uptake Inhibitors (Code: N0000000102) Norepinephrine, Serotonin, and Dopamine Reuptake Inhibitor Anorectic (Code: N0000175424) Serotonin Uptake Inhibitors (Code: N0000000109) serotonin uptake inhibitor (Code: CHEBI:50949) Anti-Obesity Agents (Code: D019440) Antidepressive Agents (Code: D000928) Appetite Depressants (Code: D001067) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1997-11-22 FDA
Click to view levosimendan cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Organism: Homo sapiens, class: Enzyme, accessions: Q14432, gene: PDE3A, swissprot: PDE3A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16116344) cGMP-inhibited 3',5'-cyclic phosphodiesterase B (Organism: Homo sapiens, class: Enzyme, accessions: Q13370, gene: PDE3B, swissprot: PDE3B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16116344) cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16116344) cAMP-specific 3',5'-cyclic phosphodiesterase 4B (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4B, swissprot: PDE4B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16116344) ATP-binding cassette sub-family C member 9 (Organism: Homo sapiens, class: Ion channel, accessions: O60706, gene: ABCC9, swissprot: ABCC9_HUMAN) opener (Source: https://www.ncbi.nlm.nih.gov/pubmed/17452812) ATP-sensitive inward rectifier potassium channel 11 (Organism: Homo sapiens, class: Ion channel, accessions: Q14654, gene: KCNJ11, swissprot: KCJ11_HUMAN) opener (Source: https://www.ncbi.nlm.nih.gov/pubmed/17452812) ATP-sensitive inward rectifier potassium channel 8 (Organism: Homo sapiens, class: Ion channel, accessions: Q15842, gene: KCNJ8, swissprot: KCNJ8_HUMAN) opener (Source: https://www.ncbi.nlm.nih.gov/pubmed/17452812) Levosimendan is a intravenous agent that exerts inotropic effects through sensitization of myofilaments to calcium and vasodilator effects by binding to cardiac troponin C in a calcium-dependent manner. It also has a vasodilatory effect, by opening adenosine triphosphate (ATP)-sensitive potassium channels in vascular smooth muscle to cause smooth muscle relaxation. cardiotonic drug (Code: CHEBI:38147) vasodilator agent (Code: CHEBI:35620) anti-arrhythmia drug (Code: CHEBI:38070) 2008-05-26 Ministry of Health of the Russian Federation
Click to view flumecinol liver microsomal drug metabolizing enzyme inducer
Click to view sulfamonomethoxine Sulfamonomethoxine is a long acting sulfonamide antibacterial agent. It is active against Streptococcus spp. (Including Streptococcus pneumoniae, Enterococcus spp.), Staphylococcus spp., Escherichia coli, Shigella spp., some strains of Proteus spp., Neisseria gonorrhoeae, Neisseria meningitides. Sulfamonomethoxine also active against Chlamydia spp., Toxoplasma gondii, Plasmodium. The relatively low toxicity. Sulfamonomethoxine is a competitive inhibitor of dihydropteroate synthetase used to block the synthesis of folic acid. It is indicated for the treatment of urinary tract infection, intestinal infection and skin and soft tissue infections. Anti-Infective Agents (Code: D000890) 1973-08-20 Ministry of Health of the Russian Federation
Click to view sulfamethoxypyridazine Folic acid synthesis protein fol1 (Organism: Pneumocystis carinii, class: Enzyme, accessions: P29251, gene: fol1, swissprot: FOL1_PNECA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7486915) Sulfamethoxypyridazine is a sulfanilamide antibacterial agent. It acts by inhibiting the enzyme dihydropteroate synthetase, required for the synthesis of nucleic acids and microbial cells. It is used for the treatment of urinary tract infections. Products containing sulfamethoxypyridazine were withdrawn in 1988. antiinfective agent (Code: CHEBI:35441) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1960-01-01 YEAR INTRODUCED
Click to view sulfameter Sulfameter is a long acting sulfonamide shows bacteriostatic effects against Gram positive and Gram negative bacteria in vivo. It is used in leprosy, urinary, and respiratory tract infections. antiinfective agent (Code: CHEBI:35441) renal agent (Code: CHEBI:35846) leprostatic drug (Code: CHEBI:35816) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Leprostatic Agents (Code: D007917) Renal Agents (Code: D012076) 1966-07-01 FDA
Click to view phenprocoumon Pol polyprotein (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72874, gene: pol, swissprot: Q72874_9HIV1 Vitamin K epoxide reductase complex subunit 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BQB6, gene: VKORC1, swissprot: VKOR1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/17275317) It used for the prevention and treatment of thromboembolic disease including venous thrombosis, thromboembolism, and pulmonary embolism as well as for the prevention of ischemic stroke in patients with atrial fibrillation. Phenprocoumon inhibits vitamin K reductase, resulting in depletion of the reduced form of vitamin K (vitamin KH2). Bleedings are the most important side -effects of oral anticoagulants. The gastrointestinal and the urinary tract are often affected; the most dangerous are intracerebral hemorrhages. Vitamin K Antagonist (Code: N0000175476) Vitamin K Inhibitors (Code: N0000175964) anticoagulant (Code: CHEBI:50249) Anticoagulants (Code: D000925) Hematologic Agents (Code: D006401) 1957-12-30 FDA
Click to view ipriflavone Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) effective for inhibiting bone resorption and enhancing bone formation, the net result being an increase in bone density and a decrease in fracture rates in osteoporotic women. bone density conservation agent (Code: CHEBI:50646) Ministry of Health of the Russian Federation
Click to view hydroxystilbamidine Trypsin (Organism: Sus scrofa, class: Unclassified, accessions: P00761, gene: None, swissprot: TRYP_PIG) an organic antimonal derivative with antiprotazoal, antifungal and anticancer activity. It was used in the treatment of blastomicosis and leishmaniasis. 1953-12-22 FDA
Click to view mefexamide proposed psychotherapeutic agent with stimulatory action
Click to view hydroxytetracaine Hydroxytetracaine is a member of phenols and a benzoate ester. It derives from a salicylic acid. Hydroxytetracaine was used as a local anesthetic. It is no longer available.
Click to view tromantadine Tromantadine is an amantadine derivative which inhibits herpes simplex virus type 1 (KOS strain)-induced cytopathic effect and herpes simplex virus type 1 and type 2 replication. Tromantadine inhibits absorption of virions to cell surfaces, as well as penetration and uncoating of the virus. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 1995-02-03 CDSCO (INDIA)
Click to view imipramine Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10193665) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10193665) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10193665) Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20363235) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20363235) Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20363235) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20363235) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20363235) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10997731) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081025) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081025) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10510461) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/9822768) Potassium voltage-gated channel subfamily H member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O95259, gene: KCNH1, swissprot: KCNH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15365094) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12089365) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081025) The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group. Tricyclic Antidepressant (Code: N0000175752) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) adrenergic uptake inhibitor (Code: CHEBI:35640) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) 1959-04-16 FDA IXX
Click to view histapyrrodine
Click to view bamipine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: http://www.kegg.jp/entry/D07197) a sedating antihistamine with pronounced sedative effects. Bamipine is a pharmaceutical drug acting as an H1 antihistamine with anticholinergic properties. It is used as an antipruritic ointment. Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Neurotransmitter Agents (Code: D018377)
Click to view linoleic acid Free fatty acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: O14842, gene: FFAR1, swissprot: FFAR1_HUMAN) agonist (Source: ) Potassium voltage-gated channel subfamily B member 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q14721, gene: KCNB1, swissprot: KCNB1_HUMAN) activator (Source: ) Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN Adenosine receptor A1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25099, gene: Adora1, swissprot: AA1R_RAT Prostaglandin G/H synthase 2 (Organism: Ovis aries, class: Enzyme, accessions: P79208, gene: PTGS2, swissprot: PGH2_SHEEP Peroxisome proliferator-activated receptor delta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q03181, gene: PPARD, swissprot: PPARD_HUMAN Fatty acid-binding protein, heart (Organism: Homo sapiens, class: Cytosolic other, accessions: P05413, gene: FABP3, swissprot: FABPH_HUMAN Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN Seed linoleate 13S-lipoxygenase-1 (Organism: Glycine max, class: Enzyme, accessions: P08170, gene: LOX1.1, swissprot: LOX1_SOYBN Tissue factor (Organism: Homo sapiens, class: Membrane receptor, accessions: P13726, gene: F3, swissprot: TF_HUMAN Fatty acid-binding protein, adipocyte (Organism: Homo sapiens, class: Cytosolic other, accessions: P15090, gene: FABP4, swissprot: FABP4_HUMAN Free fatty acid receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q5NUL3, gene: FFAR4, swissprot: FFAR4_HUMAN) agonist (Source: ) A doubly unsaturated fatty acid, occurring widely in plant glycosides. It is an essential fatty acid in mammalian nutrition and is used in the biosynthesis of prostaglandins and cell membranes. (From Stedman, 26th ed) EIC
Click to view flufenamic acid Aldo-keto reductase family 1 member B10 (Organism: Homo sapiens, class: Enzyme, accessions: O60218, gene: AKR1B10, swissprot: AK1BA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26529431) Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23454516) Aldo-keto reductase family 1 member C2 (Organism: Homo sapiens, class: Enzyme, accessions: P52895, gene: AKR1C2, swissprot: AK1C2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23454516) Aldo-keto reductase family 1 member C1 (Organism: Homo sapiens, class: Enzyme, accessions: Q04828, gene: AKR1C1, swissprot: AK1C1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23454516) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10377455) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10377455) Potassium channel subfamily T member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q6UVM3, gene: KCNT2, swissprot: KCNT2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/22851714) Transient receptor potential cation channel subfamily A member 1 (Organism: Rattus norvegicus, class: Ion channel, accessions: Q6RI86, gene: Trpa1, swissprot: TRPA1_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19888597) Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18063373) Transient receptor potential cation channel subfamily M member 5 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NZQ8, gene: TRPM5, swissprot: TRPM5_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/15670874) Transient receptor potential cation channel subfamily M member 4 (Organism: Mus musculus, class: Unclassified, accessions: Q7TN37, gene: Trpm4, swissprot: TRPM4_MOUSE) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/15670874) Transient receptor potential cation channel subfamily M member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O94759, gene: TRPM2, swissprot: TRPM2_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/15275834) Flufenamic acid is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used topically in rheumatic disorders. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) Anti-Inflammatory Agents (Code: D000893) 1983-09-01 Italian Medicines Agency (AIFA) FLF
Click to view bibenzonium
Click to view nitrazepam Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9574817) Nitrazepam is only found in individuals that have used or taken this drug. It is a benzodiazepine derivative used as an anticonvulsant and hypnotic. Nitrazepam belongs to a group of medicines called benzodiazepines. Anti-Anxiety Agents (Code: D014151) anticonvulsant (Code: CHEBI:35623) antispasmodic drug (Code: CHEBI:53784) GABA modulator (Code: CHEBI:50268) sedative (Code: CHEBI:35717) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1973-06-01 CDSCO (INDIA)
Click to view trimetozine a sedative agent, which has been used in the treatment of anxiety.
Click to view indoprofen Fatty acid-binding protein, liver (Organism: Rattus norvegicus, class: Unclassified, accessions: P02692, gene: Fabp1, swissprot: FABPL_RAT) A drug that has analgesic and anti-inflammatory properties. Following reports of adverse reactions including reports of carcinogenicity in animal studies it was withdrawn from the market worldwide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p21) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Italian Medicines Agency (AIFA)
Click to view ciclosidomine Ciclosidomine is a peripheral vasodilator. It was developed as an antihypertensive agent. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view albendazole sulfoxide Albendazole sulfoxide is a methylcarbamate benzimidazole with a broad-spectrum anthelmintic activity. albendazole sulfoxide is a key metabolite of albendazole. Albendazole sulfoxide is active against adult and immature nematodes (Dictyocaulus, Haemonchus, Ostertagia, Thelazia, Trichostrongylus, Nematodirus, Cooperia, Oesophagostomum, Bunostomum, Chabertia etc.), tapeworms (Moniezia, Avitellinae, Thysaniezia etc.), as well as adult flukes (Fasciola, Paramphistom, and Dicrocoelium), having an egg-killing effect. The mechanism of action of albendazole sulfoxide is associated with selective inhibition of beta-tubulin polymerization, which leads to the destruction of cytoplasmic microtubules of helminth intestinal cells. Albendazole sulfoxide has been shown to induce apoptosis in human cancer cell line HT-29, possibly by arresting the cell cycle at the G2/M phase. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Anticestodal Agents (Code: D000923) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980)
Click to view piberaline an anti-depressant under the proprietary name Trelibet, which was later withdrawn.
Click to view phentolamine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist Alpha-1B adrenergic receptor (Organism: Mesocricetus auratus, class: GPCR, accessions: P18841, gene: ADRA1B, swissprot: ADA1B_MESAU Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P19328|P22086|P22909, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN Alpha-1A adrenergic receptor (Organism: Bos taurus, class: GPCR, accessions: P18130, gene: ADRA1A, swissprot: ADA1A_BOVIN Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist Alpha-2A adrenergic receptor (Organism: Bos taurus, class: GPCR, accessions: Q28838, gene: ADRA2A, swissprot: ADA2A_BOVIN Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist Nischarin (Organism: Homo sapiens, class: Cytosolic other, accessions: Q9Y2I1, gene: NISCH, swissprot: NISCH_HUMAN Alpha-2A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P22909, gene: Adra2a, swissprot: ADA2A_RAT Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist Histamine H1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P31390, gene: Hrh1, swissprot: HRH1_RAT Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease. alpha-Adrenergic Blocker (Code: N0000175553) Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) alpha-adrenergic antagonist (Code: CHEBI:37890) vasodilator agent (Code: CHEBI:35620) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 1952-01-30 FDA
Click to view diphenylpyraline Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) an antihistamine used to treat allergic rhinitis, hay fever, and allergic skin disorders, diphenylpyraline blocks the action of endogenous histamine at the histamine H1 receptor H1-receptor antagonist (Code: CHEBI:37955) cholinergic antagonist (Code: CHEBI:48873) FDA
Click to view xanomeline Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) agonist (Source: ) Muscarinic acetylcholine receptor M2 (Organism: Rattus norvegicus, class: GPCR, accessions: P10980, gene: Chrm2, swissprot: ACM2_RAT) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) a cholinergic agonist; used in the treatment of Alzheimer's disease muscarinic agonist (Code: CHEBI:38325) serotonergic agonist (Code: CHEBI:35941) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Agonists (Code: D018679) Muscarinic Agonists (Code: D018721) Neurotransmitter Agents (Code: D018377) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619)
Click to view terodiline Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Terodiline relaxes the smooth muscle and used to reduce bladder tone in treatment of urinary frequency and incontinence. Muscle relaxation caused by terodiline, is probably due to its anticholinergic and calcium antagonist activity. The (R)-enantiomer of terodiline (R(+)-terodiline) can trigger cardiovascular toxicities, such as LQTS and TdP, which led to its withdrawal in 1991. Autonomic Agents (Code: D001337) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view alverine a spasmolytic used for the treatment irritable bowel syndrome. Alverine has a specific action on the smooth muscle of the alimentary tract and uterus, without affecting the heart, blood vessels and tracheal muscle. antispasmodic drug (Code: CHEBI:53784) Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) 2009-09-30 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view niflumic acid Short transient receptor potential channel 4 (Organism: Homo sapiens, class: Unclassified protein, accessions: Q9UBN4, gene: TRPC4, swissprot: TRPC4_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388058) Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/19888597) Potassium channel subfamily T member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q6UVM3, gene: KCNT2, swissprot: KCNT2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20176855) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21030469) G-protein coupled receptor 35 (Organism: Homo sapiens, class: GPCR, accessions: Q9HC97, gene: GPR35, swissprot: GPR35_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23888932) Dihydroorotate dehydrogenase (quinone), mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q02127, gene: DHODH, swissprot: PYRD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27994748) Monocarboxylate transporter 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63344, gene: Slc16a7, swissprot: MOT2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10417314) Chloride channel protein ClC-Ka (Organism: Homo sapiens, class: Ion channel, accessions: P51800, gene: CLCNKA, swissprot: CLCKA_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17659402) Chloride channel protein ClC-Kb (Organism: Homo sapiens, class: Ion channel, accessions: P51801, gene: CLCNKB, swissprot: CLCKB_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17659402) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7947975) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7947975) GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Rattus norvegicus, class: Ion channel, accessions: P62813|P63138|P18508, gene: Gabra1|Gabrb2|Gabrg2, swissprot: GBRA1_RAT|GBRB2_RAT|GBRG2_RAT) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12920213) GABA-A receptor alpha-6/beta-2/gamma-2 (Organism: Rattus norvegicus, class: Ion channel, accessions: P30191|P63138|P18508, gene: Gabra6|Gabrb2|Gabrg2, swissprot: GBRA6_RAT|GBRB2_RAT|GBRG2_RAT) negative allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12920213) Niflumic acid is an analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis. Niflumic acid is able to inhibit both phospholipase A2 as well as COX-2, thereby acting as an antiinflamatory and pain reduction agent. Also niflumic acid is used for the treatment of osteoarthritis, bursitis and ENT pain. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1972-02-01 Spanish Agency of Medicines and Medical Products (AEMPS) NFL
Click to view artemisinin Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) a drug used to treat multi-drug resistant strains of falciparum malaria. Treatments containing an artemisinin derivative (artemisinin-combination therapies, ACTs) are now standard treatment worldwide for P. falciparum malaria. The mechanism of action of arteminisin is not known, but the most widely accepted theory was that they are first activated through cleavage after reacting with haem and iron(II) oxide, which results in the generation of free radicals that in turn damage susceptible proteins, resulting in the death of the parasite. antimalarial (Code: CHEBI:38068) Anti-Infective Agents (Code: D000890) 2015-06-01 China Food and Drug Administration (CFDA)
Click to view vedaprofen a non-steroidal anti-inflammatory drug (NSAID), nhibits the prostaglandin synthesis enzyme system (cyclo-oxygenase enzyme) and thus possesses anti-inflammatory, antipyretic and analgesic properties. Studies in the horse have demonstrated potent inhibition of prostaglandin E2 (PG E2) synthesis in exudate and thromboxane B2 synthesis in serum and exudate. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) anti-ulcer drug (Code: CHEBI:49201) non-narcotic analgesic (Code: CHEBI:35481) 27O
Click to view octatropine methylbromide Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/353090) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/353090) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist Octatropine methylbromide (methyl anisotropinium) is a quaternary ammonium compound. Octatropine methylbromide may reduce the motility and secretory activity of the gastrointestinal system, and the tone of the ureter and urinary bladder and may have a slight relaxant action on the bile ducts and gallbladder. Octatropine methylbromide inhibits the muscarinic actions of acetylcholine on structures innervated by postganglionic cholinergic nerves as well as on smooth muscles that respond to acetylcholine but lack cholinergic innervation. It is used in conjunction with antacids or histamine H2-receptor antagonists in the treatment of peptic ulcer, to reduce further gastric acid secretion and delay gastric emptying. anti-ulcer drug (Code: CHEBI:49201) muscarinic antagonist (Code: CHEBI:48876) parasympatholytic (Code: CHEBI:50370) 1962-11-23 FDA
Click to view cadralazine Cadralazine is an antihypertensive of the hydrazinophthalazine chemical class. It was introduced in 1989 for the treatment of arterial hypertension. In 1992 its association with serious side effects led to the refusal of registration in norway. Animal experiments have demonstrated drug-related impairment of thyroid function as well as potential carcinogenicity and genotoxicity. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1988-01-01 YEAR INTRODUCED
Click to view oleic acid Free fatty acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: O14842, gene: FFAR1, swissprot: FFAR1_HUMAN) agonist (Source: ) Fatty-acid amide hydrolase 1 (Organism: Homo sapiens, class: Enzyme, accessions: O00519, gene: FAAH, swissprot: FAAH1_HUMAN Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN Fatty acid-binding protein, liver (Organism: Rattus norvegicus, class: Unclassified, accessions: P02692, gene: Fabp1, swissprot: FABPL_RAT Fatty acid-binding protein, epidermal (Organism: Homo sapiens, class: Cytosolic other, accessions: Q01469, gene: FABP5, swissprot: FABP5_HUMAN Fatty acid-binding protein, liver (Organism: Homo sapiens, class: Unclassified, accessions: P07148, gene: FABP1, swissprot: FABPL_HUMAN Peroxisome proliferator-activated receptor delta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q03181, gene: PPARD, swissprot: PPARD_HUMAN Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN Seed linoleate 13S-lipoxygenase-1 (Organism: Glycine max, class: Enzyme, accessions: P08170, gene: LOX1.1, swissprot: LOX1_SOYBN Tissue factor (Organism: Homo sapiens, class: Membrane receptor, accessions: P13726, gene: F3, swissprot: TF_HUMAN Fatty acid-binding protein, adipocyte (Organism: Homo sapiens, class: Cytosolic other, accessions: P15090, gene: FABP4, swissprot: FABP4_HUMAN DNA topoisomerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P11387, gene: TOP1, swissprot: TOP1_HUMAN Free fatty acid receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q5NUL3, gene: FFAR4, swissprot: FFAR4_HUMAN) agonist (Source: ) Telomerase reverse transcriptase (Organism: Homo sapiens, class: Enzyme, accessions: O14746, gene: TERT, swissprot: TERT_HUMAN An unsaturated fatty acid that is the most widely distributed and abundant fatty acid in nature. It is used commercially in the preparation of oleates and lotions, and as a pharmaceutical solvent. (Stedman, 26th ed) solvent (Code: CHEBI:46787) OLA
Click to view tribromoethanol GABA-A receptor alpha-2/beta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P18505, gene: GABRA2|GABRB1, swissprot: GBRA1_HUMAN|GBRB1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683198) Tribromoethanol is an injectable anesthetic agent used in mice. It undergoes conjugation with glucuronic acid during metabolism in the liver, followed by excretion in the urine as TBE glucuronate. Depression of respiration and circulation, together with its general unpredictability, eventually discouraged its use. Although pharmaceutical-grade TBE has not been commercially available or routinely used for human or veterinary anesthesia for several years, the agent has received widespread acceptance for use in the various manipulations required for the production of genetically engineered mice and rats. Avertin was the trade name for Winthrop Laboratories’ proprietary Tribromoethanol formulation, which is no longer available. Anesthetics (Code: D000777) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492)
Click to view risedronic acid Farnesyl pyrophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P14324, gene: FDPS, swissprot: FPPS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10620343) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/20738860) Geranylgeranyl pyrophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: O95749, gene: GGPS1, swissprot: GGPPS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12014956) Farnesyl pyrophosphate synthase (Organism: Leishmania major, class: Enzyme, accessions: Q4QBL1, gene: FPPS, swissprot: Q4QBL1_LEIMA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14695831) Farnesyl diphosphate synthase (Organism: Toxoplasma gondii, class: Enzyme, accessions: Q197X6, gene: FPPS, swissprot: Q197X6_TOXGO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21419634) Farnesyl diphosphate synthase (Organism: Trypanosoma cruzi, class: Unclassified, accessions: Q8WS26, gene: None, swissprot: Q8WS26_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21419634) Risedronic acid is an aminobisphosphonate derivative of etidronic acid that inhibits osteoclast-mediated bone resorption and modulates bone metabolism. The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Risedronate also targets farnesyl pyrophosphate synthase. It is used for the treatment of postmenopausal osteoporosis, osteoporosis in men, glucocorticoid-induced osteoporosis and Paget’s disease. Bisphosphonate (Code: N0000175579) Diphosphonates (Code: N0000007707) Bone Density Conservation Agents (Code: D050071) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) 1998-03-27 FDA RIS
Click to view papaveroline Papaveroline is a member of isoquinolines. Papaveroline produces a dose-related inhibition of the aggregation of platelets. It was studied in mental disorders caused by a deficit of non-focalized cerebral circulation.
Click to view afloqualone a centrally acting muscle relaxants; It has sedative and muscle-relaxant effects resulting from its agonist activity at the ? subtype of the GABAa receptor, and has had some clinical use, although it causes photosensitization as a side-effect that can cause skin problems such as dermatitis. Central Nervous System Agents (Code: D002491) Dermatologic Agents (Code: D003879) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) PMDA
Click to view levallorphan Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) antagonist Acetylcholinesterase (Organism: Electrophorus electricus, class: Enzyme, accessions: O42275, gene: ache, swissprot: ACES_ELEEL Mu-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33535, gene: Oprm1, swissprot: OPRM_RAT Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT An opioid antagonist with properties similar to those of NALOXONE; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683) Central Nervous System Agents (Code: D002491) Narcotic Antagonists (Code: D009292) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) FDA
Click to view trolnitrate Trolnitrate (Triethanolamine trinitrate) is an organic nitrate that causes dilation of blood vessels. Trolnitrate has a coronary vasodilator action. Trolnitrate biphosphate was used for the treatment of angina pectoris.
Click to view tropisetron 5-hydroxytryptamine receptor 3B (Organism: Homo sapiens, class: Ion channel, accessions: O95264, gene: HTR3B, swissprot: 5HT3B_HUMAN) antagonist (Source: https://www.medsafe.govt.nz/profs/Datasheet/t/tropisetronaftinj.pdf) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.medsafe.govt.nz/profs/Datasheet/t/tropisetronaftinj.pdf) 5-hydroxytryptamine receptor 3E (Organism: Homo sapiens, class: Ion channel, accessions: A5X5Y0, gene: HTR3E, swissprot: 5HT3E_HUMAN) antagonist (Source: https://www.medsafe.govt.nz/profs/Datasheet/t/tropisetronaftinj.pdf) 5-hydroxytryptamine receptor 3D (Organism: Homo sapiens, class: Ion channel, accessions: Q70Z44, gene: HTR3D, swissprot: 5HT3D_HUMAN) antagonist (Source: https://www.medsafe.govt.nz/profs/Datasheet/t/tropisetronaftinj.pdf) 5-hydroxytryptamine receptor 3C (Organism: Homo sapiens, class: Ion channel, accessions: Q8WXA8, gene: HTR3C, swissprot: 5HT3C_HUMAN) antagonist (Source: https://www.medsafe.govt.nz/profs/Datasheet/t/tropisetronaftinj.pdf) 5-hydroxytryptamine receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q13639, gene: HTR4, swissprot: 5HT4R_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11218067) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10428078) Glycine receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: P23416, gene: GLRA2, swissprot: GLRA2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10428078) Glycine receptor subunit beta (Organism: Homo sapiens, class: Ion channel, accessions: P48167, gene: GLRB, swissprot: GLRB_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10428078) Tropisetron is an indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, tropisetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy-and radiotherapy-induced nausea and vomiting. serotonergic antagonist (Code: CHEBI:48279) antiemetic (Code: CHEBI:50919) nicotinic acetylcholine receptor agonist (Code: CHEBI:47958) trypanocidal drug (Code: CHEBI:36335) immunomodulator (Code: CHEBI:50846) neuroprotective agent (Code: CHEBI:63726) anti-inflammatory agent (Code: CHEBI:67079) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) 1995-02-17 ANSM (French National Agency for Medicines and Health Products Safety) TKT
Click to view tropicamide Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27085897) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27085897) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27085897) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27085897) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27085897) Tropicamide is a synthetic muscarinic antagonist with actions similar to atropine and with an anticholinergic property. Upon ocular administration, tropicamide binds to and blocks the muscarinic receptors in the sphincter and ciliary muscle in the eye. This inhibits the responses from cholinergic stimulation, producing dilation of the pupil and paralysis of the ciliary muscle. Tropicamide is a diagnostic agent and is used to produce short-duration mydriasis and cycloplegia. Anticholinergic (Code: N0000175574) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Mydriatics (Code: D009184) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) 1960-02-23 FDA
Click to view taurolidine Taurolidine is a synthetic broad-spectrum antibiotic with antibacterial, anticoagulant and potential antiangiogenic activities. Taurolidine, derived from the amino acid taurine. Its mechanism of action as an antibiotic agent is associated with a chemical reaction between the active metabolites, taurultam and taurinamide with the structures of bacterial wall. Also taurolidine exhibits the ability to neutralize bacterial endotoxins, exotoxins and lipopolysaccharides. Taurolidine is used for the treatment and for the prevention of intra-abdominal (peritonitis) and softtissue infections, and for the prevention of perioperative infections. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Antineoplastic Agents (Code: D000970) 1987-04-24 Austrian Medicines and Medical Devices Agency
Click to view sulfaethidole Sulfaethidole is an anti-infective agent that is effective against a broad spectrum of organisms covering most of the gram-positive and gram-negative bacteria causing urinary tract infections 2011-05-12 Ministry of Health of the Russian Federation
Click to view articaine Articaine is a dental local anesthetic. Articaine blocks the actions on Na+ channels. Articaine in combination with epinephrine is indicated for local, infiltrative, or conductive anesthesia in both simple and complex dental procedures. Amide Local Anesthetic (Code: N0000175682) Amides (Code: N0000007681) Local Anesthesia (Code: N0000175976) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2000-04-03 FDA
Click to view etozolin a diuretic used for the treatment of edema and hypertension Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Natriuretic Agents (Code: D045283) Italian Medicines Agency (AIFA)
Click to view methylthioninium chloride iron (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) other (Source: http://www.ncbi.nlm.nih.gov/pubmed/10533013) Glutathione reductase (Organism: Plasmodium falciparum (isolate 3D7), class: Enzyme, accessions: O15770, gene: GR3, swissprot: GSHR_PLAF7) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17967916) Glutathione reductase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P00390, gene: GSR, swissprot: GSHR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17967916) Thioredoxin reductase 1, cytoplasmic (Organism: Homo sapiens, class: Enzyme, accessions: Q16881, gene: TXNRD1, swissprot: TRXR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17967916) Microtubule-associated protein tau (Organism: Homo sapiens, class: Structural, accessions: P10636, gene: MAPT, swissprot: TAU_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23484434) Nitric oxide synthase, inducible (Organism: Homo sapiens, class: Enzyme, accessions: P35228, gene: NOS2, swissprot: NOS2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7679577) Methylene Blue is a synthetic basic dye. Methylene blue stains to negatively charged cell components like nucleic acids; when administered in the lymphatic bed of a tumor during oncologic surgery, methylene blue may stain lymph nodes draining from the tumor, thereby aiding in the visual localization of tumor sentinel lymph nodes. When administered intravenously in low doses, this agent may convert methemoglobin to hemoglobin. acid-base indicator (Code: CHEBI:50407) fluorochrome (Code: CHEBI:51217) antidepressant (Code: CHEBI:35469) cardioprotective agent (Code: CHEBI:77307) histological dye (Code: CHEBI:77178) neuroprotective agent (Code: CHEBI:63726) physical tracer (Code: CHEBI:35208) antimalarial (Code: CHEBI:38068) Enzyme Inhibitors (Code: D004791) FDA MBT
Click to view promethazine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2866055) Pleiotropic ABC efflux transporter of multiple drugs (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Transporter, accessions: P33302, gene: PDR5, swissprot: PDR5_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19188399) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11936702) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11936702) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Promethazine is a phenothiazine derivative with antiemetic and antihistaminic properties. Promethazine antagonizes the central and peripheral effects of histamine mediated by histamine H1 receptors. The effects include bronchoconstriction, vasodilation and spasmodic contractions of gastrointestinal smooth muscle. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals. Anti-Allergic Agents (Code: D018926) sedative (Code: CHEBI:35717) antiemetic (Code: CHEBI:50919) local anaesthetic (Code: CHEBI:36333) antipruritic drug (Code: CHEBI:59683) anti-allergic agent (Code: CHEBI:50857) H1-receptor antagonist (Code: CHEBI:37955) Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) Phenothiazine (Code: N0000175746) Phenothiazines (Code: N0000007544) 1951-03-29 FDA
Click to view promazine Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515014) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515014) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515014) Promazine is a phenothiazine with actions similar to chlorpromazine but with less antipsychotic activity. It has a role as a dopaminergic antagonist, a H1-receptor antagonist, a muscarinic antagonist, a serotonergic antagonist, a phenothiazine antipsychotic drug, an antiemetic and an prolyl oligopeptidase inhibitor. Promazine is indicated for short term treatment of moderate/severe psychomotor agitation and agitation or restlessness in the elderly. dopaminergic antagonist (Code: CHEBI:48561) H1-receptor antagonist (Code: CHEBI:37955) muscarinic antagonist (Code: CHEBI:48876) serotonergic antagonist (Code: CHEBI:48279) phenothiazine antipsychotic drug (Code: CHEBI:37930) antiemetic (Code: CHEBI:50919) Antiemetics (Code: D000932) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1956-04-13 FDA P2Z
Click to view lynestrenol A synthetic progestational hormone used often in mixtures with estrogens as an oral contraceptive. Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102) 2008-04-24 Ministry of Health of the Russian Federation
Click to view iprindole Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) A tricyclic antidepressant that has actions and uses similar to those of AMITRIPTYLINE, but has only weak antimuscarinic and sedative effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p257) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619)
Click to view sulfachlorpyridazine A sulfonamide antimicrobial used for urinary tract infections and in veterinary medicine. antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076)
Click to view disulfamide Disulfamide is a benzenedisulfonamide and carbonic anhydrase (CA) inhibitor with diuretic activity. Disulfamide inhibits CA, thereby preventing sodium, bicarbonate and thus water reabsorption in the proximal convoluted tubule resulting in diuresis. Its potency is intermediate between chlorothiazide and hydrochlorothiazide. It was used as a diuretic.
Click to view mazindol Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT) Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: ) Transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q9WTR4, gene: Slc6a2, swissprot: Q9WTR4_RAT) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: ) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: ) Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) 1973-06-14 FDA 29Q
Click to view diazepam GABA A receptor alpha-1/beta-1/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18505|P18507, gene: GABRA1|GABRB1|GABRG2, swissprot: GBRA1_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/2551039) GABA A receptor alpha-2/beta-1/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P18505|P18507, gene: GABRA2|GABRB1|GABRG2, swissprot: GBRA2_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/2551039) GABA A receptor alpha-3/beta-1/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P34903|P18505|P18507, gene: GABRA3|GABRB1|GABRG2, swissprot: GBRA3_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/2551039) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020648s014lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020648s014lbl.pdf) Diazepam is a benzodiazepine anticonvulsant. Although the precise mechanism by which diazepam exerts its antiseizure effects is unknown, animal and in vitro studies suggest that diazepam acts to suppress seizures through an interaction with gamma-aminobutyric acid (GABA) receptors of the A-type (GABAA). It is believed that diazepam enhances the actions of GABA by causing GABA to bind more tightly to the GABAA receptor.Diazepam is used in the management of selected, refractory, patients with epilepsy. Also diazepam was approved for the treatment of anxiety disorders as well as for such conditions as skeletal muscle spasm, alcohol withdrawal syndrom and convulsions. Adjuvants, Anesthesia (Code: D000759) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) Anti-Anxiety Agents (Code: D014151) anxiolytic drug (Code: CHEBI:35474) anticonvulsant (Code: CHEBI:35623) sedative (Code: CHEBI:35717) Anticonvulsants (Code: D000927) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Gastrointestinal Agents (Code: D005765) Hypnotics and Sedatives (Code: D006993) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) 1963-11-15 FDA DZP
Click to view probenecid Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10929807) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11426832) Transient receptor potential cation channel subfamily V member 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q9WUD2, gene: Trpv2, swissprot: TRPV2_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17850966) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25027802) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25027802) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25027802) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12023506) Solute carrier family 22 member 9 (Organism: Homo sapiens, class: Transporter, accessions: Q8IVM8, gene: SLC22A9, swissprot: S22A9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12023506) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15039294) UDP-glucuronosyltransferase 1-7 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW7, gene: UGT1A7, swissprot: UD17_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15039294) UDP-glucuronosyltransferase 1-10 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW8, gene: UGT1A10, swissprot: UD110_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15039294) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15039294) UDP-glucuronosyltransferase 1-6 (Organism: Homo sapiens, class: Enzyme, accessions: P19224, gene: UGT1A6, swissprot: UD16_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15039294) UDP-glucuronosyltransferase 2B15 (Organism: Homo sapiens, class: Enzyme, accessions: P54855, gene: UGT2B15, swissprot: UDB15_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15039294) Multidrug resistance-associated protein 5 (Organism: Homo sapiens, class: Transporter, accessions: O15440, gene: ABCC5, swissprot: MRP5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10893247) Sodium/bile acid cotransporter (Organism: Rattus norvegicus, class: Transporter, accessions: P26435, gene: Slc10a1, swissprot: NTCP_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1961729) Solute carrier family 22 member 19 (Organism: Mus musculus, class: Transporter, accessions: Q8VCA0, gene: Slc22a19, swissprot: S22AJ_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15068970) ATP-binding cassette sub-family C member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q96J66, gene: ABCC11, swissprot: ABCCB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15537867) Solute carrier organic anion transporter family member 1C1 (Organism: Mus musculus, class: Transporter, accessions: Q9ERB5, gene: Slco1c1, swissprot: SO1C1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15166123) Solute carrier family 22 member 12 (Organism: Homo sapiens, class: Transporter, accessions: Q96S37, gene: SLC22A12, swissprot: S22AC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21272127) Probenecid is a benzoic acid derivative with antihyperuricemic property. Probenecid competitively inhibits the active reabsorption of urate at the proximal tubule in the kidney thereby increasing urinary excretion of uric acid and lowering serum urate concentrations. This prevents urate deposition and promotes resolution of existing urate deposits. In addition, probenecid modulates the transport of organic acids and acidic drugs at the proximal and distal renal tubule, thereby increasing the drug serum concentration. Probenecid is used for the treatment of gout usually in combination with other agents. Adjuvants, Pharmaceutic (Code: D000277) uricosuric drug (Code: CHEBI:35841) Antirheumatic Agents (Code: D018501) Gout Suppressants (Code: D006074) Pharmaceutic Aids (Code: D010592) Renal Agents (Code: D012076) Uricosuric Agents (Code: D014528) 1951-04-26 FDA
Click to view bromebric acid a derivative of bromoacrylic acid with cytostatic and antineoplastic activity. Bromebric acid appears to inhibit purine synthesis, oxidative phosphorylation and DNA synthesis. This agent inhibits tumor cell growth and causes cell cycle arrest. This agent may also have some use in the phrophylaxis of migraine.
Click to view nifuratel Signal transducer and activator of transcription 3 (Organism: Homo sapiens, class: Transcription factor, accessions: P40763, gene: STAT3, swissprot: STAT3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/29138596) Nifuratel has a broad antibacterial spectrum of action, including both Gram-negative and Gram-positive organisms. It is active against Chlamydia trachomatis and Mycoplasma spp. and has also some degree of activity against Candida spp. and mycetes. Nifuratel alone or in complex with nystatin is indicated for the treatment of vulvovaginal and urinary tract infections. Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Antitrichomonal Agents (Code: D000994) 1965-04-05 Italian Medicines Agency (AIFA)
Click to view letrozole Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020726s035lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19198839) Steroid 17-alpha-hydroxylase/17,20 lyase (Organism: Homo sapiens, class: Enzyme, accessions: P05093, gene: CYP17A1, swissprot: CP17A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23281812) Cytochrome P450 11B1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P15538, gene: CYP11B1, swissprot: C11B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23281812) Cytochrome P450 11B2, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P19099, gene: CYP11B2, swissprot: C11B2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23281812) Letrozole is a nonsteroidal competitive inhibitor of the aromatase enzyme system; it inhibits the conversion of androgens to estrogens. Used in treatment of hormonally responsive breast cancer. Aromatase Inhibitor (Code: N0000175563) antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Aromatase Inhibitors (Code: D047072) Enzyme Inhibitors (Code: D004791) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Steroid Synthesis Inhibitors (Code: D065088) 1997-07-25 FDA
Click to view faropenem Faropenem markets it in two forms: faropenem sodium and faropenem medoxomil. The high binding affinities of faropenem to penicillin-binding proteins from gram-negative and gram-positive bacteria are mirrored by its pronounced and concentration-dependent bactericidal effect. It is usually used to treat a wide range of infections such as skin, respiratory and otorhinologic infections. The most commonly reported adverse reactions include diarrhea, abdominal pain, loose stool, rash and nausea PMDA FPM
Click to view morphine Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018565s022lbl_Duramorph.pdf) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018565s022lbl_Duramorph.pdf) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018565s022lbl_Duramorph.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12936704) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12936704) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12699389) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Morphine is an opiate alkaloid isolated from the plant Papaver somniferum and produced synthetically. Morphine binds to and activates specific opiate receptors (delta, mu and kappa), each of which are involved in controlling different brain functions. In the central nervous and gastrointestinal systems, this agent exhibits widespread effects including analgesia, anxiolysis, euphoria, sedation, respiratory depression, and gastrointestinal system smooth muscle contraction. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) mu-opioid receptor agonist (Code: CHEBI:55322) vasodilator agent (Code: CHEBI:35620) anaesthetic (Code: CHEBI:38867) opioid analgesic (Code: CHEBI:35482) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) 1984-09-18 FDA MOI
Click to view hydromorphone Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT An opioid analgesic made from MORPHINE and used mainly as an analgesic. It has a shorter duration of action than morphine. Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1984-01-11 FDA
Click to view medrylamine Medrylamine was used as an antihistamine.
Click to view mepyramine 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN Histamine H1 receptor (Organism: Cavia porcellus, class: GPCR, accessions: P31389, gene: HRH1, swissprot: HRH1_CAVPO Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Histamine H1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P31390, gene: Hrh1, swissprot: HRH1_RAT Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies. Anti-Allergic Agents (Code: D018926) H1-receptor antagonist (Code: CHEBI:37955) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) Sleep Aids, Pharmaceutical (Code: D000068776) 1948 FDA
Click to view prothipendyl a neuroleptic azaphenothiazine
Click to view isothipendyl a first generation H1 antagonist (antihistamine) and anticholinergic used as an antipruritic. It is nowadays scarcely used in the first line relief of allergies due to the anticholinergic side effect of somnolence but does have some limited use through topical application in the relief of insect bites and related itching (pruritus). Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Neurotransmitter Agents (Code: D018377)
Click to view pentazocine Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) modulator Kappa-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P41144, gene: OPRK1, swissprot: OPRK_CAVPO Mu-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33535, gene: Oprm1, swissprot: OPRM_RAT Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT Sigma non-opioid intracellular receptor 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: Q9R0C9, gene: Sigmar1, swissprot: SGMR1_RAT Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97) Adjuvants, Anesthesia (Code: D000759) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotic Antagonists (Code: D009292) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Competitive Opioid Antagonists (Code: N0000175686) Partial Opioid Agonist/Antagonist (Code: N0000175688) Partial Opioid Agonists (Code: N0000175685) 1967-07-24 FDA GM4
Click to view cladribine An antineoplastic agent used in the treatment of lymphoproliferative diseases including hairy-cell leukemia. antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) Antineoplastic Agents (Code: D000970) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Purine Antimetabolite (Code: N0000175712) 1993-02-26 FDA CL9
Click to view asenapine 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022117s022lbl.pdf) Asenapine is a second generation (atypical) antipsychotic. The mechanism of action of asenapine, in schizophrenia and bipolar I disorder, is unknown. It has been suggested that the efficacy of asenapine in schizophrenia could be mediated through a combination of antagonist activity at D2 and 5-HT2A receptors. Asenapine is used for treatment in psychosis, schizophrenia and schizoaffective disorders, manic disorders, and bipolar disorders as monotherapy or in combination. alpha-adrenergic antagonist (Code: CHEBI:37890) beta-adrenergic antagonist (Code: CHEBI:35530) dopaminergic antagonist (Code: CHEBI:48561) psychotropic drug (Code: CHEBI:35471) serotonergic antagonist (Code: CHEBI:48279) second generation antipsychotic (Code: CHEBI:65191) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) Atypical Antipsychotic (Code: N0000175430) 2009-08-13 FDA
Click to view guaimesal Guaimesal is a synthetic agent whose chemical structure includes salicylate and guaiacol rings. Guaimesal was used as an antitussive drugs in patients with chronic bronchitis. 1988 Italian Medicines Agency (AIFA)
Click to view guacetisal tolerated by patients with aspirin-asthma Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Expectorants (Code: D005100) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689) 2014-04-01 China Food and Drug Administration (CFDA)
Click to view butazopyridine Butazopyridine is an aminopyridine. Butazopyridine was used as an urinary antiseptic.
Click to view abacavir Carbovir triphosphate: Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020977s033s034,020978s036s037lbl.pdf) Abacavir: ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020977s033s034,020978s036s037lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020977s033s034,020978s036s037lbl.pdf) Adenosine kinase (Organism: Homo sapiens, class: Kinase, accessions: P55263, gene: ADK, swissprot: ADK_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9145876) Abacavir is a carbocyclic synthetic nucleoside analogue. Active metabolite, carbovir triphosphate (an analogue of deoxyguanosine-5'-triphosphate) inhibits the activity of HIV-1 reverse transcriptaseboth by competing with the natural substrate dGTP and by its incorporation into viral DNA. Abacavir is used in combination with other agents in the therapy of the human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS). Human Immunodeficiency Virus Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175462) Nucleoside Analog (Code: N0000175459) Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009947) drug allergen (Code: CHEBI:88188) antiviral drug (Code: CHEBI:36044) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 1998-12-17 FDA 1KX
Click to view methallenestril Methallenestril is an allenolic acid derivative. It is a synthetic estrogen. It was used for the treatment of postmenopausal osteoporosis in the 1950s.
Click to view thonzylamine an antihistamine and anticholinergic drug, which is used in combination with others compounds for the temporarily relieves symptoms due to the common cold: hay fever (allergic rhinitis) or other upper respiratory allergies: nasal congestion; runny nose and so on. Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Neurotransmitter Agents (Code: D018377)
Click to view androstenedione Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT Testosterone 17-beta-dehydrogenase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P37058, gene: HSD17B3, swissprot: DHB3_HUMAN Testosterone 17-beta-dehydrogenase 3 (Organism: Rattus norvegicus, class: Unclassified, accessions: O54939, gene: Hsd17b3, swissprot: DHB3_RAT Corticosteroid-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P08185, gene: SERPINA6, swissprot: CBG_HUMAN A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL. ASD
Click to view thenalidine an antihistamine with anticholinergic properties used as an antipruritic drug. It was withdrawn from the US, Canadian, and UK markets due to a risk of neutropenia.
Click to view retinol Nuclear receptor subfamily 2 group C member 2 (Organism: Homo sapiens, class: Unclassified, accessions: P49116, gene: NR2C2, swissprot: NR2C2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21068381) Cytochrome P450 27C1 (Organism: Homo sapiens, class: Enzyme, accessions: Q4G0S4, gene: CYP27C1, swissprot: C27C1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/27059013) Retinol (vitamin A) is a fat soluble vitamin necessary for health, deficiency of which can cause disorders of vision, skin, bone and immunity. Vitamin A binds to and activates retinoid receptors (RARs), thereby inducing cell differentiation and apoptosis of some cancer cell types and inhibiting carcinogenesis. Vitamin A plays an essential role in many physiologic processes, including proper functioning of the retina, growth and differentiation of target tissues, proper functioning of the reproductive organs, and modulation of immune function. Vitamin A is enriched in the liver, egg yolks, and the fat component of dairy products. The recommended daily allowance for vitamin A is 300 to 700 ?g for children and approximately 700 to 900 ?g for adults, amounts which can be provided by a normal diet. Higher doses of vitamin A can be toxic, leading to a constellation of signs and symptoms as well as liver injury, jaundice, enlargement of the liver and spleen, portal hypertension and cirrhosis. Vitamin A (Code: N0000006269) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) 1953-02-20 FDA RTL
Click to view oxazepam GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47869|P34903|P48169|P31644|Q16445|P18505|P47870|P28472|O14764|P78334|Q8N1C3|P18507|Q99928|O00591|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/6135616) Oxazepam is a synthetic benzodiazepine derivative with anxiolytic and sedative hypnotic properties. Oxazepam is used in the treatment of anxiety, alcohol withdrawal, and insomnia. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Anti-Anxiety Agents (Code: D014151) anxiolytic drug (Code: CHEBI:35474) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1965-06-04 FDA
Click to view ritodrine Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) An adrenergic beta-2 agonist used to control PREMATURE LABOR. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) Autonomic Agents (Code: D001337) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Reproductive Control Agents (Code: D012102) Sympathomimetics (Code: D013566) Tocolytic Agents (Code: D015149) 1991-01-22 FDA
Click to view brallobarbital Brallobarbital is a member of barbiturates. It was used in combination with secobarbital and hydroxyzine as hypnotic agent. It was withdrawn from the market due to appearance of new drugs with less toxicity.
Click to view fenticlor Fenticlor is an aryl sulfide. Fenticlor is an antibacterial and antifungal agent for topical use. Since it may cause photosensitivity, it is nowadays mostly used in veterinary medicine. Fenticlor has been used in the treatment of eye and ear infections. It is no longer available. antiinfective agent (Code: CHEBI:35441) drug allergen (Code: CHEBI:88188)
Click to view incadronic acid Farnesyl pyrophosphate synthase (Organism: Leishmania major, class: Enzyme, accessions: Q4QBL1, gene: FPPS, swissprot: Q4QBL1_LEIMA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14613320) Farnesyl pyrophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P14324, gene: FDPS, swissprot: FPPS_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/11160603) Incadronic acid increases serum 1,25-dihydroxyvitamin D in rats via stimulating renal 1-hydroxylase activity. Bone Density Conservation Agents (Code: D050071) 1997-01-01 PMDA
Click to view tenofovir Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/29649076) Tenofovir is an acyclic nucleoside phosphonate (nucleotide) analog of adenosine 5?-monophosphate. Tenofovir phosphorylations by cellular enzymes to form tenofovir diphosphate. Tenofovir diphosphate inhibits the activity of HIV-1 RT by competing with the natural substrate deoxyadenosine 5?-triphosphate and, after incorporation into DNA, by DNA chain termination. Tenofovir diphosphate is a weak inhibitor of mammalian DNA polymerases ?, ?, and mitochondrial DNA polymerase ?. Tenofovir is used as the fumaric acid salt in combination therapy for the treatment of HIV infection. antiviral drug (Code: CHEBI:36044) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 2009-11-05 FDA TFO
Click to view nifurtimox A nitrofuran thiazine that has been used against TRYPANOSOMIASIS. Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Trypanocidal Agents (Code: D014344) 1967-01-01 YEAR INTRODUCED
Click to view sulmazole Sulmazole is an imidazopyridine. It is an A1 adenosine receptor antagonist. sulmazole is a weak inhibitors of PDE III and PDE V. It was formerly used as a cardiotonic agent. cardiotonic drug (Code: CHEBI:38147) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Phosphodiesterase Inhibitors (Code: D010726) Protective Agents (Code: D020011)
Click to view plasmocid Plasmocid (rhodoquine) is an aminoquinoline. It induces mitochondrial dysfunction. Plasmocid was used for the treatment of malaria. It was withdrawn due to its severe neurologic adverse effects at therapeutic doses.
Click to view galantamine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18650096) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18650096) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021169Orig1s032,021224Orig1s030,021615Orig1s023lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021169Orig1s032,021224Orig1s030,021615Orig1s023lbl.pdf) Galantamine, a tertiary alkaloid, is a competitive and reversible inhibitor of acetylcholinesterase. While the precise mechanism of galantamine’s action is unknown, it is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. If this mechanism is correct, galantamine’s effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact. There is no evidence that galantamine alters the course of the underlying dementing process. Galantamine is indicated for the treatment of mild to moderate dementia of the Alzheimer’s type. Cholinesterase Inhibitor (Code: N0000175723) antidote to curare poisoning (Code: CHEBI:74530) cholinergic drug (Code: CHEBI:38323) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Nootropic Agents (Code: D018697) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) 2001-02-28 FDA GNT
Click to view etodolac Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11804398) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) UDP-glucuronosyltransferase 1-10 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW8, gene: UGT1A10, swissprot: UD110_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15370961) Etodolac is a member of the pyranocarboxylic acid group of nonsteroidal anti-inflammatory drugs. Etodolac is a racemic mixture of [-]R- and [+]S-etodolac. As with other NSAIDs, it has been demonstrated in animals that the [+]S-form is biologically active. Both enantiomers are stable and there is no [-]R to [+]S conversion in vivo. Etodolac is indicated for the treatment of osteoarthritis, rheumatoid arthritis and for the management of acute pain. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) antipyretic (Code: CHEBI:35493) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase 2 Inhibitors (Code: D052246) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1991-01-31 FDA 8QP
8QS
Click to view zolmitriptan 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020768s023,021231s014,021450s010lbl.pdf) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020768s023,021231s014,021450s010lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020768s023,021231s014,021450s010lbl.pdf) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11834243) The therapeutic activity of zolmitriptan tablets for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arteriovenous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. Serotonin 1b Receptor Agonists (Code: N0000175763) Serotonin 1d Receptor Agonists (Code: N0000175764) Serotonin-1b and Serotonin-1d Receptor Agonist (Code: N0000175765) serotonergic agonist (Code: CHEBI:35941) vasoconstrictor agent (Code: CHEBI:50514) anti-inflammatory drug (Code: CHEBI:35472) Neurotransmitter Agents (Code: D018377) Serotonin 5-HT1 Receptor Agonists (Code: D058825) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) 1997-11-25 FDA
Click to view naftifine C-8 sterol isomerase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P32352, gene: ERG2, swissprot: ERG2_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16033255) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16033255) 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Organism: Homo sapiens, class: Enzyme, accessions: Q15125, gene: EBP, swissprot: EBP_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16033255) Naftifine is a synthetic allylamine derivative. Naftifine is indicated for the topical treatment of tinea pedis, tinea cruris, and tinea corporis caused by the organisms Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Epidermophyton floccosum. Allylamine (Code: N0000007522) Allylamine Antifungal (Code: N0000175874) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 1988-02-29 FDA
Click to view cyproheptadine 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22694093) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9178521) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9178521) Histone-lysine N-methyltransferase SETD7 (Organism: Homo sapiens, class: Unclassified, accessions: Q8WTS6, gene: SETD7, swissprot: SETD7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27088648) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9616184) 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8226867) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8226867) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7925364) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11459121) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11459121) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11459121) Cyproheptadine is a serotonin and histamine antagonist with anticholinergic and sedative effects. Cyproheptadine is used to treat allergic reactions (specifically hay fever), Vasomotor rhinitis, Allergic conjunctivitis due to inhalant allergens and foods, uncomplicated allergic skin manifestations of urticaria and angioedema amelioration of allergic reactions to blood or plasma, Cold urticaria, and Dermatographism. Anti-Allergic Agents (Code: D018926) H1-receptor antagonist (Code: CHEBI:37955) serotonergic antagonist (Code: CHEBI:48279) antipruritic drug (Code: CHEBI:59683) anti-allergic agent (Code: CHEBI:50857) gastrointestinal drug (Code: CHEBI:55324) Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) 1961-10-17 FDA C7H
Click to view proxazole Proxazole is an alkylbenzene. It has anti-inflammatory and antispasmodic properties. The antiinflammatory action takes place mostly against edematous responses and is devoid of ulcerogenic effects which are instead produced by most anti-inflammatory drugs; moreover proxazole prevents indomethacin-induced ulcers without exerting any anti-secretory effect. The antispasmodic activity results in a specific inhibition of smooth muscle spasm, both at the vascular and at the intestinal level, without significant interferences with the physiologic activity of that tissue. Proxazole was used for functional gastrointestinal disorders. Italian Medicines Agency (AIFA)
Click to view procyclidine Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Histamine H1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P31390, gene: Hrh1, swissprot: HRH1_RAT Glutamate [NMDA] receptor (Organism: Homo sapiens, class: Ion channel, accessions: O15399|O60391|Q05586|Q12879|Q13224|Q14957|Q8TCU5, gene: GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B, swissprot: NMD3A_HUMAN|NMD3B_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMDE4_HUMAN|NMDZ1_HUMAN A muscarinic antagonist that crosses the blood-brain barrier and is used in the treatment of drug-induced extrapyramidal disorders and in parkinsonism. muscarinic antagonist (Code: CHEBI:48876) antiparkinson drug (Code: CHEBI:48407) antidyskinesia agent (Code: CHEBI:66956) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Anticholinergic (Code: N0000175574) 1955-07-27 FDA
Click to view cycrimine Cycrimine is a member of the class of piperidines. It binds the muscarinic acetylcholine receptor M1, effectively reducing levels of acetylcholine. It is indicated for the treatment of Parkinson's disease. antiparkinson drug (Code: CHEBI:48407) muscarinic antagonist (Code: CHEBI:48876) antidyskinesia agent (Code: CHEBI:66956) 1953-07-22 FDA
Click to view chlorproguanil dichloro-derivative of chloroguanide; RN given refers to parent cpd; structure Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981)
Click to view fospropofol Fospropofol is a prodrug and gets converted into propofol in the liver. Fospropofol is, therefore, a short acting hypnotic/sedative/anesthetic agent. It has uses in general anesthesia, procedure sedation, and veterinary medicine. (See: propofol) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 2008-12-12 FDA
Click to view piromidic acid Antibacterial against mainly gram negative organisms. It is used for urinary tract and intestinal infections. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076)
Click to view protiofate Protiofate is an antiinfective and antiseptic agent used for the treatment of vaginal infections.
Click to view difenpiramide non-steroidal anti-inflammatory agent; do not confuse with herbicide diphenamid; RN given refers to parent cpd; structure Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view estriol Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9357533) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9357533) UDP-glucuronosyltransferase 1-10 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW8, gene: UGT1A10, swissprot: UD110_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23288867) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23288867) Estriol is a steroid, a weak agonist of the estrogen receptors. Estriol is a metabolite of estrone metabolized via 16alpha-hydroxyestrone through the enzyme 16alpha-hydroxysteroid dehydrogenase or to 2- or 4-hydroxyestrone (catechol estrogens) by the action of catecho-O-methyltransferase. During pregnancy, estriol constitutes 60-70% of the total estrogens, increasing to 300-500-fold in relation to non-pregnant women. If abnormal maternal serum screening results, specifically low levels of unconjugated estriol in the second trimester are detected, a diagnosis of Smith-Lemli-Opitz syndrome (SLOS), or RSH is suspected. Estriol is used as a test to determine the general health of an unborn fetus. 1982-08-02 Ministry of Health, Welfare and Sport (Netherlands) ESL
Click to view prasterone Glucose-6-phosphate 1-dehydrogenase (Organism: Homo sapiens, class: Enzyme, accessions: P11413, gene: G6PD, swissprot: G6PD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7726568) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15994348) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15994348) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15994348) Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/18079279) Prasterone (Dehydroepiandrosterone) is identified chemically as 3beta-hydroxyandrost-5-en-17-one. It is a major C19 steroid produced from cholesterol by the adrenal cortex. It is also produced in small quantities in the testis and the ovary. Prasterone is a precursor of, androstenedione, testosterone, estradiol, estrone and estrogen. Prasterone is indicated for the treatment of moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy, due to menopause. Adjuvants, Immunologic (Code: D000276) Immunologic Factors (Code: D007155) 2004-04-29 The Office for Registration of Medicinal Products, Medical Devices and Biocidal Products (Poland) AND
Click to view phenglutarimide Phenglutarimide is a neuropsychiatric agent. Phenglutarimide possesses parasympatholytic activity. Phenglutarimide is a muscarinic acetylcholine receptor antagonist. It was used as therapeutic drug for parkinsonism. Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neurotransmitter Agents (Code: D018377)
Click to view milverine
Click to view testosterone Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14565775) Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/29476820) G-protein coupled bile acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDU6, gene: GPBAR1, swissprot: GPBAR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18307294) 3-oxo-5-alpha-steroid 4-dehydrogenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P18405, gene: SRD5A1, swissprot: S5A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11377983) Therapeutic Testosterone is a synthetic form of the endogenous androgenic steroid testosterone. In vivo, testosterone is irreversibly converted to dihydrotestosterone (DHT) in target tissues by the enzyme 5-alpha reductase. Testosterone or DHT ligand-androgen receptor complexes act as transcription factor complexes, stimulating the expression of various responsive genes. Testosterone is used as hormone replacement or substitution of diminished or absent endogenous testosterone; for management of congenital or acquired hypogonadism, hypogonadism associated with HIV infection; male climacteric (andopause); for palliative treatment of androgen-responsive, advanced, inoperable, metastatis (skeletal) carcinoma of the breast in women who are 1-5 years postmenopausal and for the management of moderate to severe vasomotor symptoms associated with menopause in women who do not respond to adequately to estrogen therapy alone. Androgen (Code: N0000175824) Androgen Receptor Agonists (Code: N0000000146) Androstanes (Code: N0000008241) Androgens (Code: D000728) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1972-07-13 FDA TES
Click to view methylestrenolone was MH 1963-92; METHYLESTRENOLONE & METHYLNORTESTOSTERONE were see NORMETHANDROLONE 1963-92; use ESTRENES to search NORMETHANDROLONE 1966-92
Click to view bupivacaine+ropivacaine 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16418020) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/29958221) ATP-sensitive inward rectifier potassium channel 11 (Organism: Homo sapiens, class: Ion channel, accessions: Q14654, gene: KCNJ11, swissprot: KCJ11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15277922) ATP-sensitive inward rectifier potassium channel 8 (Organism: Rattus norvegicus, class: Ion channel, accessions: Q63664, gene: Kcnj8, swissprot: KCNJ8_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15277922) ATP-binding cassette sub-family C member 9 (Organism: Rattus norvegicus, class: Ion channel, accessions: Q63563, gene: Abcc9, swissprot: ABCC9_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15277922) Potassium voltage-gated channel subfamily A member 5 (Organism: Homo sapiens, class: Ion channel, accessions: P22460, gene: KCNA5, swissprot: KCNA5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9400387) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10725304) Bupivacaine is related chemically and pharmacologically to the amide-type local anesthetics. It is a homologue of mepivacaine and is related chemically to lidocaine. Local anesthetics block the generation and the conduction of nerve impulses presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: pain, temperature, touch, proprioception, and skeletal muscle tone. Bupivacaine is indicated for single-dose infiltration in adults to produce postsurgical local/regional analgesia. Levobupivacaine is the S-enantiomer of bupivacaine. Levobupivacaine demonstrates less vasodilation and possesses a greater length of action in comparison to bupivacaine. It is approximately 13 per cent less potent (by molarity) than racemic bupivacaine.Levobupivacaine is indicated for local anaesthesia including infiltration, nerve block, ophthalmic, epidural and intrathecal anaesthesia in adults; and infiltration analgesia in children. Amide Local Anesthetic (Code: N0000175682) Amides (Code: N0000007681) Local Anesthesia (Code: N0000175976) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) adrenergic antagonist (Code: CHEBI:37887) local anaesthetic (Code: CHEBI:36333) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) bupivacaine: 1972-10-03 FDA levobupivacaine: 1999-08-05 FDA
Click to view methitural Methitural is a barbiturate derivative. It was used as a intravenous short-acting anesthetic. 1956 FDA
Click to view ethylestrenol Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist An anabolic steroid with some progestational activity and little androgenic effect. Anabolic Agents (Code: D045930) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1964-05-28 FDA
Click to view desalkylflurazepam Desalkylflurazepam (norfludiazepam) is a biological active final metabolite of several other benzodiazepine with a very long elimination half-life.
Click to view tetrazepam Tetrazepam is a muscle relaxant. Tetrazepam has relatively little sedative effect at low doses while still producing useful muscle relaxation and anxiety relief. Tetrazepam is an unusual benzodiazepine in its molecular structure as it has cyclohexenyl group which has substituted the typical 5-phenyl moiety seen in other benzodiazepines. Tetrazepam causes cutaneous adverse effects and toxic epidermal necrolysis. It is used for the treatment of myositis, epicondylitis, muscle spasm, spasmodic torticollis. In some countries tetrazepam was withdrawn from the market. Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 1993-03-24 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view propallylonal Propallylonal is an intermediate-acting sedative-hypnotic barbiturate with a profile similar to that of pentobarbital.
Click to view ciprofibrate Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) agonist (Source: https://pubmed.ncbi.nlm.nih.gov/23031596/) Ciprofibrate is a derivative of phenoxyisobutyric acid which has a marked hypolipidaemic action. It reduces both LDL and VLDL and hence the levels of triglyceride and cholesterol associated with these lipoprotein fractions. It also increases levels of HDL cholesterol. antilipemic drug (Code: CHEBI:35679) Antimetabolites (Code: D000963) Carcinogens (Code: D002273) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Noxae (Code: D009676) Peroxisome Proliferators (Code: D020025) 1983-12-09 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view tazanolast Tazanolast is a selective mast-cell-stabilizing drug. Tazanolast has anti-allergic and anti-asthmatic actions.
Click to view adrafinil induces hyperactivity Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-Agonists (Code: D000316) Neurotransmitter Agents (Code: D018377)
Click to view rotraxate Rotraxate is an anti-ulcerative agent. It increased gastric mucosal blood flow and possibly promoted the healing process of peptic ulcers.
Click to view atropine Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: www.accessdata.fda.gov/drugsatfda_docs/label/2014/206289s000lbl.pdf) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: www.accessdata.fda.gov/drugsatfda_docs/label/2014/206289s000lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: www.accessdata.fda.gov/drugsatfda_docs/label/2014/206289s000lbl.pdf) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15081878) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Atropine is a racemate composed of equimolar concentrations of (S)- and (R)-atropine. Hyoscyamine is the levo-isomer to atropine. It is obtained from deadly nightshade (Atropa belladonna) and other plants of the family Solanaceae. Atropine inhibits the muscarinic actions of acetylcholine on structures innervated by postganglionic cholinergic nerves, and on smooth muscles which respond to endogenous acetylcholine but are not so innervated. Responses to postganglionic cholinergic nerve stimulation also may be inhibited by atropine but this occurs less readily than with responses to injected (exogenous) choline esters. Atropine is relatively selective for muscarinic receptors. Its potency at nicotinic receptors is much lower, and actions at non-muscarinic receptors are generally undetectable clinically. Atropine does not distinguish among the M1, M2, and M3 subgroups of muscarinic receptors. Atropine is used for the treatment of poisoning by susceptible organophosphorous nerve agents having anti-cholinesterase activity (cholinesterase inhibitors) as well as organophosphorous or carbamate insecticides. Also atropine is used by injection to treat symptomatic bradycardia, severe bronchospasm and to reduce vagal stimulation. Hyoscyamine is used to provide symptomatic relief to various gastrointestinal disorders including spasms, peptic ulcers, irritable bowel syndrome, pancreatitis, colic and cystitis. It has also been used to relieve some heart problems, control some of the symptoms of Parkinson's disease, as well as for control of respiratory secretions in end of life care. Anticholinergic (Code: N0000175574) Cholinergic Muscarinic Antagonist (Code: N0000175700) Cholinergic Muscarinic Antagonists (Code: N0000000125) Adjuvants, Anesthesia (Code: D000759) Anti-Arrhythmia Agents (Code: D000889) Anti-Asthmatic Agents (Code: D018927) anti-arrhythmia drug (Code: CHEBI:38070) anaesthesia adjuvant (Code: CHEBI:60807) mydriatic agent (Code: CHEBI:50513) parasympatholytic (Code: CHEBI:50370) bronchodilator agent (Code: CHEBI:35523) antidote to sarin poisoning (Code: CHEBI:136860) muscarinic antagonist (Code: CHEBI:48876) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Mydriatics (Code: D009184) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1960-09-15 FDA OIN
Click to view improsulfan Improsulfan is an alkylsulfonate alkylating agent that cross-links with DNA, causing inhibition of DNA synthesis. Improsulfan has the topical antitumor activity against Yoshida sarcoma cells.
Click to view butaverine
Click to view dyclonine Sodium channel protein type 10 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y5Y9, gene: SCN10A, swissprot: SCNAA_HUMAN) blocker minor descriptor (66-83); on-line & Index Medicus search PROPIOPHENONES (66-83); RN given refers to parent cpd; structure Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) topical anaesthetic (Code: CHEBI:48425) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) FDA
Click to view caramiphen Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT Muscarinic acetylcholine receptor M2 (Organism: Rattus norvegicus, class: GPCR, accessions: P10980, gene: Chrm2, swissprot: ACM2_RAT Lysosomal Pro-X carboxypeptidase (Organism: Homo sapiens, class: Enzyme, accessions: P42785, gene: PRCP, swissprot: PCP_HUMAN Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT
Click to view bencyclane Bencyclane, a cycloheptane, is a vasodilator, antiplasmodic and a platelet aggregation inhibitor found to be effective in a variety of peripheral circulation disorders. Its mechanism may involve block of calcium channels. It is used to treat the symptoms of atherosclerosis, occlusive arterial disease. Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) 1967-01-01 Hungary National Institute of Pharmacy and Nutrition
Click to view triclosan Enoyl-[acyl-carrier-protein] reductase [NADPH] (Organism: Staphylococcus aureus, class: Enzyme, accessions: Q9RMI3, gene: fabI, swissprot: Q9RMI3_STAAU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11514139 Enoyl-[acyl-carrier-protein] reductase [NADH] FabI (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AEK4, gene: fabI, swissprot: FABI_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11514139) Enoyl-acyl-carrier protein reductase (Organism: Plasmodium falciparum, class: Enzyme, accessions: Q965D5, gene: fabI, swissprot: Q965D5_PLAFA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16198563) Triclosan is an aromatic ether that is phenol which is substituted at C-5 by a chloro group and at C-2 by a 2,4-dichlorophenoxy group. It is widely used as a preservative and antimicrobial agent in personal care products such as soaps, skin creams, toothpaste and deodorants as well as in household items such as plastic chopping boards, sports equipment and shoes. It has some bacteriostatic and fungistatic action. fungicide (Code: CHEBI:24127) antimalarial (Code: CHEBI:38068) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Antimetabolites (Code: D000963) Fatty Acid Synthesis Inhibitors (Code: D054872) Hypolipidemic Agents (Code: D000960) 1997-07-11 FDA TCL
Click to view quinethazone Quinethazone is a long-acting, quinazolinesulfonamide derivative with thiazide-like diuretic activity. Quinethazone inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. The antihypertensive mechanism of quinethazone is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle. Quinethazone is used for the treatment of hypertension and edema. Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) 1963-04-10 FDA
Click to view nicoclonate Nicoclonate is a nicotinic acid derivative. It has antilipidemic properties.
Click to view clofedanol Clofedanol (chlophedianol) is a centrally-acting cough suppressant, although the mechanism of action is not known. Chlophedianol suppresses the cough reflex by a direct effect on the cough center in the medulla of the brain. Clofedanol is used in the treatment of dry cough. 1960 FDA
Click to view chloropyramine Chloropyramine is an antagonist of H1 histamine receptors. It is indicated for the treatment of various forms of allergic reactions. Also chloropyramine acts as inhibitor of focal adhesion kinase and vascular endothelial growth factor receptor-3 binding. This leads to inhibition of a diverse set cancer cell types proliferation in vitro and reducing tumor growth in vivo. Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1997-04-22 Bulgarian Drug Agency (BDA)
Click to view cianidanol Prothrombin (Organism: Homo sapiens, class: Enzyme, accessions: P00734, gene: F2, swissprot: THRB_HUMAN) Arginase (Organism: Leishmania amazonensis, class: Enzyme, accessions: O96394, gene: None, swissprot: O96394_LEIAM) Prostaglandin G/H synthase 1 (Organism: Bos taurus, class: Enzyme, accessions: O62664, gene: PTGS1, swissprot: PGH1_BOVIN) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) Prostaglandin G/H synthase 1 (Organism: Ovis aries, class: Enzyme, accessions: P05979, gene: PTGS1, swissprot: PGH1_SHEEP) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) Carbonic anhydrase 13 (Organism: Homo sapiens, class: Enzyme, accessions: Q8N1Q1, gene: CA13, swissprot: CAH13_HUMAN) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) Beta-secretase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P56817, gene: BACE1, swissprot: BACE1_HUMAN) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) An antioxidant flavonoid, occurring especially in woody plants as both (+)-catechin and (-)-epicatechin (cis) forms. FDA KXN
Click to view bagrosin Bagrosin is an anticonvulsant. It was used for the treatment of epilepsy in 1950s.
Click to view trimethoprim Dihydrofolate reductase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0ABQ4, gene: folA, swissprot: DYR_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/074973s008lbl.pdf) Dihydrofolate reductase (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: Q54801, gene: dhfR, swissprot: DYR_STRPN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/074973s008lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/017377s074lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/017377s074lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/017377s074lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/017377s074lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/017377s074lbl.pdf) Dihydrofolate reductase (Organism: Rattus norvegicus, class: Enzyme, accessions: Q920D2, gene: Dhfr, swissprot: DYR_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9719595) Dihydrofolate reductase (Organism: Pneumocystis carinii, class: Enzyme, accessions: P16184, gene: None, swissprot: DYR_PNECA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9719595) Bifunctional dihydrofolate reductase-thymidylate synthase (Organism: Toxoplasma gondii, class: Enzyme, accessions: Q07422, gene: None, swissprot: DRTS_TOXGO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9719595) Dihydrofolate reductase (Organism: Lactobacillus casei, class: Enzyme, accessions: P00381, gene: folA, swissprot: DYR_LACCA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9719595) Trimethoprim is a synthetic derivative of trimethoxybenzyl-pyrimidine with antibacterial and antiprotozoal properties. As a pyrimidine inhibitor of bacterial dihydrofolate reductase, trimethoprim binds tightly to the bacterial enzyme, blocking the production of tetrahydrofolic acid from dihydrofolic acid. Trimethoprim has been shown to be active against most strains of the following microorganisms: Staphylococcus species (coagulase-negative strains, including S. saprophyticus), Enterobacter species, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis. Dihydrofolate Reductase Inhibitor Antibacterial (Code: N0000175489) Dihydrofolate Reductase Inhibitors (Code: N0000000191) Cytochrome P450 2C8 Inhibitors (Code: N0000187062) Organic Cation Transporter 2 Inhibitors (Code: N0000187061) drug allergen (Code: CHEBI:88188) antibacterial drug (Code: CHEBI:36047) diuretic (Code: CHEBI:35498) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Cytochrome P-450 CYP2C8 Inhibitors (Code: D065687) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) Metabolic Side Effects of Drugs and Substances (Code: D065606) Renal Agents (Code: D012076) 1973-07-30 FDA TOP
TRR
Click to view procaterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: ) A long-acting beta-2-adrenergic receptor agonist. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566)
Click to view ethyl piperidinoacetylaminobenzoate Ethyl piperidinoacetylaminobenzoate (sulcaine) is a benzoate ester and a member of piperidines. It derives from an acetamide. Ethyl piperidinoacetylaminobenzoate is used to treat stomach pain, nausea and gastric discomfort accompanied with gastritis. 2013-12-01 PMDA
Click to view sultiame Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588751) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase (Organism: Anopheles gambiae, class: Unclassified, accessions: Q5TU56, gene: None, swissprot: Q5TU56_ANOGA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25882523) Delta carbonic anhydrase (Organism: Thalassiosira weissflogii, class: Unclassified, accessions: Q5U9J1, gene: ca1, swissprot: Q5U9J1_THAWE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24314394) Sulthiame is a potent inhibitor of carbonic anhydrase II, VII, IX, and XII. Sulthiame is an antiepileptic drug. It is used for the treatment of benign rolandic epilepsy. Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 1967-01-01 Hungary National Institute of Pharmacy and Nutrition OSP
Click to view methylhomatropine (See: Homatropine) muscarinic antagonist (Code: CHEBI:48876) anti-ulcer drug (Code: CHEBI:49201) antispasmodic drug (Code: CHEBI:53784) 1943-03-23 FDA
Click to view oxabolone
Click to view suxamethonium Muscle-type nicotinic acetylcholine receptor (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P11230|Q07001|Q04844|P07510, gene: CHRNA1|CHRNB1|CHRND|CHRNE|CHRNG, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN|ACHE_HUMAN|ACHG_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/008453s036lbl.pdf) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/008453s036lbl.pdf) Suxamethonium is a quaternary skeletal muscle relaxant usually used in the form of its bromide, chloride, or iodide. It is a depolarizing relaxant, acting in about 30 seconds and with a duration of effect averaging three to five minutes. Succinylcholine is used in surgical, anesthetic, and other procedures in which a brief period of muscle relaxation is called for. Depolarizing Neuromuscular Blocker (Code: N0000175719) Neuromuscular Depolarizing Blockade (Code: N0000175733) muscle relaxant (Code: CHEBI:51371) drug allergen (Code: CHEBI:88188) neuromuscular agent (Code: CHEBI:51372) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Depolarizing Agents (Code: D009467) Peripheral Nervous System Agents (Code: D018373) 1952-08-20 FDA SCK
Click to view azatadine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Histamine H1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P31390, gene: Hrh1, swissprot: HRH1_RAT indulian (UD 21;71k) is dimaleate; do not confuse with AZACITIDINE H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1977-03-29 FDA
Click to view androstanolone Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Androgen receptor (Organism: Mus musculus, class: Transcription factor, accessions: P19091, gene: Ar, swissprot: ANDR_MOUSE Glucocorticoid receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P06536, gene: Nr3c1, swissprot: GCR_RAT Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT Mineralocorticoid receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P22199, gene: Nr3c2, swissprot: MCR_RAT Progesterone receptor (Organism: Oryctolagus cuniculus, class: Transcription factor, accessions: P06186, gene: PGR, swissprot: PRGR_RABIT Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN Corticosteroid-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P08185, gene: SERPINA6, swissprot: CBG_HUMAN A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE. Androgens (Code: D000728) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) DHT
Click to view androstenediol Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN Corticosteroid-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P08185, gene: SERPINA6, swissprot: CBG_HUMAN An intermediate in TESTOSTERONE biosynthesis, found in the TESTIS or the ADRENAL GLANDS. Androstenediol, derived from DEHYDROEPIANDROSTERONE by the reduction of the 17-keto group (17-HYDROXYSTEROID DEHYDROGENASES), is converted to TESTOSTERONE by the oxidation of the 3-beta hydroxyl group to a 3-keto group (3-HYDROXYSTEROID DEHYDROGENASES). Anabolic Agents (Code: D045930) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) B81
Click to view mepiperphenidol
Click to view carbinoxamine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: ) antihistamine with anticholinergic and sedative properties Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Antagonist (Code: N0000175587) H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) muscarinic antagonist (Code: CHEBI:48876) antiparkinson drug (Code: CHEBI:48407) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1974-12-27 FDA
Click to view sulfamidochrysoidine Sulfamidochrysoidine (prontosil) is a prodrug. Sulfamidochrysoidine is activated by reduction of its azo linkage to the true bacteriostatic agent, sulfanilamide.It was the first antibacterial drug. It was developed for the treatment of streptococcal infections. antibacterial drug (Code: CHEBI:36047)
Click to view befunolol synonym BFE 60 refers to HCl; RN given refers to parent cpd; structure Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Agonists (Code: D000318) Adrenergic beta-Antagonists (Code: D000319) Neurotransmitter Agents (Code: D018377)
Click to view eseridine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12166941) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12166941) Eseridine is an anticholinergic agent. It is used as eseridine salicylate for the treatment of dyspeptic disorders. 1976-12-20 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view fasudil C-C motif chemokine 2 (Organism: Homo sapiens, class: Cytokine, accessions: P13500, gene: CCL2, swissprot: CCL2_HUMAN) Rho-associated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q13464, gene: ROCK1, swissprot: ROCK1_HUMAN) inhibitor (Source: ) Protein kinase C epsilon type (Organism: Homo sapiens, class: Kinase, accessions: Q02156, gene: PRKCE, swissprot: KPCE_HUMAN) Ribosomal protein S6 kinase alpha-5 (Organism: Homo sapiens, class: Kinase, accessions: O75582, gene: RPS6KA5, swissprot: KS6A5_HUMAN) Myosin light chain kinase, smooth muscle (Organism: Homo sapiens, class: Kinase, accessions: Q15746, gene: MYLK, swissprot: MYLK_HUMAN) Rho-associated protein kinase 2 (Organism: Rattus norvegicus, class: Kinase, accessions: Q62868, gene: Rock2, swissprot: ROCK2_RAT) Rho-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: O75116, gene: ROCK2, swissprot: ROCK2_HUMAN) inhibitor (Source: ) Serine/threonine-protein kinase N2 (Organism: Homo sapiens, class: Kinase, accessions: Q16513, gene: PKN2, swissprot: PKN2_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Serine/threonine-protein kinase N1 (Organism: Homo sapiens, class: Kinase, accessions: Q16512, gene: PKN1, swissprot: PKN1_HUMAN) cAMP-dependent protein kinase catalytic subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: P17612, gene: PRKACA, swissprot: KAPCA_HUMAN) intracellular calcium antagonist Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Membrane Transport Modulators (Code: D049990) Protein Kinase Inhibitors (Code: D047428) Vasodilator Agents (Code: D014665) 1995-06-30 PMDA M77
Click to view pecilocin fungicidal antibiotic produced by Paecilomyces varioti Bainier var. antibioticus; structure
Click to view eucatropine Eucatropine is an anticholinergic agent. It acts as antagonist of muscarinic cholinergic receptors. Eucatropine was used to producing mydriasis. Also it was used for inspection of the eye fundus.
Click to view cyclopentolate Cyclopentolate is a parasympatholytic anticholinergic agent. Cyclopentolate blocks the responses of the sphincter muscle of the iris and the accommodative muscle of the ciliary body to cholinergic stimulation, producing pupillary dilation (mydriasis) and paraly sis of accommodation (cycloplegia). Cyclopentolate acts rapidly, but has a shorter duration of action than atropine. Cyclopentolate is used to produce mydriasis and cycloplegia. mydriatic agent (Code: CHEBI:50513) parasympatholytic (Code: CHEBI:50370) muscarinic antagonist (Code: CHEBI:48876) diagnostic agent (Code: CHEBI:33295) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Mydriatics (Code: D009184) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) 1974-07-31 FDA
Click to view levobunolol Beta-3 adrenergic receptor (Organism: Mus musculus, class: Unclassified, accessions: P25962, gene: Adrb3, swissprot: ADRB3_MOUSE) antagonist (Source: ) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) antagonist 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Beta-3 adrenergic receptor (Organism: Rattus norvegicus, class: Unclassified, accessions: P26255, gene: Adrb3, swissprot: ADRB3_RAT) antagonist (Source: ) The L-Isomer of bunolol. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) antiglaucoma drug (Code: CHEBI:39456) beta-adrenergic antagonist (Code: CHEBI:35530) Autonomic Agents (Code: D001337) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1985-12-19 FDA
Click to view butinoline
Click to view perlapine 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT Histamine H4 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9H3N8, gene: HRH4, swissprot: HRH4_HUMAN
Click to view penbutolol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist Alpha-1-acid glycoprotein 1 (Organism: Homo sapiens, class: Secreted, accessions: P02763, gene: ORM1, swissprot: A1AG1_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT A nonselective beta-blocker used as an antihypertensive and an antianginal agent. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 1987-12-30 FDA
Click to view terbinafine Squalene epoxidase (Organism: Trichophyton rubrum, class: Enzyme, accessions: Q4JEY0, gene: None, swissprot: Q4JEY0_TRIRU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020539s033lbl.pdf) Squalene monooxygenase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q92206, gene: ERG1, swissprot: ERG1_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2769687) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020539s033lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020539s033lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020539s033lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020539s033lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020539s033lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020539s033lbl.pdf) Terbinafine, an allylamine antifungal, inhibits biosynthesis of ergosterol, an essential component of fungal cell membrane, via inhibition of squalene epoxidase enzyme. This results in fungal cell death primarily due to the increased membrane permeability mediated by the accumulation of high concentrations of squalene but not due to ergosterol deficiency. Terbinafine has been shown to be active against most strains of the following microorganisms: Trichophyton mentagrophytes and Trichophyton rubrum. Terbinafine indicated for the treatment of onychomycosis of the toenail or fingernail due to dermatophytes (tinea unguium). Allylamine (Code: N0000007522) Allylamine Antifungal (Code: N0000175874) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Enzyme Inhibitors (Code: D004791) 1992-12-30 FDA
Click to view melitracen Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619)
Click to view lobenzarit prevents autoimmune kidney disease in hybrid mice; RN given refers to parent cpd Adjuvants, Immunologic (Code: D000276) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view zomepirac Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10377455) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10377455) Zomepirac is a pyrrole-acetic acid structurally related to tolmetin. Zomepirac is a prostaglandin synthetase inhibitor and is not an opioid, an opioid antagonist, or a salicylate. Zomepirac was indicated for the management of mild to severe pain. Later zomepirac was found to be associated with fatal and near-fatal anaphylactoid reactions. The manufacturer voluntarily removed zomepirac from market in March 1983. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) cardiovascular drug (Code: CHEBI:35554) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1980 YEAR INTRODUCED ZOM
Click to view leucinocaine Leucinocaine is a local anauthetic of the ester type. It was used as a leucinocaine mesylate used for surface anaesthesia.
Click to view ambucetamide Ambucetamide is an amino acid amide. Ambucetamide has antispasmodic action on the uterus. it was used for the treatment of menstrual pain.
Click to view butedronic acid Butedronic acid is a bone resorption inhibitor. Butedronic acid in combination with technetium (99mTc) is used as bone imaging agent.
Click to view brimonidine Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/204708s005lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/204708s005lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/204708s005lbl.pdf) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8905918) Brimonidine is an alpha adrenergic agonist. Brimonidine is a relatively selective alpha-2 adrenergic agonist. Brimonidine is indicated for the topical treatment of persistent (nontransient) facial erythema of rosacea or for the lowering of intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-2 Receptor Agonists (Code: D058647) Adrenergic alpha-Agonists (Code: D000316) adrenergic agonist (Code: CHEBI:37886) antihypertensive agent (Code: CHEBI:35674) alpha-adrenergic agonist (Code: CHEBI:35569) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 1996-09-06 FDA
Click to view cloranolol tobanum is for (+-)-isomer, HCl salt; RN given refers to parent cpd Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377)
Click to view edetic acid lead (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/008922s016lbl.pdf) calcium (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/008922s016lbl.pdf) Beta-lactamase VIM-1 (Organism: Pseudomonas aeruginosa, class: Unclassified, accessions: Q9XAY4, gene: blaVIM, swissprot: Q9XAY4_PSEAI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18644957) Beta-lactamase (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: Q79MP6, gene: blaIMP-1, swissprot: Q79MP6_PSEAI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22921080) Edetic Acid (EDTA )is the acid form of edetate, a chelating agent with anti-hypercalcemic and anticoagulant properties. Edetic acid binds calcium and heavy metal ions, forming soluble stable complexes which are readily excreted by the kidneys. This results in a decrease in serum calcium levels. Edetic acid is used as a edetate calcium disodium for the reduction of blood levels and depot stores of lead in lead poisoning (acute and chronic) and lead encephalopathy; as a dicobalt edetate for the emergensy treatment of cyanide poisoning. Also it is used as a chromium edetate (51Cr) for the renal diagnostic. Lead Chelating Activity (Code: N0000175962) Lead Chelator (Code: N0000175963) Anti-coagulant (Code: N0000175980) Decreased Coagulation Factor Activity (Code: N0000008556) Calcium Chelating Activity (Code: N0000175089) antidote (Code: CHEBI:50247) anticoagulant (Code: CHEBI:50249) Anticoagulants (Code: D000925) Calcium Chelating Agents (Code: D065096) Chelating Agents (Code: D002614) Food Additives (Code: D005503) Hematologic Agents (Code: D006401) Sequestering Agents (Code: D064449) 1953-07-16 FDA EDT
Click to view tiamiprine Thiamiprine is a cytotoxic purine antagonist that has both immunosuppressive and antiarthritic activity.
Click to view bifluranol Bifluranol is a fluorinated bibenzyl drug. It has antiandrogenic properties. It was studied for the treatment of benign prostatic hyperplasia.
Click to view carteolol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist A beta-adrenergic antagonist used as an anti-arrhythmia agent, an anti-angina agent, an antihypertensive agent, and an antiglaucoma agent. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) beta-adrenergic antagonist (Code: CHEBI:35530) antihypertensive agent (Code: CHEBI:35674) sympatholytic agent (Code: CHEBI:66991) antiglaucoma drug (Code: CHEBI:39456) anti-arrhythmia drug (Code: CHEBI:38070) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1988-12-28 FDA
Click to view dimetindene Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12593665) A histamine H1 antagonist. It is used in hypersensitivity reactions, in rhinitis, for pruritus, and in some common cold remedies. Anti-Allergic Agents (Code: D018926) Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1960 FDA
Click to view perfosfamide Perfosfamide (4-Hydroperoxycyclophosphamide) is an active derivative of cyclophosphamide and is a tautomer of aldophosphamide. Perfosfamide doesnot need to be activated by the hepatic cytochrome P-450 system. Perfosfamide alkylates DNA, thereby inhibiting DNA replication and RNA and protein synthesis. Perfosfamide was used for the ex-vivo treatment of autologous bone marrow and subsequent reinfusion in patients with acute myelogenous leukemia, also referred to as acute nonlymphocytic leukemia.
Click to view pimethixene Transcriptional activator protein luxR (Organism: Aliivibrio fischeri, class: Unclassified, accessions: P12746, gene: luxR, swissprot: LUXR_ALIFS 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT
Click to view oxaprozin Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9650852) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9650852) Bifunctional epoxide hydrolase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P34913, gene: EPHX2, swissprot: HYES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27009944) Oxaprozin is a nonsteroidal anti-inflammatory drug. Oxaprozin has analgesic, anti-inflammatory, and antipyretic properties. Oxaprozin is a potent inhibitor of prostaglandin synthesis in vitro. Oxaprozin is indicated for the relief of signs and symptoms of osteoarthritis, rheumatoid arthritis and juvenile rheumatoid arthritis. Cyclooxygenase Inhibitors (Code: N0000000160) Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) analgesic (Code: CHEBI:35480) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1992-10-29 FDA
Click to view ondansetron 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020103s036,020605s020,020781s020lbl.pdf) 5-hydroxytryptamine receptor 3B (Organism: Homo sapiens, class: Ion channel, accessions: O95264, gene: HTR3B, swissprot: 5HT3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020103s036,020605s020,020781s020lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020103s036,020605s020,020781s020lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020103s036,020605s020,020781s020lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020103s036,020605s020,020781s020lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16946512) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16946512) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) GABA-A receptor; anion channel (Organism: Rattus norvegicus, class: Ion channel, accessions: P62813|P23576|P20236|P28471|P19969|P30191|P15431|P63138|P63079|P18506|P23574|P18508|P28473|Q9ES14|O09028|Q91ZM7, gene: Gabra1|Gabra2|Gabra3|Gabra4|Gabra5|Gabra6|Gabrb1|Gabrb2|Gabrb3|Gabrd|Gabrg1|Gabrg2|Gabrg3|Gabre|Gabrp|Gabrq, swissprot: GBRA1_RAT|GBRA2_RAT|GBRA3_RAT|GBRA4_RAT|GBRA5_RAT|GBRA6_RAT|GBRB1_RAT|GBRB2_RAT|GBRB3_RAT|GBRD_RAT|GBRG1_RAT|GBRG2_RAT|GBRG3_RAT|GBRE_RAT|GBRP_RAT|Q91ZM7_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10780899) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12873512) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21599003) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21599003) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21599003) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Ondansetron is a competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties. Anti-Anxiety Agents (Code: D014151) Antiemetics (Code: D000932) Antipruritics (Code: D000982) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dermatologic Agents (Code: D003879) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Tranquilizing Agents (Code: D014149) Serotonin 3 Receptor Antagonists (Code: N0000175817) Serotonin-3 Receptor Antagonist (Code: N0000175818) 1991-01-04 FDA
Click to view anastrozole Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020541s031lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020541s031lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020541s031lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020541s031lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020541s031lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21175441) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21175441) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21175441) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21175441) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23712697) Anastrozole is a non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone. Anastrozole is indicated for adjuvant treatment of postmenopausal women with hormone receptorpositive early breast cancer, for frst-line treatment of postmenopausal women with hormone receptorpositive or hormone receptor unknown locally advanced or metastatic breast cance, treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. Aromatase Inhibitor (Code: N0000175563) antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Aromatase Inhibitors (Code: D047072) Enzyme Inhibitors (Code: D004791) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Steroid Synthesis Inhibitors (Code: D065088) 1995-12-27 FDA
Click to view pramocaine Pramocaine (pramoxine) is a topical anesthetic and antipruritic. Pramocaine acts by preventing ionic fluctuations needed for neuron membrane depolarization and action potential propagation. Pramocaine reversibly binds and inhibits voltage gated sodium channels on neurons decreasing sodium permeability into the cell. This stabilizes the membrane and prevents ionic fluctuations needed for depolarization stopping any action potential propagation. Pramocaine is used to temporarily relieve itching and pain caused by minor skin irritation such as minor burns, sunburn, eczema, insect bites, cold sores, or rashes from poison ivy, poison oak, or poison sumac. Some products containing pramocaine are also used to temporarily relieve the itching and discomfort from hemorrhoids and certain other problems of the genital or anal area. Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) local anaesthetic (Code: CHEBI:36333) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1976-08-13 FDA PX9
Click to view mabuterol Mabuterol is a long acting beta 2-adrenergic agonist which stimulates adenylyl cyclase activity and the closing of calcium channels. Studies indicate that the R enantiomer of mabuterol is more potent than the S enantiomer. It was used as a bronchodilator. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1986 PMDA
Click to view butoxycaine Butoxycaine is a local anaesthetic of the ester type. It was used as the base or hydrochloride for surface anesthesia
Click to view amitriptylinoxide Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN
Click to view dimazole Dimazole (diamthazole) is an antifungal. It was used for the treatment of tinea pedis. It was withdrawn in 1972 due to neuropsychiatric reactions.
Click to view prozapine
Click to view pramiverine long acting cholinolytic proposed for gastrointestinal spasms; minor descriptor (78-84); on-line & Index Medicus search CYCLOHEXYLAMINES (78-84); RN given refers to parent cpd
Click to view butriptyline Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) a tricyclic antianxiety and antidepressive agent similar to, but with less side effects than amitriptyline; minor descriptor (75-86); on line & INDEX MEDICUS search DIBENZOCYCLOHEPTENES (75-86); RN given refers to parent cpd Anti-Anxiety Agents (Code: D014151) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view budipine Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Glutamate [NMDA] receptor (Organism: Homo sapiens, class: Ion channel, accessions: O15399|O60391|Q05586|Q12879|Q13224|Q14957|Q8TCU5, gene: GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B, swissprot: NMD3A_HUMAN|NMD3B_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMDE4_HUMAN|NMDZ1_HUMAN Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491)
Click to view lumiracoxib Prostaglandin G/H synthase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q05769, gene: Ptgs2, swissprot: PGH2_MOUSE) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: ) A selective non-steroidal anti-inflammatory drug (NSAID) that belongs to the group cyclo-oxygenase 2 (COX-2) inhibitors. It blocks the COX-2 enzyme, resulting in a reduction in the production of prostaglandins, substances that are involved in the inflammation process. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase 2 Inhibitors (Code: D052246) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2003-09-12 UK Medicines and Healthcare Products Regulatory Agency (MHRA) LUR
Click to view iomeglamic acid Iomeglamic Acid is an iodinated aryldicarboxylic acid monoamide. Iomeglamic acid was applied for radioscopy of the gall-bladder.
Click to view lidofenin Lidofenin is ligand for a coordination complex consisting of the radioisotope technetium-99m. Following intravenous administration, technetium Tc 99m–labeled IDA derivatives, such as lidofenin, become bound to plasma proteins (mainly albumin). In the liver, in the space of Disse, technetium Tc 99m lidofenin becomes dissociated from the proteins and enters the hepatocyte by a mechanism similar to that of serum bilirubin. Technetium Tc 99m lidofenin traverses through the hepatocyte unmetabolized and enters the bile canaliculi. Flow beyond the canaliculi is influenced to a large extent by the tone of the sphincter of Oddi and the patency of the bile ducts. Technetium lidofenin is indicated as a hepatobiliary imaging agent for the evaluation of hepatobiliary tract patency to differentiate jaundice, to differentiate extrahepatic biliary atresia from neonatal hepatitis; to detect cystic duct obstruction associated with acute cholecystitis nd to detect bile leaks. 1986-10-31 FDA
Click to view rosoxacin Rosoxacin is a quinolone derivative and an antibiotic. Rosoxacin binds to and inhibits two enzymes topoisomerase II (DNA gyrase), which is required for bacterial DNA replication, transcription, repair, and recombination. It is used for the treatment of respiratory tract, urinary tract, gastrointestinal infections. antibacterial drug (Code: CHEBI:36047) antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) 1981-04-10 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view sulfametomidine Sulfametomidine is a long-acting sulfonamide.
Click to view sulfacytine Sulfacytine is a short-acting sulfonamide. Sulfacytine is a competitive inhibitor of the enzyme dihydropteroate synthetase. It inhibits bacterial synthesis of of dihydrofolic acid by preventing the condensation of the pteridine with para-aminobenzoic acid (PABA), a substrate of the enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid. Sulfacytine is used for the treatment of acute urinary tract infections. 1975-09-12 FDA
Click to view troxipide Troxipide is a member of benzamides. It exerts its activity by increasing mucus production, cytoprotective prostaglandin secretion, regeneration of collagen fibers, reducing inflammatory mediator induced neutrophil migration and reactive oxygen species generation in gastric mucosa, enhancing gastric mucosal metabolism and microcirculation. It is used for the treatment of gastric uclers and for amelioration of gastric mucosal lesions (erosion, hemorrhage, redness and edema) in the diseases such as acute gastritis, acute exacerbation stage of chronic gastritis. 1994-07-01 PMDA
Click to view alosetron 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf) 5-hydroxytryptamine receptor 3B (Organism: Homo sapiens, class: Ion channel, accessions: O95264, gene: HTR3B, swissprot: 5HT3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021107s029lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18448342) Alosetron is a potent and selective antagonist of the serotonin 5-HT3 receptor type. Activation of these channels and the resulting neuronal depolarization affect the regulation of visceral pain, colonic transit, and gastrointestinal secretions, processes that relate to the pathophysiology of IBS. 5-HT3 receptor antagonists such as alosetron inhibit activation of non-selective cation channels, which results in the modulation of the enteric nervous system. Alosetron reduces pain and exaggerates motor responses, possibly due to blockade of 5-HT3 receptors. Alosetron is indicated only for women with severe diarrhea-predominant irritable bowel syndrome (IBS) who have chronic IBS symptoms (generally lasting 6 months or longer), had anatomic or biochemical abnormalities of the gastrointestinal tract excluded, and not responded adequately to conventional therapy. Serotonin 3 Receptor Antagonists (Code: N0000175817) Serotonin-3 Receptor Antagonist (Code: N0000175818) gastrointestinal drug (Code: CHEBI:55324) serotonergic antagonist (Code: CHEBI:48279) antiemetic (Code: CHEBI:50919) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) 2000-02-09 FDA
Click to view norgestrienone A synthetic steroid with progestational and contraceptive activities. Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102)
Click to view propoxycaine Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN) blocker (Source: ) A local anesthetic of the ester type that has a rapid onset of action and a longer duration of action than procaine hydrochloride. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1017) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) FDA
Click to view proparacaine Proparacaine is a topical anesthetic drug of the amino ester group. The exact mechanism whereby proparacaine and other local anesthetics influence the permeability of the cell membrane is unknown. Proparacaine may alter epithelial sodium channels through interaction with channel protein residues. Proparacaine is indicated for procedures in which a topical ophthalmic anesthetic is indicated: corneal anesthesia of short duration, e.g. tonometry, gonioscopy, removal of corneal foreign bodies, and for short corneal and conjunctival procedures. Local Anesthesia (Code: N0000175976) Local Anesthetic (Code: N0000175539) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1953-07-01 FDA
Click to view eburnamonine Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) allosteric modulator (Source: ) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view vinburnine Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) allosteric modulator (Source: )
Click to view noxiptiline proposed tricyclic antidepressent; minor descriptor (75-86); on line & INDEX MEDICUS search DIBENZOCYCLOHEPTENES (75-86); RN given refers to parent cpd Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619)
Click to view trimipramine Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: ) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: ) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: ) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: ) Tricyclic antidepressant similar to IMIPRAMINE, but with more antihistaminic and sedative properties. Tricyclic Antidepressant (Code: N0000175752) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) 1979-06-12 FDA
Click to view dimetacrine Apical membrane antigen 1 (Organism: Plasmodium falciparum (isolate 3D7), class: Unclassified, accessions: Q7KQK5, gene: AMA1, swissprot: Q7KQK5_PLAF7 minor descriptor (75-84); on-line & Index Medicus search ACRIDINES (75-84); RN given refers to parent cpd without isomeric designation
Click to view sodium tetradecyl sulfate An anionic surface-active agent used for its wetting properties in industry and used in medicine as an irritant and sclerosing agent for hemorrhoids and varicose veins. detergent (Code: CHEBI:27780) Cardiovascular Agents (Code: D002317) Pharmaceutical Solutions (Code: D019999) Sclerosing Solutions (Code: D012597) Surface-Active Agents (Code: D013501) 1946-08-13 FDA
Click to view sodium tetradecyl sulfate Sodium tetradecyl sulfate (sodium myristyl sulfate) is an anionic surfactant used as a sclerosing agent. Upon injection into a varicose vein, sodium myristyl sulfate interacts with lipids on the vein walls thereby causing intimal inflammation, destruction of the vein, and thrombus and fibrous tissue formation. This eventually leads to occlusion of the injected vein. It is used in medicine as an irritant and sclerosing agent for hemorrhoids and varicose veins. 1987-10-06 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view indobufen Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) thromboxane A2 antagonist Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Peripheral Nervous System Agents (Code: D018373) Platelet Aggregation Inhibitors (Code: D010975) Sensory System Agents (Code: D018689) 1984-01-01 YEAR INTRODUCED
Click to view floredil Floredil is a coronary stabilizer, vasodilator. It is no longer available. 1973 YEAR INTRODUCED
Click to view tiadenol Tiadenol is an aliphatic sulfide and an absorbable hypolipidemic agent. It was used for the treatment of hypercholesterolemia. It is no longer available. Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) 1987-06-17 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view estazolam GABA-A receptor alpha-5/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P28472|P31644, gene: GABRA5|GABRB3|GABRG2, swissprot: GBRA5_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator GABA-A receptor alpha-3/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P28472|P34903, gene: GABRA3|GABRB3|GABRG2, swissprot: GBRA3_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator GABA-A receptor alpha-2/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P28472|P47869, gene: GABRA2|GABRB3|GABRG2, swissprot: GBRA2_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Anti-Anxiety Agents (Code: D014151) anxiolytic drug (Code: CHEBI:35474) anticonvulsant (Code: CHEBI:35623) GABA modulator (Code: CHEBI:50268) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1990-12-26 FDA
Click to view bucloxic acid water insoluble anti-inflammatory agent with analgesic & antipyretic properties Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373)
Click to view glyconiazide Glyconiazide is an antibacterial drug with high antitubercular activity. It is no longer available.
Click to view azidamfenicol Azidamfenicol is an amphenicol antibiotic, which has similar profile to chloramphenicol. It is used topically as ophthalmic solution for the treatment of bacterial infections. 1981-07-20 National Organization for Medicines (Greece)
Click to view nimetazepam Nimetazepam is an intermediate-acting hypnotic drug which is a benzodiazepine derivative. It does possess hypnotic, anxiolytic, sedative, and skeletal muscle relaxant properties. Nimetazepam is also an anticonvulsant. It was used for the treatment of short-term severe insomnia. Nimetazepam is currently a Schedule IV drug under the international Convention on Psychotropic Substances of 1971. Nimetazepam can only be used legally by health professionals and for university research purposes. Anti-Anxiety Agents (Code: D014151) sedative (Code: CHEBI:35717) antispasmodic drug (Code: CHEBI:53784) anticonvulsant (Code: CHEBI:35623) GABA modulator (Code: CHEBI:50268) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1977-05-16 PMDA
Click to view mebendazole Tubulin beta chain (Organism: Trichuris trichiura (Whipworm), class: Structural, accessions: O44388, gene: None, swissprot: TBB_TRITR) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208398s000lbl.pdf) Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22795629) Calmodulin-domain protein kinase 1 (Organism: Toxoplasma gondii, class: Kinase, accessions: Q9BJF5, gene: CDPK1, swissprot: Q9BJF5_TOXGO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22795629) Mebendazole is an antihelmintic agent used commonly for roundworm (pinworm and hookworm) infections, trichinosis, capillariasis and toxocariasis and other parasitic worm infections. Mebendazole interferes with cellular tubulin formation in the helminth and causes ultrastructural degenerative changes in its intestine. As a result, its glucose uptake and the digestive and reproductive functions are disrupted, leading to immobilization, inhibition of egg production and death of the helminth. Antihelminthic (Code: N0000175481) Anthelmintics (Code: D000871) antinematodal drug (Code: CHEBI:35444) Anti-Infective Agents (Code: D000890) Antimitotic Agents (Code: D050256) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Mitosis Modulators (Code: D050258) Tubulin Modulators (Code: D050257) 1974-06-28 FDA
Click to view esmolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019386s043lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/019386s043lbl.pdf) Esmolol is a beta1-selective (cardioselective) adrenergic receptor blocking agent with rapid onset, a very short duration of action, and no significant intrinsic sympathomimetic or membrane stabilizing activity at therapeutic dosages. Esmolol inhibits the beta1 receptors located chiefly in cardiac muscle, but this preferential effect is not absolute and at higher doses it begins to inhibit beta2 receptors located chiefly in the bronchial and vascular musculature. Esmolol is indicated for the short-term control of ventricular rate in supraventricular tachycardia including atrial fibrillation and atrial flutter and control of heart rate in noncompensatory sinus tachycardia and control of perioperative tachycardia and hypertension. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) beta-adrenergic antagonist (Code: CHEBI:35530) anti-arrhythmia drug (Code: CHEBI:38070) Neurotransmitter Agents (Code: D018377) 1986-12-31 FDA
Click to view dibenzepin Dibenzepin is a tricyclic antidepressant of the dibenzo-epine group. It is a selective noradrenaline uptake inhibitor, which exhibits in vitro and in vivo imipramine-like effects. It binds strongly to histamine H1 receptors in the brain and, to a lesser extent, to cholinergic receptors. The pharmacological profile of dibenzepin corresponds widely to its biochemical properties: histamine antagonism, tetrabenazine antagonism, potentiation of various noradrenergic effects and anticholinergic effects. Dibenzepin was used for the treatment of depression. It is no longer available. Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619)
Click to view sumatriptan 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020626s027lbl.pdf) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020626s027lbl.pdf) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020626s027lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11708905) Sumatriptan is a sulfonamide triptan with vasoconstrictor activity. Sumatriptan presumably exerts its therapeutic effects in the treatment of migraine headache through agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels and sensory nerves of the trigeminal system, which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. vasoconstrictor agent (Code: CHEBI:50514) serotonergic agonist (Code: CHEBI:35941) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Serotonin 5-HT1 Receptor Agonists (Code: D058825) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Vasoconstrictor Agents (Code: D014662) Serotonin 1b Receptor Agonists (Code: N0000175763) Serotonin 1d Receptor Agonists (Code: N0000175764) Serotonin-1b and Serotonin-1d Receptor Agonist (Code: N0000175765) 1992-12-28 FDA
Click to view difemetorex
Click to view pridinol Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antispasmodic & muscle relaxant; RN given refers to parent cpd; structure in Merck Index, 9th ed, #7539 muscle relaxant (Code: CHEBI:51371) antiparkinson drug (Code: CHEBI:48407)
Click to view normethadone Normethadone is a derivate of opioid analgetic methadone. Normethadone activates central opioid receptors in the medulla to supress the cough reflex. It also likely activates peripheral opioid receptors to inhibit signalling by irritant receptors of the airway. Normethadone is used as an opioid antitussive in combination with Oxilofrine. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689) 1957-12-31 Health Canada
Click to view picoperine
Click to view tertatolol Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14744619) Tertatolol is a beta-blocker with unique renal vasodilatatory effects, mainly at the level of the microcirculation. The mechanisms of this renal vasodilatation are not fully understood but might involve renal 5-HT1A receptor stimulation. It is a potent competitive antagonist of 5-HT1A and 5-HT1B receptors. Tertatolol inhibits human mesangial cell proliferation. Tertatolol is used for the treatment of hypertension. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 1986-04-25 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view pizotifen 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: ) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN Serotonin antagonist used against MIGRAINE DISORDERS and vascular headaches. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) serotonergic antagonist (Code: CHEBI:48279) muscarinic antagonist (Code: CHEBI:48876) histamine antagonist (Code: CHEBI:37956) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702)
Click to view dosulepin Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) A tricyclic antidepressant with some tranquilizing action. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) 1962-01-01 YEAR INTRODUCED
Click to view diisopromine
Click to view chlorothiazide Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991988) Chlorothiazide is a diuretic and antihypertensive. Chlorothiazide affects the distal renal tubular mechanism of electrolyte reabsorption. Chlorothiazide increases excretion of sodium and chloride in approximately equivalent amounts. Natriuresis may be accompanied by some loss of potassium and bicarbonate. Chlorothiazide is indicated as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Chlorothiazide has also been found useful in edema due to various forms of renal dysfunction such as nephrotic syndrome, acute glomerulonephritis, and chronic renal failure. Also chlorothiazide is indicated in the management of hypertension either as the sole therapeutic agent or to enhance the effectiveness of other antihypertensive drugs in the more severe forms of hypertension. Increased Diuresis (Code: N0000175359) Thiazide Diuretic (Code: N0000175419) Thiazides (Code: N0000166469) diuretic (Code: CHEBI:35498) antihypertensive agent (Code: CHEBI:35674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) 1958-09-04 FDA
Click to view chloropyrilene not carcinogenic; RN given refers to parent cpd; structure given in first source
Click to view sulfarside Sulfarside is a sulfa drug with the arsenical type. It is effective against sub-acute, acute and chronic amebiasis. Sulfarside also has some anti-giardial and trichomonacidal activity.
Click to view meclofenamic acid Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23454516) Aldo-keto reductase family 1 member C2 (Organism: Homo sapiens, class: Enzyme, accessions: P52895, gene: AKR1C2, swissprot: AK1C2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23454516) Aldo-keto reductase family 1 member C1 (Organism: Homo sapiens, class: Enzyme, accessions: Q04828, gene: AKR1C1, swissprot: AK1C1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23454516) Prostaglandin G/H synthase 1 (Organism: Ovis aries, class: Enzyme, accessions: P05979, gene: PTGS1, swissprot: PGH1_SHEEP) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11844663) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11844663) Arachidonate 5-lipoxygenase (Organism: Rattus norvegicus, class: Enzyme, accessions: P12527, gene: Alox5, swissprot: LOX5_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8515419) Potassium voltage-gated channel subfamily KQT member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O43526, gene: KCNQ2, swissprot: KCNQ2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15598972) Potassium voltage-gated channel subfamily KQT member 3 (Organism: Homo sapiens, class: Ion channel, accessions: O43525, gene: KCNQ3, swissprot: KCNQ3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15598972) Solute carrier organic anion transporter family member 1C1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9EPZ7, gene: Slco1c1, swissprot: SO1C1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18845642) Meclofenamic acid is a non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis. Meclofenamic acid is indicated for reduction of fever, for relief of mild to moderate pain, signs and symptoms of juvenile arthritis, rheumatoid arthritis, osteoarthritis, for treatment of primary dysmenorrhea. Also it is indicated for acute or long-term use in the relief of signs and symptoms of ankylosing spondylitis, acute painful shoulder (Acute subacromial bursitis/supraspinatus tendinitis), acute gouty arthritis. Meclofenamic acid is also indicated for the treatment of idiopathic heavy menstrual blood loss. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antirheumatic drug (Code: CHEBI:35842) antineoplastic agent (Code: CHEBI:35610) anticonvulsant (Code: CHEBI:35623) analgesic (Code: CHEBI:35480) antipyretic (Code: CHEBI:35493) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1980-06-25 FDA JMS
Click to view diclofenac Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/204592s007s008lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/204592s007s008lbl.pdf) A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) drug allergen (Code: CHEBI:88188) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Decreased Prostaglandin Production (Code: N0000008836) Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) 1988-07-28 FDA DIF
Click to view tritiozine Tritiozine is an antisecretory agent. It was used for the treatment of peptic ulcer.
Click to view trifluridine trifluridine: Thymidine kinase (Organism: Homo sapiens, class: Kinase, accessions: P23919, gene: DTYMK, swissprot: KTHY_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00000133.PDF) Thymidine phosphorylase (Organism: Homo sapiens, class: Enzyme, accessions: P19971, gene: TYMP, swissprot: TYPH_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207981s008lbl.pdf) Sodium/nucleoside cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: O00337, gene: SLC28A1, swissprot: S28A1_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/lonsurf-epar-product-information_en.pdf) Equilibrative nucleoside transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q99808, gene: SLC29A1, swissprot: S29A1_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/lonsurf-epar-product-information_en.pdf) Equilibrative nucleoside transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q14542, gene: SLC29A2, swissprot: S29A2_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/lonsurf-epar-product-information_en.pdf) trifluridine monophosphate: Thymidylate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P04818, gene: TYMS, swissprot: TYSY_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00000133.PDF) trifluridine triphosphate: DNA polymerase catalytic subunit (Organism: Human herpesvirus 1 (strain 17), class: Enzyme, accessions: P04293, gene: None, swissprot: DPOL_HHV11) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00000133.PDF) DNA polymerase catalytic subunit (Organism: Varicella-zoster virus (strain Dumas), class: Enzyme, accessions: P09252, gene: None, swissprot: DPOL_VZVD) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00000133.PDF) Trifluridine is a nucleoside metabolic inhibitor. Trifluridine is phosphorylated by a cellular thymidine kinase to its nucleotide monophosphate. Trifluridine monophosphate is an inhibitor of thymidylate synthetase, the target enzyme for the action of monofluorinated pyrimidines. Trifluridine monophosphate is further phosphorylated by cellular enzymes to the triphosphate which is incorporated into DNA (but not RNA) by competitively inhibiting the incorporation of the natural nucleotide, thymidine triphosphate (dTTP). Viral DNA polymerase has a higher affinity for trifluridine triphosphate than does the DNA polymerase of uninfected cells, resulting in the preferential incorporation of the analogue into viral DNA. Trifluridine is active against the following DNA viruses: herpes simplex types 1 and 2, varicella zoster, adenovirus and vaccinia virus. Trifluridine is used for the treatment of primary keratoconjunctivitis and recurrent epithelial keratitis due to herpes simplex viruses, types 1 and 2. Trifluridine is also effective in the treatment of epithelial keratitis. Also trifluridine is used in combination with thymidine phosphorylase inhibitor, tipiracil, for the treatment of metastatic colorectal cancer and metastatic gastric or gastroesophageal junction adenocarcinoma. Nucleoside Analog (Code: N0000175459) Nucleoside Analog Antiviral (Code: N0000175466) Nucleoside Metabolic Inhibitor (Code: N0000175595) Nucleic Acid Synthesis Inhibitors (Code: N0000000233) antiviral drug (Code: CHEBI:36044) antineoplastic agent (Code: CHEBI:35610) Anti-Infective Agents (Code: D000890) Antimetabolites (Code: D000963) Antiviral Agents (Code: D000998) Noxae (Code: D009676) 1980-04-10 FDA
Click to view bermoprofen Bermoprofen is a nonsteroidal anti-inflammatory drug with antipyretic, analgesic and anti-inflammatory effects. The drug was found to be teratogenic in rats.
Click to view exiproben Exiproben is a choleretic. When administered, exiproben potently stimulates the production of bile. It was used for the treatment of hepatobiliary disorders. Italian Medicines Agency (AIFA)
Click to view propizepine Propizepine is a benzodiazepinone derivative. It is an antidepressive, antihistaminic, antianaphylactic, thymoanaleptic, antiserotonine, antispasmodic, and analgetic compound. Propizepine was used for the treatment of depression in the 1980s. 1988-07-27 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view glycyclamide Glycyclamide is a cyclohexyl-containing sulfonylurea compound with antihyperglycemic activity. Tolcyclamide is closely related to tolbutamide. It was used for the symptomatic treatment of diabetes mellitus.
Click to view bentazepam Bentazepam is a benzodiazepine analog. Bentazepam possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. A severe benzodiazepine overdose with bentazepam may result in coma and respiratory failure. Severe liver damage and hepatitis has also been associated with bentazepam. It was used as a short-action anxiolytic. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1980-07-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view exemestane Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020753s020lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020753s020lbl.pdf) a hormonal antineoplastic agent antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Aromatase Inhibitors (Code: D047072) Enzyme Inhibitors (Code: D004791) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Steroid Synthesis Inhibitors (Code: D065088) Aromatase Inhibitor (Code: N0000175563) 1999-10-21 FDA EXM
Click to view ethinylestradiol Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209627s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020472s016lbl.pdf) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19454483) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19454483) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15290871) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14681337) Sulfotransferase 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P50225, gene: SULT1A1, swissprot: ST1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22593037) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21030469) Ethinylestradiol is a synthetic derivative of the natural estrogen estradiol. It has high estrogenic potency when administered orally and is often used as the estrogenic component in oral contraceptives. Ethinylestradiol is used for treatment of moderate to severe vasomotor symptoms associated with the menopause, female hypogonadism, prostatic carcinoma-palliative therapy of advanced disease, breast cancer, as an oral contraceptive, and as emergency contraceptive. Estrogen (Code: N0000175825) Estrogen Receptor Agonists (Code: N0000000100) xenoestrogen (Code: CHEBI:76988) Estrogens (Code: D004967) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1943-06-25 FDA 3WF
Click to view palonosetron 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021372s008s010lbl.pdf) 5-hydroxytryptamine receptor 3B (Organism: Homo sapiens, class: Ion channel, accessions: O95264, gene: HTR3B, swissprot: 5HT3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021372s008s010lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021372s008s010lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021372s008s010lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021372s008s010lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Palonosetron is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting. Palonosetron did not inhibit the antitumor activity of the five chemotherapeutic agents tested (cisplatin, cyclophosphamide, cytarabine, doxorubicin and mitomycin C) in murine tumor models. Serotonin 3 Receptor Antagonists (Code: N0000175817) Serotonin-3 Receptor Antagonist (Code: N0000175818) antiemetic (Code: CHEBI:50919) serotonergic antagonist (Code: CHEBI:48279) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) 2003-07-25 FDA
Click to view dimevamide
Click to view parathiazine Parathiazine is a member of phenothiazines.
Click to view methdilazine Methdilazine is a phenothiazine compound with antihistaminic activity. Methdilazine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. It is used in the treatment of various dermatoses to relieve pruritus. 1960 FDA
Click to view disulfiram Aldehyde dehydrogenase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P05091, gene: ALDH2, swissprot: ALDH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17220694) Dopamine beta-hydroxylase (Organism: Homo sapiens, class: Enzyme, accessions: P09172, gene: DBH, swissprot: DOPO_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19720750) Disulfiram is a carbamate derivative used as an alcohol deterrent. It is a relatively nontoxic substance when administered alone, but markedly alters the intermediary metabolism of alcohol. When alcohol is ingested after administration of disulfiram, blood acetaldehyde concentrations are increased, followed by flushing, systemic vasodilation, respiratory difficulties, nausea, hypotension, and other symptoms (acetaldehyde syndrome). It acts by inhibiting aldehyde dehydrogenase. Its main metabolite is a ditiocarb. Acetaldehyde Dehydrogenase Inhibitors (Code: D065086) Alcohol Deterrents (Code: D000427) angiogenesis inhibitor (Code: CHEBI:48422) fungicide (Code: CHEBI:24127) antineoplastic agent (Code: CHEBI:35610) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Acetyl Aldehyde Dehydrogenase Inhibitors (Code: N0000000183) Aldehyde Dehydrogenase Inhibitor (Code: N0000175679) 1951-08-28 FDA
Click to view fenclofenac Fenclofenac is an acetic acid nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Fenclofenac was used to treat pain, dysmenorrhea, ocular inflammation, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and actinic keratosis. Due to its side effects it was withdrawn from the market in 1984. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view enilconazole Indoleamine 2,3-dioxygenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P14902, gene: IDO1, swissprot: I23O1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25036789) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/19070657) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19070657) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21115097) Enilconazole is a fungicide. Enilconazole is a synthetic broad-spectrum antimycotic with a high activity against most of the common dermatophytes and various other fungi and yeasts. Enilconazole is active against Microsporum sp., Trichophyton sp., Aspergillus sp., Penicillium sp. and yeasts such as Candida sp.. It inhibits fungal cytochrome p450 dependent 14alpha-dimethylation of lanosterol. It is widely used in agriculture, particularly in the growing of citrus fruits. Also it is used in veterinary medicine. antifungal agrochemical (Code: CHEBI:86328) Fungicides, Industrial (Code: D005659) Pesticides (Code: D010575)
Click to view nelarabine Adenosine deaminase (Organism: Homo sapiens, class: Enzyme, accessions: P00813, gene: ADA, swissprot: ADA_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021877s009lbl.pdf) Deoxycytidine kinase (Organism: Homo sapiens, class: Kinase, accessions: P27707, gene: DCK, swissprot: DCK_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021877s009lbl.pdf) Nelarabine is a prodrug of the deoxyguanosine analogue 9-beta-D-arabinofuranosylguanine (ara-G), a nucleoside metabolic inhibitor. Nelarabine is demethylated by adenosine deaminase (ADA) to ara-G, mono-phosphorylated by deoxyguanosine kinase and deoxycytidine kinase, and subsequently converted to the active 5’-triphosphate, ara-GTP. Accumulation of ara-GTP in leukemic blasts allows for incorporation into deoxyribonucleic acid (DNA), leading to inhibition of DNA synthesis and cell death. Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) 2005-10-28 FDA
Click to view ibuprofen piconol Ibuprofen piconol, the pyridyl ester and a prodrug of ibuprofen, is a potent non-steroidal, anti-inflammatory (NSAID) drug marketed in Japan. It Is used to treat acute eczema, contact dermatitis, atopic dermatitis, chronic eczema, rosacea-like dermatitis/perioral dermatitis, herpes zoster and acne vulgaris. (See: ibuprofen) PMDA
Click to view glybuzole Glybuzole is a sulfonamide derivative with antihyperglycemic activity. Like sulfonylureas, glybuzole is able to lower blood glucose levels by increasing the release of insulin from pancreatic beta cells. PMDA
Click to view imipramine oxide
Click to view tolindate Tolindate, a thiocarbamate, is a synthetic antifungal. It has strong topical antifungal activity. It was used for topical application in the treatment of various dermatoses.
Click to view duloxetine 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11750180) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11750180) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11750180) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19480470) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12481192) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12481192) a selective serotonin and norepinephrine reuptake inhibitor widely used as an antidepressant and for neuropathic pain. Duloxetine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury. Norepinephrine Uptake Inhibitors (Code: N0000000102) Serotonin and Norepinephrine Reuptake Inhibitor (Code: N0000175749) Serotonin Uptake Inhibitors (Code: N0000000109) Analgesics (Code: D000700) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) Serotonin and Noradrenaline Reuptake Inhibitors (Code: D000068760) 2004-08-03 FDA 29E
Click to view dimantine
Click to view hydrochlorothiazide Solute carrier family 12 member 3 (Organism: Rattus norvegicus, class: Transporter, accessions: P55018, gene: Slc12a3, swissprot: S12A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10894798) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049739) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17135398) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26691758) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26691758) Delta carbonic anhydrase (Organism: Thalassiosira weissflogii, class: Unclassified, accessions: Q5U9J1, gene: ca1, swissprot: Q5U9J1_THAWE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24314394) Hydrochlorothiazide is a thiazide diuretic. Thiazides affect the renal tubular mechanisms of electrolyte reabsorption, directly increasing excretion of sodium and chloride in approximately equivalent amounts. The mechanism of the antihypertensive effect of thiazides is not fully understood. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism. Increased Diuresis (Code: N0000175359) Thiazide Diuretic (Code: N0000175419) Thiazides (Code: N0000166469) diuretic (Code: CHEBI:35498) antihypertensive agent (Code: CHEBI:35674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) 1959-02-12 FDA HCZ
Click to view amlexanox Phosphodiesterase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27815|Q07343|Q08493|Q08499, gene: PDE4A|PDE4B|PDE4C|PDE4D, swissprot: PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN) inhibitor (Source: ) Inhibitor of nuclear factor kappa-B kinase subunit epsilon (Organism: Homo sapiens, class: Kinase, accessions: Q14164, gene: IKBKE, swissprot: IKKE_HUMAN) inhibitor (Source: ) Serine/threonine-protein kinase TBK1 (Organism: Homo sapiens, class: Kinase, accessions: Q9UHD2, gene: TBK1, swissprot: TBK1_HUMAN) inhibitor (Source: ) The mechanism of action by which amlexanox accelerates healing of aphthous ulcers is unknown. In vitro studies have demonstrated amlexanox to be a potent inhibitor of the formation and/or release of inflammatory mediators (histamine and leukotrienes) from mast cells, neutrophils and mononuclear cells. Decreased Histamine Release (Code: N0000175628) Anti-Allergic Agents (Code: D018926) anti-allergic agent (Code: CHEBI:50857) anti-ulcer drug (Code: CHEBI:49201) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) 1996-12-17 FDA ANW
Click to view metochalcone ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/22112540/) Metochalcone is a chalcone. It was isolated from heartwood of Pterocarpus marsupium. It was used as choleretic and diuretic agent.
Click to view piribedil D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388667) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7473180) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7473180) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11356907) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11356907) Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11356907) Piribedil is a non-ergot dopamine D2 agonist. It is used in the treatment of Parkinson's disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist. Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) 1988-04-20 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view nialamide An MAO inhibitor that is used as an antidepressive agent. Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Monoamine Oxidase Inhibitors (Code: D008996) Psychotropic Drugs (Code: D011619)
Click to view zaltoprofen Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9650852) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9650852) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12236850) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12236850) Zaltoprofen is a non-steroidal anti-inflammatory (NSAID). The main mechanism of action involves the inhibition of COX-2. Additional mechanism may be associated with the inhibitory effect of zaltoprofen on bradykinin-induced nociceptive responses that happens without blocking bradykinin receptors. Zaltoprofen is used as an anti-inflammatory and analgesic for rheumatoid arthritis, osteoarthritis, lumbago, periarthritis, after surgery, trauma and tooth extraction. 2004-02-05 PMDA
Click to view artemether quinghaosu derivative Anthelmintics (Code: D000871) antimalarial (Code: CHEBI:38068) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Antiprotozoal Agents (Code: D000981) Coccidiostats (Code: D003049) Schistosomicides (Code: D012556) 2009-04-07 FDA
Click to view phenacaine Phenacaine (holocaine) is a local anesthetic used in ophthalmic medicine. Like other local anesthetics it inhibits the specific calmodulin-dependent stimulation of erythrocyte Ca2+-ATPase (ATP phosphohydrolase) and cyclic nucleotide phosphodiesterases (3',5'-cyclic-nucleotide 5'-nucleotidohydrolase) from brain and heart. Phenacaine was used in combination with bacitracin for the treatment of superficial ocular infections.
Click to view carazolol Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://pubmed.ncbi.nlm.nih.gov/8719421/) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://pubmed.ncbi.nlm.nih.gov/18829308/) Carazolol is a beta1/beta2 adrenoreceptor blocking agent. Now, carazolol is used in veterinary medicine to reduce stress in animals during transportation. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Neurotransmitter Agents (Code: D018377) CAU
Click to view minaprine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT Acetylcholinesterase (Organism: Rattus norvegicus, class: Enzyme, accessions: P37136, gene: Ache, swissprot: ACES_RAT Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN Agr 1240 refers to di-HCl; short-acting type A MAO inhibitor (MAOI) of mild potency; structure antidepressant (Code: CHEBI:35469) serotonin uptake inhibitor (Code: CHEBI:50949) dopamine uptake inhibitor (Code: CHEBI:51039) cholinergic drug (Code: CHEBI:38323) antiparkinson drug (Code: CHEBI:48407) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619)
Click to view piprozolin 10 articles in Arzneim Forsch 27(2b):467;1977; structure
Click to view methestrol
Click to view norethynodrel Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist A synthetic progestational hormone with actions and uses similar to those of PROGESTERONE. It has been used in the treatment of functional uterine bleeding and endometriosis. As a contraceptive, it has usually been administered in combination with MESTRANOL. Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102) 1961-03-09 FDA
Click to view norethisterone Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/018977s041lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294327) Norethisterone is a synthetic progestational hormone with actions similar to those of progesterone but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for contraception. Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) synthetic oral contraceptive (Code: CHEBI:49326) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102) 1962-05-21 FDA NDR
Click to view benzestrol
Click to view alimemazine Alimemazine is a phenothiazine used as antipsychotic drug. Alimemazine competes with free histamine for binding at H-receptor sites. This antagonizes the effects of histamine on H-receptors, leading to a reduction of the negative symptoms brought on by histamine H-receptor binding. Alimemazine is used to treat neurosis, depression and anxiety of different origins. Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1985 FDA
Click to view diethazine Pleiotropic ABC efflux transporter of multiple drugs (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Transporter, accessions: P33302, gene: PDR5, swissprot: PDR5_YEAST phenothiazine derivative anti-Parkinson agent with anticholinergic and antihistaminic actions; is effective against Parkinson tremor; minor descriptor (75-86); on-line & INDEX MEDICUS search PHENOTHIAZINES (75-86); RN given refers to cpd without isomeric designation
Click to view ricinoleic acid
Click to view rosaprostol Anti-Ulcer Agents (Code: D000897) Expectorants (Code: D005100) Gastrointestinal Agents (Code: D005765) Respiratory System Agents (Code: D019141)
Click to view imipenem Penicillin-binding protein 1A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918, gene: mrcA, swissprot: PBPA_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050587s081lbl.pdf) Penicillin-binding protein 1A (Organism: Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG 12228), class: Enzyme, accessions: Q07806, gene: mrcA, swissprot: PBPA_PSEAE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050587s081lbl.pdf) Penicillin-binding protein 1B (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02919, gene: mrcB, swissprot: PBPB_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050587s081lbl.pdf) Penicillin-binding protein 1B (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: Q9X6W0, gene: ponB, swissprot: Q9X6W0_PSEAI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050587s081lbl.pdf) Penicillin-binding protein 2 (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD65, gene: mrdA, swissprot: PBP2_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050587s081lbl.pdf) Dipeptidase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P16444, gene: DPEP1, swissprot: DPEP1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050587s081lbl.pdf) Beta-lactamase TEM (Organism: Escherichia coli, class: Enzyme, accessions: P62593, gene: bla; blaT-3; blaT-4;, swissprot: BLAT_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19884379) Beta-lactamase SHV-1 (Organism: Klebsiella pneumoniae, class: Enzyme, accessions: P0AD64, gene: bla, swissprot: BLA1_KLEPN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19884379) Beta-lactamase (Organism: Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG 12228), class: Enzyme, accessions: P24735, gene: ampC, swissprot: AMPC_PSEAE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19884379) Imipenem is a derivative of thienamycin, which is produced by Streptomyces cattleya. Imipenem is a penem antibacterial drug. The bactericidal activity of imipenem results from the inhibition of cell wall synthesis. Its greatest affinity is for penicillin binding proteins (PBPs) 1A, 1B, 2, 4, 5 and 6 of Escherichia coli, and 1A, 1B, 2, 4 and 5 of Pseudomonas aeruginosa. The lethal effect is related to binding to PBP 2 and PBP 1B. Imipenem is a potent inhibitor of betalactamases from certain Gram-negative bacteria which are inherently resistant to most beta-lactam antibacterials, e.g., Pseudomonas aeruginosa, Serratia spp., and Enterobacter spp. Imipenem has been shown to be active against Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalactiae (Group B streptococci), Streptococcus pneumoniae, Streptococcus pyogenes, Acinetobacter spp., Citrobacter spp., Enterobacter spp., Escherichia coli, Gardnerella vaginalis, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp., Morganella morganii, Proteus vulgaris, Providencia rettgeri, Pseudomonas aeruginosa, Serratia spp. (including S. marcescens), Bifidobacterium spp., Clostridium spp., Eubacterium spp., Peptococcus spp., Peptostreptococcus spp., Propionibacterium spp., Bacteroides spp. (including B. fragilis), Fusobacterium spp. Imipenem is used alone or in combination with cilastatin for the treatment of lower respiratory tract infections, urinary tract infections, intra-abdominal infections, gynecologic infections, bacterial septicemia, bone and joint infections, skin and skin structure infections, endocarditis. antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1985-11-26 FDA
Click to view metopon Metopon is a morphinane alkaloid. Metopon was developed as an analgesic opium derivative. Metopon is listed under Schedule II of the US Controlled Substances Act 1970.
Click to view hydrocodone Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) agonist Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist Narcotic analgesic related to CODEINE, but more potent and more addicting by weight. It is used also as cough suppressant. Opioid Agonist (Code: N0000175690) Opioid Agonists (Code: N0000000174) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) mu-opioid receptor agonist (Code: CHEBI:55322) opioid analgesic (Code: CHEBI:35482) antitussive (Code: CHEBI:51177) Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689) 1943-03-23 FDA
Click to view codeine Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7885194) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7885194) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022402s010s011lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23835420) An opioid analgesic related to morphine but with less potent analgesic properties and mild sedative effects. It also acts centrally to suppress cough. Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) antitussive (Code: CHEBI:51177) opioid receptor agonist (Code: CHEBI:60606) prodrug (Code: CHEBI:50266) opioid analgesic (Code: CHEBI:35482) Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689) 1952-01-21 FDA
Click to view buphenine Adrenergic receptor alpha-1 (Organism: Homo sapiens, class: GPCR, accessions: P25100|P35348|P35368, gene: ADRA1A|ADRA1B|ADRA1D, swissprot: ADA1A_HUMAN|ADA1B_HUMAN|ADA1D_HUMAN A beta-adrenergic agonist. Nylidrin causes peripheral vasodilation, a positive inotropic effect, and increased gastric volume of gastric juice. It is used in the treatment of peripheral vascular disorders and premature labor. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Reproductive Control Agents (Code: D012102) Sympathomimetics (Code: D013566) Tocolytic Agents (Code: D015149) Vasodilator Agents (Code: D014665)
Click to view thiazinam Thiazinam is a first-generation phenothiazine H1-antihistamine. Thiazinam is an anti-cholinergic phenothiazine derivative, which also has antihistaminic properties. Thiazinamium was used the treatment of asthma since the early 1960s but currently withdrawn in most countries.
Click to view palmidrol Fatty-acid amide hydrolase 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P97612, gene: Faah, swissprot: FAAH1_RAT Cannabinoid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: P34972, gene: CNR2, swissprot: CNR2_HUMAN) Cannabinoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P21554, gene: CNR1, swissprot: CNR1_HUMAN) G-protein coupled receptor 55 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y2T6, gene: GPR55, swissprot: GPR55_HUMAN) agonist (Source: ) a cannabinoid receptor-inactive eCB-related molecule used as prophylactic in helping to prevent respiratory viral infection; structure Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) anti-inflammatory drug (Code: CHEBI:35472) antihypertensive agent (Code: CHEBI:35674) neuroprotective agent (Code: CHEBI:63726) anticonvulsant (Code: CHEBI:35623) Anti-Infective Agents (Code: D000890) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Antiviral Agents (Code: D000998) Cannabinoid Receptor Agonists (Code: D063386) Cannabinoid Receptor Modulators (Code: D063385) Central Nervous System Agents (Code: D002491) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view lanatoside C Lanatoside C (or isolanid) is a cardiac glycoside, a type of drug that can be used in the treatment of congestive heart failure and cardiac arrhythmia. 1967-07-11 Ministry of Health of the Russian Federation
Click to view traxanox - Antirheumatic Agents (Code: D018501) Diuretics (Code: D004232) Gout Suppressants (Code: D006074) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Natriuretic Agents (Code: D045283) Neurotransmitter Agents (Code: D018377) Renal Agents (Code: D012076) Uricosuric Agents (Code: D014528)
Click to view chlordiazepoxide GABA-A receptor alpha-2/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P28472|P18507, gene: GABRA2|GABRB3|GABRG2, swissprot: GBRA2_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15125950) GABA-A receptor alpha-3/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P34903|P28472|P18507, gene: GABRA3|GABRB3|GABRG2, swissprot: GBRA3_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15125950) GABA-A receptor alpha-5/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P31644|P28472|P18507, gene: GABRA5|GABRB3|GABRG2, swissprot: GBRA5_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15125950) GABA-A receptor alpha-1/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P28472|P18507, gene: GABRA1|GABRB3|GABRG2, swissprot: GBRA1_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15125950) Thyrotropin-releasing hormone receptor (Organism: Mus musculus, class: GPCR, accessions: P21761, gene: Trhr, swissprot: TRFR_MOUSE) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2175902) Chlordiazepoxide is a benzodiazepine which acts as depressants of the central nervous system, producing all levels of CNS depression from mild sedation to coma depending on the dose taken. Chlordiazepoxide acts on benzodiazepine allosteric sites that are part of the GABAA receptor/ion-channel complex and this results in an increased binding of the inhibitory neurotransmitter GABA to the GABAA receptor thereby producing inhibitory effects on the central nervous system and body similar to the effects of other benzodiazepines. Chlordiazepoxide is indicated for the management of anxiety disorders or for the short-term relief of symptoms of anxiety, withdrawal symptoms of acute alcoholism, and preoperative apprehension and anxiety. Also it (in combination with clidinium bromide) is indicated as adjunctive therapy in the treatment of peptic ulcer and in the treatment of the irritable bowel syndrome and acute entero-colitis, when these are associated with excessive anxiety and tension. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Adjuvants, Anesthesia (Code: D000759) Anti-Anxiety Agents (Code: D014151) anaesthesia adjuvant (Code: CHEBI:60807) sedative (Code: CHEBI:35717) anxiolytic drug (Code: CHEBI:35474) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1960-02-24 FDA
Click to view metoclopramide Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14635269) D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871571) Serotonin 3 (5-HT3) receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35563|Q9JJ16, gene: Htr3a|Htr3b, swissprot: 5HT3A_RAT|5HT3B_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871571) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14521403) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16248836) 5-hydroxytryptamine receptor 4 (Organism: Mus musculus, class: Unclassified, accessions: P97288, gene: Htr4, swissprot: 5HT4R_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8946946) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8818349) Muscarinic acetylcholine receptor M3 (Organism: Rattus norvegicus, class: GPCR, accessions: P08483, gene: Chrm3, swissprot: ACM3_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15105209) Metoclopramide is an oral prokinetic and antiemetic agent used in the therapy of gastroesophageal reflux disease, gastroparesis and severe or chemotherapy induced nausea. Dopamine D2 Antagonists (Code: N0000175799) Dopamine-2 Receptor Antagonist (Code: N0000175800) antiemetic (Code: CHEBI:50919) dopaminergic antagonist (Code: CHEBI:48561) gastrointestinal drug (Code: CHEBI:55324) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Dopamine D2 Receptor Antagonists (Code: D065127) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) 1979-02-07 FDA
Click to view tazobactam Beta-lactamase TEM (Organism: Escherichia coli, class: Enzyme, accessions: P62593, gene: bla; blaT-3; blaT-4;, swissprot: BLAT_ECOLX) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050684s094lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206829s009lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206829s009lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206829s009lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206829s009lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206829s009lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206829s009lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206829s009lbl.pdf) Tazobactam is a derivative of the penicillin nucleus and a penicillanic acid sulfone. Tazobactam is a beta-lactamase inhibitor of the Molecular class A enzymes. It varies in its ability to inhibit class II and IV (2a & 4) penicillinases. Tazobactam is used in combination with penicillin-class antibacterial for the treatment of intra-abdominal infections (caused by beta-lactamase producing isolates of E.coli, B. fragilis, B. ovatus, B. thetaiotaomicron, or B. vulgatus.), skin and skin structure infections (caused by beta-lactamase producing isolates of Staphylococcus aureus), female pelvic infections (caused by beta-lactamase producing isolates of E. coli), community-acquired pneumonia (caused by beta-lactamase producing isolates of H. influenzae) and nosocomial pneumonia (caused by beta-lactamase producing isolates of Staphylococcus aureus and by piperacillin/tazobactam-susceptible A. baumannii, H. influenzae, K. pneumoniae, and P. aeruginosa). It is also used in combination with ceftolozane for the treatment of complicated urinary tract infections, including pyelonephritis, hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia. beta Lactamase Inhibitor (Code: N0000175930) beta Lactamase Inhibitors (Code: N0000000202) antiinfective agent (Code: CHEBI:35441) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) beta-Lactamase Inhibitors (Code: D065093) Enzyme Inhibitors (Code: D004791) 1993-10-22 FDA
Click to view carbazochrome a hemostatic which increases capillary resistance & activates platelet factors, Note: Adona is a multimeaning tradename Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490)
Click to view azapropazone Xanthine dehydrogenase/oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P47989, gene: XDH, swissprot: XDH_HUMAN) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) An anti-inflammatory agent used in the treatment of rheumatoid arthritis. It also has uricosuric properties and has been used to treat gout. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) uricosuric drug (Code: CHEBI:35841) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Gout Suppressants (Code: D006074) Peripheral Nervous System Agents (Code: D018373) Renal Agents (Code: D012076) Sensory System Agents (Code: D018689) Uricosuric Agents (Code: D014528) 1972-01-01 YEAR INTRODUCED
Click to view testolactone Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: ) An antineoplastic agent that is a derivative of progesterone and used to treat advanced breast cancer. Aromatase Inhibitor (Code: N0000175563) Aromatase Inhibitors (Code: N0000175080) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) 1969-06-03 FDA
Click to view alitretinoin Retinoic acid receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P13631, gene: RARG, swissprot: RARG_HUMAN) agonist Retinoic acid receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10826, gene: RARB, swissprot: RARB_HUMAN) agonist Retinoic acid receptor RXR-gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P48443, gene: RXRG, swissprot: RXRG_HUMAN) agonist Retinoic acid receptor RXR-beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P28702, gene: RXRB, swissprot: RXRB_HUMAN) agonist Retinoic acid receptor RXR-alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P19793, gene: RXRA, swissprot: RXRA_HUMAN) agonist Retinoic acid receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10276, gene: RARA, swissprot: RARA_HUMAN) agonist Nuclear receptor ROR-gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P51449, gene: RORC, swissprot: RORG_HUMAN Retinoic acid receptor alpha (Organism: Mus musculus, class: Transcription factor, accessions: P11416, gene: Rara, swissprot: RARA_MOUSE Retinoic acid receptor RXR-gamma (Organism: Mus musculus, class: Transcription factor, accessions: P28705, gene: Rxrg, swissprot: RXRG_MOUSE Retinoic acid receptor RXR-beta (Organism: Mus musculus, class: Transcription factor, accessions: P28704, gene: Rxrb, swissprot: RXRB_MOUSE Retinoic acid receptor gamma (Organism: Mus musculus, class: Transcription factor, accessions: P18911, gene: Rarg, swissprot: RARG_MOUSE Retinoic acid receptor RXR-alpha (Organism: Mus musculus, class: Transcription factor, accessions: P28700, gene: Rxra, swissprot: RXRA_MOUSE Retinoic acid receptor RXR-alpha (Organism: Rattus norvegicus, class: Unclassified, accessions: Q05343, gene: Rxra, swissprot: RXRA_RAT Retinoic acid receptor beta (Organism: Mus musculus, class: Transcription factor, accessions: P22605, gene: Rarb, swissprot: RARB_MOUSE an RXR agonist Retinoid (Code: N0000175607) Retinoids (Code: N0000007700) antineoplastic agent (Code: CHEBI:35610) keratolytic drug (Code: CHEBI:50176) Antineoplastic Agents (Code: D000970) 1999-02-02 FDA 9CR
Click to view norvinisterone
Click to view norgesterone
Click to view tretinoin Retinoic acid receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P13631, gene: RARG, swissprot: RARG_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209353s000lbl.pdf) Retinoic acid receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10826, gene: RARB, swissprot: RARB_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209353s000lbl.pdf) Retinoic acid receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10276, gene: RARA, swissprot: RARA_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209353s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11093772) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11093772) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11093772) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11093772) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11093772) Cytochrome P450 3A7 (Organism: Homo sapiens, class: Enzyme, accessions: P24462, gene: CYP3A7, swissprot: CP3A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11093772) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11093772) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11093772) Cytochrome P450 4A11 (Organism: Homo sapiens, class: Enzyme, accessions: Q02928, gene: CYP4A11, swissprot: CP4AB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11093772) Cytochrome P450 2C18 (Organism: Homo sapiens, class: Enzyme, accessions: P33260, gene: CYP2C18, swissprot: CP2CI_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11093772) Indoleamine 2,3-dioxygenase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q8R0V5, gene: Ido2, swissprot: I23O2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Retinoic acid receptor RXR-alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P19793, gene: RXRA, swissprot: RXRA_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12482435) Retinoic acid receptor RXR-beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P28702, gene: RXRB, swissprot: RXRB_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12482435) Retinoic acid receptor RXR-gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P48443, gene: RXRG, swissprot: RXRG_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12482435) Nuclear receptor subfamily 2 group C member 2 (Organism: Homo sapiens, class: Unclassified, accessions: P49116, gene: NR2C2, swissprot: NR2C2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21068381) Tretinoin, also known as all-trans-retinoic acid (ATRA), is a naturally occurring derivative of vitamin A (retinol). Retinoids such as tretinoin are important regulators of cell reproduction, proliferation, and differentiation and are used to treat acne and photodamaged skin and to manage keratinization disorders such as ichthyosis and keratosis follicularis. Tretinoin also represents the class of anticancer drugs called differentiating agents and is used in the treatment of acute promyelocytic leukemia (APL). antineoplastic agent (Code: CHEBI:35610) keratolytic drug (Code: CHEBI:50176) anti-inflammatory agent (Code: CHEBI:67079) retinoic acid receptor agonist (Code: CHEBI:67198) Antineoplastic Agents (Code: D000970) Dermatologic Agents (Code: D003879) Keratolytic Agents (Code: D007641) Retinoid (Code: N0000175607) Retinoids (Code: N0000007700) 1971-10-20 FDA REA
Click to view metandienone Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9593936) Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/9593936) Metandienone is a synthetic steroid with anabolic properties that are more pronounced than its androgenic effects. Metandienone was discontinued and withdrawn in most countries since 1982. Anabolic Agents (Code: D045930) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1963-02-01 CDSCO (INDIA)
Click to view isotretinoin Retinoic acid receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10826, gene: RARB, swissprot: RARB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021951s014lbl.pdf) A topical dermatologic agent that is used in the treatment of acne vulgaris and several other skin diseases. Isotretinoin has teratogenic and other adverse effects. Retinoid (Code: N0000175607) Retinoids (Code: N0000007700) keratolytic drug (Code: CHEBI:50176) antineoplastic agent (Code: CHEBI:35610) Dermatologic Agents (Code: D003879) Noxae (Code: D009676) Teratogens (Code: D013723) 1982-05-07 FDA
Click to view etynodiol Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) A synthetic progestational hormone used alone or in combination with estrogens as an oral contraceptive. Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102) 1966-03-23 FDA
Click to view allylestrenol A synthetic steroid with progestational activity. Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Progestins (Code: D011372)
Click to view temazepam Nuclear receptor subfamily 1 group I member 3 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q14994, gene: NR1I3, swissprot: NR1I3_HUMAN) GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1981-02-27 FDA
Click to view clobazam Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202067s005,203993s007lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202067s005,203993s007lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202067s005,203993s007lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202067s005,203993s007lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202067s005,203993s007lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202067s005,203993s007lbl.pdf) Clobazam is a 1,5-benzodiazepine. Its exact mechanism of action is not fully understood but is thought to involve potentiation of GABAergic neurotransmission resulting from binding at the benzodiazepine site of the GABAA receptor. Clobazam is indicated for adjunctive treatment of seizures associated with Lennox-Gastaut syndrome. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) anticonvulsant (Code: CHEBI:35623) anxiolytic drug (Code: CHEBI:35474) GABA modulator (Code: CHEBI:50268) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 2011-10-21 FDA
Click to view etifoxine Etifoxine is a non-benzodiazepine anxiolytic with an anticonvulsant effect. Etifoxine appears to produce anxiolytic effects directly by binding to 2 or 3 subunits of the GABAA receptor complex. It also modulates GABAA receptors indirectly via stimulation of neurosteroid production after etifoxine binds to the 18 kDa translocator protein (TSPO) of the outer mitochondrial membrane in the central and peripheral nervous systems, previously known as the peripheral benzodiazepine receptor (PBR). Therefore, the effects of etifoxine are not completely reversed by the benzodiazepine antagonist flumazenil. Etifoxine is used for various emotional and bodily reactions followed by anxiety. Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1979-06-19 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view clomacran Clomacran is an acridan derivative. It was used as a neuroleptic in schizophrenia. It was withdrawn in 1982.
Click to view chlorcyclizine Chlorcyclizine is a first generation phenylpiperazine class antihistamine used to treat urticaria, rhinitis, pruritus, and other allergy symptoms. Chlorcyclizine also has some local anesthetic, anticholinergic, and antiserotonergic properties, and can be used as an antiemetic. Also it is used in combination with cinnarizine for the treatment of motion sickness. 1990-05-20 Ministry of Health, Welfare and Sport (Netherlands)
Click to view bromindione Bromindione is a potent long-acting anticoagulant. It is an inandione derivative. It is no longer available.
Click to view isobromindione Isobromindione is a member of indanones and a cyclic ketone. It was used as a uricosuric agent for the treatment of gout.
Click to view oxymorphone Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) agonist Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) agonist Opioid receptors; mu and delta (Organism: Mus musculus, class: GPCR, accessions: P32300|P42866, gene: Oprd1|Oprm1, swissprot: OPRD_MOUSE|OPRM_MOUSE Kappa-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P41144, gene: OPRK1, swissprot: OPRK_CAVPO Delta-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P32300, gene: Oprd1, swissprot: OPRD_MOUSE Mu-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P42866, gene: Oprm1, swissprot: OPRM_MOUSE Kappa-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P34975, gene: Oprk1, swissprot: OPRK_RAT Delta-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533, gene: Oprd1, swissprot: OPRD_RAT Mu-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33535, gene: Oprm1, swissprot: OPRM_RAT Mu-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P97266, gene: OPRM1, swissprot: OPRM_CAVPO Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist An opioid analgesic with actions and uses similar to those of MORPHINE, apart from an absence of cough suppressant activity. It is used in the treatment of moderate to severe pain, including pain in obstetrics. It may also be used as an adjunct to anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1092) Adjuvants, Anesthesia (Code: D000759) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) 1959-04-02 FDA
Click to view spaglumic acid Metabotropic glutamate receptor 3 (Organism: Rattus norvegicus, class: Unclassified, accessions: P31422, gene: Grm3, swissprot: GRM3_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10884552) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16627568) Spaglumic acid is the beta-aspartyl isoform of N-Acetyl-l-aspartylglutamate (isospaglumic Acid is N-(N-Acetyl-l-alpha-aspartyl)-l-glutamic acid). In eye drops, spaglumic acid is either a magnesium or sodium salt of N-Acetyl-l-aspartylglutamate. Spaglumic acid is a mast cell stabilizer. Thus it is used in allergic conditions such as allergic conjunctivitis. 1991-12-12 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view isoxsuprine A beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Reproductive Control Agents (Code: D012102) Sympathomimetics (Code: D013566) Tocolytic Agents (Code: D015149) Vasodilator Agents (Code: D014665) FDA
Click to view dobutamine Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020201s036lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020201s036lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6270308) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6270308) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6270308) Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11907189) Dobutamine is a sympathomimetic drug. Dobutamine is a direct-acting inotropic agent whose primary activity results from stimulation of the ?-receptors of the heart while producing comparatively mild chronotropic, hypertensive, arrhythmogenic, and vasodilative effects. It does not cause the release of endogenous norepinephrine, as does dopamine. Dobutamine directly stimulates beta-1 receptors of the heart to increase myocardial contractility and stroke volume, resulting in increased cardiac output. Levdobutamine is the active (S)-isomer with positive ionotropic activity. Dobutamine is indicated when parenteral therapy is necessary for inotropic support in the short-term treatment of adults with cardiac decompensation due to depressed contractility resulting either from organic heart disease or from cardiac surgical procedures. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-1 Receptor Agonists (Code: D058665) Adrenergic beta-Agonists (Code: D000318) cardiotonic drug (Code: CHEBI:38147) sympathomimetic agent (Code: CHEBI:35524) beta-adrenergic agonist (Code: CHEBI:35522) Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sympathomimetics (Code: D013566) 1978-07-18 FDA Y00
Click to view dihydrocodeine Dihydrocodeine: Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9431830) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9431830) Dihydromorphine: Mu-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33535, gene: Oprm1, swissprot: OPRM_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3007760) Delta-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533, gene: Oprd1, swissprot: OPRD_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3007760) Kappa-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P34975, gene: Oprk1, swissprot: OPRK_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3007760) Dihydrocodeine is an opioid analgesic. Dihydrocodeine is metabolized to dihydromorphine - a highly active metabolite with a high affinity for mu opioid receptors. Dihydrocodeine is used for the treatment of moderate to severe pain, including post-operative and dental pain. It can also be used to treat chronic pain, breathlessness and coughing. Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1958-07-07 FDA
Click to view tegaserod 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) 5-hydroxytryptamine receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q13639, gene: HTR4, swissprot: 5HT4R_HUMAN) partial agonist (Source: ) 5-hydroxytryptamine receptor 4 (Organism: Cavia porcellus, class: GPCR, accessions: O70528, gene: HTR4, swissprot: 5HT4R_CAVPO) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source Serotonin 4 Receptor Antagonists (Code: N0000175816) Serotonin-4 Receptor Antagonist (Code: N0000175815) serotonergic agonist (Code: CHEBI:35941) gastrointestinal drug (Code: CHEBI:55324) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) 2002-07-24 FDA
Click to view trihexyphenidyl Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1994002) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1994002) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1994002) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1994002) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1994002) Trihexyphenidyl is an anticholinergic, a selective M1 muscarinic acetylcholine receptor antagonist used in the symptomatic treatment of parkinsonism and drug induced extrapyramidal reactions. Trihexyphenidyl possesses both anticholinergic and antihistaminic effects. Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) 1949-05-13 FDA
Click to view bisulepine Bisulepine is a H1-antihistaminic agent. It has hypnotic, antiadrenergic and selective anticholinergic, antihistamine and antiserotonergic effects. It is used for the treatment of symptoms of type I hypersensitivity, acute allergic conditions, allergic rhinitis, bronchial asthma, urticaria, Quincke's edema, atopic dermatitis. 1973-02-05 State Institute for Drug Control (SUKL) Czech Republic
Click to view benoxaprofen Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) Benoxaprofen is a monocarboxylic acid that is propionic acid substituted at position 2 by a 2-(4-chlorophenyl)-1,3-benzoxazol-5-yl group. It was used as a non-steroidal anti-inflammatory drug until 1982 when it was withdrawn from the market due to adverse side-effects including liver necrosis, photosensitivity, and carcinogenicity in animals. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antipyretic (Code: CHEBI:35493) non-narcotic analgesic (Code: CHEBI:35481) antipsoriatic (Code: CHEBI:50748) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Dermatologic Agents (Code: D003879) Enzyme Inhibitors (Code: D004791) Lipoxygenase Inhibitors (Code: D016859) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1982-04-19 FDA
Click to view eritrityl tetranitrate Erythrityl Tetranitrate is a vasodilator with general properties similar to nitroglycerin. Similar to other nitrites and organic nitrates, erythrityl tetranitrate is converted to an active intermediate compound which activates the enzyme guanylate cyclase. This stimulates the synthesis of cyclic guanosine 3', 5'-monophosphate (cGMP) which then activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells, eventually resulting in the dephosphorylation of the myosin light chain of the smooth muscle fiber. The subsequent release of calcium ions results in the relaxation of the smooth muscle cells and vasodilation. Erythrityl Tetranitrate is indicated for the prevention of angina. vasodilator agent (Code: CHEBI:35620) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view quercetin A flavonol widely distributed in plants. It is an antioxidant, like many other phenolic heterocyclic compounds. Glycosylated forms include RUTIN and quercetrin. antineoplastic agent (Code: CHEBI:35610) Antioxidants (Code: D000975) Protective Agents (Code: D020011) QUE
Click to view olsalazine Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN) inhibitor (Source: ) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: ) Cyclooxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P23219|P35354, gene: PTGS1|PTGS2, swissprot: PGH1_HUMAN|PGH2_HUMAN) inhibitor (Source: ) cpd with 2 salicylate molecules linked together by an azo bond Aminosalicylate (Code: N0000175781) Aminosalicylic Acids (Code: N0000005760) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) prodrug (Code: CHEBI:50266) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1990-07-31 FDA
Click to view hesperetin Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) Glycogen synthase kinase-3 beta (Organism: Homo sapiens, class: Kinase, accessions: P49841, gene: GSK3B, swissprot: GSK3B_HUMAN) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) aglycone of HESPERIDIN; structure antineoplastic agent (Code: CHEBI:35610) 6JP
Click to view terizidone Terizidone is a Schiff base consisting of 2 D-cycloserine molecules and 1 molecule of terephthalaldehyde. Terizidone is a prodrug, which hydrolyzes after oral intake into cycloserine. The mechanism of action of cycloserine is based on the breakdown of the bacterial cell wall synthesis through inhibition of the alanine-racemase and D-alanyl-D-alanine-synthetase. This is competitive inhibition. 1981-06-01 CDSCO (INDIA)
Click to view florantyrone
Click to view masoprocol Arachidonate 5-lipoxygenase (Organism: Mus musculus, class: Enzyme, accessions: P48999, gene: Alox5, swissprot: LOX5_MOUSE Arachidonate 15-lipoxygenase (Organism: Oryctolagus cuniculus, class: Enzyme, accessions: P12530, gene: ALOX15, swissprot: LOX15_RABIT Arachidonate 5-lipoxygenase (Organism: Rattus norvegicus, class: Enzyme, accessions: P12527, gene: Alox5, swissprot: LOX5_RAT Seed linoleate 13S-lipoxygenase-1 (Organism: Glycine max, class: Enzyme, accessions: P08170, gene: LOX1.1, swissprot: LOX1_SOYBN Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN Arachidonate 15-lipoxygenase, type II (Organism: Homo sapiens, class: Enzyme, accessions: O15296, gene: ALOX15B, swissprot: LX15B_HUMAN Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN 5-lipoxygenase (Organism: Bos taurus, class: Enzyme, accessions: Q9BEG3, gene: None, swissprot: Q9BEG3_BOVIN Arachidonate 12-lipoxygenase, 12S-type (Organism: Homo sapiens, class: Enzyme, accessions: P18054, gene: ALOX12, swissprot: LOX12_HUMAN Arachidonate 15-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P16050, gene: ALOX15, swissprot: LOX15_HUMAN Cyclooxygenase (Organism: Bos taurus, class: Enzyme, accessions: O62664|O62698, gene: PTGS1|PTGS2, swissprot: PGH1_BOVIN|PGH2_BOVIN Prostaglandin G/H synthase 1 (Organism: Bos taurus, class: Enzyme, accessions: O62664, gene: PTGS1, swissprot: PGH1_BOVIN Insulin-like growth factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P08069, gene: IGF1R, swissprot: IGF1R_HUMAN Leukotriene B4 receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q15722, gene: LTB4R, swissprot: LT4R1_HUMAN Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN Transthyretin (Organism: Homo sapiens, class: Secreted, accessions: P02766, gene: TTR, swissprot: TTHY_HUMAN Cytoplasmic zinc-finger protein (Organism: Caenorhabditis elegans, class: Unclassified, accessions: G5EF15, gene: pos-1, swissprot: G5EF15_CAEEL Lipoxygenase (Organism: Glycine max, class: Unclassified, accessions: Q39829, gene: None, swissprot: Q39829_SOYBN Zinc finger protein mex-5 (Organism: Caenorhabditis elegans, class: Cytosolic other, accessions: Q9XUB2, gene: mex-5, swissprot: MEX5_CAEEL A potent lipoxygenase inhibitor that interferes with arachidonic acid metabolism. The compound also inhibits formyltetrahydrofolate synthetase, carboxylesterase, and cyclooxygenase to a lesser extent. It also serves as an antioxidant in fats and oils. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) antineoplastic agent (Code: CHEBI:35610) hypoglycemic agent (Code: CHEBI:35526) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antioxidants (Code: D000975) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Lipoxygenase Inhibitors (Code: D016859) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sensory System Agents (Code: D018689) 1992-09-04 FDA
Click to view aminopropylone Aminopropylone is a nonsteroidal anti-inflammatory drug. It was used in topical preparations, for the local treatment of pain and inflammatory conditions. It is no longer available. 1976-10-16 Italian Medicines Agency (AIFA)
Click to view formestane Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/16190763/) Formestane is a type I, steroidal, selective aromatase inhibitor. It inhibits the aromatase enzyme responsible for converting androgens to estrogens, thereby preventing estrogen production. Estrogen-sensitive breast cancer cells depend on estrogen for viability. Formestane was the first selective aromatase inhibitor to be developed as a prescription drug. It was used in the treatment of estrogen receptor-positive breast cancer in postmenopausal women. With the emergence of newer and more effective aromatase inhibitors, however, formestane soon lost market presence at a rapid rate. antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Aromatase Inhibitors (Code: D047072) Enzyme Inhibitors (Code: D004791) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Steroid Synthesis Inhibitors (Code: D065088) 1993-01-01 YEAR INTRODUCED
Click to view formylsulfamethin Formylsulfamethin is a sulfonamide.
Click to view epimestrol A synthetic steroid with estrogenic activity. Estrogens (Code: D004967) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view emedastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/20706slr011_emadine_lbl.pdf) Emedastine is a relatively selective, histamine H1 antagonist. Emedastine appears to be devoid of effects on adrenergic, dopaminergic and serotonin receptors. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. Emedastine is indicated for the temporary relief of the signs and symptoms of allergic conjunctivitis. Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Inhibitor (Code: N0000175519) Anti-Allergic Agents (Code: D018926) H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) antipruritic drug (Code: CHEBI:59683) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1997-12-29 FDA
Click to view neticonazole Neticonazole is an antifungal drug. It is especially active against Candida glabrata, Trichophyton, Microsporum, Aspergillus and Fonsecaea spp. Neticonazole is used for the treatment of mycoses like trichophytosis, candidiasis, and different types of tinea. 1993-09-01 PMDA
Click to view oxendolone
Click to view methyltestosterone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist (Source: ) A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL). Anabolic Agents (Code: D045930) antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Androgen (Code: N0000175824) Androgen Receptor Agonists (Code: N0000000146) Androstanes (Code: N0000008241) 1973-12-03 FDA
Click to view butamirate Butamirate is centrally acting cough suppressant which is neither chemically nor pharmacologically related to opium alkaloids. Butamirate is used for the symptomatic treatment of non-productive (dry) cough. In addition to its antitussive effect, Butamirate also decreases the airway resistance. Butamirate is rapidly and fully hydrolysed mainly into 2-phenylbutyric acid and diethylaminoetoxyethanol. In experiments on different animal species, the two major metabolites have been shown to exhibit also a cough-soothing effect. 1996-11-11 Hungary National Institute of Pharmacy and Nutrition
Click to view eicosapentaenoic acid Oxoeicosanoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDS5, gene: OXER1, swissprot: OXER1_HUMAN Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN Prostaglandin G/H synthase 2 (Organism: Ovis aries, class: Enzyme, accessions: P79208, gene: PTGS2, swissprot: PGH2_SHEEP Peroxisome proliferator-activated receptor delta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q03181, gene: PPARD, swissprot: PPARD_HUMAN Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN Tissue factor (Organism: Homo sapiens, class: Membrane receptor, accessions: P13726, gene: F3, swissprot: TF_HUMAN Prostaglandin G/H synthase 1 (Organism: Bos taurus, class: Enzyme, accessions: O62664, gene: PTGS1, swissprot: PGH1_BOVIN Important polyunsaturated fatty acid found in fish oils. It serves as the precursor for the prostaglandin-3 and thromboxane-3 families. A diet rich in eicosapentaenoic acid lowers serum lipid concentration, reduces incidence of cardiovascular disorders, prevents platelet aggregation, and inhibits arachidonic acid conversion into the thromboxane-2 and prostaglandin-2 families. FDA EPA
Click to view norethandrolone A synthetic hormone with anabolic and androgenic properties and moderate progestational activity. Anabolic Agents (Code: D045930) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view methenolone A synthetic steroid that has been used for its anabolic action. Anabolic Agents (Code: D045930) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view tricyclamol chloride
Click to view fludiazepam Fludiazepam is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is used in the short-term treatment of anxiety disorders. Anti-Anxiety Agents (Code: D014151) anxiolytic drug (Code: CHEBI:35474) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1981-01-05 PMDA
Click to view broxyquinoline Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Broxyquinoline is a oxyquinoline derivative. It was used as an intestinal antiseptics in combination with broxaldine. This combination was thought to be the cause of neurological symptoms.
Click to view ethacrynic acid Glutathione S-transferase P (Organism: Homo sapiens, class: Enzyme, accessions: P09211, gene: GSTP1, swissprot: GSTP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16675217) Glutathione S-transferase A1 (Organism: Homo sapiens, class: Enzyme, accessions: P08263, gene: GSTA1, swissprot: GSTA1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16675217) UDP-glucose 4-epimerase (Organism: Homo sapiens, class: Enzyme, accessions: Q14376, gene: GALE, swissprot: GALE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16962325) Ethacrynic acid is an unsaturated ketone derivative of an aryloxyacetic acid. Ethacrynic acid inhibits symport of sodium, potassium, and chloride primarily in the ascending limb of Henle, but also in the proximal and distal tubules. This pharmacological action results in excretion of these ions, increased urinary output, and reduction in extracellular fluid. Ethacrynic acid is indicated for treatment of edema associated with congestive heart failure, cirrhosis of the liver, and renal disease, including the nephrotic syndrome, for the short-term management of ascites due to malignancy, idiopathic edema, and lymphedema, for the short-term management of hospitalized pediatric patients (other than infants) with congenital heart disease or the nephrotic syndrome and for rapid onset of diuresis is desired, e.g., in acute pulmonary edema, or when gastrointestinal absorption is impaired or oral medication is not practicable. Increased Diuresis at Loop of Henle (Code: N0000175366) loop diuretic (Code: CHEBI:77608) Diuretics (Code: D004232) Enzyme Inhibitors (Code: D004791) Natriuretic Agents (Code: D045283) 1967-01-10 FDA EAA
Click to view narcobarbital Narcobarbital is a member of barbiturates. It was used as an anesthetic agent in gynecological surgery and electroconvulsive treatment. It was withdrawn from the market.
Click to view Iofetamine (123I) lofetamine (123I) is the N-isopropyl derivative of amphetamine with iodine 123(I123) at the para position to serve as the tracer. Iofetamine is rapidly taken up by the lungs, then redistributed principally to the liver and brain. The precise mechanism of localization has not been determined, but is believed to result from nonspecific receptor binding. Iofetamine is indicated as a radiopharmaceutical for cerebral perfusion imaging. It was used as a diagnostic aid in determining the localization of and in the evaluation of non-lacunar stroke and complex partial seizures, as well as in the early diagnosis of Alzheimer's disease in 1987. However it was discontinued in USA. 1987-12-24 FDA
Click to view flumazenil GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47869|P34903|P48169|P31644|Q16445|P18505|P47870|P28472|O14764|P78334|Q8N1C3|P18507|Q99928|O00591|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18973287) Flumazenil, an imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system. Flumazenil competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex. Flumazenil is a weak partial agonist in some animal models of activity, but has little or no agonist activity in man. In animals pretreated with high doses of benzodiazepines over several weeks, Flumazenil elicited symptoms of benzodiazepine withdrawal, including seizures. A similar effect was seen in adult human subjects. Flumazenil is used for the complete or partial reversal of the sedative effects of benzodiazepines in cases where general anesthesia has been induced and/or maintained with benzodiazepines, where sedation has been produced with benzodiazepines for diagnostic and therapeutic procedures, and for the management of benzodiazepine overdose. Benzodiazepine Antagonist (Code: N0000175680) GABA antagonist (Code: CHEBI:65259) antidote to benzodiazepine poisoning (Code: CHEBI:90757) Antidotes (Code: D000931) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1991-12-20 FDA FYP
Click to view pipemidic acid Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26936044) Pipemidic Acid is a pyridopyrimidine antibiotic derivative of piromidic acid with activity against gram-negative bacteria, as well as some gram-positive bacteria. It’s used in the treatment of urinary tract infections, recidive cystitis, prolongation of the therapy of pyelonephritis (prolonged therapy at patients with tendency to recidives). antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076) 1981-08-01 PMDA
Click to view scopolamine Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist Muscarinic acetylcholine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08482|P08483|P08485|P08911|P10980, gene: Chrm1|Chrm2|Chrm3|Chrm4|Chrm5, swissprot: ACM1_RAT|ACM2_RAT|ACM3_RAT|ACM4_RAT|ACM5_RAT Muscarinic receptor M1 (Organism: Bos taurus, class: GPCR, accessions: Q8WMX0, gene: None, swissprot: Q8WMX0_BOVIN Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT Muscarinic acetylcholine receptor M3 (Organism: Rattus norvegicus, class: GPCR, accessions: P08483, gene: Chrm3, swissprot: ACM3_RAT Muscarinic acetylcholine receptor M2 (Organism: Rattus norvegicus, class: GPCR, accessions: P10980, gene: Chrm2, swissprot: ACM2_RAT Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) An alkaloid from SOLANACEAE, especially DATURA and SCOPOLIA. Scopolamine and its quaternary derivatives act as antimuscarinics like ATROPINE, but may have more central nervous system effects. Among the many uses are as an anesthetic premedication, in URINARY INCONTINENCE, in MOTION SICKNESS, as an antispasmodic, and as a mydriatic and cycloplegic. Anticholinergic (Code: N0000175574) Adjuvants, Anesthesia (Code: D000759) anaesthesia adjuvant (Code: CHEBI:60807) antispasmodic drug (Code: CHEBI:53784) mydriatic agent (Code: CHEBI:50513) adjuvant (Code: CHEBI:60809) antidepressant (Code: CHEBI:35469) antiemetic (Code: CHEBI:50919) muscarinic antagonist (Code: CHEBI:48876) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Mydriatics (Code: D009184) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) 1979-12-31 FDA
Click to view fenoterol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14730417) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14730417) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14730417) Fenoterol is a short-acting sympathomimetic agent with bronchodilator activity. Fenoterol stimulates beta-2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP concentrations relax bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. Fenoterol is used for the treatment of asthma. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) bronchodilator agent (Code: CHEBI:35523) sympathomimetic agent (Code: CHEBI:35524) beta-adrenergic agonist (Code: CHEBI:35522) tocolytic agent (Code: CHEBI:66993) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Reproductive Control Agents (Code: D012102) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566) Tocolytic Agents (Code: D015149) 1965-01-01 YEAR INTRODUCED
Click to view cocaine Serotonin 3 receptor (5HT3) (Organism: Homo sapiens, class: Ion channel, accessions: O95264|P46098, gene: HTR3A|HTR3B, swissprot: 5HT3A_HUMAN|5HT3B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11489465) Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15566309) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14592523) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15351386 Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15351386) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9876137) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15351386) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3047364) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17470523) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9812985) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12873512) An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) adrenergic uptake inhibitor (Code: CHEBI:35640) dopamine uptake inhibitor (Code: CHEBI:51039) serotonin uptake inhibitor (Code: CHEBI:50949) vasoconstrictor agent (Code: CHEBI:50514) local anaesthetic (Code: CHEBI:36333) central nervous system stimulant (Code: CHEBI:35337) sympathomimetic agent (Code: CHEBI:35524) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Vasoconstrictor Agents (Code: D014662) 1860-01-01 YEAR INTRODUCED COC
Click to view vildagliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/jalra-epar-product-information_en.pdf) Dipeptidyl peptidase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q6V1X1, gene: DPP8, swissprot: DPP8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16392822) Dipeptidyl peptidase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q86TI2, gene: DPP9, swissprot: DPP9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17034148) Prolyl endopeptidase FAP (Organism: Homo sapiens, class: Enzyme, accessions: Q12884, gene: FAP, swissprot: SEPR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25164763) Vildagliptin, a member of the islet enhancer class, is a potent and selective DPP-4 inhibitor. The administration of vildagliptin results in a rapid and complete inhibition of DPP-4 activity, resulting in increased fasting and postprandial endogenous levels of the incretin hormones GLP-1 (glucagon-like peptide 1) and GIP (glucose-dependent insulinotropic polypeptide). Vildagliptin is indicated in the treatment of type 2 diabetes mellitus in adults. Dipeptidyl-Peptidase IV Inhibitors (Code: D054873) Enzyme Inhibitors (Code: D004791) Hypoglycemic Agents (Code: D007004) Protease Inhibitors (Code: D011480) 2007-09-26 EMA Bound
Click to view piroheptine
Click to view clofarabine Clofarabine is sequentially metabolized intracellularly to the 5’-monophosphate metabolite by deoxycytidine kinase and mono- and di-phospho-kinases to the active 5’-triphosphate metabolite. Clofarabine inhibits DNA synthesis by decreasing cellular deoxynucleotide triphosphate pools through an inhibitory action on ribonucleotide reductase, and by terminating DNA chain elongation and inhibiting repair through incorporation into the DNA chain by competitive inhibition of DNA polymerases. The affinity of clofarabine triphosphate for these enzymes is similar to or greater than that of deoxyadenosine triphosphate. In preclinical models, clofarabine has demonstrated the ability to inhibit DNA repair by incorporation into the DNA chain during the repair process. Clofarabine 5’-triphosphate also disrupts the integrity of mitochondrial membrane, leading to the release of the pro-apoptotic mitochondrial proteins, cytochrome C and apoptosis-inducing factor, leading to programmed cell death. Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) antineoplastic agent (Code: CHEBI:35610) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Noxae (Code: D009676) 2004-12-28 FDA CFB
Click to view phenoxybenzamine Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: ) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901|P19020|P25115|P30729|P61169, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_RAT|DRD2_RAT|DRD3_RAT|DRD4_RAT|DRD5_RAT Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist An alpha-adrenergic antagonist with long duration of action. It has been used to treat hypertension and as a peripheral vasodilator. alpha-Adrenergic Blocker (Code: N0000175553) Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) 1953-01-26 FDA
Click to view chlorphenoxamine minor descriptor (66-84); on-line & Index Medicus search ETHYLAMINES (66-84); RN given refers to parent cpd Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377)
Click to view chlorambucil DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) alkylating agent (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/010669s030lbl.pdf) Glutathione S-transferase P (Organism: Homo sapiens, class: Enzyme, accessions: P09211, gene: GSTP1, swissprot: GSTP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18511072) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25618019) Chlorambucil is an orally-active antineoplastic aromatic nitrogen mustard. Chlorambucil is extensively metabolized in the liver primarily to phenylacetic acid mustard, which has antineoplastic activity. Chlorambucil acts as alkylating agent wgich alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis. Chlorambucil is used for the treatment of chronic lymphatic (lymphocytic) leukemia, malignant lymphomas including lymphosarcoma, giant follicular lymphoma, and Hodgkin’s disease. Alkylating Agents (Code: D000477) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) 1957-03-18 FDA CBL
Click to view flupirtine Potassium voltage-gated channel subfamily KQT member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O43526, gene: KCNQ2, swissprot: KCNQ2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/14736843) Flupirtine is a triaminopyridine derivative and a centrally acting, non-opioid analgesic. Flupirtine is the first representative of a pharmacological class denoted the 'selective neuronal potassium channel openers'. The generation of the M-current is facilitated by flupirtine via the opening of neuronal Kv7 potassium channels. The opening of these channels inhibits exaggerated neuronal action potential generation and controls neuronal excitability. It is used for the treatment of a variety of pain states. Analgesics (Code: D000700) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1986-01-01 YEAR INTRODUCED
Click to view xyloylsulfamine Xyloylsulfamine is a sulfonamide.
Click to view tilisolol Tilisolol is a non-selective beta-adrenergic blocking agent. It was used for the treatment of hypertension and angina pectoris. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377)
Click to view quinupramine
Click to view mesterolone Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN 17 beta-Hydroxy-1 alpha-methyl-5 alpha-androstan-3-one. A synthetic steroid with anabolic and androgenic activities. Anabolic Agents (Code: D045930) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view mestanolone Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist (Source: http://www.kegg.jp/entry/D01533) non-virilizing androgenic steroid; RN given refers to (5alpha,17beta)-isomer; structure
Click to view methandriol A synthetic steroid with anabolic and androgenic properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1188) Anabolic Agents (Code: D045930) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view cetylpyridinium Cetylpyridinium is a quaternary ammonium with broad-spectrum antiseptic properties. It is suggested that interaction with bacteria occurs by the disruption of membrane function, leakage of cytoplasmic material, and ultimately the collapse of the intra-cellular equilibrium. Its salt form, cetylpyridinium chloride, is typically found as an active ingredient in mouthwashes, toothpastes, lozenges, throat sprays, breath sprays, and nasal sprays. In these products, it generally mediates an antiseptic activity and protective action against dental plaque and reducing gingivitis. antiseptic drug (Code: CHEBI:48218) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Detergents (Code: D003902) Surface-Active Agents (Code: D013501) FDA
Click to view clobuzarit Clobuzarit is a methylpropionic acid derivative. Clobuzarit was developed for the treatment of atherosclerosis. It was later found to possess antirheumatic and weak anti-inflammatory properties and was evaluated as a disease-modifying antirheumatic drug. It was withdrawn because of several reports of Stevens-Johnson syndrome.
Click to view chlorfenethazine Intercellular adhesion molecule 1 (Organism: Homo sapiens, class: Unclassified protein, accessions: P05362, gene: ICAM1, swissprot: ICAM1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11052808) Chlorfenethazine is a member of phenothiazines. It was used for the treatment of insomnia, anxiety and as a premedication.
Click to view acediasulfone Acediasulfone is a long-acting prodrug of dapsone. It was used in the treatment of leprosy. (See: dapsone)
Click to view dichlorphenamide Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/011366s033lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/011366s033lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/011366s033lbl.pdf) Carbonic anhydrase (Organism: Helicobacter pylori (strain ATCC 700392 / 26695), class: Enzyme, accessions: O24855, gene: cynT, swissprot: CYNT_HELPY) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Enzyme, accessions: P40881, gene: None, swissprot: CAH_METTE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase 13 (Organism: Homo sapiens, class: Enzyme, accessions: Q8N1Q1, gene: CA13, swissprot: CAH13_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21620713) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Delta carbonic anhydrase (Organism: Thalassiosira weissflogii, class: Unclassified, accessions: Q5U9J1, gene: ca1, swissprot: Q5U9J1_THAWE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24314394) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19193158) Dichlorphenamide is a carbonic anhydrase inhibitor. However, the precise mechanism by which dichlorphenamide exerts its therapeutic effects in patients with primary periodic paralysis is unknown. Dichlorphenamide is indicated for the treatment of primary hyperkalemic periodic paralysis, primary hypokalemic periodic paralysis, and related variants. Carbonic Anhydrase Inhibitor (Code: N0000175517) Sulfonamides (Code: N0000008048) antiglaucoma drug (Code: CHEBI:39456) ophthalmology drug (Code: CHEBI:66981) Carbonic Anhydrase Inhibitors (Code: D002257) Enzyme Inhibitors (Code: D004791) 1958-07-22 FDA I7A
Click to view delorazepam Delorazepam is a benzodiazepine with anxiolytic effects. It is a metabolite of diclazepam. Delorazepam possesses anxiolytic, skeletal muscle relaxant, hypnotic and anticonvulsant properties. It may have adverse effects such as drowsiness, and cognitive impairments such as short term memory impairment. It is indicated for the treatment of anxiety, tension and other somatic or psychiatric manifestations associated with anxiety syndrome, insomnia. Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 2005-03-01 Italian Medicines Agency (AIFA)
Click to view mannomustine Nitrogen mustard derivative alkylating agent used as antineoplastic. It causes severe bone marrow depression and is a powerful vesicant. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676)
Click to view melphalan DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) cross-linking agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/207155s000lbl.pdf) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Enzyme, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19190342) Melphalan is the active L-isomer of the compound, the D-isomer, known as medphalan, is less active against certain animal tumors, and the dose needed to produce effects on chromosomes is larger than that required with the L-isomer. The racemic (DL–) form is known as merphalan or sarcolysin. Sarcolysin is a phenylalanine mustard derivative. Melphalan is an alkylating agent of the bischloroethylamine type. As a result, its cytotoxicity appears to be related to the extent of its interstrand cross-linking with DNA, probably by binding at the N7 position of guanine. Like other bifunctional alkylating agents, it is active against both resting and rapidly dividing tumor cells. Melphalan is indicated for the palliative treatment of multiple myeloma and for the palliation of non-resectable epithelial carcinoma of the ovary. Alkylating Agents (Code: D000477) drug allergen (Code: CHEBI:88188) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Myeloablative Agonists (Code: D019653) Noxae (Code: D009676) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) 1964-01-17 FDA
Click to view vorinostat Histone deacetylase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBN7, gene: HDAC6, swissprot: HDAC6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021991s009lbl.pdf) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021991s009lbl.pdf) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021991s009lbl.pdf) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021991s009lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021991s009lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021991s009lbl.pdf) Histone deacetylase 11 (Organism: Homo sapiens, class: Enzyme, accessions: Q96DB2, gene: HDAC11, swissprot: HDA11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23252603) Histone deacetylase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BY41, gene: HDAC8, swissprot: HDAC8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23252603) Histone deacetylase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P56524, gene: HDAC4, swissprot: HDAC4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23252603) Histone deacetylase 5 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UQL6, gene: HDAC5, swissprot: HDAC5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23252603) Histone deacetylase 10 (Organism: Homo sapiens, class: Enzyme, accessions: Q969S8, gene: HDAC10, swissprot: HDA10_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26331334) Histone deacetylase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UKV0, gene: HDAC9, swissprot: HDAC9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26331334) Histone deacetylase 7 (Organism: Homo sapiens, class: Enzyme, accessions: Q8WUI4, gene: HDAC7, swissprot: HDAC7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26331334) Lysine-specific demethylase 4E (Organism: Homo sapiens, class: Enzyme, accessions: B2RXH2, gene: KDM4E, swissprot: KDM4E_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21596573) Vorinostat is a dicarboxylic acid diamide comprising suberic (octanedioic) acid coupled to aniline and hydroxylamine. Vorinostat is a histone deacetylase inhibitor. Vorinostat inhibits the enzymatic activity of histone deacetylases HDAC1, HDAC2 and HDAC3 (Class I) and HDAC6 (Class II) at nanomolar concentrations (IC50<86 nM). Vorinostat is indicated for the treatment of cutaneous manifestations in patients with cutaneous T-cell lymphoma (CTCL) who have progressive, persistent or recurrent disease on or following two systemic therapies. Histone Deacetylase Inhibitor (Code: N0000175588) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Histone Deacetylase Inhibitors (Code: D056572) antineoplastic agent (Code: CHEBI:35610) 2006-10-06 FDA SHH
Click to view entacapone Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020796s026lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11038168) Entacapone is an inhibitor of catechol-O-methyltransferase (COMT). When entacapone is given in conjunction with levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of levodopa are greater and more sustained than after administration of levodopa and an aromatic amino acid decarboxylase inhibitor alone. It is believed that at a given frequency of levodopa administration, these more sustained plasma levels of levodopa result in more constant dopaminergic stimulation in the brain, leading to greater effects on the signs and symptoms of Parkinson’s disease. It is used in the treatment of Parkinson’s disease as an adjunct to levodopa and carbidopa therapy. Catechol-O-Methyltransferase Inhibitor (Code: N0000175757) central nervous system drug (Code: CHEBI:35470) antidyskinesia agent (Code: CHEBI:66956) antiparkinson drug (Code: CHEBI:48407) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Catechol O-Methyltransferase Inhibitors (Code: D065098) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) 1999-10-19 FDA PD9
Click to view zaleplon GABA-A receptor alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P14867, gene: GABRA1, swissprot: GBRA1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12404558) a benzodiazepine receptor agonist and hypnotic that is used as a sleeping pill. gamma-Aminobutyric Acid A Receptor Agonist (Code: N0000183360) GABA A Agonists (Code: N0000000196) Central Nervous System Depression (Code: N0000175728) anticonvulsant (Code: CHEBI:35623) central nervous system depressant (Code: CHEBI:35488) sedative (Code: CHEBI:35717) anxiolytic drug (Code: CHEBI:35474) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) 1999-08-13 FDA
Click to view cetraxate broad spectrum peptide hydrolase inhibitor; RN given refers to (trans)-isomer; structure Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765)
Click to view bucumolol Bucumolol is a specific beta-adrenergic blocking agent with a greater potency and a less cardiac depression than propranolol. Itis indicated for the treatment of myocardial ischemia and hypertension. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) beta-adrenergic antagonist (Code: CHEBI:35530) anti-arrhythmia drug (Code: CHEBI:38070) Neurotransmitter Agents (Code: D018377) PMDA
Click to view atropine oxyde Atropine oxyde is an alkaloid of the belladonna plants. It is the major metabolite of atropine. It is a competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors. Atropine oxyde was used for the symptomatic treatment of pain related to functional disorders of gastrointestinal tract. 1995-05-15 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view capsaicin Transient receptor potential cation channel subfamily V member 1 (Organism: Mus musculus, class: Unclassified, accessions: Q704Y3, gene: Trpv1, swissprot: TRPV1_MOUSE) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022395lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00012269.PDF) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00012269.PDF) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00012269.PDF) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00012269.PDF) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00012269.PDF) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00012269.PDF) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12641434) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12641434) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12641434) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12641434) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12641434) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12641434) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12641434) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12641434) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12641434) Acetylcholinesterase (Organism: Electrophorus electricus, class: Enzyme, accessions: O42275, gene: ache, swissprot: ACES_ELEEL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18069241) Butyrylcholinesterase (Organism: Equus caballus, class: Enzyme, accessions: Q9N1N9, gene: BCHE, swissprot: Q9N1N9_HORSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18069241) Potassium voltage-gated channel subfamily A member 7 (Organism: Mus musculus, class: Unclassified, accessions: Q17ST2, gene: Kcna7, swissprot: KCNA7_MOUSE) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/9488722) Potassium voltage-gated channel subfamily A member 1 (Organism: Mus musculus, class: Unclassified, accessions: P16388, gene: Kcna1, swissprot: KCNA1_MOUSE) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/7517498) Potassium voltage-gated channel subfamily A member 3 (Organism: Mus musculus, class: Ion channel, accessions: P16390, gene: Kcna3, swissprot: KCNA3_MOUSE) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/7517498) Potassium voltage-gated channel subfamily C member 1 (Organism: Mus musculus, class: Unclassified, accessions: P15388, gene: Kcnc1, swissprot: KCNC1_MOUSE) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/7517498) Potassium voltage-gated channel subfamily A member 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P63142, gene: Kcna2, swissprot: KCNA2_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/7517498) Potassium voltage-gated channel subfamily A member 5 (Organism: Homo sapiens, class: Ion channel, accessions: P22460, gene: KCNA5, swissprot: KCNA5_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/7517498) Capsaicin is a synthetic equivalent of the naturally occurring compound found in chili peppers. Capsaicin is an agonist for the transient receptor potential vanilloid I receptor (TRPVI). Topical administration of capsaicin causes an initial enhanced stimulation of the TRPVI -expressing cutaneous nociceptors that may be associated with painful sensations. This is followed by pain relief thought to be mediated by a reduction in TRPV 1expressing nociceptive nerve endings. Zucapsaicin is a synthetic cis isomer of natural capsaicin that has shown therapeutic efficacy in pain accompanying osteoarthritis of the knee. Capsaicin is indicated for the management of neuropathic pain associated with postherpetic neuralgia. Zucapsaicin is indicated to be used in conjunction with oral COX-2 inhibitors or NSAIDs for the relief of severe pain in adult patients with osteoarthritis of the knee, not controlled with oral COX-2 inhibitors or NSAIDs alone, for a duration of no more than three months. non-narcotic analgesic (Code: CHEBI:35481) Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) capsaicin: 2009-11-16 FDA zucapsaicin: 2011-08-24 Health Canada 4DY
Click to view roxatidine acetate Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) antagonist a histamine H2 receptor antagonist drug used to treat gastric ulcers Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H2 Antagonists (Code: D006635) Neurotransmitter Agents (Code: D018377) 1986-01-01 YEAR INTRODUCED
Click to view clioquinol Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P27139, gene: Ca2, swissprot: CAH2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18242985) Amyloid beta A4 protein (Organism: Homo sapiens, class: Unclassified, accessions: P05067, gene: APP, swissprot: A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23799643) Botulinum neurotoxin type A (Organism: Clostridium botulinum, class: Enzyme, accessions: P10845, gene: botA, swissprot: BXA1_CLOBO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24387280) Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Clioquinol is a potentially neurotoxic 8-hydroxyquinoline derivative long used as a topical anti-infective, intestinal antiamebic, and vaginal trichomonacide. The oral preparation has been shown to cause subacute myelo-optic neuropathy and has been banned worldwide. Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) antineoplastic agent (Code: CHEBI:35610) antiprotozoal drug (Code: CHEBI:35820) 1963 FDA CQL
Click to view nicofibrate Nicofibrate is a derivative of clofibrate and nicotinic acid and an antilipidemic drug.
Click to view fenoldopam D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) (Source: ) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: ) D(2) dopamine receptor (Organism: Bos taurus, class: GPCR, accessions: P20288, gene: DRD2, swissprot: DRD2_BOVIN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: ) Lysine-specific demethylase 4E (Organism: Homo sapiens, class: Enzyme, accessions: B2RXH2, gene: KDM4E, swissprot: KDM4E_HUMAN) D(1A) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901, gene: Drd1, swissprot: DRD1_RAT) Adrenergic receptor alpha-1 (Organism: Homo sapiens, class: GPCR, accessions: P25100|P35348|P35368, gene: ADRA1A|ADRA1B|ADRA1D, swissprot: ADA1A_HUMAN|ADA1B_HUMAN|ADA1D_HUMAN) D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT) FAD-linked sulfhydryl oxidase ALR (Organism: Homo sapiens, class: Enzyme, accessions: P55789, gene: GFER, swissprot: ALR_HUMAN) Adenosine A2b receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P29276, gene: Adora2b, swissprot: AA2BR_RAT) A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation. Dopaminergic Agonist (Code: N0000175580) dopaminergic antagonist (Code: CHEBI:48561) vasodilator agent (Code: CHEBI:35620) alpha-adrenergic agonist (Code: CHEBI:35569) dopamine agonist (Code: CHEBI:51065) antihypertensive agent (Code: CHEBI:35674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) 1997-09-23 FDA
Click to view sertraline Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019839s091lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019839s091lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15547048) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15547048) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15547048) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15547048) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15547048) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15547048) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15547048) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15547048) Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871604) Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871604) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21093273) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21093273) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Sertraline is a selective serotonin uptake inhibitor that is used in the treatment of depression. In vitro studies in animals also suggest that sertraline is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. In vitro studies have shown that sertraline has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors. Sertraline is used in the therapy of depression, anxiety disorders and obsessive-compulsive disorder. Serotonin Reuptake Inhibitor (Code: N0000175696) serotonin uptake inhibitor (Code: CHEBI:50949) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) 1991-12-30 FDA SRE
Click to view fluconazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf) Lanosterol 14-alpha demethylase (Organism: Candida tropicalis , class: Enzyme, accessions: P14263, gene: ERG11, swissprot: CP51_CANTR) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf) Fluconazole is a synthetic triazole with antifungal activity. Fluconazole preferentially inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols, the loss of normal fungal sterols, and fungistatic activity. Mammalian cell demethylation is much less sensitive to fluconazole inhibition. Fluconazole is indicated for the treatment of vaginal yeast infections due to Candida, Oropharyngeal and esophageal candidiasis, Candida urinary tract infections, peritonitis, and systemic Candida infections including candidemia, disseminated candidiasis, pneumonia and Cryptococcal meningitis. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) 14-alpha Demethylase Inhibitors (Code: D058888) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Cytochrome P-450 CYP2C19 Inhibitors (Code: D065689) Cytochrome P-450 CYP2C9 Inhibitors (Code: D065688) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) 1990-01-29 FDA TPF
Click to view phenolphthalol
Click to view propentofylline Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23791077) Propentofylline is a xanthine derivative and phosphodiesterase inhibitor with purported neuroprotective effects. It was development for the treatment of Alzheimer's disease and vascular dementia. Now it is used in veterinary medicine. Central Nervous System Agents (Code: D002491) Neuroprotective Agents (Code: D018696) Protective Agents (Code: D020011) POY
Click to view amprotropine
Click to view oxandrolone Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist A synthetic hormone with anabolic and androgenic properties. Anabolic Agents (Code: D045930) Androgens (Code: D000728) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1964-07-21 FDA
Click to view butacaine Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN was MH 1965-92; BUTAPROBENZ & BUTOCAIN were see BUTACAINE 1978-92; use 4-AMINOBENZOIC ACID to search BUTACAINE 1966-92 Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view broxuridine Broxuridine is a halogenated thymidine analogue with potential antineoplastic and radiosensitizing activities. Bromodeoxyuridine competes with thymidine for incorporation into DNA, resulting in DNA mutation and the inhibition of cell proliferation. As a radiosensitizer, this agent is associated with the inhibition of repair of radiation-induced DNA double-strand breaks. The most popular use of BrdU is as a tracer of DNA synthesis. It has been given orphan drug status for use in the treatment of primary brain tumors. antineoplastic agent (Code: CHEBI:35610) Anti-Infective Agents (Code: D000890) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Antiviral Agents (Code: D000998) Noxae (Code: D009676) Radiation-Sensitizing Agents (Code: D011838) U33
Click to view valethamate Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN
Click to view plaunotol antineoplastic agent (Code: CHEBI:35610) anti-ulcer drug (Code: CHEBI:49201) nephroprotective agent (Code: CHEBI:76595) vulnerary (Code: CHEBI:73336) Anti-Infective Agents (Code: D000890) Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765)
Click to view epitiostanol used in therapy of advanced breast cancer; structure
Click to view moxaverine Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view nitazoxanide Pyruvate dehydrogenase [NADP(+)] (Organism: Cryptosporidium parvum, class: Enzyme, accessions: Q968X7, gene: PFOR, swissprot: PNO_CRYPV) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021497s001,021498s004lbl.pdf) Pyruvate:ferredoxin oxidoreductase (Organism: Giardia intestinalis, class: Enzyme, accessions: Q24982, gene: None, swissprot: Q24982_GIAIN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021497s001,021498s004lbl.pdf) Nitazoxanide is a synthetic antiprotozoal.The antiprotozoal activity of nitazoxanide is believed to be due to interference with the pyruvate:ferredoxin oxidoreductase (PFOR) enzyme-dependent electron transfer reaction which is essential to anaerobic energy metabolism. Nitazoxanide and its metabolite, tizoxanide, are active in vitro in inhibiting the growth of sporozoites and oocysts of C. parvum and trophozoites of G. lamblia. Nitazoxanide is indicated for the treatment of diarrhea caused by Giardia lamblia or Cryptosporidium parvum. Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal (Code: N0000175485) 2002-11-22 FDA NTI
Click to view glutathione Glutathione S-transferase omega-1 (Organism: Homo sapiens, class: Enzyme, accessions: P78417, gene: GSTO1, swissprot: GSTO1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17226937) Microsomal glutathione S-transferase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O14880, gene: MGST3, swissprot: MGST3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9278457) Glutathione S-transferase A1 (Organism: Homo sapiens, class: Enzyme, accessions: P08263, gene: GSTA1, swissprot: GSTA1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20606271) Glutathione S-transferase A4 (Organism: Homo sapiens, class: Enzyme, accessions: O15217, gene: GSTA4, swissprot: GSTA4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20085333) Glutathione is a tripeptide which conjugates to drugs to make them more soluble for excretion, is a cofactor for some enzymes such as, glutathione reductase, glutathione peroxidases, peroxiredoxins. Glutathione S-transferases catalyse the conjugation of glutathione via a sulfhydryl group to electrophilic centers on a wide variety of substrates in order to make the compounds more water-soluble. Glutathione is an important nutrient for brain function and loss of glutathione has been implicated in Parkinson's disease. Glutathione is used for nutritional supplementation, also for treating dietary shortage or imbalance. skin lightening agent (Code: CHEBI:85046) 1989-11-02 Italian Medicines Agency (AIFA) GSH
Click to view carbocysteine-lysine Carbocysteine-lysine is a mucoactive drug effective in the treatment of bronchopulmonary diseases characterized by mucus alterations, including COPD. 1995-05-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view sulfasymazine Sulfasymazine is a sulfanilamide derivative. It was developed as an antibacterial agents for Staphylococcus and Streptococcus infections. In preclinical models, Sulfasymazine was not as potent as sulfadiazine. Anti-Infective Agents (Code: D000890)
Click to view ibopamine Epinine: D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_005121_032900_RCP.pdf&retry=0&sys=m0b1l3) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_005121_032900_RCP.pdf&retry=0&sys=m0b1l3) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_005121_032900_RCP.pdf&retry=0&sys=m0b1l3) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_005121_032900_RCP.pdf&retry=0&sys=m0b1l3) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_005121_032900_RCP.pdf&retry=0&sys=m0b1l3) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_005121_032900_RCP.pdf&retry=0&sys=m0b1l3) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_005121_032900_RCP.pdf&retry=0&sys=m0b1l3) Ibopamine is the prodrug of epinine. Ibopamine and epinine stimulate the DA1 dopaminergic receptors, alpha adrenoceptors. Ibopamine is used to producing mydriasis, for inspection of the eye fundus. Also it is used for the treatment of post-surgical ocular hypotension. Autonomic Agents (Code: D001337) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Mydriatics (Code: D009184) Natriuretic Agents (Code: D045283) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Vasodilator Agents (Code: D014665) 1997-07-01 Italian Medicines Agency (AIFA)
Click to view buflomedil C-8 sterol isomerase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P32352, gene: ERG2, swissprot: ERG2_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16033255) 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Organism: Homo sapiens, class: Enzyme, accessions: Q15125, gene: EBP, swissprot: EBP_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16033255) Buflomedil is a vasoactive agent, a medicine which has an effect on blood circulation. Buflomendil increases the blood flow to the brain and other parts of the body by widening the blood vessels. It is used to treat the symptoms of peripheral arterial occlusive disease stage II. It was withdrawn from European market due to its fatal side effects, such a convulsions and status epilepticus. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1980-06-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view talastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/13499132)
Click to view zolpidem Gamma-aminobutyric acid receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P14867, gene: GABRA1, swissprot: GBRA1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019908s045lbl.pdf) Gamma-aminobutyric acid receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: P47869, gene: GABRA2, swissprot: GBRA2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019908s045lbl.pdf) Gamma-aminobutyric acid receptor subunit alpha-3 (Organism: Homo sapiens, class: Ion channel, accessions: P34903, gene: GABRA3, swissprot: GBRA3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019908s045lbl.pdf) Zolpidem is a gamma-Aminobutyric Acid-ergic Agonist. The mechanism of action of zolpidem is as a GABA A Agonist. The physiologic effect of zolpidem is by means of Central Nervous System Depression. Zolpidem is used for the treatment of insomnia. gamma-Aminobutyric Acid-ergic Agonist (Code: N0000175759) GABA A Agonists (Code: N0000000196) Pyridines (Code: N0000007570) Central Nervous System Depression (Code: N0000175728) central nervous system depressant (Code: CHEBI:35488) GABA agonist (Code: CHEBI:51373) sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Agonists (Code: D018755) GABA-A Receptor Agonists (Code: D058785) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) 1992-12-16 FDA
Click to view tolnaftate 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) Lanosterol 14-alpha demethylase (Organism: Homo sapiens, class: Enzyme, accessions: Q16850, gene: CYP51A1, swissprot: CP51A_HUMAN A synthetic antifungal agent. antifungal drug (Code: CHEBI:86327) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) FDA
Click to view fabomotizole Sigma non-opioid intracellular receptor 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: Q9R0C9, gene: Sigmar1, swissprot: SGMR1_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/28726201) Fabomotizole is a selective non-benzodiazepine anxiolytic. The drug is used for the treatment of wide range of diseases: generalized anxious disorders, neurasthenia, adaptation disorders, sleep disorders, for alleviation of withdrawal syndrome. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. Fabomotizole action is related to the interaction with sigma-1 receptors. Its mechanism of action remains poorly defined however. 2005-12-23 Ministry of Health of the Russian Federation
Click to view betaxolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019507s008lbl.pdf) Beta-1 adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18090, gene: Adrb1, swissprot: ADRB1_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10079020) Beta-2 adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P10608, gene: Adrb2, swissprot: ADRB2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10079020) Betaxolol is a beta1-selective (cardioselective) adrenergic receptor blocking agent. that has weak membrane-stabilizing activity and no intrinsic sympathomimetic (partial agonist) activity. The preferential effect on beta1 receptors is not absolute, however, and some inhibitory effects on beta2 receptors (found chiefly in the bronchial and vascular musculature) can be expected at higher doses. Animal studies suggest levobetaxolol (S-isomer) is the more active enantiomer of betaxolol (racemate). Betaxolol is indicated for lowering intraocular pressure in patients with chronic open-angle glaucoma or ocular hypertension or in the management of hypertension. It may be used alone or concomitantly with other antihypertensive agents, particularly thiazide-type diuretics. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) sympatholytic agent (Code: CHEBI:66991) beta-adrenergic antagonist (Code: CHEBI:35530) antihypertensive agent (Code: CHEBI:35674) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) betaxolol: 1985-08-30 FDA levobetaxolol: 2000-02-23 FDA
Click to view benzatropine Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15857139) Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7562926) Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7562926) Muscarinic acetylcholine receptor M2 (Organism: Rattus norvegicus, class: GPCR, accessions: P10980, gene: Chrm2, swissprot: ACM2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7562926) Sodium-dependent neutral amino acid transporter B(0)AT1 (Organism: Homo sapiens, class: Unclassified, accessions: Q695T7, gene: SLC6A19, swissprot: S6A19_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28176326) Benzatropine is a synthetic compound containing structural features found in atropine and diphenhydramine. Benzatropine possesses both anticholinergic and antihistaminic effects, although only the former have been established as therapeutically significant in the management of parkinsonism. Benzatropine is indicated for use as an adjunct in the therapy of all forms of parkinsonism. antidyskinesia agent (Code: CHEBI:66956) muscarinic antagonist (Code: CHEBI:48876) antiparkinson drug (Code: CHEBI:48407) parasympatholytic (Code: CHEBI:50370) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Anticholinergic (Code: N0000175574) Antihistamine (Code: N0000175750) Histamine Receptor Antagonists (Code: N0000000207) 1954-03-05 FDA CXQ
Click to view mitobronitol Mitobronitol (dibromomannitol) is a brominated analog of mannitol with potential antineoplastic activity. Mitobronitol most likely acts through alkylation via derived epoxide groups. Mitolactol (also known as dibromo galactitol or dibromodulcitol) is an diastereoisomer for mitobronitol. This two isomirs differ in activity spectrum against solid tumors and its relative lack of nephrotoxicity. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676)
Click to view pirenoxine Pirenoxine, a pyridophenoxazine compound, competitively inhibits the sulfhydryl combination of quinoid substances with lens proteins. Pirenoxine is used for the treatment of cataract. 1984-06-01 PMDA
Click to view sulisobenzone Sulisobenzone is a member of benzophenones. Sulisobenzone works to filter out both UVA and UVB rays, protecting the skin from sun UV damage. Sulisobenzone is widely used an ingredient in sunscreening agents which are indicated to prevent sunburn, actinic keratosis, and premature skin aging and to reduce the incidence of skin cancer. 1997-04-04 Health Canada
Click to view nimesulide Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10377455) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10377455) Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17315855) Myeloperoxidase (Organism: Homo sapiens, class: Enzyme, accessions: P05164, gene: MPO, swissprot: PERM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22793255) Sodium-dependent neutral amino acid transporter B(0)AT1 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q2A865, gene: Slc6a19, swissprot: S6A19_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24704252) Nimesulide is a nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Nimesulide inhibits the cyclooxygenase-mediated conversion of arachidonic acid to pro-inflammatory prostaglandins. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1985 Italian Medicines Agency (AIFA) NIM
Click to view warfarin Vitamin K epoxide reductase complex subunit 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BQB6, gene: VKORC1, swissprot: VKOR1_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00039447.PDF) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00039447.PDF) Cytochrome P450 2C18 (Organism: Homo sapiens, class: Enzyme, accessions: P33260, gene: CYP2C18, swissprot: CP2CI_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00039447.PDF) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00039447.PDF) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00039447.PDF) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00039447.PDF) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00039447.PDF) Proprotein convertase subtilisin/kexin type 7 (Organism: Homo sapiens, class: Enzyme, accessions: Q16549, gene: PCSK7, swissprot: PCSK7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21510613) Warfarin is an anticoagulant which acts by inhibiting vitamin K-dependent coagulation factors. Chemically, it is 3-(?-acetonylbenzyl)-4-hydroxycoumarin and is a racemic mixture of the R- and S-enantiomers. The more potent warfarin S-enantiomer (60% of the overall anticoagulation response) is metabolized by CYP2C9 while the R-enantiomer is metabolized by CYP1A2 and 3A4. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, and pulmonary embolism. It is also indicated for the prophylaxis and/or treatment of the thromboembolic complications associated with atrial fibrillation and/or cardiac valve replacement. Vitamin K Antagonist (Code: N0000175476) Vitamin K Inhibitors (Code: N0000175964) anticoagulant (Code: CHEBI:50249) rodenticide (Code: CHEBI:33288) Anticoagulants (Code: D000925) Hematologic Agents (Code: D006401) Pesticides (Code: D010575) Rodenticides (Code: D012378) 1954-06-08 FDA RWF
SWF
Click to view roquinimex Roquinimex is a quinoline-3-carboxamide with pleiotropic immune modulating capacity. Roquinimex possesses potential antineoplastic activity. Roquinimex inhibits endothelial cell proliferation, migration, and basement membrane invasion; reduces the secretion of the angiogenic factor tumor necrosis factor alpha by tumor-associated macrophages; and inhibits angiogenesis.Roquinimex has been evaluated in clinical trials for multiple sclerosis, and was indeed shown to have disease inhibitory effects. However, clinical trials was required due to unexpected side effects. Adjuvants, Immunologic (Code: D000276) Angiogenesis Inhibitors (Code: D020533) Angiogenesis Modulating Agents (Code: D043924) Antineoplastic Agents (Code: D000970) Growth Inhibitors (Code: D006131) Growth Substances (Code: D006133) Immunologic Factors (Code: D007155)
Click to view nifenazone Nifenazone is a derivative of pyrazolone with anti-inflammatory and anaesthetic actions. Also nifenazone has hepatic and medullary toxicity, and ulcerogenic properties. Nifenazone was used for the treatment of rheumatic conditions. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Italian Medicines Agency (AIFA)
Click to view ubenimex Aminopeptidase N (Organism: Mus musculus, class: Enzyme, accessions: P97449, gene: Anpep, swissprot: AMPN_MOUSE) Cytosol aminopeptidase (Organism: Homo sapiens, class: Enzyme, accessions: P28838, gene: LAP3, swissprot: AMPL_HUMAN) 72 kDa type IV collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P08253, gene: MMP2, swissprot: MMP2_HUMAN) Aminopeptidase N (Organism: Rattus norvegicus, class: Unclassified, accessions: P15684, gene: Anpep, swissprot: AMPN_RAT) Bacterial leucyl aminopeptidase (Organism: Vibrio proteolyticus, class: Enzyme, accessions: Q01693, gene: None, swissprot: AMPX_VIBPR) Cytosol aminopeptidase (Organism: Bos taurus, class: Enzyme, accessions: P00727, gene: LAP3, swissprot: AMPL_BOVIN) Aminopeptidase B (Organism: Rattus norvegicus, class: Enzyme, accessions: O09175, gene: Rnpep, swissprot: AMPB_RAT) Leucyl-cystinyl aminopeptidase (Organism: Rattus norvegicus, class: Enzyme, accessions: P97629, gene: Lnpep, swissprot: LCAP_RAT) Leukotriene A-4 hydrolase (Organism: Homo sapiens, class: Enzyme, accessions: P09960, gene: LTA4H, swissprot: LKHA4_HUMAN) Aminopeptidase B (Organism: Mus musculus, class: Enzyme, accessions: Q8VCT3, gene: Rnpep, swissprot: AMPB_MOUSE) Aminopeptidase N (Organism: Homo sapiens, class: Enzyme, accessions: P15144, gene: ANPEP, swissprot: AMPN_HUMAN) Aminopeptidase N (Organism: Sus scrofa, class: Enzyme, accessions: P15145, gene: ANPEP, swissprot: AMPN_PIG) M1 family aminopeptidase (Organism: Plasmodium falciparum (isolate FcB1 / Columbia), class: Enzyme, accessions: O96935, gene: None, swissprot: AMP1_PLAFQ) growth inhibitor; RN given refers to ((L-Leu)-(S-(R*,S*)))-isomer; structure Adjuvants, Immunologic (Code: D000276) Anti-Bacterial Agents (Code: D000900) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Immunologic Factors (Code: D007155) Protease Inhibitors (Code: D011480) BES
Click to view phenylbutazone Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://europepmc.org/abstract/CTX/c6849) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Phenylbutazone is a synthetic, pyrazolone derivative. It is a nonhormonal anti-inflammatory, antipyretic compound useful in the management of inflammatory conditions. Phenylbutazone binds to and inactivates prostaglandin H synthase and prostacyclin synthase through peroxide mediated deactivation. The reduced production of prostaglandin leads to reduced inflammation of the surrounding tissues. Phenylbutazone is especially effective in the treatment of ankylosing spondylitis. It also is useful in rheumatoid arthritis and Reiter's syndrome. Although phenylbutazone is effective in gouty arthritis, risk/benefit considerations indicate that this drug should not be employed for this disease. In some countries phenylbutazone was discontinued for human use because of its harmful side effects. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-narcotic analgesic (Code: CHEBI:35481) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antirheumatic drug (Code: CHEBI:35842) peripheral nervous system drug (Code: CHEBI:49110) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1980-01-10 FDA P1Z
Click to view gestrinone Gestrinone is a non-estrogenic contraceptive which is a weak progestin with strong anti-progesterone properties. It is effective if used once a week orally or can also be used in intravaginal devices. Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Progestins (Code: D011372) Reproductive Control Agents (Code: D012102) 1994-10-28 Therapeutic Goods Administration (TGA)
Click to view metabutoxycaine local anesthetic in operative dentistry
Click to view oxybuprocaine Sodium channel protein type 10 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y5Y9, gene: SCN10A, swissprot: SCNAA_HUMAN) blocker Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN) blocker Oxybuprocaine is a local anesthetic, which is used especially in ophthalmology and otolaryngology. Oxybuprocaine binds to sodium channel and reversibly stabilizes the neuronal membrane which decreases its permeability to sodium ions. Depolarization of the neuronal membrane is inhibited thereby blocking the initiation and conduction of nerve impulses. Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) local anaesthetic (Code: CHEBI:36333) topical anaesthetic (Code: CHEBI:48425) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1957-03-01 Italian Medicines Agency (AIFA)
Click to view indecainide Indecainide is an antiarrhythmic agent classified as type IC. Indecainide have mediated the pharmacological actions through a blocking of Na+-channel. Indecainide was used for the treatment of life-threatening dysrhythmias and sustained ventricular tachycardia. However, that usage was discontinued. 1989-12-29 FDA
Click to view pinazepam Pinazepam is a benzodiazepine derivative, differs from other drugs of its class by the presence of an unsaturated bond, the propargyl group, at the N-1 position. Pinazepam is used in the treatment of anxiety and insomnia associated with anxiety. Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1975 Italian Medicines Agency (AIFA)
Click to view alprazolam GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47869|P34903|P48169|P31644|Q16445|P18505|P47870|P28472|O14764|P78334|Q8N1C3|P18507|Q99928|O00591|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/14978513) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/021726s008lbl.pdf) Alprazolam is a triazolo analog of the 1,4 benzodiazepine class of central nervous system-active compounds. The exact mechanism of action of alprazolam is unknown. Benzodiazepines bind to gamma aminobutyric acid (GABA) receptors in the brain and enhance GABA-mediated synaptic inhibition; such actions may be responsible for the efficacy of alprazolam in anxiety disorder and panic disorder. Alprazolam is indicated for the treatment of generalized anxiety disorder and of panic disorder, with or without agoraphobia. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Anti-Anxiety Agents (Code: D014151) GABA agonist (Code: CHEBI:51373) anxiolytic drug (Code: CHEBI:35474) anticonvulsant (Code: CHEBI:35623) muscle relaxant (Code: CHEBI:51371) sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1981-10-16 FDA 08H
Click to view aminaphtone Aminaphtone is a synthetic molecule derived from 4-aminobenzoic acid. Aminaphtone significantly protects endothelium permeability and stabilises endothelial cells organised in capillary-like structures, modulating VE-cadherin expression. In addition aminaphtone modulate expression of several inflammatory and vasoactive factors. Aminaphtone is used in the treatment of vascular disorders, especially chronic venous disease. Also it is uded in dermatology for the treatment of ecchymosis. Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) 1985-01-30 National Authority of Medicines and Health Products (Portugal)
Click to view fluoxetine Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021860s011lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021860s011lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021860s011lbl.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9050900) Neuronal acetylcholine receptor; alpha2/beta4 (Organism: Rattus norvegicus, class: Ion channel, accessions: P12389|P12392, gene: Chrna2|Chrnb4, swissprot: ACHA2_RAT|ACHB4_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/9050901) Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Rattus norvegicus, class: Ion channel, accessions: P04757|P12392, gene: Chrna3|Chrnb4, swissprot: ACHA3_RAT|ACHB4_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/9050901) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16967046) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10997938) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10997938) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10997938) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10997938) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10997938) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10997938) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11270912) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10192756) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12649369) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16162005) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16162005) Potassium channel subfamily K member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O95069, gene: KCNK2, swissprot: KCNK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26588045) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11104741) 5-hydroxytryptamine receptor 2C (Organism: Rattus norvegicus, class: GPCR, accessions: P08909, gene: Htr2c, swissprot: 5HT2C_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11104741) 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11104741) Potassium voltage-gated channel subfamily C member 1 (Organism: Rattus norvegicus, class: Unclassified, accessions: P25122, gene: Kcnc1, swissprot: KCNC1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11543764) G protein-activated inward rectifier potassium channel 2 (Organism: Mus musculus, class: Ion channel, accessions: P48542, gene: Kcnj6, swissprot: KCNJ6_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12684268) G protein-activated inward rectifier potassium channel 1 (Organism: Mus musculus, class: Ion channel, accessions: P63250, gene: Kcnj3, swissprot: KCNJ3_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12684268) Fluoxetine is the first agent of the class of antidepressants known as selective serotonin-reuptake inhibitors. Fluoxetine is a racemic mixture of the R- and S- enantiomers and are of equivalent pharmacologic activity. The S-fluoxetine enantiomer is eliminated more slowly and is the predominant enantiomer present in plasma at steady state. Antagonism of muscarinic, histaminergic, and ?1-adrenergic receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects of classical tricyclic antidepressant (TCA) drugs. Fluoxetine binds to these and other membrane receptors from brain tissue much less potently in vitro than do the tricyclic drugs. Fluoxetine is indicated for the treatment of major depressive disorder, obsessive compulsive disorder, bulimia nervosa, panic disorder and premenstrual dysphoric disorder. Serotonin Reuptake Inhibitor (Code: N0000175696) drug allergen (Code: CHEBI:88188) serotonin uptake inhibitor (Code: CHEBI:50949) analgesic (Code: CHEBI:35480) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Cytochrome P-450 CYP2D6 Inhibitors (Code: D065690) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Membrane Transport Modulators (Code: D049990) Metabolic Side Effects of Drugs and Substances (Code: D065606) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) 1987-12-29 FDA RFX
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Click to view isomethadone Isomethadone is a structural isomer of methadone. Isomethadone is synthesized as a racemate, and its pharmacological examination has shown that practically all of the analgesic action and most other effects are produced by the levo-isomer. Isomethadone was used as both an analgesic and antitussive agents. Isomethadone is regulated internationally as a Schedule I controlled substance under the United Nations Single Convention on Narcotic Drugs of 1961.
Click to view glymidine was MH 1975-92 (see under SULFONAMIDES 1975-90); GLIDIAZINE & GLYCODIAZINE were see GLYMIDINE 1975-92; use SULFONAMIDES to search GLYMIDINE 1975-92; a sulfonamide hypoglycemic agent which stimulates insulin secretion
Click to view sulfaguanole Sulfaguanole is an antibacterial sulfanilamide drug. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Italian Medicines Agency (AIFA)
Click to view diacetazotol Diacetylaminoazotoluene is a member of azobenzenes. Diacetazotol inhibits dioxin-induced ethoxyresorufin-O-deethylase activity.
Click to view nadolol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: ) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: ) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) antagonist (Source: ) A non-selective beta-adrenergic antagonist with a long half-life, used in cardiovascular disease to treat arrhythmias, angina pectoris, and hypertension. Nadolol is also used for MIGRAINE DISORDERS and for tremor. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) anti-arrhythmia drug (Code: CHEBI:38070) antihypertensive agent (Code: CHEBI:35674) sympatholytic agent (Code: CHEBI:66991) beta-adrenergic antagonist (Code: CHEBI:35530) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1979-12-10 FDA
Click to view metipranolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist A beta-adrenergic antagonist effective for both beta-1 and beta-2 receptors. It is used as an antiarrhythmic, antihypertensive, and antiglaucoma agent. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) beta-adrenergic antagonist (Code: CHEBI:35530) anti-arrhythmia drug (Code: CHEBI:38070) antihypertensive agent (Code: CHEBI:35674) antiglaucoma drug (Code: CHEBI:39456) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1989-12-29 FDA
Click to view croconazole Croconazole is an imidazole derivative with antifungal activity. it is active against T. mentagrophytes, T. rubrum, M. canis, Microsporum gypseum, and Epidermophyton floccosum. It was used for the treatment of dermatomycoses and candidiasis. It is no longer available.
Click to view dioxadrol Sigma non-opioid intracellular receptor 1 (Organism: Cavia porcellus, class: Membrane other, accessions: Q60492, gene: SIGMAR1, swissprot: SGMR1_CAVPO See also records for d- and l-forms which are referred to as dexoxadrol and levoxadrol, respectfully Analgesics (Code: D000700) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view amolanone
Click to view benzydamine Benzydamine, available as the hydrochloride salt, is a locally-acting nonsteroidal anti-inflammatory drug (NSAID) with local anaesthetic and analgesic properties. It is used topically for pain relief and anti-inflammatory treatment of the mouth, throat, or muscoskeletal system. Anti-Inflammatory Agents (Code: D000893) 1986-02-06 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view ketotifen Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/1999/21066lbl.pdf) 6-phosphogluconate dehydrogenase, decarboxylating (Organism: Homo sapiens, class: Enzyme, accessions: P52209, gene: PGD, swissprot: 6PGD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20235752) Ketotifen is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators. Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Inhibitor (Code: N0000175519) Anti-Allergic Agents (Code: D018926) H1-receptor antagonist (Code: CHEBI:37955) anti-asthmatic drug (Code: CHEBI:49167) Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1999-07-02 FDA
Click to view methadone Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/006134s049lbl.pdf) Glutamate [NMDA] receptor (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q12879|Q13224|Q14957|O15399|Q8TCU5|O60391, gene: GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B, swissprot: NMDZ1_HUMAN|NMDE1_HUMAN|NMDE2_HUMAN|NMDE3_HUMAN|NMDE4_HUMAN|NMD3A_HUMAN|NMD3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/006134s049lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/006134s049lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/006134s049lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/006134s049lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/006134s049lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/006134s049lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/006134s049lbl.pdf) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19131665) 5-hydroxytryptamine receptor 3B (Organism: Homo sapiens, class: Ion channel, accessions: O95264, gene: HTR3B, swissprot: 5HT3B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19131665) Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25196810) Neuronal acetylcholine receptor subunit alpha-3 (Organism: Homo sapiens, class: Ion channel, accessions: P32297, gene: CHRNA3, swissprot: ACHA3_HUMAN) antaagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25196810) Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P17787, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) antaagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25196810) Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20410453) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15911273) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11408360) Methadone is a mu-agonist and a synthetic opioid with multiple actions qualitatively similar to those of morphine, the most prominent of which involves the central nervous system and organs composed of smooth muscle. The methadone withdrawal syndrome, although qualitatively similar to that of morphine, differs in that the onset is slower, the course is more prolonged, and the symptoms are less severe. Some data also indicate that methadone acts as an antagonist at the N-methyl-D-aspartate (NMDA) receptor. The contribution of NMDA receptor antagonism to methadone’s efficacy is unknown. Racemic methadone formulation contains both (R)- and (S)-enantiomers. The (R)-enantiomer (levomethadone) is responsible for therapeutic effects. The (S)-enantiomer is a poor mu agonist and can block hERG channels to a greater degree than the (R)-enantiomer, which has been postulated to be responsible for cardiac adverse events in methadone use The principal therapeutic uses for methadone are for analgesia and for detoxification or maintenance in opioid addiction. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322) Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689) Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) 1947-08-13 FDA
Click to view diphenidol D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN shows anti-arrhythmic activity; RN given refers to unlabeled parent cpd Emesis Suppression (Code: N0000009034) antiemetic (Code: CHEBI:50919) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373) 1967-04-05 FDA
Click to view metixene Cholinesterase (Organism: Equus caballus, class: Enzyme, accessions: P81908, gene: BCHE, swissprot: CHLE_HORSE) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/21459491/) Metixene is a tertiary antimuscarinic with actions similar to those of atropine; it also has antihistaminic and direct antispasmodic properties. It is used for the symptomatic treatment of parkinsonism, including the alleviation of the extrapyramidal syndrome induced by other drugs such as phenothiazines, but, like other antimuscarinics, it is of no value against tardive dyskinesias. Metixene has been discontinued. antiparkinson drug (Code: CHEBI:48407) muscarinic antagonist (Code: CHEBI:48876) histamine antagonist (Code: CHEBI:37956) FDA
Click to view dicycloverine Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2704370) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2704370) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2704370) A muscarinic antagonist used as an antispasmodic and in urinary incontinence. It has little effect on glandular secretion or the cardiovascular system. It does have some local anesthetic properties and is used in gastrointestinal, biliary, and urinary tract spasms. muscarinic antagonist (Code: CHEBI:48876) antispasmodic drug (Code: CHEBI:53784) parasympatholytic (Code: CHEBI:50370) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Anticholinergic (Code: N0000175574) 1950-05-11 FDA
Click to view chloralose Chloralose is a derivative of chloral hydrate that was used as a sedative but has been replaced by safer and more effective drugs. Its most common use is as a general anesthetic in animal experiments. Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993)
Click to view picrotin Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) Glycine receptor subunit alpha-3 (Organism: Homo sapiens, class: Ion channel, accessions: O75311, gene: GLRA3, swissprot: GLRA3_HUMAN) Glycine receptor subunit beta (Organism: Homo sapiens, class: Ion channel, accessions: P48167, gene: GLRB, swissprot: GLRB_HUMAN) blocker (Source: ) Glycine receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: P23416, gene: GLRA2, swissprot: GLRA2_HUMAN) blocker (Source: ) the less toxic component of picrotoxin lacking GABA activity
Click to view fotemustine Fotemustine is a phosphoalanine-modified nitrosurea. Decomposition of nitrosoureas generates electrophilic species, which are responsible for DNA alkylation, thus producing therapeutic effects. The action mechanism of fotemustine seems to be similar to that of other nitrosoureas. Fotemustine is used for the treatment of disseminated malignant melanoma and primary brain tumors. antineoplastic agent (Code: CHEBI:35610) Antineoplastic Agents (Code: D000970) 1989-04-14 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view sulfadoxine Dihydropteroate synthetase (Organism: Plasmodium falciparum, class: Kinase, accessions: Q25704, gene: PPPK-DHPS, swissprot: Q25704_PLAFA) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/18557slr015_fansidar_lbl.pdf) Sulfadoxine is folic acid antagonist. Sulfadoxine inhibits the activity of dihydropteroate synthase. Sulfadoxine is active against the asexual erythrocytic stages of Plasmodium falciparum. Sulfadoxine is used in combination with pyrimethamine for the treatment of acute, uncomplicated P. falciparum malaria for those patients in whom chloroquine resistance is suspected. Sulfonamide (Code: N0000175880) Sulfonamides (Code: N0000008048) antibacterial drug (Code: CHEBI:36047) antimalarial (Code: CHEBI:38068) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Renal Agents (Code: D012076) 1981-10-28 FDA
Click to view sulfadimethoxine Folic acid synthesis protein fol1 (Organism: Pneumocystis carinii, class: Enzyme, accessions: P29251, gene: fol1, swissprot: FOL1_PNECA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7486915) Sulfadimethoxine is a long-acting sulfonamide antibiotic. Sulfadimethoxine inhibits bacterial synthesis of folic acid by competing with para-aminobenzoic acid (PABA) for the binding site on dihydropteroate synthase. Sulfadimethoxine is used to treat many infections including treatment of respiratory, urinary tract, enteric, and soft tissue infections. It is most frequently used in veterinary medicine, although it is approved in some countries for use in humans. antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) 1967-01-31 Ministry of Health of the Russian Federation
Click to view trepibutone Trepibutone promotes secretion of the bile and pancreatic juice, and accelerates flaccidity of the smooth muscle in the gastrointestinal tract (sphincter of hepatopancreatic ampulla etc.) to lower internal pressure of the gallbladder and bile duct. It improves the symptoms of the bile duct and pancreatic disease. It is usually used for improvement of cramp and bile secretion associated with cholelithiasis, cholecystitis, cholangitis, dyskinesia of the biliary tract or postcholecystectomy syndrome, or pain and gastrointestinal symptoms associated with chronic pancreatitis. 1981-02-01 PMDA
Click to view cetamolol Cetamolol is a beta-adrenoceptor blocker with partial agonist activity and cardioselectivity. Cetamolol lacked membrane-stabilizing activity.
Click to view bifonazole Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15554355) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9574817) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15135088) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15135088) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15135088) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15135088) Lanosterol 14-alpha demethylase (Organism: Homo sapiens, class: Enzyme, accessions: Q16850, gene: CYP51A1, swissprot: CP51A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17194716) Indoleamine 2,3-dioxygenase 1 (Organism: Mus musculus, class: Enzyme, accessions: P28776, gene: Ido1, swissprot: I23O1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25036789) Bifonazole is an azole antifungal drug. Bifonazole works by inhibiting the production of a substance called ergosterol, which is an essential component of fungal cell membranes. It acts to destabilize the fungal cyctochrome p450 51 enzyme (also known as Lanosterol 14-alpha demethylase). This is vital in the cell membrance structure of the fungus. Its inhibition leads to cell lysis. Bifonazole is used for the treatment of various topical fungal infections, including athlete's foot (tinea pedis). Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 1984-12-10 ANSM (French National Agency for Medicines and Health Products Safety) TMI
Click to view mestranol Cannabinoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P21554, gene: CNR1, swissprot: CNR1_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) The 3-methyl ether of ETHINYL ESTRADIOL. It must be demethylated to be biologically active. It is used as the estrogen component of many combination ORAL CONTRACEPTIVES. Estrogen (Code: N0000175825) Estrogen Receptor Agonists (Code: N0000000100) prodrug (Code: CHEBI:50266) xenoestrogen (Code: CHEBI:76988) Estrogens (Code: D004967) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1961-03-09 FDA
Click to view gestodene Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12899669) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12899669) Gestodene (17alpa-ethynyl-13beta-ethyl-17beta-hydroxy-4,15-gonadien-3-one) is the potent synthetic progestin. It is used as a fertility regulating agent in a number of contraceptive formulations because of its high effectiveness, safety and acceptability. Gestodene is androgenically neutral, meaning that contraceptive pills containing gestodene do not exhibit the androgenic side effects (e.g. acne, hirsutism, weight gain) often associated with second-generation contraceptive pills. Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Progestins (Code: D011372) Reproductive Control Agents (Code: D012102) 1987-10-24 Italian Medicines Agency (AIFA)
Click to view pecazine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Membrane-associated progesterone receptor component 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: P70580, gene: Pgrmc1, swissprot: PGRC1_RAT) FAD-linked sulfhydryl oxidase ALR (Organism: Homo sapiens, class: Enzyme, accessions: P55789, gene: GFER, swissprot: ALR_HUMAN Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT major descriptor (66-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search MEPAZINE (66-85); RN given refers to parent cpd
Click to view desogestrel Desogestrel, a prodrug, is a third generation progestogen and hence, a member of the gonane family. Desogestrel is rapidly and almost completely absorbed and converted into etonogestrel, its biologically active metabolite. Desogestrel is used as oral contraceptove medicine. (See: etonogestrel) contraceptive drug (Code: CHEBI:49323) synthetic oral contraceptive (Code: CHEBI:49326) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Progestins (Code: D011372) Reproductive Control Agents (Code: D012102) Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) 1992-12-10 FDA
Click to view alloclamide Alloclamide is a cough suppressant.
Click to view desloratadine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021165s022,021300s019,021312s020,021563s008lbl.pdf) Desloratadine is a long-acting piperidine derivate with selective H1 antihistaminergic and non-sedating properties. Desloratadine diminishes the typical histaminergic effects on H1-receptors in bronchial smooth muscle, capillaries and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching and spasmodic contractions of gastrointestinal smooth muscle. Desloratadine is used to provide symptomatic relieve of allergic symptoms. H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) cholinergic antagonist (Code: CHEBI:48873) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Neurotransmitter Agents (Code: D018377) Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Antagonist (Code: N0000175587) 2001-12-21 FDA
Click to view nalorphine Kappa-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P41144, gene: OPRK1, swissprot: OPRK_CAVPO Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT Mu-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33535, gene: Oprm1, swissprot: OPRM_RAT Opioid receptor (Organism: Mus musculus, class: GPCR, accessions: O55242|P32300|P33534|P42866, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_MOUSE|OPRK_MOUSE|OPRM_MOUSE|SGMR1_MOUSE A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete. Central Nervous System Agents (Code: D002491) Narcotic Antagonists (Code: D009292) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view butofilolol Butofilolol is a beta-blocking agent. It was used for the treatment of hypertension. It is no longer available. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Neurotransmitter Agents (Code: D018377)
Click to view tolazamide Arachidonate 15-lipoxygenase (Organism: Oryctolagus cuniculus, class: Enzyme, accessions: P12530, gene: ALOX15, swissprot: LOX15_RABIT) Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) blocker (Source: ) A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. Sulfonylurea (Code: N0000175608) Sulfonylurea Compounds (Code: N0000008054) hypoglycemic agent (Code: CHEBI:35526) Hypoglycemic Agents (Code: D007004) 1966-07-18 FDA
Click to view metahexamide major descriptor (64-83); on-line search SULFONYLUREA COMPOUNDS (64-83); Index Medicus search METAHEXAMIDE (64-83); RN given refers to parent cpd; structure
Click to view fomocaine a basic ether with local anesthetic action & relative low toxicity & systemic effects; minor descriptor (77-86); on-line & INDEX MEDICUS search PHENYL ETHERS (77-86); RN given refers to parent cpd
Click to view femoxetine Sodium-dependent dopamine transporter (Organism: Mus musculus, class: Transporter, accessions: Q61327, gene: Slc6a3, swissprot: SC6A3_MOUSE Sodium-dependent noradrenaline transporter (Organism: Mus musculus, class: Transporter, accessions: O55192, gene: Slc6a2, swissprot: SC6A2_MOUSE Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) serotonin uptake inhibitor; RN given refers to (3R-trans)-isomer Anti-Infective Agents (Code: D000890) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367)
Click to view dienogest Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022252s004lbl.pdf) an orally-active, semisynthetic, fourth generation, nonethinylated progestogen with antiproliferative, antiandrogenic, anti-inflammatory and antiangiogenic activities that is used in hormone therapy and as a female contraceptive synthetic oral contraceptive (Code: CHEBI:49326) progesterone receptor agonist (Code: CHEBI:70709) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptive Agents, Male (Code: D003272) Contraceptives, Oral (Code: D003276) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Reproductive Control Agents (Code: D012102) Progestin (Code: N0000175602) Progesterone Congeners (Code: N0000011301) 2010-05-06 FDA
Click to view adiphenine Acetylcholine receptor subunit gamma (Organism: Mus musculus, class: Ion channel, accessions: P04760, gene: Chrng, swissprot: ACHG_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19422391) Adiphenine is a ternary amino ligand. Adiphenine reduced the muscle tone of the gastrointestinal tract, bile duct and gallbladder, bronchi, bladder. It affects the tone of the muscles of the eye, causing the pupil dilated (mydriasis), increased intraocular pressure, and paralysis of accommodation. Influences on the cardiovascular system, causing tachycardia and improving AV-conduction. It is used as a local anesthetic that reduces the frequency of acetylcholine-induced single-channel currents. It was originally introduced as a spasmolytic agent. 1964-04-30 Ministry of Health of the Russian Federation
Click to view ambutonium
Click to view dimepheptanol
Click to view biperiden Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1346637) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1346637) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1346637) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1346637) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1346637) Biperiden is a weak peripheral anticholinergic agent. It has, therefore, some antisecretory, antispasmodic and mydriatic effects. In addition, biperiden possesses nicotinolytic activity. Biperiden was used as an adjunct in the therapy of all forms of parkinsonism and in the control of extrapyramidal disorders due to central nervous system drugs. Anticholinergic (Code: N0000175574) antidote to sarin poisoning (Code: CHEBI:136860) antidyskinesia agent (Code: CHEBI:66956) muscarinic antagonist (Code: CHEBI:48876) parasympatholytic (Code: CHEBI:50370) antiparkinson drug (Code: CHEBI:48407) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) 1959-09-08 FDA
Click to view lodoxamide G-protein coupled receptor 35 (Organism: Homo sapiens, class: GPCR, accessions: Q9HC97, gene: GPR35, swissprot: GPR35_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/24113750) Lodoxamide is a mast cell stabilizer that inhibits the in vivo Type I immediate hypersensitivity reaction. Lodoxamide therapy inhibits the increases in cutaneous vascular permeability that are associated with reagin or IgE and antigen-mediated reactions. When applied topically to the eye, this drug prevents the symptoms associated with keratitis or conjunctivitis. Decreased Histamine Release (Code: N0000175628) Mast Cell Stabilizer (Code: N0000175630) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1993-09-23 FDA
Click to view pyrrobutamine
Click to view propamidine Propamidine is a member of the aromatic diamidine class of compounds, which possess bacteriostatic properties against a wide range of organisms. These diamidines exert antibacterial action against pyogenic cocci, antibiotic resistant staphylococci and some gram negative bacilli. It also has antifungal properties. It is used topically as a isethionic salt for the treatment of minor eye infections such as conjunctivitis and blepharitis. antiseptic drug (Code: CHEBI:48218) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) 1990-10-12 UK Medicines and Healthcare Products Regulatory Agency (MHRA) TNT
Click to view sulfaphenazole Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Dihydropteroate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AC13, gene: folP, swissprot: DHPS_ECOLI) inhibitor (Source: ) A sulfonilamide anti-infective agent. antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) 1974-04-02 FDA
Click to view artemotil Artemotil is a semi-synthetic derivative of artemisinin, a natural product of the Chinese plant Artemisia annua. It was used for the treatment of severe malaria infections in children and adolescents. Amebicides (Code: D000563) Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Antiprotozoal Agents (Code: D000981) Schistosomicides (Code: D012556)
Click to view ibuprofen guaiacol ester Ibuprofen guaiacol ester is a ibuprofen prodrug. (See: ibuprofen) (See: guaiacol)
Click to view oseltamivir Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19439487) Oseltamivir is an prodrug requiring ester hydrolysis for conversion to the active form, oseltamivir carboxylate. Oseltamivir carboxylate is an inhibitor of influenza virus neuraminidase affecting release of viral particles. prodrug (Code: CHEBI:50266) EC 3.2.1.18 (exo-alpha-sialidase) inhibitor (Code: CHEBI:52425) antiviral drug (Code: CHEBI:36044) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Neuraminidase Inhibitor (Code: N0000175524) Neuraminidase Inhibitors (Code: N0000175436) 1999-10-27 FDA
Click to view praziquantel Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12920490) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12920490) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12920490) Praziquantel induces a rapid contraction of schistosomes by a specific effect on the permeability of the cell membrane. The drug further causes vacuolization and disintegration of the schistosome tegument. However, the mechanism of action is unknown. Praziquantel is active against schistosoma (for example, Schistosoma mekongi, Schistosoma japonicum, Schistosoma mansoni and Schistosoma hematobium), and infections due to the liver flukes, Clonorchis sinensis/Opisthorchis viverrini. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antihelminthic (Code: N0000175481) 1982-12-29 FDA PZQ
Click to view granisetron 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022198s016lbl.pdf) 5-hydroxytryptamine receptor 3B (Organism: Homo sapiens, class: Ion channel, accessions: O95264, gene: HTR3B, swissprot: 5HT3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022198s016lbl.pdf) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022198s016lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022198s016lbl.pdf) Granisetron is a selective 5-hydroxytryptamine3 (5-HT3) receptor antagonist with little or no affinity for other serotonin receptors, including 5-HT1, 5-HT1A, 5-HT1B/C, 5-HT2; for alpha1-, alpha2-, or beta-adrenoreceptors; for dopamine-D2; or for histamine-H1; benzodiazepine; picrotoxin or opioid receptors. Granisetron is indicated for the prevention of nausea and vomiting in patients receiving moderately and/or highly emetogenic chemotherapy for up to 5 consecutive days. Serotonin 3 Receptor Antagonists (Code: N0000175817) Serotonin-3 Receptor Antagonist (Code: N0000175818) serotonergic antagonist (Code: CHEBI:48279) antiemetic (Code: CHEBI:50919) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) 1993-12-29 FDA CWB
Click to view glybuthiazol Glybuthiazol is a sulfonamide derivative with antihyperglycemic activity. Like sulfonylureas, glybuthiazol is able to lower blood glucose levels by increasing the release of insulin from pancreatic beta cells.
Click to view olanzapine D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) 5-hydroxytryptamine receptor 3B (Organism: Homo sapiens, class: Ion channel, accessions: O95264, gene: HTR3B, swissprot: 5HT3B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Dimethylaniline monooxygenase [N-oxide-forming] 3 (Organism: Homo sapiens, class: Enzyme, accessions: P31513, gene: FMO3, swissprot: FMO3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020592s071,021086s046,021253s059lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12031686) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25863120) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12873512) Olanzapine is an atypical antipsychotic that is used currently in the treatment of schizophrenia and bipolar illness. The mechanism of action of olanzapine, as with other drugs having efficacy in schizophrenia, is unknown. As a selective monoaminergic antagonist, olanzapine binds with high affinity binding to the following receptors: serotoninergic, dopaminergic, muscarinic M1-5, histamine H1, and alpha-1-adrenergic receptors; it binds weakly to gamma-aminobutyric acid type A, benzodiazepine, and beta-adrenergic receptors. histamine antagonist (Code: CHEBI:37956) muscarinic antagonist (Code: CHEBI:48876) serotonergic antagonist (Code: CHEBI:48279) dopaminergic antagonist (Code: CHEBI:48561) antiemetic (Code: CHEBI:50919) serotonin uptake inhibitor (Code: CHEBI:50949) second generation antipsychotic (Code: CHEBI:65191) Antiemetics (Code: D000932) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Gastrointestinal Agents (Code: D005765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) Tranquilizing Agents (Code: D014149) Atypical Antipsychotic (Code: N0000175430) 1996-09-30 FDA
Click to view tibolone Tibolone is rapidly metabolised into three compounds. Two of the metabolites (3?-OH-tibolone and 3?-OH-tibolone) have oestrogenic-like activities, whereas the third metabolite (4?-isomer of tibolone) has progestogenic and androgenic-like activities. Tibolone is indicated for the treatment of oestrogen deficiency symptoms in postmenopausal women, more than one year after menopause and for the prevention of osteoporosis in postmenopausal women at high risk of future fractures who are intolerant of, or contraindicated for, other medicinal products approved for the prevention of osteoporosis. Anabolic Agents (Code: D045930) Androgen Antagonists (Code: D000726) bone density conservation agent (Code: CHEBI:50646) hormone agonist (Code: CHEBI:51060) Antihypertensive Agents (Code: D000959) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Cardiovascular Agents (Code: D002317) Estrogen Receptor Modulators (Code: D020847) Hormone Antagonists (Code: D006727) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1987-12-12 Ministry of Health, Welfare and Sport (Netherlands)
Click to view levonorgestrel 3-oxo-5-alpha-steroid 4-dehydrogenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P18405, gene: SRD5A1, swissprot: S5A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11075290) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19836445) Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6645495) A synthetic progestational hormone with actions similar to those of progesterone. It is used for contraception, control of menstrual disorders, and treatment of endometriosis. Inhibit Ovum Fertilization (Code: N0000175830) Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) Progestin-containing Intrauterine Device (Code: N0000175832) contraceptive drug (Code: CHEBI:49323) synthetic oral contraceptive (Code: CHEBI:49326) female contraceptive drug (Code: CHEBI:49324) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102) 1968-04-16 FDA NOG
Click to view ethisterone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Polyphenol oxidase 2 (Organism: Agaricus bisporus, class: Enzyme, accessions: O42713, gene: PPO2, swissprot: PPO2_AGABI Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN 17 alpha-Hydroxypregn-4-en-20-yn-3-one. A synthetic steroid hormone with progestational effects.
Click to view dydrogesterone Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14670641) A synthetic progestational hormone with no androgenic or estrogenic properties. Unlike many other progestational compounds, dydrogesterone produces no increase in temperature and does not inhibit OVULATION. Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Progestins (Code: D011372) FDA
Click to view demegestone a norprogesterone derivative that acts like PROGESTERONE in increasing SEX HORMONE-BINDING GLOBULIN; structure
Click to view profenamine Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/21459491/) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/21459491/) Butyrylcholinesterase (Organism: Equus caballus, class: Enzyme, accessions: Q9N1N9, gene: BCHE, swissprot: Q9N1N9_HORSE) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/21740955/) Profenamine (ethopropazine) is a medication derived from phenothiazine. Ethopropazine's antiparkinson action can be attributed to its anticholinergic properties. Ethopropazine partially blocks central (striatal) cholinergic receptors, thereby helping to balance cholinergic and dopaminergic activity in the basal ganglia; salivation may be decreased, and smooth muscle may be relaxed. Ethopropazine's local anesthetic effect is due to its antagonism of the NMDA glutamate receptor. It wasy used as an antidyskinetic to treat parkinsonism. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) muscarinic antagonist (Code: CHEBI:48876) antiparkinson drug (Code: CHEBI:48407) histamine antagonist (Code: CHEBI:37956) adrenergic antagonist (Code: CHEBI:37887) antidyskinesia agent (Code: CHEBI:66956) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) 1952-12-31 Health Canada BUW
Click to view lonazolac Lonazolac is a nonsteroidal anti-inflammatory drug and an acetic acid derivative. Lonazolac is indicated for the treatment of painful inflammatory rheumatic diseases of the joints and the spine. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antineoplastic agent (Code: CHEBI:35610) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1984-12-03 National Authority of Medicines and Health Products (Portugal)
Click to view brompheniramine Brompheniramine is a first-generation antihistamine. Brompheniramine is a histamine H1 antagonist (or more correctly, an inverse histamine agonist) of the alkylamine class. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies. Dexbrompheniramine is the (pharmacologically active) (S)-(+)-enantiomer of brompheniramine. Brompheniramine is used for the treatment of the symptoms of the common cold and allergic rhinitis, such as runny nose, itchy eyes, watery eyes, and sneezing. Anti-Allergic Agents (Code: D018926) H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) brompheniramine: 1957-08-23 FDA dexbrompheniramine : 1963-10-18 FDA
Click to view flunitrazepam GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47870|P18507, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18430052) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12640218) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9848110) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9848110) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9848110) Flunitrazepam is an intermediate-acting benzodiazepine with general properties similar to those of diazepam. It is used for short-term treatment for chronic or severe insomniacs who are unresponsive to other hypnotics. The main pharmacological effects of Flunitrazepam are the enhancement of GABA at the GABAA receptor. It causes partial amnesia. Chronic use of Flunitrazepam can result in physical dependence and the appearance of a withdrawal syndrome when the drug is discontinued. Flunitrazepam impairs cognitive and psychomotor functions affecting reaction time and driving skill. Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1976-01-01 YEAR INTRODUCED
Click to view flubendazole Flubendazole is a member of the class of mebendazole. Flubendazole is a broad-spectrum anthelmintic, it is used, particularly in veterinary medicine, for the treatment of nematodal infections. Anthelmintics (Code: D000871) antinematodal drug (Code: CHEBI:35444) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) 1980-03-10 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view benorilate Benorilate is the acetylsalicylic ester of paracetamol. It has analgesic, anti-inflammatory and antipyretic properties. It is used in the treatment of common cold or influenza. Alto it is used to relieve mild to moderate pain such as headache, joint pain, migraine, toothache, muscle pain, neuralgia, dysmenorrhea. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) China Food and Drug Administration (CFDA)
Click to view ethylmorphine A narcotic analgesic and antitussive. It is metabolized in the liver by ETHYLMORPHINE-N-DEMETHYLASE and used as an indicator of liver function. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689)
Click to view xenysalate
Click to view reboxetine Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200323/8e4d3975fd525061fe33f93a1d51390f754055b1) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200323/8e4d3975fd525061fe33f93a1d51390f754055b1) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200323/8e4d3975fd525061fe33f93a1d51390f754055b1) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200323/8e4d3975fd525061fe33f93a1d51390f754055b1) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200323/8e4d3975fd525061fe33f93a1d51390f754055b1) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/12649369/) Reboxetine is a highly selective and potent inhibitor of noradrenaline reuptake. It has only a weak effect on the 5-HT reuptake and does not affect the uptake of dopamine. Reboxetine is indicated for the acute treatment of depressive illness/major depression and for maintaining the clinical improvement in patients initially responding to treatment. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) 1997-11-06 Italian Medicines Agency (AIFA) 41X
Click to view arbutamine Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/8723169) Arbutamine is a synthetic catecholamine with positive chronotropic and inotropic properties. The chronotropic (increase in heart rate [HR]) and inotropic (increase in force of contraction) effects of arbutamine serve to mimic exercise by increasing cardiac work (producing stress) and provoke myocardial ischemia in patients with compromised coronary arteries. The beta-agonist activity of arbutamine provides cardiac stress by increasing HR, cardiac contractility, and systolic blood pressure. Arbutamine was indicated for diagnosing the presence or absence of coronary artery disease in patients. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) beta-adrenergic agonist (Code: CHEBI:35522) cardiotonic drug (Code: CHEBI:38147) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1997-09-12 FDA
Click to view oxyfedrine A drug used in the treatment of angina pectoris, heart failure, conduction defects, and myocardial infarction. It is a partial agonist at beta adrenergic receptors and acts as a coronary vasodilator and cardiotonic agent. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) Vasodilator Agents (Code: D014665)
Click to view indisetron 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/19967488) an anti-emetic agent, indisetron hydrochloride was developed in Japan
Click to view fenalcomine
Click to view chlorozotocin 2-chloroethyl analog of streptozotocin with superior activity against leukemia L1210 and reduced bone marrow toxicity; RN given refers to (D)-isomer; structure Antineoplastic Agents (Code: D000970) Carcinogens (Code: D002273) Noxae (Code: D009676)
Click to view amoxapine 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: ) 5-hydroxytryptamine receptor 2C (Organism: Rattus norvegicus, class: GPCR, accessions: P08909, gene: Htr2c, swissprot: 5HT2C_RAT) antagonist (Source: ) 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT) antagonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT) antagonist (Source: ) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: ) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) Sodium- and chloride-dependent glycine transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y345, gene: SLC6A5, swissprot: SC6A5_HUMAN) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT The N-demethylated derivative of the antipsychotic agent LOXAPINE that works by blocking the reuptake of norepinephrine, serotonin, or both. It also blocks dopamine receptors. Tricyclic Antidepressant (Code: N0000175752) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) antidepressant (Code: CHEBI:35469) adrenergic uptake inhibitor (Code: CHEBI:35640) dopaminergic antagonist (Code: CHEBI:48561) serotonin uptake inhibitor (Code: CHEBI:50949) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) 1980-09-22 FDA
Click to view dantrolene Ryanodine receptor 1 (Organism: Homo sapiens, class: Ion channel, accessions: P21817, gene: RYR1, swissprot: RYR1_HUMAN) antagonist (Source: ) Ryanodine receptor 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q15413, gene: RYR3, swissprot: RYR3_HUMAN) antagonist (Source: ) Skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in the muscle fiber. It is used in spasticity and other neuromuscular abnormalities. Although the mechanism of action is probably not central, dantrolene is usually grouped with the central muscle relaxants. Decreased Striated Muscle Contraction (Code: N0000008953) Decreased Striated Muscle Tone (Code: N0000175735) Skeletal Muscle Relaxant (Code: N0000175738) muscle relaxant (Code: CHEBI:51371) Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) 1974-01-15 FDA
Click to view pimefylline Pimefylline is an oxopurine. It was used in pimefylline nicotinate form as a coronary vasodilator and muscle relaxant. Italian Medicines Agency (AIFA)
Click to view rofecoxib Prostaglandin E2 receptor EP2 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43116, gene: PTGER2, swissprot: PE2R2_HUMAN) Prostaglandin G/H synthase 1 (Organism: Ovis aries, class: Enzyme, accessions: P05979, gene: PTGS1, swissprot: PGH1_SHEEP) Prostaglandin G/H synthase 2 (Organism: Ovis aries, class: Enzyme, accessions: P79208, gene: PTGS2, swissprot: PGH2_SHEEP) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) Prostaglandin G/H synthase 2 (Organism: Bos taurus, class: Enzyme, accessions: O62698, gene: PTGS2, swissprot: PGH2_BOVIN) Prostaglandin G/H synthase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q05769, gene: Ptgs2, swissprot: PGH2_MOUSE) Prostaglandin G/H synthase 2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P35355, gene: Ptgs2, swissprot: PGH2_RAT) Prostaglandin G/H synthase 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: Q63921, gene: Ptgs1, swissprot: PGH1_RAT) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: ) a sulfonylphenyl furanone; withdrawn out of concern for TOXICITY Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) analgesic (Code: CHEBI:35480) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase 2 Inhibitors (Code: D052246) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1999-05-20 FDA RCX
Click to view valdecoxib Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21341lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21341lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21341lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21341lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/21341lbl.pdf) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Carbonic anhydrase 13 (Organism: Homo sapiens, class: Enzyme, accessions: Q8N1Q1, gene: CA13, swissprot: CAH13_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23067387) Carbonic anhydrase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P53615, gene: NCE103, swissprot: CAN_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19124253) Delta carbonic anhydrase (Organism: Thalassiosira weissflogii, class: Unclassified, accessions: Q5U9J1, gene: ca1, swissprot: Q5U9J1_THAWE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24314394) Valdecoxib is a diaryl substituted isoxazole. Valdecoxib is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic and antipyretic properties in animal models. The mechanism of action is believed to be due to inhibition of prostaglandin synthesis primarily through inhibition of cyclooxygenase-2 (COX-2). At therapeutic plasma concentrations in humans valdecoxib does not inhibit cyclooxygenase-1 (COX-1). Valdecoxib is indicated for relief of the signs and symptoms of osteoarthritis and adult rheumatoid arthritis and for the treatment of primary dysmenorrhea. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antirheumatic drug (Code: CHEBI:35842) antipyretic (Code: CHEBI:35493) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase 2 Inhibitors (Code: D052246) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2001-11-16 FDA COX
Click to view ranitidine Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/019090s053,019593s042lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10223772) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10223772) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10223772) ATP-dependent translocase ABCB1 (Organism: Rattus norvegicus, class: Transporter, accessions: P43245, gene: Abcb1, swissprot: MDR1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12954186) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/29236753) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/29236753) Ranitidine is a member of the class of histamine H2-receptor antagonists with antacid activity. Ranitidine is a competitive and reversible inhibitor of the action of histamine, released by enterochromaffin-like (ECL) cells, at the histamine H2-receptors on parietal cells in the stomach, thereby inhibiting the normal and meal-stimulated secretion of stomach acid. Ranitidine is used for treatment of acid-peptic disease. Histamine H2 Receptor Antagonists (Code: N0000000151) Histamine-2 Receptor Antagonist (Code: N0000175784) H2-receptor antagonist (Code: CHEBI:37961) anti-ulcer drug (Code: CHEBI:49201) drug allergen (Code: CHEBI:88188) Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H2 Antagonists (Code: D006635) Neurotransmitter Agents (Code: D018377) 1977-08-29 FDA
Click to view methopromazine Methopromazine is the 2-methoxy derivative of promazine. Methopromazine was developed as a neuroleptic agent with antipsychotic activity.
Click to view dronabinol Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) activator (Source: ) G-protein coupled receptor 55 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y2T6, gene: GPR55, swissprot: GPR55_HUMAN Cannabinoid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: P34972, gene: CNR2, swissprot: CNR2_HUMAN Cannabinoid receptor (Organism: Homo sapiens, class: GPCR, accessions: P21554|P34972, gene: CNR1|CNR2, swissprot: CNR1_HUMAN|CNR2_HUMAN N-arachidonyl glycine receptor (Organism: Homo sapiens, class: GPCR, accessions: Q14330, gene: GPR18, swissprot: GPR18_HUMAN Cannabinoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P21554, gene: CNR1, swissprot: CNR1_HUMAN) agonist Cannabinoid receptor 1 (Organism: Mus musculus, class: GPCR, accessions: P47746, gene: Cnr1, swissprot: CNR1_MOUSE Cannabinoid receptor 1 (Organism: Rattus norvegicus, class: GPCR, accessions: P20272, gene: Cnr1, swissprot: CNR1_RAT Cannabinoid receptor 2 (Organism: Mus musculus, class: GPCR, accessions: P47936, gene: Cnr2, swissprot: CNR2_MOUSE Cannabinoid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P20272|Q9QZN9, gene: Cnr1|Cnr2, swissprot: CNR1_RAT|CNR2_RAT Glycine receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: P23416, gene: GLRA2, swissprot: GLRA2_HUMAN) allosteric modulator (Source: ) Glycine receptor subunit alpha-3 (Organism: Homo sapiens, class: Ion channel, accessions: O75311, gene: GLRA3, swissprot: GLRA3_HUMAN) allosteric modulator (Source: ) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN Transient receptor potential cation channel subfamily V member 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q9WUD2, gene: Trpv2, swissprot: TRPV2_RAT) activator (Source: ) A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound. Cannabinoid (Code: N0000175782) Cannabinoids (Code: N0000008010) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-narcotic analgesic (Code: CHEBI:35481) hallucinogen (Code: CHEBI:35499) Cannabinoid Receptor Agonists (Code: D063386) Cannabinoid Receptor Modulators (Code: D063385) Central Nervous System Agents (Code: D002491) Hallucinogens (Code: D006213) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) 1985-05-31 FDA TCI
Click to view progesterone Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019781s017,020843s011lbl.pdf) Cation channel sperm-associated protein 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q8NEC5, gene: CATSPER1, swissprot: CTSR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21412339) Cation channel sperm-associated protein 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q7RTX7, gene: CATSPER4, swissprot: CTSR4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21412339) Cation channel sperm-associated protein 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q96P56, gene: CATSPER2, swissprot: CTSR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21412339) Cation channel sperm-associated protein 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q86XQ3, gene: CATSPER3, swissprot: CTSR3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21412339) Short transient receptor potential channel 5 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UL62, gene: TRPC5, swissprot: TRPC5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21108630) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/28949811) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/28949811) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: P24462, gene: CYP3A7, swissprot: CP3A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/28949811) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9328296) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9328296) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9667077) Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12781197) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12781197) Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9464360) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17890094) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17890094) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12110607) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12110607) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12110607) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20448812) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/20448812) Progesterone is a hormone that occurs naturally in females, and is essential for endometrial receptivity, embryo implantation, and the successful establishment of pregnancy. Progesterone is used in various contraceptive preparations to prevent ovulation and fertilization 15, 8 as well as in other formulations to promote and support pregnancy. Pharmaceutical progesterone is made from a plant source as a starting material and is chemically identical to progesterone of human ovarian origin. Progesterone is indicated in amenorrhea and abnormal uterine bleeding due to hormonal imbalance in the absence of organic pathology. contraceptive drug (Code: CHEBI:49323) progesterone receptor agonist (Code: CHEBI:70709) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Progestins (Code: D011372) Progesterone (Code: N0000005934) 1976-02-04 FDA STR
Click to view sulbentine Sulbentine is an antifungal agent.It was used in a concentration of 3% for the treatment of derrnatophyte infections.
Click to view pergolide 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT) agonist (Source: ) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/19385slr030,031,035_permax_lbl.pdf) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) agonist Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) Dopamine receptor (Organism: Bos taurus, class: GPCR, accessions: P20288|Q95136, gene: DRD1|DRD2, swissprot: DRD1_BOVIN|DRD2_BOVIN D(2) dopamine receptor (Organism: Bos taurus, class: GPCR, accessions: P20288, gene: DRD2, swissprot: DRD2_BOVIN D(3) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19020, gene: Drd3, swissprot: DRD3_RAT Dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901|P19020|P25115|P30729|P61169, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_RAT|DRD2_RAT|DRD3_RAT|DRD4_RAT|DRD5_RAT Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P19328|P22086|P22909, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT Cerebral cortex alpha adrenergic receptor (Organism: Bos taurus, class: GPCR, accessions: P18130|Q28838, gene: ADRA1A|ADRA2A, swissprot: ADA1A_BOVIN|ADA2A_BOVIN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) agonist (Source: ) A long-acting dopamine agonist which has been used to treat PARKINSON DISEASE and HYPERPROLACTINEMIA but withdrawn from some markets due to potential for HEART VALVE DISEASES. Ergot Alkaloids (Code: N0000007620) Ergot-derived Dopamine Receptor Agonist (Code: N0000175767) antiparkinson drug (Code: CHEBI:48407) dopamine agonist (Code: CHEBI:51065) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) 1988-12-30 FDA
Click to view clorazepate Clorazepate is an unusually long-lasting benzodiazepine . Clorazepate is a prodrug that is metabolized to its active metabolite nordiazepam. It has depressant effects on the central nervous system. Clorazepate is used in the form of a dipotassium salt. Clorazepate is indicated for the management of anxiety disorders or for theatment of epilepsy and as an anxiolytic for therapy of anxiety and alcohol withdrawal. (See: nordiazepam) Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Anti-Anxiety Agents (Code: D014151) prodrug (Code: CHEBI:50266) anticonvulsant (Code: CHEBI:35623) anxiolytic drug (Code: CHEBI:35474) GABA modulator (Code: CHEBI:50268) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1972-06-23 FDA
Click to view clobenzepam Clobenzepam is a dibenzodiazepine and an antihistaminic.
Click to view homochlorcyclizine
Click to view clomipramine Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12695316) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26372073) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17471183) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22537153) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17471183) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17471183) Glutathione S-transferase P (Organism: Homo sapiens, class: Enzyme, accessions: P09211, gene: GSTP1, swissprot: GSTP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15094841) Trypanothione reductase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P28593, gene: TPR, swissprot: TYTR_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19414258) G protein-activated inward rectifier potassium channel 2 (Organism: Mus musculus, class: Ion channel, accessions: P48542, gene: Kcnj6, swissprot: KCNJ6_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15150531) G protein-activated inward rectifier potassium channel 4 (Organism: Mus musculus, class: Ion channel, accessions: P48545, gene: Kcnj5, swissprot: KCNJ5_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15150531) Clomipramine is a tricyclic antidepressant similar to imipramine that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine. serotonin uptake inhibitor (Code: CHEBI:50949) antidepressant (Code: CHEBI:35469) serotonergic antagonist (Code: CHEBI:48279) serotonergic drug (Code: CHEBI:48278) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) Tricyclic Antidepressant (Code: N0000175752) 1989-12-29 FDA CXX
Click to view loflucarban Loflucarban is a member of thioureas. It is a local fungicide. It is no longer available.
Click to view oxycodone Kappa-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P33534, gene: Oprk1, swissprot: OPRK_MOUSE Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN Acetylcholinesterase (Organism: Electrophorus electricus, class: Enzyme, accessions: O42275, gene: ache, swissprot: ACES_ELEEL Mu-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P42866, gene: Oprm1, swissprot: OPRM_MOUSE Kappa-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P34975, gene: Oprk1, swissprot: OPRK_RAT Delta-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533, gene: Oprd1, swissprot: OPRD_RAT Mu-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33535, gene: Oprm1, swissprot: OPRM_RAT Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist A semisynthetic derivative of CODEINE. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322) antitussive (Code: CHEBI:51177) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) 1950-04-12 FDA
Click to view alizapride D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3397992) Alizapride is a dopamine antagonist with prokinetic and antiemetic effects. The anti-emetic action of alizapride is due to its antagonist activity at D2 receptors in the chemoreceptor trigger zone in the central nervous system. Alizapride is indicated for the treatment and for the prevention of nausea and vomiting. Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373) 1979-01-09 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view protizinic acid Protizinic acid is a phenothiazine derivative. It has antiinflammatory and analgesic activities.
Click to view mitiglinide Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/11716850) a rapid and short-acting hypoglycemic agent; acts on sulfonylurea receptor closing KATP channels; considered one of the glinides-an imprecise grouping; structure given in first source Hypoglycemic Agents (Code: D007004) 2011-04-22 PMDA
Click to view saxagliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022350s023lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022350s023lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022350s023lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022350s023lbl.pdf) Dipeptidyl peptidase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q6V1X1, gene: DPP8, swissprot: DPP8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18468582) Dipeptidyl peptidase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q86TI2, gene: DPP9, swissprot: DPP9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18468582) Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus. Saxagliptin is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other oral hypoglycemic agents. hypoglycemic agent (Code: CHEBI:35526) Dipeptidyl-Peptidase IV Inhibitors (Code: D054873) Enzyme Inhibitors (Code: D004791) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Hypoglycemic Agents (Code: D007004) Incretins (Code: D054795) Protease Inhibitors (Code: D011480) 2009-07-31 FDA
Click to view fendiline Extracellular calcium-sensing receptor (Organism: Homo sapiens, class: GPCR, accessions: P41180, gene: CASR, swissprot: CASR_HUMAN Transcriptional activator protein luxR (Organism: Aliivibrio fischeri, class: Unclassified, accessions: P12746, gene: luxR, swissprot: LUXR_ALIFS 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN Extracellular calcium-sensing receptor (Organism: Bos taurus, class: GPCR, accessions: P35384, gene: CASR, swissprot: CASR_BOVIN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/9520489) Coronary vasodilator; inhibits calcium function in muscle cells in excitation-contraction coupling; proposed as antiarrhythmic and antianginal agents. Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990)
Click to view pamaquine
Click to view rotigotine D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18691132) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18691132) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18691132) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18691132) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18691132) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18691132) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021829s016lbl.pdf) UDP-glucuronosyltransferase 2B15 (Organism: Homo sapiens, class: Enzyme, accessions: P54855, gene: UGT2B15, swissprot: UDB15_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021829s016lbl.pdf) Rotigotine is a non-ergoline dopamine agonist used in the therapy of Parkinson disease and restless leg syndrome. The precise mechanism of action of rotigotine as a treatment for Parkinson's disease is unknown, although it is thought to be related to its ability to stimulate dopamine receptors within the caudate-putamen in the brain. The precise mechanism of action of rotigotine as a treatment for Restless Legs Syndrome is unknown but is thought to be related to its ability to stimulate dopamine receptors. Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) 2007-05-09 FDA
Click to view triclocarban Epoxide hydrolase; Epoxide hydrolase EphB (Organism: Mycobacterium tuberculosis (strain CDC 1551 / Oshkosh), class: Enzyme, accessions: P95276, gene: None, swissprot: P95276_MYCTO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18585390) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/23524099) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/23524099) Triclocarban is a triclosan analogue with an antibmicrobial property. Triclocarban exerts its effect by inhibiting the activity of enoyl-(acyl-carrier protein) (ACP) reductase, which is ubiquitously distributed in bacteria, fungi and various plants. Triclocarban is effective against Gram-positive bacteria such as Staphylococcus aureus. It has been used in a wide range of personal cleansing products including deodorant and bar soaps, deodorants, detergents, cleansing lotions, and wipes. But in 2016 U.S. Food and Drug Administration banned containing triclocarban and triclosan consumer antiseptic wash products from further marketing in USA because of a potential damage to human health, resulting from extended exposure to antiseptic active ingredients on a regular bases. antiseptic drug (Code: CHEBI:48218) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Environmental Pollutants (Code: D004785) Water Pollutants, Chemical (Code: D014874) 1983-12-31 Health Canada
Click to view efavirenz Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020972s057,021360s045lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020972s057,021360s045lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020972s057,021360s045lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020972s057,021360s045lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020972s057,021360s045lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020972s057,021360s045lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020972s057,021360s045lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25914645) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21189339) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21189339) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/21189339) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/21189339) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/21189339) Efavirenz is a non-nucleoside reverse transcriptase (RT) inhibitor of HIV-1. Efavirenz activity is mediated predominantly by noncompetitive inhibition of HIV-1 reverse transcriptase. HIV-2 RT and human cellular DNA polymerases alpha, beta, gamma, and delta are not inhibited by efavirenz. For HIV infection that has not previously been treated, efavirenz and lamivudine in combination with zidovudine or tenofovir is the preferred NNRTI-based regimen. Efavirenz is also used in combination with other antiretroviral agents as part of an expanded postexposure prophylaxis regimen to prevent HIV transmission for those exposed to materials associated with a high risk for HIV transmission. Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175463) Non-Nucleoside Analog (Code: N0000175460) Non-Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009948) Cytochrome P450 3A Inducers (Code: N0000190118) Cytochrome P450 2B6 Inducers (Code: N0000187064) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) antiviral drug (Code: CHEBI:36044) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Cytochrome P-450 CYP2B6 Inducers (Code: D065695) Cytochrome P-450 CYP2C19 Inhibitors (Code: D065689) Cytochrome P-450 CYP2C9 Inhibitors (Code: D065688) Cytochrome P-450 CYP3A Inducers (Code: D065701) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Metabolic Side Effects of Drugs and Substances (Code: D065606) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 1998-09-17 FDA EFZ
Click to view clonazepam GABA-A receptor alpha-1/beta-1/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18505|P18507, gene: GABRA1|GABRB1|GABRG2, swissprot: GBRA1_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/2551039) GABA-A receptor alpha-2/beta-1/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P47869|P18505|P18507, gene: GABRA2|GABRB1|GABRG2, swissprot: GBRA2_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/2551039) GABA-A receptor alpha-3/beta-1/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P34903|P18505|P18507, gene: GABRA3|GABRB1|GABRG2, swissprot: GBRA3_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/2551039) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9574817) Clonazepam is an anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of gamma-aminobutyric acid receptor responses. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) anticonvulsant (Code: CHEBI:35623) GABA modulator (Code: CHEBI:50268) anxiolytic drug (Code: CHEBI:35474) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Neurotransmitter Agents (Code: D018377) 1975-06-04 FDA
Click to view fentiazac Prostaglandin D2 receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5Y4, gene: PTGDR2, swissprot: PD2R2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20031403) Fentiazac is a non-steroidal anti-inflammatory agent. It was used for the treatment of musculoskeletal, joint, and peri-articular disorders and pain. It is no longer available. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1980-05-30 National Authority of Medicines and Health Products (Portugal)
Click to view chlorprothixene 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2891550) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6149136) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://link.springer.com/article/10.1007%2Fs00210-011-0704-0) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) antagonist (Source: https://link.springer.com/article/10.1007%2Fs00210-011-0704-0) Histamine H3 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5N1, gene: HRH3, swissprot: HRH3_HUMAN) antagonist (Source: https://link.springer.com/article/10.1007%2Fs00210-011-0704-0) Histamine H4 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9H3N8, gene: HRH4, swissprot: HRH4_HUMAN) agonist (Source: https://link.springer.com/article/10.1007%2Fs00210-011-0704-0) Pleiotropic ABC efflux transporter of multiple drugs (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Transporter, accessions: P33302, gene: PDR5, swissprot: PDR5_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19188399) Chlorprothixene is a thioxanthine derivative. Chlorprothixene exerts its activity by binding to and inhibiting serotonin receptors, dopamine receptors, muscarinic acetylcholine receptor, histamine H1 receptor and alpha1-adrenergic receptor. It is used for the treatment of psychotic disorders. non-narcotic analgesic (Code: CHEBI:35481) antiemetic (Code: CHEBI:50919) sedative (Code: CHEBI:35717) cholinergic antagonist (Code: CHEBI:48873) dopaminergic antagonist (Code: CHEBI:48561) first generation antipsychotic (Code: CHEBI:65190) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1967-06-19 FDA
Click to view pentaerithrityl tetranitrate Pentaerythritol tetranitrate is a vasodilator with general properties similar to nitroglycerin but with a more prolonged duration of action. Pentaerythritol tetranitrate is used for the treatment of angina pectoris. vasodilator agent (Code: CHEBI:35620) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1974-04-12 Ministry of Health of the Russian Federation
Click to view bromazepam Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00034107.PDF) Bromazepam is a benzodiazepine derivative. Bromazepam binds to the GABA receptor GABAA, causing a conformational change and increasing the inhibitory effects of GABA. It is useful for the short-term, symptomatic relief of manifestations of excessive anxiety in patients with anxiety neurosis. Also it is used as a premedicant prior to minor surgery. Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1975-03-01 Italian Medicines Agency (AIFA)
Click to view febuxostat Xanthine dehydrogenase/oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P47989, gene: XDH, swissprot: XDH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021856s013lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021856s013lbl.pdf) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021856s013lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021856s013lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021856s013lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021856s013lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021856s013lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021856s013lbl.pdf) Febuxostat is an orally available, non-purine inhibitor of xanthine oxidase with uric acid lowering activity. Upon oral administration, febuxostat selectively and noncompetitively inhibits the activity of xanthine oxidase, an enzyme that converts oxypurines, including hypoxanthine and xanthine, into uric acid. By inhibiting xanthine oxidase, uric acid production is reduced and serum uric acid levels are lowered. Febuxostat may provide protection against acute renal failure caused by the excessive release of uric acid that occurs upon massive tumor cell lysis resulting from the treatment of some malignancies. Xanthine Oxidase Inhibitor (Code: N0000175698) Xanthine Oxidase Inhibitors (Code: N0000000206) Antirheumatic Agents (Code: D018501) Gout Suppressants (Code: D006074) 2009-02-13 FDA TEI
Click to view tinoridine Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/19751980) proposed anti-inflammatory agent; minor descriptor (75-86); on-line & INDEX MEDICUS seach PYRIDINES (75-86) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view timolol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021516s005lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021516s005lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17431033) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17431033) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23563132) Timolol is a beta-adrenergic antagonist similar in action to propranolol. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of migraine disorderS and tremor. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) antihypertensive agent (Code: CHEBI:35674) anti-arrhythmia drug (Code: CHEBI:38070) beta-adrenergic antagonist (Code: CHEBI:35530) antiglaucoma drug (Code: CHEBI:39456) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 1978-08-17 FDA TIM
Click to view butalamine Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view pregnenolone succinate Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Glucose-6-phosphate 1-dehydrogenase (Organism: Homo sapiens, class: Enzyme, accessions: P11413, gene: G6PD, swissprot: G6PD_HUMAN Corticosteroid-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P08185, gene: SERPINA6, swissprot: CBG_HUMAN A 21-carbon steroid, derived from CHOLESTEROL and found in steroid hormone-producing tissues. Pregnenolone is the precursor to GONADAL STEROID HORMONES and the adrenal CORTICOSTEROIDS.
Click to view calusterone was MH 1975-92 (see under METHYLTESTOSTERONE 1975-90); use METHYLTESTOSTERONE to search CALUSTERONE 1975-92
Click to view nilutamide Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020169s008lbl.pdf) NADPH--cytochrome P450 reductase (Organism: Rattus norvegicus, class: Enzyme, accessions: P00388, gene: Por, swissprot: NCPR_RAT) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/1311586/) Nilutamide is a nonsteroidal antiandrogen. Nilutamide has demonstrated antiandrogenic activity without other hormonal (estrogen, progesterone, mineralocorticoid, and glucocorticoid) effects. In vitro, nilutamide blocks the effects of testosterone at the androgen receptor level. In vivo, nilutamide interacts with the androgen receptor and prevents the normal androgenic response. Nilutamide is indicated for use in combination with surgical castration for the treatment of metastatic prostate cancer (Stage D2). Androgen Receptor Antagonists (Code: N0000000243) Androgen Receptor Inhibitor (Code: N0000175560) Androgen Antagonists (Code: D000726) antineoplastic agent (Code: CHEBI:35610) androgen antagonist (Code: CHEBI:35497) Antineoplastic Agents (Code: D000970) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1996-09-19 FDA
Click to view zimeldine Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) One of the SEROTONIN UPTAKE INHIBITORS formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of GUILLAIN-BARRE SYNDROME associated with its use. (From Martindale, The Extra Pharmacopoeia, 29th ed, p385) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367)
Click to view oxyphenisatine Oxyphenisatin is a stimulant laxative. Oxyphenisatin was introduced in 1959. Oxyphenisatin was used as a cleansing enema apart from x-ray studies and prior to urinary, gastro-intestinal and cholecystography x-ray examination. Oxyphenisatin was also used for preoperative preparation of the large intestine and colon. Oxyphenisatin was withdrawn in most countries in the early 1970s.
Click to view denopamine Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://pubmed.ncbi.nlm.nih.gov/10531390/) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/18788725/) Denopamine is a selective agonist of beta-1 adrenergic receptor. It is used for the treatment of chronic heart failure. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Protective Agents (Code: D020011) 1988-04-01 PMDA
Click to view tetrabenazine Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021894s013lbl.pdf) Carbonyl reductase [NADPH] 1 (Organism: Homo sapiens, class: Enzyme, accessions: P16152, gene: CBR1, swissprot: CBR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021894s013lbl.pdf) Tetrabenazine is a reversible human vesicular monoamine transporter type 2 inhibitor. It acts within the basal ganglia and promotes depletion of monoamine neurotransmitters serotonin, norepinephrine, and dopamine from stores. It also decreases uptake into synaptic vesicles. Dopamine is required for fine motor movement, so the inhibition of its transmission is efficacious for hyperkinetic movement. Tetrabenazine is indicated for the treatment of chorea associated with Huntington’s disease. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) antipsychotic agent (Code: CHEBI:35476) adrenergic uptake inhibitor (Code: CHEBI:35640) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Vesicular Monoamine Transporter 2 Inhibitor (Code: N0000190856) Vesicular Monoamine Transporter 2 Inhibitors (Code: N0000190855) 2008-08-15 FDA
Click to view nateglinide Sulfonylurea receptor 2, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: O60706|Q14654, gene: ABCC9|KCNJ11, swissprot: ABCC9_HUMAN|KCJ11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021204s023lbl.pdf) Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021204s023lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021204s023lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021204s023lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021204s023lbl.pdf) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17082235) Monocarboxylate transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P53985, gene: SLC16A1, swissprot: MOT1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12237260) Solute carrier family 15 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63424, gene: Slc15a2, swissprot: S15A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10748266) Solute carrier family 15 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P51574, gene: Slc15a1, swissprot: S15A1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10748266) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10854830) Nateglinide is an oral blood glucose-lowering drug of the glinide class used for the treatment of non-insulin-dependent diabetes mellitus. Nateglinide lowers blood glucose levels by stimulating insulin secretion from the pancreas. Nateglinide interacts with the ATP-sensitive potassium (K+ATP ) channel on pancreatic beta-cells. Nateglinide is highly tissue selective with low affinity for heart and skeletal muscle. Glinide (Code: N0000175428) Potassium Channel Antagonists (Code: N0000175448) hypoglycemic agent (Code: CHEBI:35526) Hypoglycemic Agents (Code: D007004) 2000-12-22 FDA
Click to view docosanol Envelope glycoprotein (Organism: Human herpesvirus 1 (strain 17), class: Membrane other, accessions: O09800|P04288|P04488|P06477|P06480|P06484|P06487|P10185|P10211|P10228|P68331|Q69091, gene: gB|gC|gD|gE|gG|gH|gI|gJ|gK|gL|gM|gN, swissprot: GB_HHV11|GC_HHV11|GD_HHV11|GE_HHV11|GG_HHV11|GH_HHV11|GI_HHV11|GJ_HHV11|GK_HHV11|GL_HHV11|GM_HHV11|GN_HHV11) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15571473) Docosanol is used for topical treatment for recurrent herpes simplex labialis episodes (episodes of cold sores or fever blisters). Docosanol exhibits antiviral activity against many lipid enveloped viruses including herpes simplex virus (HSV). Docosanol inhibits fusion between the plasma membrane and the herpes simplex virus (HSV) envelope, thereby preventing viral entry into cells and subsequent viral replication. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2000-07-25 FDA
Click to view butenafine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) Membrane-associated progesterone receptor component 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: P70580, gene: Pgrmc1, swissprot: PGRC1_RAT) Enoyl-[acyl-carrier-protein] reductase [NADH] (Organism: Francisella tularensis subsp. tularensis (strain SCHU S4 / Schu 4), class: Enzyme, accessions: Q5NGQ3, gene: fabI, swissprot: Q5NGQ3_FRATT Squalene epoxidase (Organism: Trichophyton rubrum, class: Enzyme, accessions: Q4JEY0, gene: None, swissprot: Q4JEY0_TRIRU) inhibitor Squalene monooxygenase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q92206, gene: ERG1, swissprot: ERG1_CANAL) studied on experimental dermatophytosis antifungal drug (Code: CHEBI:86327) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Benzylamine Antifungal (Code: N0000175875) Benzylamines (Code: N0000007566) 1996-10-18 FDA
Click to view hexocyclium Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT) antagonist (Source: ) FDA
Click to view amorolfine Amorolfine is a morpholine antifungal drug with broad spectrum of activity. Its fungistatic and fungicidal efficacy is based on an alteration of the fungal cell membrane targeted primarily on sterol biosynthesis. The ergosterol content is reduced and at the same time unusual sterically nonplanar sterols accumulate. Amorolfine is a broad spectrum antimycotic. It is highly active against Candida albicans and other species of Candida, Trichophyton rubrum, Trichophyton interdigitale, Trichophyton mentagrophytes, and other species of Trichophyton, Epidermophyton floccosum, Microsporum, Scopulariops, Aspergillus, Fusarium, Mucorale, Hendersonula, Alternaria, Cladospirum. Amorolfine is administered as a nail lacquer in patients suffering from onychomycosis, as a cream in patients suffering from dermatomycosis. Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 1992-01-09 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view mecloxamine
Click to view pazufloxacin Pazufloxacin is a tricyclic quinolone and broad-spectrum antibiotic. Pazufloxacin inhibits both DNA gyrase and topoisomerase IV enzyme. It is used for the treatment of several infections due to Gram-positive and Gram-negative organisms including anaerobic and drug-resistant strains. Pazufloxacin is indicated for the treatment of the respiratory tract infections including lung abscess and pneumonia, endometritis, prostatitis, cystitis, pyelonephritis, liver abscess, intra-abdominal infections, peritonitis, cholecystitis and other secondary infections due to injuries, post-surgical wounds and burns. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Antitubercular Agents (Code: D000995) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 2002-04-11 PMDA
Click to view phenolphthalein Thymidylate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P04818, gene: TYMS, swissprot: TYSY_HUMAN Thymidylate synthase (Organism: Lactobacillus casei, class: Enzyme, accessions: P00469, gene: thyA, swissprot: TYSY_LACCA Thymidylate synthase (Organism: Enterococcus faecalis (strain ATCC 700802 / V583), class: Enzyme, accessions: Q834R3, gene: thyA, swissprot: TYSY_ENTFA Thymidylate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A884, gene: thyA, swissprot: TYSY_ECOLI An acid-base indicator which is colorless in acid solution, but turns pink to red as the solution becomes alkaline. It is used medicinally as a cathartic. Indicators and Reagents (Code: D007202)
Click to view fluvoxamine Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021519s009lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021519s009lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021519s009lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021519s009lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021519s009lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021519s009lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10774624) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10774624) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7742153) Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/6492080) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Cavia porcellus, class: Ion channel, accessions: O35505, gene: CACNA1C, swissprot: CAC1C_CAVPO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Fluvoxamine is a 2-aminoethyl oxime ether of aralkylketones, with antidepressant, antiobsessive-compulsive, and anxiolytic properties. Fluvoxamine, chemically unrelated to other selective serotonin reuptake inhibitors, selectively blocks serotonin reuptake by inhibiting the serotonin reuptake pump at the presynaptic neuronal membrane. This increases serotonin levels within the synaptic cleft, prolongs serotonergic transmission and decreased serotonin turnover, thereby leading to antidepressant, anxiolytic and antiobsessive-compulsive effects. Fluvoxamine shows no significant affinity for histaminergic, alpha or beta adrenergic, muscarinic, or dopaminergic receptors in vitro. Fluvoxamine is indicated for the treatment of obsessions and compulsions in patients with obsessive compulsive disorder. Serotonin Reuptake Inhibitor (Code: N0000175696) Anti-Anxiety Agents (Code: D014151) serotonin uptake inhibitor (Code: CHEBI:50949) anxiolytic drug (Code: CHEBI:35474) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Cytochrome P-450 CYP1A2 Inhibitors (Code: D065609) Cytochrome P-450 CYP2C19 Inhibitors (Code: D065689) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Membrane Transport Modulators (Code: D049990) Metabolic Side Effects of Drugs and Substances (Code: D065606) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) Tranquilizing Agents (Code: D014149) 1994-12-05 FDA FVX
Click to view methscopolamine Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN A muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors. Anticholinergic (Code: N0000175574) Cholinergic Antagonists (Code: N0000175370) Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) 1953-04-09 FDA 3C0
Click to view oxymesterone
Click to view bietamiverine Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN
Click to view tiemonium
Click to view eltanolone GABA-A receptor; anion channel (Organism: Rattus norvegicus, class: Ion channel, accessions: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14, gene: Gabra1|Gabra2|Gabra3|Gabra4|Gabra5|Gabra6|Gabrb1|Gabrb2|Gabrb3|Gabrd|Gabre|Gabrg1|Gabrg2|Gabrg3|Gabrp|Gabrq, swissprot: GBRA1_RAT|GBRA2_RAT|GBRA3_RAT|GBRA4_RAT|GBRA5_RAT|GBRA6_RAT|GBRB1_RAT|GBRB2_RAT|GBRB3_RAT|GBRD_RAT|GBRE_RAT|GBRG1_RAT|GBRG2_RAT|GBRG3_RAT|GBRP_RAT|Q91ZM7_RAT GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) A pregnane found in the urine of pregnant women and sows. It has anesthetic, hypnotic, and sedative properties. Anesthetics (Code: D000777) intravenous anaesthetic (Code: CHEBI:38877) sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) P9N
Click to view tridihexethyl Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist synonym Pathilon refers to chloride; RN given refers to parent cpd; structure anti-ulcer drug (Code: CHEBI:49201) muscarinic antagonist (Code: CHEBI:48876) antispasmodic drug (Code: CHEBI:53784) 1954-09-15 FDA
Click to view lixisenatide Glucagon-like peptide 1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P43220, gene: GLP1R, swissprot: GLP1R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208471Orig1s000lbl.pdf) A synthetic glucagon-like peptide-1 receptor agonist that binds glp-1 receptor that is used to control blood sugar levels in patients with type 2 diabetes; amino acid sequence is H-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSK KKKKK-NH2 (ZP10A). Hypoglycemic Agents (Code: D007004) neuroprotective agent (Code: CHEBI:63726) hypoglycemic agent (Code: CHEBI:35526) GLP-1 Receptor Agonist (Code: N0000178480) Glucagon-Like Peptide 1 (Code: N0000170335) Glucagon-like Peptide-1 (GLP-1) Agonists (Code: N0000020058) 2013-02-01 EMA
Click to view tiludronic acid 72 kDa type IV collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P08253, gene: MMP2, swissprot: MMP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24071448) Tiludronic acid is a first generation (non-nitrogenous) bisphosphonate characterized by a (4-chlorophenylthio) group on the carbon atom of the basic P-C-P structure common to all bisphosphonates. tiludronate disodium acts primarily on bone through a mechanism that involves inhibition of osteoclastic activity with a probable reduction in the enzymatic and transport processes that lead to resorption of the mineralized matrix. Tiludronic acid is indicated for treatment of Paget's disease of bone (osteitis deformans) in patients who have a level of serum alkaline phosphatase at least twice the upper limit of normal, or who are symptomatic, or who are at risk for future complications of their disease. Bone Density Conservation Agents (Code: D050071) Bisphosphonate (Code: N0000175579) Diphosphonates (Code: N0000007707) 1997-03-07 FDA
Click to view clotiazepam GABA-A receptor alpha-1/beta-2/gamma-1 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47870|Q8N1C3, gene: GABRA1|GABRB2|GABRG1, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16272224) Clotiazepam is a compound of the benzodiazepine class. Clotiazepam exerts its action by binding and activating GABA-A receptors. This agonizes the action of GABA, increasing the frequency of opening of the channel chlorinates and penetration of the ions chlorinates through the ionophore. Increase in membrane polarization decreases the probability of discharge of neurons. In some countries it is a schedule drug. It is used for the treatment of insomnia, anxiety and before anesthesia. 1981-03-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view chlorpromazine 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9655845) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8301582) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8301582) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11561066) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9760039) 5-hydroxytryptamine receptor 7 (Organism: Mus musculus, class: GPCR, accessions: P32304, gene: Htr7, swissprot: 5HT7R_MOUSE) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8394987) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15821958) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15821958) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1826762) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1826762) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12788816) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2835476) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15765260) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15765260) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15765260) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10901285) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10901285) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9574817) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1654884) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12031686) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12031686) Trypanothione reductase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P28593, gene: TPR, swissprot: TYTR_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8879546) Calmodulin-1 (Organism: Homo sapiens, class: Cytosolic other, accessions: P0DP23, gene: CALM1, swissprot: CALM1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19013822) Potassium channel subfamily K member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O95069, gene: KCNK2, swissprot: KCNK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26588045) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20853847) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12739759) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2606755) Pleiotropic ABC efflux transporter of multiple drugs (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Transporter, accessions: P33302, gene: PDR5, swissprot: PDR5_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19188399) Chlorpromazine is a phenothiazine and traditional antipsychotic agent with anti-emetic activity. Chlorpromazine acts as an antagonist on different postsysnaptic receptors - on dopaminergic-receptors, serotonergic-receptors, histaminergic-receptors, alpha1/alpha2-receptors and on muscarinic M1/M2-receptors. Additionally, Chlorpromazine is a weak presynaptic inhibitor of Dopamine reuptake, which may lead to (mild) antidepressive and antiparkinsonian effects. Chlorpromazine is used for treating psihotic disorders, the manic phase of manic-depressive disorder, anxiety and restlessness before surgery, the blood disease porphyria, severe behavioral and conduct disorders in children, nausea and vomiting, and severe hiccups. Phenothiazine (Code: N0000175746) Phenothiazines (Code: N0000007544) antiemetic (Code: CHEBI:50919) dopaminergic antagonist (Code: CHEBI:48561) phenothiazine antipsychotic drug (Code: CHEBI:37930) Antiemetics (Code: D000932) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1957-09-18 FDA Z80
Click to view ibandronic acid Farnesyl pyrophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P14324, gene: FDPS, swissprot: FPPS_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021858s022lbl.pdf) Farnesyl pyrophosphate synthase (Organism: Rattus norvegicus, class: Unclassified, accessions: P05369, gene: Fdps, swissprot: FPPS_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18325729) a potent inhibitor of bone resorption. Ibandronic Acid is used in the treatment of hypercalcemia associated with malignancy, for the prevention of fracture and bone complications in patients with breast cancer and bone metastases, and for the treatment and prevention of postmenopausal osteoporosis. Bisphosphonate (Code: N0000175579) Diphosphonates (Code: N0000007707) Bone Density Conservation Agents (Code: D050071) 2003-05-16 FDA BFQ
Click to view norfloxacin DNA gyrase subunit A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES4, gene: gyrA, swissprot: GYRA_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019384s067lbl.pdf) DNA topoisomerase 4 subunit A (Organism: Staphylococcus aureus, class: Enzyme, accessions: P0C1U9, gene: parC, swissprot: PARC_STAAU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16392790) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10411577) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10411577) Norfloxacin inhibits bacterial deoxyribonucleic acid synthesis and is bactericidal. At the molecular level, three specific events are attributed to norfloxacin in E. coli cells: 1) inhibition of the ATP-dependent DNA supercoiling reaction catalyzed by DNA gyrase, 2) inhibition of the relaxation of supercoiled DNA, 3) promotion of double-stranded DNA breakage. The fluorine atom at the 6 position provides increased potency against gram-negative organisms, and the piperazine moiety at the 7 position is responsible for antipseudomonal activity. Quinolone Antimicrobial (Code: N0000175937) Quinolones (Code: N0000007606) antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Cytochrome P-450 CYP1A2 Inhibitors (Code: D065609) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Metabolic Side Effects of Drugs and Substances (Code: D065606) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1986-10-31 FDA
Click to view oxetorone treatment of migraine; RN given refers to parent cpd; structure
Click to view epalrestat Aldo-keto reductase family 1 member B10 (Organism: Homo sapiens, class: Enzyme, accessions: O60218, gene: AKR1B10, swissprot: AK1BA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20304656) Aldose reductase (Organism: Homo sapiens, class: Enzyme, accessions: P15121, gene: AKR1B1, swissprot: ALDR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22104435) Aldo-keto reductase family 1 member A1 (Organism: Homo sapiens, class: Enzyme, accessions: P14550, gene: AKR1A1, swissprot: AK1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22104435) Epalrestat is a non-competitive, reversible inhibitor of aldose reductase, with potential antineoplastic, antioxidant, and anti-inflammatory activities. Epalrestat is used for the improvement of subjective neuropathy symptoms, abnormality of vibration sense, and abnormal changes in heart beat associated with diabetic peripheral neuropathy. Enzyme Inhibitors (Code: D004791) 1992-01-01 PMDA
Click to view cyclodrine
Click to view lanoconazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10520160) Lanoconazole is a conazole antifungal drug and an imidazole antifungal drug. Lanoconazole is a racemic mixture, and further studies revealed that its antifungal activity is attributed to the R-enantiomer, and the latter has at least two-fold more potent antifungal activity when compared with the racemic compound. Lanoconazole was used in the treatment of hyperkeratotic type tinea pedis. 1994 PMDA
Click to view glyhexamide Glyhexamide is a sulfonylurea with antihyperglycemic activity. This hypoglycemic activity is not accompanied by increases in serum (immunoreactive) insulin concentrations.
Click to view chloroquine Glutathione S-transferase (Organism: Plasmodium falciparum, class: Enzyme, accessions: Q8MU52, gene: GST, swissprot: GST_PLAFA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16385005) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12756207) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12756207) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12756207) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12756207) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) weak substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16917012) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16917012) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14729380) Ribosyldihydronicotinamide dehydrogenase [quinone] (Organism: Homo sapiens, class: Enzyme, accessions: P16083, gene: NQO2, swissprot: NQO2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21074425) Toll-like receptor 7 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q9NYK1, gene: TLR7, swissprot: TLR7_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22239408) Major prion protein (Organism: Homo sapiens, class: Surface antigen, accessions: P04156, gene: PRNP, swissprot: PRIO_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12904059) Chloroquine is an anti-protozoal agent. The precise mechanism by which it exhibits activity is not known. Chloroquine, may exert its effect against Plasmodium species by concentrating in the acid vesicles of the parasite and by inhibiting polymerization of heme. It can also inhibit certain enzymes by its interaction with DNA. Chloroquine is active against the erythrocytic forms of susceptible strains of Plasmodium falciparum, Plasmodium malariae, Plasmodium ovale, and Plasmodium vivax. Chloroquine is not active against the gametocytes and the exoerythrocytic forms including the hypnozoite stage of the Plasmodium parasites. Chloroquine is active against the trophozoites of Entamoeba histolytica. Chloroquine is used for the treatment of uncomplicated malaria due to susceptible strains of P. falciparum, P.malariae, P. ovale, and P.vivax, for the prophylaxis of malaria in geographic areas where resistance to chloroquine is not present and for the treatment of extraintestinal amebiasis. Amebicides (Code: D000563) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anthelmintics (Code: D000871) antirheumatic drug (Code: CHEBI:35842) dermatologic drug (Code: CHEBI:50177) antimalarial (Code: CHEBI:38068) Anti-Infective Agents (Code: D000890) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antimalarials (Code: D000962) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Antirheumatic Agents (Code: D018501) Filaricides (Code: D005369) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1949-10-31 FDA 0TX
CLQ
Click to view enoxacin DNA gyrase subunit A (Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd), class: Enzyme, accessions: P43700, gene: gyrA, swissprot: GYRA_HAEIN) V-type proton ATPase subunit B, brain isoform (Organism: Homo sapiens, class: Enzyme, accessions: P21281, gene: ATP6V1B2, swissprot: VATB2_HUMAN) Topoisomerase IV (Organism: Neisseria gonorrhoeae, class: Enzyme, accessions: P48374|Q5EP76, gene: parC|topB, swissprot: PARC_NEIGO|Q5EP76_NEIGO) inhibitor (Source: ) DNA gyrase (Organism: Neisseria gonorrhoeae, class: Enzyme, accessions: P22118|P48371, gene: gyrA|gyrB, swissprot: GYRA_NEIGO|GYRB_NEIGO) inhibitor (Source: ) A broad-spectrum 6-fluoronaphthyridinone antibacterial agent that is structurally related to NALIDIXIC ACID. antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Cytochrome P-450 CYP1A2 Inhibitors (Code: D065609) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Metabolic Side Effects of Drugs and Substances (Code: D065606) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1991-12-31 FDA
Click to view mycophenolic acid Inosine-5'-monophosphate dehydrogenase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P12268, gene: IMPDH2, swissprot: IMDH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/050791s024lbl.pdf) Inosine-5'-monophosphate dehydrogenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P20839, gene: IMPDH1, swissprot: IMDH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/050791s024lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15258099) UDP-glucuronosyltransferase 1-7 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW7, gene: UGT1A7, swissprot: UD17_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15258099) UDP-glucuronosyltransferase 1-10 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW8, gene: UGT1A10, swissprot: UD110_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15258099) UDP-glucuronosyltransferase 1-8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW9, gene: UGT1A8, swissprot: UD18_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15258099) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15258099) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21123165) Mycophenolic Acid is an antineoplastic antibiotic derived from various Penicillium fungal species. Mycophenolic acid is an active metabolite of the prodrug mycophenolate mofetil. Mycophenolic Acid blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase. Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-cells, lymphocytes, and the formation of antibodies from B-cells. It may also inhibit recruitment of leukocytes to sites of inflammation. Antimetabolite Immunosuppressant (Code: N0000175613) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antibiotics, Antineoplastic (Code: D000903) Antibiotics, Antitubercular (Code: D000904) Antineoplastic Agents (Code: D000970) Antitubercular Agents (Code: D000995) Enzyme Inhibitors (Code: D004791) 2004-02-27 FDA MOA
Click to view eterobarb Eterobarb is a barbiturate derivative. It is an effective anticonvulsant as demonstrated in animal and clinical studies. Hypnotic side effects usually associated with barbiturates appear absent. It was not in widespread medical use. It is no longer available.
Click to view mitotane Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/016885s027lbl.pdf) Cytochrome P450 11B1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P15538, gene: CYP11B1, swissprot: C11B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11889204) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9705896) Mitotane is a synthetic derivative of the insecticide dichlorodiphenyl trichloroethane (DDT) with anti-adrenocorticoid properties. Mitotane is an oral chemotherapeutic agent indicated in the treatment of inoperable adrenal cortical carcinoma of both functional and nonfunctional types. Cytochrome P450 3A4 Inducers (Code: N0000185506) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) 1970-07-08 FDA
Click to view feprazone A pyrazole that has analgesic, anti-inflammatory, and antipyretic properties. It has been used in mild to moderate pain, fever, and inflammation associated with musculoskeletal and joint disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p15) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view dibunate
Click to view camylofin Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view timepidium Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10374898) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10374898) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10374898) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10374898) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10374898) Timepidium is a quaternary ammonium antimuscarinic. it is used as a bromide salt used for the symptomatic treatment of visceral painful spasms caused by gastritis, pancreatitis. 1984-08-01 PMDA
Click to view lorazepam GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18384456) Fatty acid-binding protein, liver (Organism: Rattus norvegicus, class: Unclassified, accessions: P02692, gene: Fabp1, swissprot: FABPL_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18533710) Lorazepam is a benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Anti-Anxiety Agents (Code: D014151) Anticonvulsants (Code: D000927) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Gastrointestinal Agents (Code: D005765) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1977-09-30 FDA
Click to view capobenic acid Capobenic acid is an antiarrythmetic agent, vasodilator. It was used for the treatment of cardiac infarction.
Click to view lonidamine Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26831515) Monocarboxylate transporter 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63344, gene: Slc16a7, swissprot: MOT2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26831515) Monocarboxylate transporter 4 (Organism: Rattus norvegicus, class: Transporter, accessions: O35910, gene: SLC16A3, swissprot: MOT4_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26831515) Lonidamine is a derivative of the indazole-3-carboxylic acid. It has potential in modulating the activities of conventional chemotherapeutic agents such as N-mustard alkylating agents and anthracyclines as well as hyperthermia, radiation therapy and photodynamic therapy. Lonidamine is selective against a broad range of tumors with little to no effect on normal tissues. Lonidamine inhibits lactate export by the proton-linked monocarboxylate transporter and pyruvate uptake into mitochondria via the mitochondrial pyruvate carrier. There is also evidence that the drug may indirectly inhibit hexokinase. It was used for the treatment of lung, breast, prostate and brain neoplasms. It is no longer available. Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Antispermatogenic Agents (Code: D000988) Contraceptive Agents (Code: D003270) Contraceptive Agents, Male (Code: D003272) Noxae (Code: D009676) Radiation-Sensitizing Agents (Code: D011838) Reproductive Control Agents (Code: D012102) Trypanocidal Agents (Code: D014344) Italian Medicines Agency (AIFA)
Click to view carboquone An alkylating agent structurally similar to MITOMYCIN and found to be effective in the treatment of leukemia and various other neoplasms in mice. It causes leukemia and thrombocytopenia in almost all human patients. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676)
Click to view famciclovir Famciclovir is a prodrug of penciclovir, which has demonstrated inhibitory activity against herpes simplex virus types 1 (HSV-1) and 2 (HSV-2) and varicella zoster virus (VZV). In cells infected with HSV-1, HSV-2 or VZV, the viral thymidine kinase phosphorylates penciclovir to a monophosphate form that, in turn, is converted by cellular kinases to the active form penciclovir triphosphate. Biochemical studies demonstrate that penciclovir triphosphate inhibits HSV-2 DNA polymerase competitively with deoxyguanosine triphosphate. Consequently, ?-herpes viral DNA synthesis and, therefore, replication are selectively inhibited. DNA Polymerase Inhibitors (Code: N0000020060) Herpes Simplex Virus Nucleoside Analog DNA Polymerase Inhibitor (Code: N0000180187) Nucleoside Analog (Code: N0000175459) prodrug (Code: CHEBI:50266) antiviral drug (Code: CHEBI:36044) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 1994-06-29 FDA
Click to view gabexate Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) Membrane primary amine oxidase (Organism: Rattus norvegicus, class: Enzyme, accessions: O08590, gene: Aoc3, swissprot: AOC3_RAT) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) Tryptase alpha/beta-1 (Organism: Homo sapiens, class: Enzyme, accessions: Q15661, gene: TPSAB1, swissprot: TRYB1_HUMAN) inhibitor (Source: ) A serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin. Anticoagulants (Code: D000925) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842)
Click to view kebuzone proposed antirheumatic agent; minor descriptor (75-86); on-line & INDEX MEDICUS search PHENYLBUTAZONE/AA Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view phenazocine Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN Mu-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P97266, gene: OPRM1, swissprot: OPRM_CAVPO Mu-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P42866, gene: Oprm1, swissprot: OPRM_MOUSE An opioid analgesic with actions and uses similar to MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1095) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view dihexyverine
Click to view clopidogrel Clopidogrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets. Decreased Platelet Aggregation (Code: N0000008832) P2Y12 Platelet Inhibitor (Code: N0000182142) P2Y12 Receptor Antagonists (Code: N0000182143) Cytochrome P450 2C8 Inhibitors (Code: N0000187062) platelet aggregation inhibitor (Code: CHEBI:50427) anticoagulant (Code: CHEBI:50249) Hematologic Agents (Code: D006401) Neurotransmitter Agents (Code: D018377) Platelet Aggregation Inhibitors (Code: D010975) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P2 Receptor Antagonists (Code: D058919) Purinergic P2Y Receptor Antagonists (Code: D058921) 1997-11-17 FDA CGE
Click to view minodronic acid Farnesyl pyrophosphate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P14324, gene: FDPS, swissprot: FPPS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20394422) Farnesyl diphosphate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P22939, gene: ispA, swissprot: ISPA_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17149863) Minodronic acid is a third-generation bisphosphonate. This drug increases the bone mineral density and the strength by inhibiting osteoclastic bone resorption. It is used for the oral treatment of osteoporosis. 2011-07-11 PMDA M0N
Click to view cyclocoumarol Cyclocoumarol is a member of 4-hydroxycoumarin group and an anti-coagulant/ Its duration is longer than that of dicoumarol without the appearance of haemorrhagic manifestation.
Click to view zeranol A non-steroidal estrogen analog. Estrogens (Code: D004967) Estrogens, Non-Steroidal (Code: D004968) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 27J
Click to view mequitazine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9454781) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9454781) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9454781) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8100134) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8100134) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8100134) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8100134) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8100134) Mequitazine is a histamine H1 antagonist (antihistamine). It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. It provides effective, temporary relief of sneezing, watery and itchy eyes, and runny nose due to hay fever and other upper respiratory allergies. Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1984-12-14 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view aprindine Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y3Q4, gene: HCN4, swissprot: HCN4_HUMAN) Sodium/calcium exchanger 1 (Organism: Homo sapiens, class: Transporter, accessions: P32418, gene: SLC8A1, swissprot: NAC1_HUMAN) Proteasome subunit alpha type-1 (Organism: Homo sapiens, class: Enzyme, accessions: P25786, gene: PSMA1, swissprot: PSA1_HUMAN) Calmodulin (Organism: Homo sapiens, class: Cytosolic other, accessions: P0DP23|P0DP24|P0DP25, gene: CALM1|CALM2|CALM3, swissprot: CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN) inhibitor Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) A class Ib anti-arrhythmia agent used to manage ventricular and supraventricular arrhythmias. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1996-01-01 YEAR INTRODUCED
Click to view bisaramil Bisaramil is an antiarrhythmic drug. It was developed as an inhibitor of calcium transport and as a membrane stabilizer.
Click to view clostebol
Click to view chloramphenicol Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14576103) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) weak inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14576103) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14576103) Chloramphenicol acetyltransferase (Organism: Escherichia coli, class: Enzyme, accessions: P62577, gene: cat, swissprot: CAT_ECOLX) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11709351) Chloramphenicol 3-O phosphotransferase (Organism: Streptomyces venezuelae, class: Enzyme, accessions: Q56148, gene: SVEN_4064, swissprot: CPT_STRVP) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7592948) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10411577) Chloramphenicol is a broad-spectrum antibiotic originally isolated from Streptomyces venezuelae. It is primarily bacteriostatic and acts by inhibition of protein synthesis by interfering with the transfer of activated amino acids from soluble RNA to ribosomes. Chloramphenicol has been active against S. aureus, S. pneumonia, Enterobacter sp., E.coli, H. influenzae, Klebsiella sp., M.lacunata, Neisseria sp. antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) Amphenicol-class Antibacterial (Code: N0000175480) Amphenicols (Code: N0000175479) 1950-12-08 FDA CLM
Click to view mepixanox respiratory analeptic; RN given refers to parent cpd; & in Negwer, 5th ed, #6503
Click to view dimefline
Click to view gliclazide Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17517049) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17517049) Gliclazide is an oral sulfonylurea hypoglycemic agent which is used in type 2 diabetes to stimulate insulin production. hypoglycemic agent (Code: CHEBI:35526) Hypoglycemic Agents (Code: D007004) 1972-01-01 YEAR INTRODUCED GCZ
Click to view guaiapate
Click to view bufetolol proposed beta adrenergic blockader similar to propranolol; minor desriptor (77-86); on line & INDEX MEDICUS search PROPANOLAMINES (77-86); RN given refers to parent compound Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Neurotransmitter Agents (Code: D018377)
Click to view cicloprolol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN)
Click to view piperidolate
Click to view cinnamaverine
Click to view lysergide 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) agonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN Serotonin 2 (5-HT2) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P30994, gene: Htr2a|Htr2b|Htr2c, swissprot: 5HT2A_RAT|5HT2B_RAT|5HT2C_RAT D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN D(1A) dopamine receptor (Organism: Mus musculus, class: GPCR, accessions: Q61616, gene: Drd1, swissprot: DRD1_MOUSE 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN 5-hydroxytryptamine receptor 2C (Organism: Rattus norvegicus, class: GPCR, accessions: P08909, gene: Htr2c, swissprot: 5HT2C_RAT 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Semisynthetic derivative of ergot (Claviceps purpurea). It has complex effects on serotonergic systems including antagonism at some peripheral serotonin receptors, both agonist and antagonist actions at central nervous system serotonin receptors, and possibly effects on serotonin turnover. It is a potent hallucinogen, but the mechanisms of that effect are not well understood. serotonergic agonist (Code: CHEBI:35941) dopamine agonist (Code: CHEBI:51065) hallucinogen (Code: CHEBI:35499) Central Nervous System Agents (Code: D002491) Hallucinogens (Code: D006213) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Serotonin Receptor Agonists (Code: D017366) 1957-01-01 YEAR INTRODUCED 7LD
Click to view tolciclate antifungal drug (Code: CHEBI:86327) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935)
Click to view cyamemazine 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: ) phototoxic neuroleptic effects
Click to view difemerine
Click to view oxysonium
Click to view trofosfamide cyclophosphamide analog; structure Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Mutagens (Code: D009153) Noxae (Code: D009676)
Click to view furaltadone Furaltadone is a nitrofuran antibiotic. It was formerly used oraly but withdrawn due to toxicity, it is used topically (as the hydrochloride salt) for treatment of ear disorders. It is effective against bacterial infections in birds when added to feed or drinking water. antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076)
Click to view efloxate
Click to view valaciclovir Valacyclovir is the L-valyl ester of the antiviral drug acyclovir. After oral administration, valacyclovir is rapidly absorbed from the gastrointestinal tract and nearly completely converted to aciclovir and L-valine by first-pass intestinal and/or hepatic metabolism. (See: aciclovir) Valacyclovir is indicated for the treatment of Cold Sores (Herpes Labialis), Genital Herpes, Herpes Zoster, Chickenpox. DNA Polymerase Inhibitors (Code: N0000020060) Herpes Simplex Virus Nucleoside Analog DNA Polymerase Inhibitor (Code: N0000180187) Herpes Zoster Virus Nucleoside Analog DNA Polymerase Inhibitor (Code: N0000180188) Herpesvirus Nucleoside Analog DNA Polymerase Inhibitor (Code: N0000175468) Nucleoside Analog (Code: N0000175459) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 1995-06-23 FDA TXC
Click to view dolasetron Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/1397053) Dolasetron mesylate is an antinauseant and antiemetic agent. Dolasetron mesylate and its active metabolite, hydrodolasetron (MDL 74,156), are selective serotonin 5-HT3 receptor antagonists not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serotonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. Serotonin 3 Receptor Antagonists (Code: N0000175817) Serotonin-3 Receptor Antagonist (Code: N0000175818) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) 1997-09-11 FDA
Click to view arbutin Tyrosinase (Organism: Homo sapiens, class: Enzyme, accessions: P14679, gene: TYR, swissprot: TYRO_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9711535) Arbutin is a beta-D-glucopyranoside of Hydroquinone which is extracted from the dried leaves of bearberry plant in the Ericaceae family. It is found in foods, over-the-counter drugs, and herbal dietary supplements. Most commonly, it is an active ingredient in skincare and cosmetic products as a skin-lightening agent for the prevention of melanin formation in various skin conditions that involve cutaneous hyperpigmentation or hyperactive melanocyte function. 1994-12-31 Health Canada
Click to view amphotalide
Click to view oxyphenbutazone Cyclooxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P23219|P35354, gene: PTGS1|PTGS2, swissprot: PGH1_HUMAN|PGH2_HUMAN) inhibitor Prostacyclin synthase (Organism: Homo sapiens, class: Enzyme, accessions: Q16647, gene: PTGIS, swissprot: PTGIS_HUMAN) fMet-Leu-Phe receptor (Organism: Homo sapiens, class: GPCR, accessions: P21462, gene: FPR1, swissprot: FPR1_HUMAN) A non-steroidal anti-inflammatory drug. Oxyphenbutazone eyedrops have been used abroad in the management of postoperative ocular inflammation, superficial eye injuries, and episcleritis. (From AMA, Drug Evaluations Annual, 1994, p2000) It had been used by mouth in rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis but such use is no longer considered justified owing to the risk of severe hematological adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p27) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) gout suppressant (Code: CHEBI:35845) antineoplastic agent (Code: CHEBI:35610) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1960-12-21 FDA OPB
Click to view ditazole
Click to view nitracrine Acridine antineoplastic agent used in mammary and ovarian tumors. It inhibits RNA synthesis. Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384)
Click to view citalopram Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT Transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q63380, gene: NET, swissprot: Q63380_RAT Sodium-dependent dopamine transporter (Organism: Mus musculus, class: Transporter, accessions: Q61327, gene: Slc6a3, swissprot: SC6A3_MOUSE Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q9WTR4, gene: Slc6a2, swissprot: Q9WTR4_RAT Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Citalopram is a selective serotonin reuptake inhibitor with a chemical structure unrelated to that of other SSRIs or of tricyclic, tetracyclic, or other available antidepressant agents. Citalopram is a racemic mixture (50/50), and the inhibition of 5-HT reuptake by citalopram is primarily due to the (S)-enantiomer. Escitalopram is at least 100-fold more potent than the R-enantiomer with respect to inhibition of 5-HT reuptake and inhibition of 5-HT neuronal firing rate. Serotonin Reuptake Inhibitor (Code: N0000175696) serotonin uptake inhibitor (Code: CHEBI:50949) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) Citalopram: 1998-07-17 FDA Escitalopram: 2002-08-14 FDA 68P
Click to view acetohexamide Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/10742287) A sulfonylurea hypoglycemic agent that is metabolized in the liver to 1-hydrohexamide. hypoglycemic agent (Code: CHEBI:35526) Hypoglycemic Agents (Code: D007004) 1964-12-23 FDA
Click to view viquidil
Click to view dorzolamide Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020408s050lbl.pdf) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25913118) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8875343) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17826101) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25913118) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8875343) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) topically effective ocular hypotensive carbonic anhydrase inhibitor; RN refers to mono-HCl (4S-trans)-isomer antihypertensive agent (Code: CHEBI:35674) antiglaucoma drug (Code: CHEBI:39456) Antihypertensive Agents (Code: D000959) Carbonic Anhydrase Inhibitors (Code: D002257) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Carbonic Anhydrase Inhibitor (Code: N0000175517) 1994-12-09 FDA ETS
Click to view etonogestrel Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021529s018lbl.pdf) Etonogestrel structurally derived from 19-nortestosterone, is the synthetic biologically active metabolite of the synthetic progestin desogestrel. Etonogestrel is administered in subdermal implants as long-acting reversible contraception. It is known to be effective in postpartum insertion including breastfeeding women. The implant's effect can remain for 5 years. Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) contraceptive drug (Code: CHEBI:49323) female contraceptive drug (Code: CHEBI:49324) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Reproductive Control Agents (Code: D012102) 2001-10-03 FDA
Click to view diampromide
Click to view vorozole Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9797019) Vorozole is a specific, non-steroidal inhibitor of aromatase enzyme. It was developed for the treatment of advanced breast cancer. Antineoplastic Agents (Code: D000970) Aromatase Inhibitors (Code: D047072) Enzyme Inhibitors (Code: D004791) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Steroid Synthesis Inhibitors (Code: D065088)
Click to view prazepam GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator A benzodiazepine that is used in the treatment of ANXIETY DISORDERS. Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) FDA
Click to view elcatonin synthetic S-S bond between 1-7 amino acids displaced by C-C bond; deamino dicarba analog of eel calcitonin; has been given orphan drug approval for intrathecal treatment of intractable pain
Click to view ergometrine D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT) agonist (Source: ) Ergometrine is an ergot alkaloid that has a particularly powerful action on the uterus. Like other ergot alkaloids, ergometrine produces arterial vasoconstriction by stimulation of alpha-adrenergic and serotonin receptors and inhibition of endothelial-derived relaxation factor release. The drug has only slight alpha-adrenergic blocking activity and its vasoconstrictor effects are less than those of ergotamine. Ergometrines maleate (and formerly tartrate) salt is used in the active management of the third stage of labour, and to prevent or treat postpartum of postabortal haemorrhage caused by uterine atony: by maintaining uterine contraction and tone, blood vessels in the uterine wall are compressed and blood flow reduced. oxytocic (Code: CHEBI:36063) diagnostic agent (Code: CHEBI:33295) Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102) 1969-12-31 New Zealand Medicines and Medical Devices Safety Authority
Click to view mecillinam Penicillin-binding protein 2 (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD65, gene: mrdA, swissprot: PBP2_ECOLI) inhibitor An amidinopenicillanic acid derivative with broad spectrum antibacterial action. antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076) FDA
Click to view bisoprolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019982s016lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019982s016lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16671962) Bisoprolol is a synthetic, beta1-selective (cardioselective) adrenoceptor blocking agent without significant membrane stabilizing activity or intrinsic sympathomimetic activity in its therapeutic dosage range. Cardioselectivity is not absolute, however, and at higher doses (? 20 mg) bisoprolol also inhibits beta2-adrenoceptors, chiefly located in the bronchial and vascular musculature; to retain selectivity it is therefore important to use the lowest effective dose. Bisoprolol is indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) antihypertensive agent (Code: CHEBI:35674) beta-adrenergic antagonist (Code: CHEBI:35530) anti-arrhythmia drug (Code: CHEBI:38070) sympatholytic agent (Code: CHEBI:66991) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565) 1992-07-31 FDA
Click to view ifenprodil Glutamate receptor ionotropic, NMDA 1 (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439, gene: Grin1, swissprot: NMDZ1_RAT Glutamate NMDA receptor; GRIN1/GRIN2B (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q13224, gene: GRIN1|GRIN2B, swissprot: NMDE2_HUMAN|NMDZ1_HUMAN Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Alpha-2A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P22909, gene: Adra2a, swissprot: ADA2A_RAT Sigma non-opioid intracellular receptor 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: Q9R0C9, gene: Sigmar1, swissprot: SGMR1_RAT 5-hydroxytryptamine receptor 2A (Organism: Bos taurus, class: GPCR, accessions: Q75Z89, gene: HTR2A, swissprot: 5HT2A_BOVIN Glutamate receptor ionotropic, NMDA 2B (Organism: Homo sapiens, class: Ion channel, accessions: Q13224, gene: GRIN2B, swissprot: NMDE2_HUMAN 3-beta-hydroxysteroid-delta(8),delta(7)-isomerase (Organism: Cavia porcellus, class: Unclassified, accessions: Q60490, gene: EBP, swissprot: EBP_CAVPO Sigma non-opioid intracellular receptor 1 (Organism: Cavia porcellus, class: Membrane other, accessions: Q60492, gene: SIGMAR1, swissprot: SGMR1_CAVPO 5-hydroxytryptamine receptor 1A (Organism: Mus musculus, class: GPCR, accessions: Q64264, gene: Htr1a, swissprot: 5HT1A_MOUSE Glutamate [NMDA] receptor subunit epsilon 2 (Organism: Rattus norvegicus, class: Ion channel, accessions: Q00960, gene: Grin2b, swissprot: NMDE2_RAT NMDA receptor antagonist; RN given refers to parent cpd without isomeric designation; structure Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Cardiovascular Agents (Code: D002317) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) QEL
Click to view etafenone used in therapy of anigna pectoris; RN given refers to parent cpd; synonym baxacor is HCl; structure Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view dapiprazole Dapiprazole is an alpha-1 adrenergic receptors antagonist. It was used for for the treatment of drug induced mydriasis produced by adrenergic or parasympatholytic agents. It was withdrawn from market due to its slow effect. Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) alpha-adrenergic antagonist (Code: CHEBI:37890) miotic (Code: CHEBI:51068) antipsychotic agent (Code: CHEBI:35476) ophthalmology drug (Code: CHEBI:66981) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) alpha-Adrenergic Blocker (Code: N0000175553) 1990-12-31 FDA
Click to view tolterodine Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020771s028lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020771s028lbl.pdf) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020771s028lbl.pdf) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020771s028lbl.pdf) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020771s028lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020771s028lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020771s028lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9531513) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9531513) Tolterodine is a competitive muscarinic receptor antagonist. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of the 5-hydroxymethyl derivative, a major pharmacologically active metabolite. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Tolterodine has a pronounced effect on bladder function. The main effects of tolterodine were an increase in residual urine, reflecting an incomplete emptying of the bladder, and a decrease in detrusor pressure. Tolterodine is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Cholinergic Muscarinic Antagonist (Code: N0000175700) Cholinergic Muscarinic Antagonists (Code: N0000000125) muscarinic antagonist (Code: CHEBI:48876) antispasmodic drug (Code: CHEBI:53784) muscle relaxant (Code: CHEBI:51371) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Urological Agents (Code: D064804) 1998-03-25 FDA
Click to view dimenoxadol
Click to view midazolam GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47869|P34903|P48169|P31644|Q16445|P18505|P47870|P28472|O14764|P78334|Q8N1C3|P18507|Q99928|O00591|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) potentiator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211321s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211321s000lbl.pdf) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20939765) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12814972) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12699389) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10565838) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10565838) Midazolam is a short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Adjuvants, Anesthesia (Code: D000759) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1985-12-20 FDA 08J
Click to view clemizole Histamine H4 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9H3N8, gene: HRH4, swissprot: HRH4_HUMAN) Heme oxygenase 2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P23711, gene: Hmox2, swissprot: HMOX2_RAT histamine antagonist (Code: CHEBI:37956)
Click to view nipradilol Nipradilol is a beta blocker and nitric oxide donor. It is usually used to treat glaucoma and intraocular hypertension. Also nipradilol is used for the treatment of essential hypertension and angina pectoris. Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) 1990 PMDA
Click to view bumadizone an anlgesic, antipyretic and anti-inflammatory agent; minor descriptor (75-86); on line & INDEX MEDICUS search MALONATES (75-86); RN given refers to parent cpd Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antipyretic (Code: CHEBI:35493) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view octabenzone
Click to view moxestrol Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372|Q92731, gene: ESR1|ESR2, swissprot: ESR1_HUMAN|ESR2_HUMAN Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view acitretin Acitretin is a retinoid and a metabolite of etretinate and is related to both retinoic acid and retinol (vitamin A). Acitretin is indicated for the treatment of severe psoriasis in adults. Because of significant adverse effects associated with its use, acitretin should be prescribed only by those knowledgeable in the systemic use of retinoids. Retinoid (Code: N0000175607) Retinoids (Code: N0000007700) keratolytic drug (Code: CHEBI:50176) Dermatologic Agents (Code: D003879) Keratolytic Agents (Code: D007641) 1996-10-28 FDA
Click to view hydroquinidine Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Sodium channel subunit beta-4 (Organism: Homo sapiens, class: Ion channel, accessions: Q8IWT1, gene: SCN4B, swissprot: SCN4B_HUMAN) Sodium channel subunit beta-3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NY72, gene: SCN3B, swissprot: SCN3B_HUMAN) Sodium channel subunit beta-2 (Organism: Homo sapiens, class: Ion channel, accessions: O60939, gene: SCN2B, swissprot: SCN2B_HUMAN) Sodium channel subunit beta-1 (Organism: Homo sapiens, class: Ion channel, accessions: Q07699, gene: SCN1B, swissprot: SCN1B_HUMAN) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) urinary quinine metabolite; RN given refers to (9S)-isomer; structure in Merck Index, 9th ed, #4703 Anti-Arrhythmia Agents (Code: D000889) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view ajmaline Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) An alkaloid found in the root of RAUWOLFIA SERPENTINA, among other plant sources. It is a class Ia antiarrhythmic agent that apparently acts by changing the shape and threshold of cardiac action potentials. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567)
Click to view tiazesim
Click to view acepromazine Major prion protein (Organism: Homo sapiens, class: Surface antigen, accessions: P04156, gene: PRNP, swissprot: PRIO_HUMAN A phenothiazine that is used in the treatment of PSYCHOSES. phenothiazine antipsychotic drug (Code: CHEBI:37930) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view aceprometazine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: http://www.has-sante.fr/portail/upload/docs/application/pdf/2012-09/mepronizine_ct_8952.pdf) anxiolytic drug (Code: CHEBI:35474) sedative (Code: CHEBI:35717) histamine antagonist (Code: CHEBI:37956) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view promegestone Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT A synthetic progestin which is useful for the study of progestin distribution and progestin tissue receptors, as it is not bound by transcortin and binds to progesterone receptors with a higher association constant than progesterone. progesterone receptor agonist (Code: CHEBI:70709) antineoplastic agent (Code: CHEBI:35610)
Click to view bunaftine N-Butyl-N-(2-(diethylamino)ethyl)-1-naphthamide. A proposed antiarrhythmic that prolongs myocardial refractory period and stabilizes cell membranes. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317)
Click to view etymemazine
Click to view bromochlorosalicylanilide Bromochlorosalicylanilide is an antifungal. It was used for the topical treatment of fungal infections.
Click to view clozapine 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203479s000lbl.pdf) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10976659) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19934256) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19934256) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10422890) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10422890) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10422890) Clozapine is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent. serotonergic antagonist (Code: CHEBI:48279) dopaminergic antagonist (Code: CHEBI:48561) adrenergic antagonist (Code: CHEBI:37887) histamine antagonist (Code: CHEBI:37956) muscarinic antagonist (Code: CHEBI:48876) GABA antagonist (Code: CHEBI:65259) second generation antipsychotic (Code: CHEBI:65191) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Antagonists (Code: D018756) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Tranquilizing Agents (Code: D014149) Atypical Antipsychotic (Code: N0000175430) 1989-09-26 FDA
Click to view niclosamide Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11124226) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11124226) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inductor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11124226) Signal transducer and activator of transcription 3 (Organism: Homo sapiens, class: Transcription factor, accessions: P40763, gene: STAT3, swissprot: STAT3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24900231) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24900231) Tyrosine-protein kinase JAK2 (Organism: Homo sapiens, class: Kinase, accessions: O60674, gene: JAK2, swissprot: JAK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24900231) Niclosamide is an antihelmintic that is active against most tapeworms. It may act by the uncoupling of the electron transport chain to ATP synthase. The disturbance of this crucial metabolic pathway prevents creation of adenosine tri-phosphate (ATP), an essential molecule that supplies energy for metabolism. Niclosamide may work as a molluscicide by binding to and damaging DNA. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Anticestodal Agents (Code: D000923) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Molluscacides (Code: D008975) Pesticides (Code: D010575) 1982-05-13 FDA
Click to view leteprinim a neuroprotective agent that has been shown to improve memory; induces NGF-dependent nociceptive nerve sprouting
Click to view tranilast Hematopoietic prostaglandin D synthase (Organism: Homo sapiens, class: Enzyme, accessions: O60760, gene: HPGDS, swissprot: HPGDS_HUMAN antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis; structure Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Allergic Agents (Code: D018926) nephroprotective agent (Code: CHEBI:76595) anti-allergic agent (Code: CHEBI:50857) antineoplastic agent (Code: CHEBI:35610) hepatoprotective agent (Code: CHEBI:62868) anti-asthmatic drug (Code: CHEBI:49167) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Hematologic Agents (Code: D006401) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Platelet Aggregation Inhibitors (Code: D010975) Sensory System Agents (Code: D018689) D27
Click to view naloxone Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208411lbl.pdf) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208411lbl.pdf) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208411lbl.pdf) Estrogen receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16546975) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10871297) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12438524) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16250647) Naloxone is a specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors which is used intravenously in emergency situations to reverse the respiratory depression caused by overdoses of heroin, morphine or other opioids. Opioid Antagonist (Code: N0000175691) Opioid Antagonists (Code: N0000000154) central nervous system depressant (Code: CHEBI:35488) antidote to opioid poisoning (Code: CHEBI:90755) Central Nervous System Agents (Code: D002491) Narcotic Antagonists (Code: D009292) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1971-04-13 FDA
Click to view benactyzine A centrally acting muscarinic antagonist. Benactyzine has been used in the treatment of depression and is used in research to investigate the role of cholinergic systems on behavior. Antidepressive Agents (Code: D000928) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619)
Click to view norelgestromin Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist transdermal hormonal contraceptive Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Combined (Code: D003277) Reproductive Control Agents (Code: D012102) 2001-11-20 FDA
Click to view butorphanol Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) partial agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/19890s17lbl.pdf) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/19890s17lbl.pdf) Butorphanol is a mixed agonist-antagonist with low intrinsic activity at receptors of the mu-opioid type (morphine-like). It is also an agonist at k-opioid receptors. Its interactions with these receptors in the central nervous system apparently mediate most of its pharmacologic effects, including analgesia. Butorphanol is indicated for the management of pain when the use of an opioid analgesic is appropriate. Butorphanol is also indicated as a preoperative or preanesthetic medication, as a supplement to balanced anesthesia, and for the relief of pain during labor. Competitive Opioid Antagonists (Code: N0000175686) Opioid Agonist/Antagonist (Code: N0000175692) Partial Opioid Agonists (Code: N0000175685) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) antitussive (Code: CHEBI:51177) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322) kappa-opioid receptor agonist (Code: CHEBI:59282) Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotic Antagonists (Code: D009292) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689) 1978-08-22 FDA
Click to view tifenamil
Click to view aminopromazine
Click to view ranimustine Ranimustine is a chloroethylnitrosourea derivative that inhibits proliferation and growth of tumor cells by alkylation and cross-linkage of DNA strands of tumor cells. Ranimustine is used for the treatment of glioblastoma, myeloma, malignant lymphoma, chronic myelogenous leukemia, polycythemia vera and thrombocytosis. Antineoplastic Agents (Code: D000970) 1987-07-01 PMDA
Click to view clofibride Clofibride is a hypolipaemic drug of p-chlorophenoxyisobutyric type. Clofibride is a derivative of clofibrate. Clofibride hypolipaemic effects could be due, partially, to a reduction of hormono-dependent lipolysis. It was used for the treatment of hyperlipidemia. It is no longer available. 1988-10-27 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view loxapine 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: ) Histamine H4 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9H3N8, gene: HRH4, swissprot: HRH4_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: ) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist Histamine H1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P31390, gene: Hrh1, swissprot: HRH1_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT 5-hydroxytryptamine receptor 2C (Organism: Rattus norvegicus, class: GPCR, accessions: P08909, gene: Htr2c, swissprot: 5HT2C_RAT 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) Potassium channel subfamily T member 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q5JUK3, gene: KCNT1, swissprot: KCNT1_HUMAN) activator (Source: ) An antipsychotic agent used in SCHIZOPHRENIA. antipsychotic agent (Code: CHEBI:35476) dopaminergic antagonist (Code: CHEBI:48561) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1975-02-25 FDA
Click to view diloxanide furoate Diloxanide furoate is an anti-protozoal drug. Diloxanide furoate is a prodrug, and is hydrolyzed in the gastrointestinal tract to produce diloxanide, the active ingredient. It is used in the treatment of Entamoeba histolytica and some other protozoal infections. Amebicides (Code: D000563) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) 1984-09-01 CDSCO (INDIA)
Click to view labetalol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018716s026lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018716s026lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018716s026lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018716s026lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/018716s026lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/18098064/) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/18098064/) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/18098064/) Labetalol is an adrenergic receptor blocking agent that have both selective alpha1-adrenergic and nonselective beta-adrenergic receptor blocking actions in a single substance. Dilevalol, the R,R- stereoisomer, makes up 25% of racemic labetalol. Labetalol is indicated in the management of hypertension alone or in combination with other antihypertensive agents, especially thiazide and loop diuretics. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) antihypertensive agent (Code: CHEBI:35674) sympatholytic agent (Code: CHEBI:66991) alpha-adrenergic antagonist (Code: CHEBI:37890) beta-adrenergic antagonist (Code: CHEBI:35530) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1984-08-01 FDA
Click to view tiapride D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11520476) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11520476) Tiapride is a benzamide derivative with dopamine antagonist actions similar to sulpiride. It has been used as an antipsychotic and in the treatment of various movement disorders and alcoholism. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1976-09-01 Italian Medicines Agency (AIFA)
Click to view liranaftate Liranaftate is a thiocarbamate and squalene epoxidase inhibitor with antifungal activity. Liranaftate inhibits fungal squalene epoxidase, an enzyme that plays a key role in the synthesis of sterol which is essential for cell membrane integrity. By preventing ergosterol synthesis and causing accumulation of squalene, this agent increases cell membrane permeability, cell leakage and eventually cell lysis. It has strong antifungal activity against dermatophytes (Trichophyton, Microsporum, Epidermophyton). It is used for the treatment of tinea pedis. 2000-08-01 PMDA
Click to view suplatast Suplatast is a immunomodulator that can adjust the imbalance in the Th1/Th2 immune response. Suplatast helps to suppress the production of IgE, to block the production of cytokines and to suppress allergy-related eosinophils. It is used as suplatast tosilate for the treatment of bronchial asthma, allergic rhinitis and atopic dermatitis. Anti-Allergic Agents (Code: D018926) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Neurotransmitter Agents (Code: D018377) 1995-04-01 PMDA
Click to view levomepromazine D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2870716) Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2870716) Alpha-2A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P22909, gene: Adra2a, swissprot: ADA2A_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2870716) Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2870716) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10954064) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2899826) Pleiotropic ABC efflux transporter of multiple drugs (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Unclassified, accessions: P33302, gene: PDR5, swissprot: PDR5_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19188399) Levomepromazine is a phenothiazine and typical antipsychotic agent, with sedative/hypnotic, anxiolytic, antiemetic, analgesic and antipsychotic activities. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) phenothiazine antipsychotic drug (Code: CHEBI:37930) dopaminergic antagonist (Code: CHEBI:48561) serotonergic antagonist (Code: CHEBI:48279) cholinergic antagonist (Code: CHEBI:48873) non-narcotic analgesic (Code: CHEBI:35481) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) Tranquilizing Agents (Code: D014149) FDA
Click to view promestriene 3 propyl-ether-17 beta-methyl-ether of ESTRADIOL
Click to view retinol acetate Retinol-binding protein 4 (Organism: Homo sapiens, class: Secreted, accessions: P02753, gene: RBP4, swissprot: RET4_HUMAN Beta-lactoglobulin (Organism: Bos taurus, class: Unclassified, accessions: P02754, gene: LGB, swissprot: LACB_BOVIN Adjuvants, Immunologic (Code: D000276) Anticarcinogenic Agents (Code: D016588) Antineoplastic Agents (Code: D000970) Immunologic Factors (Code: D007155) Protective Agents (Code: D020011) FDA
Click to view stanozolol Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist A synthetic steroid that has anabolic and androgenic properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1194) Anabolic Agents (Code: D045930) Androgens (Code: D000728) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1962-01-09 FDA
Click to view ciclonium
Click to view oxazolam Oxazolam is a prodrug for the benzodiazepine desmethyl-diazepam (nordazepam) and is itself a metabolic product of other benzodiazepines. It has anxiolytic, sedative, and anticonvulsant properties. It is a GABA-A receptor agonist. Oxazolam is usually used to treat anxiety, tension, depression, and sleeping disorder in neurosis. It is used to treat somatic symptoms in psychosomatic disorders (gastrointestinal diseases, circulatory diseases, endocrine diseases, and autonomic dystonia), anxiety, tension, and depression. It is also used as a preanesthetic medication. (See: nordazepam) 1970-11-01 PMDA
Click to view clorexolone Clorexolone is a sulfonamide-based diuretic with thiazide-like activity. Cloreloxone has actions similar to that of thiazide diuretics. It was used for the treatment of hypertension. 1966 YEAR INTRODUCED
Click to view eberconazole Eberconazole is an antifungal drug with broad antimicrobial spectrum of activity. Eberconazole exerts fungicidal or fungistatic activity depending on concentration, being fungicidal at higher concentration and fungistatic at lower concentrations. It prevents the fungal ergosterol synthesis by inhibiting lanosterol 14alpha-demethylase enzyme that is responsible for the formation of 14 alpha-methylsterols. Eberconazole is used for the treatment of fungal skin infections such as Tinea corporis, Tinea cruris and Tinea pedis. 2004-03-18 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view nitisinone 4-hydroxyphenylpyruvate dioxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P32754, gene: HPD, swissprot: HPPD_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209449s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209449s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209449s000lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209449s000lbl.pdf) Nitisinone is a competitive inhibitor of 4-hydroxyphenyl-pyruvate dioxygenase, an enzyme upstream of FAH in the tyrosine catabolic pathway. By inhibiting the normal catabolism of tyrosine in patients with hereditary tyrosinemia type 1 (HT-1), nitisinone prevents the accumulation of the catabolic intermediates maleylacetoacetate and fumarylacetoacetate. In patients with HT-1, these catabolic intermediates are converted to the toxic metabolites succinylacetone and succinylacetoacetate, which are responsible for the observed liver and kidney toxicity. Hydroxyphenyl-Pyruvate Dioxygenase Inhibitor (Code: N0000175809) Hydroxyphenylpyruvate Dioxygenase Inhibitors (Code: N0000175808) 4-Hydroxyphenyl-Pyruvate Dioxygenase Inhibitor (Code: N0000175809) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) Enzyme Inhibitors (Code: D004791) 2002-01-18 FDA
Click to view flumethiazide Flumethiazide is a potent diuretic related chemically to chlorothiazide and with similar pharmacologic actions. It was used for the treatment of essential hypertension.
Click to view etofylline nicotinate (See: etofylline)
Click to view paroxetine Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020031s074lbl.pdf) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12359676) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17101742) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12649369) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871604) P2X purinoceptor 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q99571, gene: P2RX4, swissprot: P2RX4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19389225) Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23477943) Sodium-dependent noradrenaline transporter (Organism: Mus musculus, class: Transporter, accessions: O55192, gene: Slc6a2, swissprot: SC6A2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12359676) Paroxetine is a selective serotonin reuptake inhibitor. In vitro radioligand binding studies indicate that paroxetine has little affinity for muscarinic, alpha1-, alpha2-, beta-adrenergic-, dopamine (D2)-, 5-HT1-, 5-HT2-, and histamine (H1)-receptors. Paroxetine is used in the therapy of depression, anxiety disorders and obsessive-compulsive disorder. anxiolytic drug (Code: CHEBI:35474) serotonin uptake inhibitor (Code: CHEBI:50949) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Cytochrome P-450 CYP2D6 Inhibitors (Code: D065690) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Membrane Transport Modulators (Code: D049990) Metabolic Side Effects of Drugs and Substances (Code: D065606) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) Serotonin Reuptake Inhibitor (Code: N0000175696) 1992-12-29 FDA 8PR
Click to view trilostane 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2 (Organism: Homo sapiens, class: Enzyme, accessions: P26439, gene: HSD3B2, swissprot: 3BHS2_HUMAN) inhibitor inhibits conversion of pregnenolone to progesterone; adrenal blocking agent used in treatment of Cushing's syndrome Abortifacient Agents (Code: D000019) Abortifacient Agents, Steroidal (Code: D000021) antineoplastic agent (Code: CHEBI:35610) abortifacient (Code: CHEBI:50691) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Reproductive Control Agents (Code: D012102) FDA
Click to view bornaprine beneficial effect in Parkinsonism due to inhibition of muscarinic or nicotinic transmission Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377)
Click to view androisoxazole Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) 1961-01-01 YEAR INTRODUCED
Click to view prenylamine Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Voltage-gated L-type calcium channel (Organism: Rattus norvegicus, class: Ion channel, accessions: P22002|P27732|Q02485, gene: Cacna1c|Cacna1d|Cacna1s, swissprot: CAC1C_RAT|CAC1D_RAT|CAC1S_RAT A drug formerly used in the treatment of angina pectoris but superseded by less hazardous drugs. Prenylamine depletes myocardial catecholamine stores and has some calcium channel blocking activity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1406) Adrenergic Agents (Code: D018663) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665)
Click to view cloperastine
Click to view flurbiprofen axetil Flurbiprofen axetil is a prodrug prepared by esterification of flurbiprofen, which makes the compound lipophilic and soluble in soybean oil in the lipid microsphere. Flurbiprofen axetil injection is composed of lipid microspheres and flurbiprofen axetil. Lipid microsphere is a targeted drug delivery carrier. Flurbiprofen axetil is used in treatment of moderate or severe pain, especially breakthrough pain, and suit to patients who can not take oral drugs for the reason of constipation and psychosomatic symptoms. (See: flurbiprofen) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1992-07-01 PMDA
Click to view malathion Acetylcholinesterase (Organism: Pediculus humanus capitis, class: Enzyme, accessions: A2PZ98, gene: Ace1, swissprot: A2PZ98_9NEOP) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/018613s017lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15557345) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15557345) Malathion is an organophosphate agent which acts as a pediculicide by inhibiting cholinesterase activity in vivo. Inadvertent transdermal absorption of malathion has occurred from its agricultural use. In such cases, acute toxicity was manifested by excessive cholinergic activity, i.e., increased sweating, salivary and gastric secretion, gastrointestinal and uterine motility, and bradycardia. Malathion is indicated for patients infected with Pediculus humanus capitis (head lice and their ova) of the scalp hair. Cholinesterase Inhibitor (Code: N0000175723) insecticide (Code: CHEBI:24852) scabicide (Code: CHEBI:73333) agrochemical (Code: CHEBI:33286) pediculicide (Code: CHEBI:38706) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Insecticides (Code: D007306) Neurotransmitter Agents (Code: D018377) Pesticides (Code: D010575) 1982-08-02 FDA
Click to view almecillin Almecillin (penicillin O) is an antibiotic that can be safely substituted for penicillin G in instances of hypersensitivity reactions to the latter. It was isolated from Penicillium chrysogenum. 1950 FDA
Click to view oxomemazine selective for M1 muscarinic receptors
Click to view mivotilate Cytochrome P450 2E1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P05182, gene: Cyp2e1, swissprot: CP2E1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8579361) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/8649358) Mivotilate is an orally-active hepatoprotective agent. Mivotilate was shown to exert multiple effects on the hepatic cytochrome P450 system, particularly to inhibit CYP2E1 expression and to up-regulate the CYP1A1 expression. It is used for the treatment of liver cirrhosis and hepatitis-B infection.
Click to view desoxycortone 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: ) Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) agonist (Source: ) Corticosteroid-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P08185, gene: SERPINA6, swissprot: CBG_HUMAN A steroid metabolite that is the 11-deoxy derivative of CORTICOSTERONE and the 21-hydroxy derivative of PROGESTERONE Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Mineralocorticoids (Code: D008901) 1CA
Click to view prasterone acetate Prasterone acetate (Dehydroepiandrosterone acetate) is dehydroepiandrosterone derivatives. (See: prasterone)
Click to view dipiproverine
Click to view icosapent ethyl Diacylglycerol O-acyltransferase 1 (Organism: Homo sapiens, class: Enzyme, accessions: O75907, gene: DGAT1, swissprot: DGAT1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202057s009lbl.pdf) anticholesteremic drug (Code: CHEBI:35821) antipsychotic agent (Code: CHEBI:35476) antidepressant (Code: CHEBI:35469) prodrug (Code: CHEBI:50266) 2012-07-26 FDA
Click to view teprenone ; RN given refers to isomeric cpd without isomeric designation; mixture of (5E,9E,13E) & (5Z,9E,13E)-isomers anti-ulcer drug (Code: CHEBI:49201) cardioprotective agent (Code: CHEBI:77307) hepatoprotective agent (Code: CHEBI:62868) nephroprotective agent (Code: CHEBI:76595) neuroprotective agent (Code: CHEBI:63726) Anti-Ulcer Agents (Code: D000897) Antineoplastic Agents (Code: D000970) Gastrointestinal Agents (Code: D005765)
Click to view oxeladin Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141)
Click to view furosemide Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Corticosteroid 11-beta-dehydrogenase isozyme 1 (Organism: Homo sapiens, class: Enzyme, accessions: P28845, gene: HSD11B1, swissprot: DHI1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18653260) Corticosteroid 11-beta-dehydrogenase isozyme 1 (Organism: Mus musculus, class: Enzyme, accessions: P50172, gene: Hsd11b1, swissprot: DHI1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18653260) G-protein coupled receptor 35 (Organism: Homo sapiens, class: GPCR, accessions: Q9HC97, gene: GPR35, swissprot: GPR35_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23888932) Furosemide is a chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It has been demonstrated that furosemide inhibits primarily the absorption of sodium and chloride not only in the proximal and distal tubules but also in the loop of Henle. The high degree of efficacy is largely due to the unique site of action. The action on the distal tubule is independent of any inhibitory effect on carbonic anhydrase and aldosterone. It is a loop diuretic used in the treatment of congestive heart failure. Increased Diuresis at Loop of Henle (Code: N0000175366) loop diuretic (Code: CHEBI:77608) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Potassium Chloride Symporter Inhibitors (Code: D049994) 1966-07-01 FDA FUN
Click to view chlorbetamide Chlorbetamide is dichlorobenzene derivative. It has antimicrobial and amebicidal activity. It was investigated for the treatment of amebiasis.
Click to view tienilic acid Tienilic acid is a diuretic with uricosuric action, it has been used as an antihypertensive agent, withdrawn shortly after approval due to liver toxicity. loop diuretic (Code: CHEBI:77608) antihypertensive agent (Code: CHEBI:35674) Antihypertensive Agents (Code: D000959) Antirheumatic Agents (Code: D018501) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Gout Suppressants (Code: D006074) Natriuretic Agents (Code: D045283) Renal Agents (Code: D012076) Uricosuric Agents (Code: D014528) 1979-05-02 FDA
Click to view hydroflumethiazide Hydroflumethiazide is a thiazide diuretic that inhibits water reabsorption in the nephron by inhibiting the sodium-chloride symporter in the distal convoluted tubule. Hydroflumethiazide effectively reduces the osmotic gradient and water reabsorption throughout the nephron. Hydroflumethiazide is used as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Also used in the management of hypertension either as the sole therapeutic agent or to enhance the effect of other antihypertensive drugs in the more severe forms of hypertension. Increased Diuresis (Code: N0000175359) Thiazide Diuretic (Code: N0000175419) Thiazides (Code: N0000166469) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) 1959-07-22 FDA HFZ
Click to view ciprofloxacin DNA gyrase subunit A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES4, gene: gyrA, swissprot: GYRA_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/19847s26lbl.pdf) DNA topoisomerase 4 subunit A (Organism: Staphylococcus aureus, class: Enzyme, accessions: P0C1U9, gene: parC, swissprot: PARC_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/19847s26lbl.pdf) DNA topoisomerase 4 subunit A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AFI2, gene: parC, swissprot: PARC_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/19847s26lbl.pdf) DNA topoisomerase 4 subunit A (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: P72525, gene: parC, swissprot: PARC_STRPN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/19847s26lbl.pdf) DNA gyrase (Organism: Neisseria gonorrhoeae, class: Enzyme, accessions: P22118|P48371, gene: gyrA|gyrB, swissprot: GYRA_NEIGO|GYRB_NEIGO) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/19847s26lbl.pdf) DNA gyrase (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: P48372|Q9I7C2, gene: gyrA|gyrB, swissprot: GYRA_PSEAE|GYRB_PSEAE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/19847s26lbl.pdf) DNA gyrase (Organism: Staphylococcus epidermidis (strain ATCC 35984 / RP62A), class: Enzyme, accessions: Q5HK04|Q5HK03, gene: gyrA|gyrB, swissprot: GYRA_STAEQ|GYRB_STAEQ) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/19847s26lbl.pdf) DNA gyrase subunit A (Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd), class: Enzyme, accessions: P43700, gene: gyrA, swissprot: GYRA_HAEIN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/19847s26lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19026171) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19026171) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8894516) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Multidrug and toxin extrusion protein 1 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q5I0E9, gene: Slc47a1, swissprot: S47A1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19004926) Ciprofloxacin is a synthetic fluoroquinolone antibacterial agent. The bactericidal action of ciprofloxacin results from interference with the enzyme DNA gyrase, which is needed for the synthesis of bacterial DNA. In vitro studies demonstrated cross-resistance between ciprofloxacin and some fluoroquinolones. There is generally no cross-resistance between ciprofloxacin and other classes of antibacterial agents, such as beta-lactams or aminoglycosides. Ciprofloxacin has been shown to be active against Enterococcus faecalis, Staphylococcus aureus (methicillin-susceptible strains only), Staphylococcus epidermidis (methicillin-susceptible strains only), Staphylococcus saprophyticus, Streptococcus pneumoniae (penicillin-susceptible strains), Streptococcus pyogenes, Citrobacter diversus, Morganella morganii, Citrobacter freundii, Proteus mirabilis, Enterobacter cloacae, Proteus vulgaris, Escherichia coli, Providencia rettgeri, Haemophilus influenzae, Providencia stuartii, Haemophilus parainfluenzae, Pseudomonas aeruginosa, Klebsiella pneumoniae, Serratia marcescens,Moraxella catarrhalis. Ciprofloxacin is used for the treatment of otitis media and otitis externa, urinary tract infections, lower respiratory tract infections, nosocomial pneumonia, skin and skin structure infections, bone and joint infections, intra-abdominal infections, acute sinusitis, chronic bacterial prostatitis, febrile neutropenic, inhalational anthrax. Quinolone Antimicrobial (Code: N0000175937) Quinolones (Code: N0000007606) antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Cytochrome P-450 CYP1A2 Inhibitors (Code: D065609) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Metabolic Side Effects of Drugs and Substances (Code: D065606) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1987-10-22 FDA CPF
Click to view piroxicam Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/018147s048lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/018147s048lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/018147s048lbl.pd) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991954) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Piroxicam is a cyclooxygenase inhibiting, non-steroidal anti-inflammatory agent (NSAID) that is well established in treating rheumatoid arthritis and osteoarthritis and used for musculoskeletal disorders, dysmenorrhea, and postoperative pain. Its long half-life enables it to be administered once daily. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) antirheumatic drug (Code: CHEBI:35842) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) analgesic (Code: CHEBI:35480) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1982-04-06 FDA
Click to view protokylol Protokylolis a sympathomimetic drug and a beta-adrenergic receptor agonist. It was used as a bronchodilator. It was withdrawm from market in 1974. FDA
Click to view oxyclipine
Click to view nizatidine Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/21494s001lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19319690) Nizatidine is a competitive, reversible inhibitor of histamine at the histamine H2-receptors, particularly those in the gastric parietal cells. Nizatidine significantly inhibited nocturnal gastric acid secretion and secretion stimulated by food, caffeine, betazole, and pentagastrin. Nizatidine is indicated for the treatment of active duodenal ulcer, for maintenance therapy for duodenal and gastric ulcer patients, for the treatment of endoscopically diagnosed esophagitis, including erosive and ulcerative esophagitis, and associated heartburn due to GERD. anti-ulcer drug (Code: CHEBI:49201) H2-receptor antagonist (Code: CHEBI:37961) cholinergic drug (Code: CHEBI:38323) Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H2 Antagonists (Code: D006635) Neurotransmitter Agents (Code: D018377) Histamine H2 Receptor Antagonists (Code: N0000000151) Histamine-2 Receptor Antagonist (Code: N0000175784) 1988-04-12 FDA
Click to view glypinamide Glypinamide is a second-generation sulfonylurea with antihyperglycemic activity. Glypinamide, also called azepinamide, is a chlorinated analogue of tolazamide. It was used as an antidiabetic drug.
Click to view zotepine 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: https://pubmed.ncbi.nlm.nih.gov/15821958/) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://pubmed.ncbi.nlm.nih.gov/15821958/) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://pubmed.ncbi.nlm.nih.gov/10991983/) Sodium-dependent noradrenaline transporter (Organism: Mus musculus, class: Transporter, accessions: O55192, gene: Slc6a2, swissprot: SC6A2_MOUSE) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/20223878/) Sodium-dependent serotonin transporter (Organism: Mus musculus, class: Transporter, accessions: Q60857, gene: Slc6a4, swissprot: SC6A4_MOUSE) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/20223878/) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://pubmed.ncbi.nlm.nih.gov/20223878/) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://pubmed.ncbi.nlm.nih.gov/23427194/) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://pubmed.ncbi.nlm.nih.gov/23427194/) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/10219963/) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/10219963/) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/10219963/) Zotepine is a potent antipsychotic and antidepressive drug. Zotepine has high affinity to D2, 5-HT2A, 5-HT2C, 5-HT6, 5-HT7, alpha1A, H1, and D1 receptors at therapeutically relevant concentrations and has similar affinities to 5-HT1A, alpha2A, and M1 receptors at high concentrations. In human zotepine is metabolized to a major metabolite, norzotepine, which has profile similar to that of zotepine for important neurotransmitter receptors known to be responsible for zotepine antipsychotic activity. It is used for the treatment of schizophrenia. second generation antipsychotic (Code: CHEBI:65191) alpha-adrenergic drug (Code: CHEBI:48539) serotonergic drug (Code: CHEBI:48278) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1995-07-01 PMDA
Click to view dibromol Dibromol (3,5-Dibromo-4-hydroxybenzenesulfonic acid) is an organosulfur compound and a sulfonic acid derivative. It is used as a disinfectant.
Click to view zanamivir Neuraminidase (Organism: Influenza A virus (strain A/Puerto Rico/8/1934 H1N1), class: Enzyme, accessions: P03468, gene: NA, swissprot: NRAM_I34A1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021036s030lbl.pdf) Neuraminidase (Organism: Influenza A virus (strain A/Bangkok/1/1979 H3N2), class: Enzyme, accessions: P06818, gene: NA, swissprot: NRAM_I79A0) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021036s030lbl.pdf) Neuraminidase (Organism: Influenza B virus (strain B/Victoria/3/1985), class: Enzyme, accessions: P16207, gene: NA, swissprot: NRAM_INBVI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021036s030lbl.pdf) Neuraminidase (Organism: Influenza B virus (strain B/Beijing/1/1987), class: Enzyme, accessions: P27907, gene: NA, swissprot: NRAM_INBBE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021036s030lbl.pdf) a sialic acid-analogue neuraminidase inhibitor with antiviral activity. Administered into the respiratory tract by aerosol inhalation, zanamivir selectively binds to and inhibits influenza A and B virus neuraminidase-mediated cleavage of sialic acid residues in host cell membrane-bound glycoprotein receptors for influenza viruses, preventing the release of progeny viruses from host cell surfaces and, so, further viral replication. Neuraminidase Inhibitor (Code: N0000175524) Neuraminidase Inhibitors (Code: N0000175436) EC 3.2.1.18 (exo-alpha-sialidase) inhibitor (Code: CHEBI:52425) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) 1999-07-26 FDA
Click to view spectinomycin Spectinomycin is an aminocyclitol aminoglycoside antibiotic derived from Streptomyces spectabilis with bacteriostatic activity. Spectinomycin binds to the bacterial 30S ribosomal subunit. As a result, this agent interferes with the initiation of protein synthesis and with proper protein elongation. This eventually leads to bacterial cell death. Spectinomycin is indicated in the treatment of acute gonorrheal urethritis and proctitis in the male and acute gonorrheal cervicitis and proctitis in the female when due to susceptible strains of Neisseria gonorrhoeae. antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1971-06-30 FDA SCM
Click to view acedapsone Acedapsone is a long acting prodrug of Dapsone, the diacetyl derivative of diaminophenyl sulfone. (See: dapsone) antimicrobial drug (Code: CHEBI:36043) antimalarial (Code: CHEBI:38068) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Leprostatic Agents (Code: D007917)
Click to view oxitropium Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view ipratropium Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Rattus norvegicus, class: GPCR, accessions: P08482, gene: Chrm1, swissprot: ACM1_RAT Muscarinic acetylcholine receptor M3 (Organism: Rattus norvegicus, class: GPCR, accessions: P08483, gene: Chrm3, swissprot: ACM3_RAT Muscarinic acetylcholine receptor M2 (Organism: Rattus norvegicus, class: GPCR, accessions: P10980, gene: Chrm2, swissprot: ACM2_RAT Ipratropium is a synthetic anticholinergic agent that is used as an inhalant for treatment of acute bronchospasm due to chronic bronchitis and emphysema. Ipratropium has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury. Anticholinergic (Code: N0000175574) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1986-12-29 FDA X8M
Click to view oxymetholone Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) A synthetic hormone with anabolic and androgenic properties. It is used mainly in the treatment of anemias. According to the Fourth Annual Report on Carcinogens (NTP 85-002), this compound may reasonably be anticipated to be a carcinogen. (From Merck Index, 11th ed) Anabolic Agents (Code: D045930) Androgens (Code: D000728) anti-anaemic agent (Code: CHEBI:75835) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1972-01-18 FDA
Click to view alfaxalone GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) Sodium- and chloride-dependent GABA transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P30531, gene: SLC6A1, swissprot: SC6A1_HUMAN) GABA-A receptor; anion channel (Organism: Rattus norvegicus, class: Ion channel, accessions: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14, gene: Gabra1|Gabra2|Gabra3|Gabra4|Gabra5|Gabra6|Gabrb1|Gabrb2|Gabrb3|Gabrd|Gabre|Gabrg1|Gabrg2|Gabrg3|Gabrp|Gabrq, swissprot: GBRA1_RAT|GBRA2_RAT|GBRA3_RAT|GBRA4_RAT|GBRA5_RAT|GBRA6_RAT|GBRB1_RAT|GBRB2_RAT|GBRB3_RAT|GBRD_RAT|GBRE_RAT|GBRG1_RAT|GBRG2_RAT|GBRG3_RAT|GBRP_RAT|Q91ZM7_RAT GABA A receptor alpha-2/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P47869|P47870, gene: GABRA2|GABRB2|GABRG2, swissprot: GBRA2_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN constituent of alphadione; RN given refers to (3alpha,5alpha)-isomer; structure Anesthetics (Code: D000777) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) 1972-01-01 YEAR INTRODUCED
Click to view brivudine Thymidine kinase (Organism: Human herpesvirus 1, class: Kinase, accessions: Q9QNF7, gene: TK, swissprot: KITH_HHV1) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14584954) Brivudine is an analog of the nucleoside thymidine. Brivudine is used in the treatment of herpes zoster ("shingles"). Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2000-07-06 Italian Medicines Agency (AIFA) BVD
Click to view pefloxacin DNA topoisomerase 1 (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P06612, gene: topA, swissprot: TOP1_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2830840) DNA gyrase subunit B (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES6, gene: gyrB, swissprot: GYRB_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2830840) DNA gyrase subunit A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES4, gene: gyrA, swissprot: GYRA_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2830840) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10096258) Pefloxacin is a synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria. Pefloxacin is used for the treatment of uncomplicated gonococcal urethritis in males and for gram-negative-bacterial infections in the gastrointestinal system and the genitourinary tract. antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Cytochrome P-450 CYP1A2 Inhibitors (Code: D065609) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Metabolic Side Effects of Drugs and Substances (Code: D065606) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1985-01-01 YEAR INTRODUCED
Click to view drotebanol Analgesics (Code: D000700) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view pentoxyverine Sigma non-opioid intracellular receptor 1 (Organism: Cavia porcellus, class: Membrane other, accessions: Q60492, gene: SIGMAR1, swissprot: SGMR1_CAVPO) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14691051) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19034038) Kappa-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P33534, gene: Oprk1, swissprot: OPRK_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8872359) Mu-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P42866, gene: Oprm1, swissprot: OPRM_MOUSE) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8872359) Pentoxyverine (carbetapentane) is a non-opioid central acting antitussive with antimuscarinic, anticonvulsant, and local anesthetic properties. It is an active ingredient in over-the-counter cough suppressants in combination with guaifenesin and H1-receptor antagonists. Pentoxyverine acts on sigma-1 receptors, as well as kappa and mu-opioid receptors. Pentoxyverine is indicated as a cough suppressant to relieve cough caused by the common cold, flu, bronchitis, and sinusitis. Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141) 1986-03-13 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view deptropine Soluble acetylcholine receptor (Organism: Aplysia californica, class: Unclassified, accessions: Q8WSF8, gene: None, swissprot: Q8WSF8_APLCA Acetylcholine-binding protein (Organism: Lymnaea stagnalis, class: Unclassified, accessions: P58154, gene: None, swissprot: ACHP_LYMST minor descriptor (65-85); on-line & Index Medicus search TROPANES (66-85); RN given refers to parent cpd parasympatholytic (Code: CHEBI:50370) H1-receptor antagonist (Code: CHEBI:37955) muscarinic antagonist (Code: CHEBI:48876) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377)
Click to view tropatepine
Click to view bromfenac Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206911s000lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/206911s000lbl.pdf) Bromfenac is a nonsteroidal anti-inflammatory drug (NSAID). The mechanism of its action is thought to be due to its ability to block prostaglandin synthesis by inhibiting cyclooxygenase 1 and 2, prostaglandins are mediators of certain kinds of intraocular inflammation. Bromfenac is indicated for the treatment of postoperative inflammation and prevention of ocular pain in patients undergoing cataract surgery. Cyclooxygenase Inhibitors (Code: N0000000160) Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2005-03-24 FDA 27R
Click to view bromazine Bromazine (bromodiphenhydramine) is a brominated derivative of diphenhydramine, an ethanolamine derivative and histamine H1 receptor antagonist with anti-allergic, sedative, antiemetic and anticholinergic properties. Bromazine competitively and selectively blocks central and peripheral histamine H1 receptors, thereby alleviating the symptoms caused by endogenous histamine on bronchial, capillary and gastrointestinal smooth muscles. Bromazine indicated for the treatment of allergic symptoms. muscarinic antagonist (Code: CHEBI:48876) H1-receptor antagonist (Code: CHEBI:37955) 1954-04-28 FDA
Click to view mitomycin DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) cross-linking (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022572s003lbl.pdf) Mitomycin is an antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional alkylating agents causing cross-linking of DNA and inhibition of DNA synthesis. Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) antineoplastic agent (Code: CHEBI:35610) Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Cross-Linking Reagents (Code: D003432) Enzyme Inhibitors (Code: D004791) Indicators and Reagents (Code: D007202) Noxae (Code: D009676) Nucleic Acid Synthesis Inhibitors (Code: D019384) 1981-08-24 FDA
Click to view tetroxoprim Dihydrofolate reductase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0ABQ4, gene: folA, swissprot: DYR_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/43863) Tetroxoprim is an inhibitor of bacterial dihydrofolate reductase. In combination with sulfadiazine (co-tetroxazine) it was used for the treatment of susceptible bacterial infections. Now it is used in veterinary medicine. Anti-Infective Agents (Code: D000890)
Click to view pimobendan Type-1 angiotensin II receptor (Organism: Bos taurus, class: GPCR, accessions: P25104, gene: AGTR1, swissprot: AGTR1_BOVIN Phosphodiesterase 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q13370|Q14432, gene: PDE3A|PDE3B, swissprot: PDE3A_HUMAN|PDE3B_HUMAN) inhibitor produces arterial & venous dilatation in dogs; structure given in first source cardiotonic drug (Code: CHEBI:38147) vasodilator agent (Code: CHEBI:35620) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Phosphodiesterase Inhibitors (Code: D010726) Protective Agents (Code: D020011) Vasodilator Agents (Code: D014665) 1994-01-01 YEAR INTRODUCED
Click to view benzylpenicillin Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11306713) Solute carrier family 22 member 9 (Organism: Homo sapiens, class: Transporter, accessions: Q8IVM8, gene: SLC22A9, swissprot: S22A9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10873595) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10873595) Solute carrier organic anion transporter family member 4A1 (Organism: Homo sapiens, class: Transporter, accessions: Q96BD0, gene: SLCO4A1, swissprot: SO4A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10873595) Solute carrier organic anion transporter family member 3A1 (Organism: Homo sapiens, class: Transporter, accessions: Q9UIG8, gene: SLCO3A1, swissprot: SO3A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10873595) Benzylpenicillin (Penicillin G) exerts a bactericidal action against penicillin-susceptible microorganisms during the stage of active multiplication. It acts through the inhibition of biosynthesis of cell-wall peptidoglycan, rendering the cell wall osmotically unstable. Penicillin is not active against penicillinase-producing bacteria or against organisms resistant to beta-lactams because of alterations in the penicillin-binding proteins. Resistance to benzylpenicillin has not been reported in Streptococcus pyogenes. Benzylpenicillin has been shown to be active against beta-hemolytic streptococci (groups A, B, C, G, H, L and M), Treponema pallidum, Treponema carateum. Benzylpenicillin is indicated for the treatment of mild-to-moderate infections of the upper-respiratory tract due to susceptible streptococci, venereal infections (syphilis, yaws, bejel, and pinta) and for the prophylaxis of rheumatic fever and/or chorea. Penicillin-class Antibacterial (Code: N0000175497) Penicillins (Code: N0000011281) antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1947-02-06 FDA PNN
Click to view proglumide Histamine H2 receptor (Organism: Rattus norvegicus, class: Unclassified, accessions: P25102, gene: Hrh2, swissprot: HRH2_RAT Gastrin/cholecystokinin type B receptor (Organism: Homo sapiens, class: GPCR, accessions: P32239, gene: CCKBR, swissprot: GASR_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/2863192) A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers. opioid analgesic (Code: CHEBI:35482) cholinergic antagonist (Code: CHEBI:48873) anti-ulcer drug (Code: CHEBI:49201) cholecystokinin antagonist (Code: CHEBI:73296) gastrointestinal drug (Code: CHEBI:55324) Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765)
Click to view strychnine Taste receptor type 2 member 46 (Organism: Homo sapiens, class: GPCR, accessions: P59540, gene: TAS2R46, swissprot: T2R46_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/20022913) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) allosteric modulator (Source: ) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison. cholinergic antagonist (Code: CHEBI:48873) neurotransmitter agent (Code: CHEBI:35942) rodenticide (Code: CHEBI:33288) avicide (Code: CHEBI:33289) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Convulsants (Code: D003292) Glycine Agents (Code: D018684) Neurotransmitter Agents (Code: D018377) Noxae (Code: D009676) Poisons (Code: D011042) SY9
Click to view fenalamide
Click to view progabide GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) GABA-A receptor; anion channel (Organism: Rattus norvegicus, class: Ion channel, accessions: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14, gene: Gabra1|Gabra2|Gabra3|Gabra4|Gabra5|Gabra6|Gabrb1|Gabrb2|Gabrb3|Gabrd|Gabre|Gabrg1|Gabrg2|Gabrg3|Gabrp|Gabrq, swissprot: GBRA1_RAT|GBRA2_RAT|GBRA3_RAT|GBRA4_RAT|GBRA5_RAT|GBRA6_RAT|GBRB1_RAT|GBRB2_RAT|GBRB3_RAT|GBRD_RAT|GBRE_RAT|GBRG1_RAT|GBRG2_RAT|GBRG3_RAT|GBRP_RAT|Q91ZM7_RAT GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN GABA agonist; structure Anti-Dyskinesia Agents (Code: D018726) Anticonvulsants (Code: D000927) Antidepressive Agents (Code: D000928) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) GABA Agents (Code: D018682) GABA Agonists (Code: D018755) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) 1985-01-01 YEAR INTRODUCED
Click to view lormetazepam Lormetazepam is a 3-hydroxy benzodiazepine derivative. Lormetazepam is a short-acting benzodiazepine. It possesses hypnotic, anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Lormetazepam works by acting on receptors in the brain called GABA receptors. This causes the release of a neurotransmitter called GABA in the brain. Neurotransmitters are chemicals that are stored in nerve cells in the brain and nervous system. Lormetazepam is considered a hypnotic benzodiazepine and is officially indicated for moderate to severe insomnia. sedative (Code: CHEBI:35717) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1981-09-12 Italian Medicines Agency (AIFA)
Click to view isoxicam Isoxicam is an anti-inflammatory drug and a benzothiazine derivative of the oxicam class of drugs. it was withdrawn from the market in the 1980s following its association with cases of Stevens-Johnson syndrome. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antirheumatic drug (Code: CHEBI:35842) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1983-01-01 YEAR INTRODUCED ICD
Click to view sulfachrysoidine Sulfachrysoidine (sulfamidochrysoidine) is a prodrug. Sulfachrysoidine exerted its antibacterial activity through the release in vivo of para-aminobenzenesulfonamide (sulfanilamide).
Click to view naratriptan 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020763s011lbl.pdf) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020763s011lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10193663) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1019366) Naratriptan is a triptan drug used for the treatment of migraine headaches. It is a selective 5-hydroxytryptamine 1 receptor subtype agonist. The therapeutic activity of naratriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system, which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. serotonergic agonist (Code: CHEBI:35941) vasoconstrictor agent (Code: CHEBI:50514) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Serotonin 5-HT1 Receptor Agonists (Code: D058825) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Vasoconstrictor Agents (Code: D014662) Serotonin 1b Receptor Agonists (Code: N0000175763) Serotonin 1d Receptor Agonists (Code: N0000175764) Serotonin-1b and Serotonin-1d Receptor Agonist (Code: N0000175765) 1998-02-10 FDA
Click to view almotriptan 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021001s015lbl.pdf) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021001s015lbl.pdf) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021001s015lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021001s015lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021001s015lbl.pdf) Almotriptan is a selective 5-hydroxytryptamine 1B/1D receptor agonist. The therapeutic activity of almotriptan in migraine can most likely be attributed to agonist effects at 5-HT1B/1D receptors on the extracerebral, intracranial blood vessels that become dilated during a migraine attack and on nerve terminals in the trigeminal system. Activation of these receptors results in cranial vessel constriction, inhibition of neuropeptide release, and reduced transmission in trigeminal pain pathways. Almotriptan has weak affinity for 5-HT1A and 5-HT7 receptors, but has no significant affinity or pharmacological activity at 5-HT2, 5-HT3, 5-HT4, 5-HT6; alpha or beta adrenergic; adenosine (A1, A2); angiotensin (AT1, AT2); dopamine (D1, D2); endothelin (ETA, ETB); or tachykinin (NK1, NK2, NK3) binding sites. Almotriptan is indicated for acute treatment of migraine attacks with or without aura. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) serotonergic agonist (Code: CHEBI:35941) vasoconstrictor agent (Code: CHEBI:50514) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Serotonin 1b Receptor Agonists (Code: N0000175763) Serotonin 1d Receptor Agonists (Code: N0000175764) Serotonin-1b and Serotonin-1d Receptor Agonist (Code: N0000175765) 2001-05-07 FDA
Click to view norpipanone
Click to view droprenilamine secondary amine structurally related to prenylamine; RN given refers to parent cpd; synonym MG 8926 refers to HCl; structure
Click to view pirifibrate Pirifibrate is a fibrate agent with antilipidemic activity. Pirifibrate was used in the treatment of hyperlipoproteinemia.
Click to view hydroxychloroquine Toll-like receptor 9 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q9NR96, gene: TLR9, swissprot: TLR9_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18220957) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26429523) Hydroxychloroquine is a chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase.Hydroxychloroquine is active against the erythrocytic forms of chloroquine sensitive strains of Plasmodium falciparum, Plasmodium malariae, Plasmodium ovale, and Plasmodium vivax. It is also indicated for the treatment of discoid and systemic lupus erythematosus, and rheumatoid arthritis. Antirheumatic Agent (Code: N0000175713) antirheumatic drug (Code: CHEBI:35842) dermatologic drug (Code: CHEBI:50177) antimalarial (Code: CHEBI:38068) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Antirheumatic Agents (Code: D018501) Enzyme Inhibitors (Code: D004791) 1955-04-18 FDA
Click to view nifurzide Nifurzide is a member of thiophenes and a C-nitro compound. Nifurzide is a synthetic antimicrobial agent. It is active against Campylobacter spp., Shigella spp., Aeromonas spp., Salmonella spp. and Yersinia enterocolitica. It was used for the treatment of intestinal invections.
Click to view dicoumarol Vitamin K epoxide reductase complex subunit 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BQB6, gene: VKORC1, swissprot: VKOR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17275317) NAD(P)H dehydrogenase [quinone] 1 (Organism: Homo sapiens, class: Enzyme, accessions: P15559, gene: NQO1, swissprot: NQO1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10683249) G-protein coupled receptor 35 (Organism: Homo sapiens, class: GPCR, accessions: Q9HC97, gene: GPR35, swissprot: GPR35_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20919992) Dicumarol is an coumarin-like compound found in sweet clover. It is used as oral anticoagulant and acts by inhibiting the hepatic synthesis of vitamin K-dependent coagulation factors (prothrombin and factors VII, IX, and X). It results in decresed prothrombin levels and a decrease in the amount of thrombin generated and bound to fibrin. This reduces the thrombogenicity of clots. Dicumarol is used along with heparin for treatment of deep vein thrombosis. anticoagulant (Code: CHEBI:50249) Anticoagulants (Code: D000925) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Uncoupling Agents (Code: D014475) 1944-07-31 FDA
Click to view acebutolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT A cardioselective beta-1 adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm, as well as weak inherent sympathomimetic action. beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) beta-adrenergic antagonist (Code: CHEBI:35530) anti-arrhythmia drug (Code: CHEBI:38070) antihypertensive agent (Code: CHEBI:35674) sympathomimetic agent (Code: CHEBI:35524) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) 1984-12-28 FDA
Click to view fluoxymesterone Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women. Androgen (Code: N0000175824) Androgen Receptor Agonists (Code: N0000000146) Androstanes (Code: N0000008241) Anabolic Agents (Code: D045930) antineoplastic agent (Code: CHEBI:35610) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1956-10-15 FDA
Click to view fentanyl Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/202788s016lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/202788s016lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11964599) Fentanyl is a synthetic, lipophilic phenylpiperidine opioid agonist with analgesic and anesthetic properties. Fentanyl selectively binds to the mu-receptor in the central nervous system thereby mimicking the effects of endogenous opiates. Stimulation of the mu-subtype opioid receptor stimulates the exchange of GTP for GDP on the G-protein complex and subsequently inhibits adenylate cyclase. This results in a decrease in intracellular cAMP and leads to a reduction in the release of neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline. The analgesic effect of fentanyl is likely due to its metabolite morphine. Fentanyl is indicated for short term analgesia during induction, maintenance, and recovery from general or regional anesthesia and for the management of breakthrough pain in opioid tolerant cancer patients who require around the clock pain management. Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) Adjuvants, Anesthesia (Code: D000759) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) intravenous anaesthetic (Code: CHEBI:38877) anaesthetic (Code: CHEBI:38867) adjuvant (Code: CHEBI:60809) anaesthesia adjuvant (Code: CHEBI:60807) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1968-02-19 FDA 7V7
Click to view buzepide metiodide component of vesadol
Click to view nifurfoline Nifurfoline is an imidazolidine-2,4-dione belonging to the family of nitrofurans. Nifurfolina is active against Escherichia coli , Proteus , Klebsiella , Enterobacter , staphylococci and enterococci . The antibacterial mechanism of action consists of inhibition of the Krebs cycle in terms of the formation of acetyl coenzyme A, citric acid and oxalacetic acid. This triple inhibition leads to a drastic reduction in the production of energy necessary for the multiplication or survival of bacteria. Nifurfoline was used in the treatment of urinary tract infections.
Click to view ufenamate Ufenamate is an anthranilic acid-based anti-inflammatory drug. it is used for the treatment of skin diseases, such as acute and chronic eczema, contact dermatitis, atopic dermatitis and herpes zoster. 1987-10-01 PMDA
Click to view chlorproethazine D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373)
Click to view linezolid 23S rRNA (Organism: aerobic Gram-positive bacteria, class: Ribosomal protein, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021130s037,021131s030,021132s035lbl.pdf) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12127518) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17095223) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26536532) An oxazolidinone and acetamide derived anti-bacterial agent and protein synthesis inhibitor that is used in the treatment of gram-positive bacterial infections of the skin and respiratory tract. Linezolid binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, which is essential for bacterial reproduction. The results of time-kill studies have shown linezolid to be bacteriostatic against enterococci and staphylococci. For streptococci, linezolid was found to be bactericidal for the majority of isolates. antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) Oxazolidinone Antibacterial (Code: N0000175495) Oxazolidinones (Code: N0000007568) 2000-04-18 FDA ZLD
Click to view disufenton a nitrone benzene bissulfonate in development for stroke; has neuroprotective activity Antioxidants (Code: D000975) Cardiovascular Agents (Code: D002317) Protective Agents (Code: D020011)
Click to view tenoxicam Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.medsafe.govt.nz/profs/Datasheet/t/Tilcotiltab.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.medsafe.govt.nz/profs/Datasheet/t/Tilcotiltab.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9663807) Solute carrier family 22 member 8 (Organism: Mus musculus, class: Transporter, accessions: O88909, gene: Slc22a8, swissprot: S22A8_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15100168) Tenoxicam is a NSAID with anti-inflammatory, analgesic, antipyretic properties and it also inhibits platelet aggregation. In vitro investigation on cyclo-oxygenase isoenzymes prepared from human COS-7 cells have shown that tenoxicam inhibits COX-1 and COX-2 isoenzymes approximately to the same extent i.e. COX-2/COX-1 ratio equals to 1.34. Tenoxicam is indicated for the symptomatic treatment of the following painful inflammatory and degenerative disorders of the musculoskeletal system. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1986-12-18 New Zealand Medicines and Medical Devices Safety Authority
Click to view propanidid An intravenous anesthetic that has been used for rapid induction of anesthesia and for maintenance of anesthesia of short duration. (From Martindale, The Extra Pharmacopoeia, 30th ed, p918) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492)
Click to view pargeverine used as premedication when performing endoscopic retrograde cholangiopancreatography (ERCP)
Click to view olopatadine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206276s000lbl.pdf) Protein S100-A1 (Organism: Homo sapiens, class: Unclassified protein , accessions: P23297, gene: S100A1, swissprot: S10A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11944917) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18445990) Olopatadine is a mast cell stabilizer and a histamine H1 antagonist. Olopatadine is used for the symptomatic treatment of ocular itching associated with allergic conjunctivitis in ophthalmic formulations and seasonal allergic rhinitis in intranasal formulations. Decreased Histamine Release (Code: N0000175628) Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Inhibitor (Code: N0000175519) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Allergic Agents (Code: D018926) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1996-12-18 FDA
Click to view famotidine Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019462s040lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019462s040lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019462s040lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019462s040lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019462s040lbl.pdf) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Famotidine is a propanimidamide and histamine H2-receptor antagonist with antacid activity. As a competitive inhibitor of histamine H2-receptors located on the basolateral membrane of the parietal cell, famotidine reduces basal and nocturnal gastric acid secretion, resulting in a reduction in gastric volume, acidity, and amount of gastric acid released in response to various stimuli. Famotidine is indicated for the treatment of active duodenal and gastric ulcers, symptomatic nonerosive gastroesophageal reflux disease (GERD), erosive esophagitis due to GERD, pathological hypersecretory conditions (e.g., Zollinger-Ellison syndrome, multiple endocrine neoplasias) and for the reduction of the risk of duodenal ulcer recurrence. H2-receptor antagonist (Code: CHEBI:37961) anti-ulcer drug (Code: CHEBI:49201) Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H2 Antagonists (Code: D006635) Neurotransmitter Agents (Code: D018377) Histamine H2 Receptor Antagonists (Code: N0000000151) Histamine-2 Receptor Antagonist (Code: N0000175784) 1986-10-15 FDA FO9
Click to view decimemide
Click to view danazol Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18061638) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18061638) Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18061638) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22328583) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22328583) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22328583) Danazol is a synthetic steroid derived from ethisterone. Danazol suppresses the pituitary-ovarian axis. This suppression is probably a combination of depressed hypothalamic-pituitary response to lowered estrogen production, the alteration of sex steroid metabolism, and interaction of danazol with sex hormone receptors. The only other demonstrable hormonal effect is weak androgenic activity. Danazol depresses the output of both follicle-stimulating hormone and luteinizing hormone. Recent evidence suggests a direct inhibitory effect at gonadal sites and a binding of danazol to receptors of gonadal steroids at target organs. In addition, danazol has been shown to significantly decrease IgG, IgM and IgA levels, as well as phospholipid and IgG isotope autoantibodies in patients with endometriosis and associated elevations of autoantibodies. Danazol is indicated for the treatment of endometriosis amenable to hormonal management, fibrocystic breast disease and for the prevention of attacks of angioedema of all types (cutaneous, abdominal, laryngeal) in males and females. anti-estrogen (Code: CHEBI:50751) estrogen antagonist (Code: CHEBI:50837) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Androgen (Code: N0000175824) Androgen Receptor Agonists (Code: N0000000146) Androstanes (Code: N0000008241) 1976-06-21 FDA
Click to view amineptine Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT used in treatment of neuroses with psychoasthenic, anxio-phobic & depressive manifestations; synonym S 1694 refers to HCl; structure dopamine uptake inhibitor (Code: CHEBI:51039) antidepressant (Code: CHEBI:35469) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619)
Click to view fenpiverinium Fenpiverinium is an anticholinergic and antispasmodic compound which is used in a combination drug with pitofenone hydrochloride and either nimesulide or metamizole for the treatment of smooth muscle spasms and pain. 2004-04-12 Ministry of Health of the Russian Federation
Click to view suloctidil Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) Substance-K receptor (Organism: Homo sapiens, class: GPCR, accessions: P21452, gene: TACR2, swissprot: NK2R_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT A peripheral vasodilator that was formerly used in the management of peripheral and cerebral vascular disorders. It is hepatotoxic and fatalities have occurred. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view fenquizone Fenquizone is a quinazolinone sulphonamide-based diuretic, structurally related to metolazone, with thiazide-like activity. As a thiazide-like diuretic, fenquizone acts by blocking reabsorption of sodium in the proximal tubule and the ascending branch of the loop of Henle. This causes an increase in diuresis with the elimination of chloride and sodium. Fenquizone is used for the treatment of edema and hypertension. Diuretics (Code: D004232) Natriuretic Agents (Code: D045283)
Click to view idebenone a synthetic analogue of ubiquinone. Antioxidants (Code: D000975) Protective Agents (Code: D020011) 2015-09-08 EMA
Click to view lisuride 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) agonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT) agonist (Source: ) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) agonist (Source: ) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: ) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: ) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: ) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT An ergot derivative that acts as an agonist at dopamine D2 receptors (DOPAMINE AGONISTS). It may also act as an antagonist at dopamine D1 receptors, and as an agonist at some serotonin receptors (SEROTONIN RECEPTOR AGONISTS). antiparkinson drug (Code: CHEBI:48407) serotonergic agonist (Code: CHEBI:35941) dopamine agonist (Code: CHEBI:51065) antidyskinesia agent (Code: CHEBI:66956) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366)
Click to view UREA C13 Urease (Organism: Helicobacter pylori, class: Enzyme, accessions: Q8KT33, gene: ureB, swissprot: Q8KT33_HELPY) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21314_BreathID_lbl.pdf) Urea C-13 is a radiolabelled urea molecule used to diagnose stomach ulcers caused by Heliobacter pylori. In the presence of H. pylori, urea C-13 is metabolized by urease to produce ammonia and radioactive carbon dioxide at the interface between the gastric epithelium and lumen. The radioactive carbon dioxide is absorbed in the blood and is detected when exhaled in the breath. Carbon Radioisotopes (Code: N0000166118) Helicobacter pylori Diagnostic (Code: N0000175886) Radioactive Tracers (Code: N0000166093) Urea (Code: N0000006999) 1996-09-17 FDA URE
Click to view pirmenol Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) an antiarrhythmic with class Ia activity Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) 1994-01-01 YEAR INTRODUCED
Click to view chlortalidone Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19119014) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19119014) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19119014) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19119014) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19119014) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19119014) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19119014) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19119014) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19119014) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19119014) Chlorthalidone is a monosulfonamyl diuretic. It is an oral diuretic with prolonged action and low toxicity. The site of action appears to be the cortical diluting segment of the ascending limb of Henle's loop of the nephron. The mechanism of action is associated with activation of sodium and chloride renal excretion. Chlorthalidone is is used for the treatment of hypertansion and edema. Increased Diuresis (Code: N0000175359) Thiazide-like Diuretic (Code: N0000175420) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) 1960-04-07 FDA KLT
Click to view brodimoprim Brodimoprim (2,4-diaminobenzylpyrimidine) inhibits bacterial and resistance plasmid dihydrofolate reductases to a similar or greater extent than trimethoprim. Brodimoprim is two to three times more potent than trimethoprim and has more than 100-fold the affinity for dihydrofolate reductase with analogous enzymatic activity of eukaryotic cells. antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) 1993-01-01 YEAR INTRODUCED
Click to view cefacetrile Cefacetrile is a first generation cephalosporin. It exerts high activity against Gram-positive bacteria and is less active against Gram-negative bacteria. Cephacetrile was used in the treatment of female pelvic inflammatory disease, meningitis and number of other systemic, respiratory and urinary infections. Now it is used for the treatment of bacterial infections in animals. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view mofezolac Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN Prostaglandin G/H synthase 1 (Organism: Ovis aries, class: Enzyme, accessions: P05979, gene: PTGS1, swissprot: PGH1_SHEEP Prostaglandin G/H synthase 2 (Organism: Ovis aries, class: Enzyme, accessions: P79208, gene: PTGS2, swissprot: PGH2_SHEEP Cyclooxygenase 1 inhibitor; ; RN from Toxlit Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) PMDA 63X
Click to view topiramate Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020505s060,020844s051lbl.pdf) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020505s060,020844s051lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020505s060,020844s051lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020505s060,020844s051lbl.pdf) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12747791) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14684331) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16039848) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15837316) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15837316) Carbonic anhydrase (Organism: Helicobacter pylori (strain ATCC 700392 / 26695), class: Enzyme, accessions: O24855, gene: cynT, swissprot: CYNT_HELPY) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16459077) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17125255) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17125255) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17125255) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Glutamate receptor ionotropic, kainate 1 (Organism: Rattus norvegicus, class: Ion channel, accessions: P22756, gene: Grik1, swissprot: GRIK1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19417176) GABA-A receptor; anion channel (Organism: Rattus norvegicus, class: Ion channel, accessions: P62813|P23576|P20236|P28471|P19969|P30191|P15431|P63138|P63079|P18506|P23574|P18508|P28473|Q9ES14|O09028|Q91ZM7, gene: Gabra1|Gabra2|Gabra3|Gabra4|Gabra5|Gabra6|Gabrb1|Gabrb2|Gabrb3|Gabrd|Gabrg1|Gabrg2|Gabrg3|Gabre|Gabrp|Gabrq, swissprot: GBRA1_RAT|GBRA2_RAT|GBRA3_RAT|GBRA4_RAT|GBRA5_RAT|GBRA6_RAT|GBRB1_RAT|GBRB2_RAT|GBRB3_RAT|GBRD_RAT|GBRG1_RAT|GBRG2_RAT|GBRG3_RAT|GBRE_RAT|GBRP_RAT|Q91ZM7_RAT) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/19417176) Topiramate is a sulfamate-substituted monosaccharide. with anticonvulsant property. Although the mechanism of action has not been fully elucidated, topiramate antagonizes kainate/AMPA subtype of the glutamate receptors, which are ligand-activated cation channels that mediate the fast component of excitatory postsynaptic currents in neurons of the central nervous system. This antagonistic action results in stabilizing hyper-excited neural membranes, inhibiting repetitive neuronal firing, and decreasing propagation of synaptic impulses, thereby impedes seizure occurrences. In addition, this agent augments gamma-aminobenzoic acid (GABA) activity and thereby attenuating GABAnergic inhibitory transmission. anticonvulsant (Code: CHEBI:35623) Anti-Obesity Agents (Code: D019440) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Neuroprotective Agents (Code: D018696) Protective Agents (Code: D020011) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Cytochrome P450 3A4 Inducers (Code: N0000185506) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) 1996-12-24 FDA TOR
Click to view papaverine cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12646997) cAMP-specific 3',5'-cyclic phosphodiesterase 4B (Organism: Homo sapiens, class: Enzyme, accessions: Q07343, gene: PDE4B, swissprot: PDE4B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12646997) cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12646997) cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Organism: Rattus norvegicus, class: Enzyme, accessions: Q9QYJ6, gene: Pde10a, swissprot: PDE10_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19066855) Phosphodiesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P54750|Q01064|Q14123, gene: PDE1A|PDE1B|PDE1C, swissprot: PDE1A_HUMAN|PDE1B_HUMAN|PDE1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2985781) Phosphodiesterase 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q13370|Q14432, gene: PDE3A|PDE3B, swissprot: PDE3A_HUMAN|PDE3B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2985781) cGMP-dependent 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O00408, gene: PDE2A, swissprot: PDE2A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2985781) cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y233, gene: PDE10A, swissprot: PDE10_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21602043) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16483771) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19034039) Telomerase reverse transcriptase (Organism: Homo sapiens, class: Enzyme, accessions: O14746, gene: TERT, swissprot: TERT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25111025) Papaverine is an opiate alkaloid isolated from the plant Papaver somniferum and produced synthetically. As a direct-acting smooth muscle relaxant, papaverine is not closely related to the other opium alkaloids in structure or pharmacological actions; its mechanism of action may involve the non-selective inhibition of phosphodiesterases and direct inhibition of calcium channels. Papaverine is used for the treating certain conditions that are accompanied by smooth muscle spasms. Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Phosphodiesterase Inhibitors (Code: D010726) Urological Agents (Code: D064804) Vasodilator Agents (Code: D014665) FDA EV1
Click to view xamoterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) A phenoxypropanolamine derivative that is a selective beta-1-adrenergic agonist. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-1 Receptor Agonists (Code: D058665) Adrenergic beta-Agonists (Code: D000318) Neurotransmitter Agents (Code: D018377)
Click to view panipenem synthetic cpd; structure given in first source
Click to view pipethanate
Click to view nalmefene Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/020459s006lbl.pdf) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/020459s006lbl.pdf) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/020459s006lbl.pdf) Nalmefene is an opiate receptor antagonist. Nalmefene is indicated for the complete or partial reversal of opioid drug effects (including respiratory depression, induced by either natural or synthetic opioids) and is indicated in the management of known or suspected opioid overdose. Opioid Antagonist (Code: N0000175691) Opioid Antagonists (Code: N0000000154) Central Nervous System Agents (Code: D002491) Narcotic Antagonists (Code: D009292) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1995-04-17 FDA
Click to view methylergometrine 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20958049) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15322733) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15322733) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8380639) Methylergometrine (other names include methylergonovine, methylergobasin, methergine, and D-lysergic acid 1-butanolamide) is a synthetic analogue of ergonovine, a psychedelic alkaloid found in ergot, and many species of morning glory. Methylergometrine is used for the prevention and control of excessive bleeding following vaginal childbirth. Ergolines (Code: N0000007618) Ergot Derivative (Code: N0000175827) Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102) 1946-11-19 FDA
Click to view propoxyphene Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/016862s041s042lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/016862s041s042lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/016862s041s042lbl.pdf) Propoxyphene is a centrally acting opiate analgesic. In vitro studies demonstrated propoxyphene and the metabolite norpropoxyphene inhibit sodium channels (local anesthetic effect) with norpropoxyphene being approximately 2-fold more potent than propoxyphene and propoxyphene approximately 10-fold more potent than lidocaine. Propoxyphene and norpropoxyphene inhibit the voltage-gated potassium current carried by cardiac rapidly activating delayed rectifier (hERG) channels with approximately equal potency. The dextro-isomer (dextropropoxyphene) has an analgesic effect. The levo-isomer (levopropoxyphene) exerts only an antitussive effect. Dextroropoxyphene is indicated for the relief of mild to moderate pain. Levopropoxyphene is used as an antitussive. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) dextropropoxyphene: 1957-08-16 FDA levolevopropoxyphene: 1962-03-21 FDA
Click to view propyromazine Spasmolytic and anticholinergic agent
Click to view halazepam Halazepam is a benzodiazepine derivative drug exerting anxiolytic, anticonvulsant, sedative, a muscle relaxing effects. Halazepam potentiates the inhibitory activities of gamma-aminobutyric acid (GABA) by binding to the benzodiazepine-GABA-A-chloride ionophore receptor complex located in the limbic, thalamic, and hypothalamic regions of the central nervous system (CNS). This increases the frequency of chloride channel opening, allowing the flow of chloride ions into the neuron and ultimately leading to membrane hyperpolarization and a decrease in neuronal excitability. Halazepam, like quazepam, binds to GABA-A receptors in lamina IV of the cerebral cortex, the zona incerta, substantia nigra and the cerebellum. Halazepam is used to relieve anxiety, nervousness, and tension associated with anxiety disorders. Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1981-09-24 FDA
Click to view disopyramide G protein-activated inward rectifier potassium channel 4 (Organism: Homo sapiens, class: Ion channel, accessions: P48544, gene: KCNJ5, swissprot: KCNJ5_HUMAN) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y3Q4, gene: HCN4, swissprot: HCN4_HUMAN) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) A class I anti-arrhythmic agent (one that interferes directly with the depolarization of the cardiac membrane and thus serves as a membrane-stabilizing agent) with a depressant action on the heart similar to that of guanidine. It also possesses some anticholinergic and local anesthetic properties. Antiarrhythmic (Code: N0000175426) Anti-Arrhythmia Agents (Code: D000889) anti-arrhythmia drug (Code: CHEBI:38070) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1977-09-01 FDA DP0
Click to view perazine A phenothiazine antipsychotic with actions and uses similar to those of CHLORPROMAZINE. Extrapyramidal symptoms may be more common than other side effects. phenothiazine antipsychotic drug (Code: CHEBI:37930) dopaminergic antagonist (Code: CHEBI:48561) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view rociverine Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view hexetidine Hexetidine is antiseptic with broad antibacterial and antifungal activity in vivo and in vitro. It has local-anesthetics, astringent and deodorant activity. It is used as a 0.1% mouthwash for local infections and oral hygiene. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Antifungal Agents (Code: D000935) 1960-03-01 Italian Medicines Agency (AIFA)
Click to view metipamide diuretic with a hypotensive effect
Click to view pirisudanol cerebral stimulant; RN given refers to parent cpd; synonym stivane refers to dimaleate; structure
Click to view pentamidine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN Protein-tyrosine phosphatase 4A3 (Organism: Homo sapiens, class: Enzyme, accessions: O75365, gene: PTP4A3, swissprot: TP4A3_HUMAN Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Trypsin-1 (Organism: Homo sapiens, class: Enzyme, accessions: P07477, gene: PRSS1, swissprot: TRY1_HUMAN Glutamate NMDA receptor; GRIN1/GRIN2A (Organism: Homo sapiens, class: Ion channel, accessions: Q05586|Q12879, gene: GRIN1|GRIN2A, swissprot: NMDE1_HUMAN|NMDZ1_HUMAN Acrosin (Organism: Sus scrofa, class: Unclassified, accessions: P08001, gene: ACR, swissprot: ACRO_PIG Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q8VHN2|Q9R1M7, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMD3A_RAT|NMD3B_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMDZ1_RAT Amiloride-sensitive amine oxidase [copper-containing] (Organism: Homo sapiens, class: Enzyme, accessions: P19801, gene: AOC1, swissprot: AOC1_HUMAN Suppressor of tumorigenicity 14 protein (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y5Y6, gene: ST14, swissprot: ST14_HUMAN Protein S100-B (Organism: Homo sapiens, class: Cytosolic other, accessions: P04271, gene: S100B, swissprot: S100B_HUMAN Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN Spermidine/spermine N(1)-acetyltransferase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P21673, gene: SAT1, swissprot: SAT1_HUMAN Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Antiprotozoal agent effective in trypanosomiasis, leishmaniasis, and some fungal infections; used in treatment of PNEUMOCYSTIS pneumonia in HIV-infected patients. It may cause diabetes mellitus, central nervous system damage, and other toxic effects. Antiprotozoal (Code: N0000175485) trypanocidal drug (Code: CHEBI:36335) anti-inflammatory agent (Code: CHEBI:67079) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Trypanocidal Agents (Code: D014344) 1984-10-16 FDA PNT
Click to view flutrimazole Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN Bile acid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q96RI1, gene: NR1H4, swissprot: NR1H4_HUMAN Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935)
Click to view poldine major descriptor (66-86); on-line search BENZILATES (66-86); INDEX MEDICUS search POLDINE (66-86); RN given refers to parent cpd
Click to view parapenzolate
Click to view methanthelinium Muscarinic acetylcholine receptor (Organism: Homo sapiens, class: GPCR, accessions: P08172|P08173|P08912|P11229|P20309, gene: CHRM1|CHRM2|CHRM3|CHRM4|CHRM5, swissprot: ACM1_HUMAN|ACM2_HUMAN|ACM3_HUMAN|ACM4_HUMAN|ACM5_HUMAN) antagonist (Source: http://www.kegg.jp/entry/D00721) an anticholinergic agent used as an adjunctive therapy in peptic ulcer Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) 1951-07-03 FDA
Click to view mepenzolate Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist anticholinergic, antispasmodic agent; RN given refers to parent cpd; structure Anticholinergic (Code: N0000175574) Cholinergic Antagonists (Code: N0000175370) 1956-11-14 FDA
Click to view norethindrone acetate Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN used for long-term contraception; structure in Negwer, 5th ed, #4935 synthetic oral contraceptive (Code: CHEBI:49326) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102) 1973-04-30 FDA
Click to view canrenone Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/21771637) A synthetic pregnadiene compound with anti-aldosterone activity. Diuretics (Code: D004232) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Mineralocorticoid Receptor Antagonists (Code: D000451) Natriuretic Agents (Code: D045283)
Click to view ethylhydrocupreine
Click to view terguride Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: ) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: ) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: ) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: ) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: ) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: ) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT D(1A) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901, gene: Drd1, swissprot: DRD1_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) pronounced antifertility agent in rats; lactation suppressor in other species; serotonin antagonist; RN given refers to parent cpd; structure Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) PMDA
Click to view propiomazine Propiomazine is a phenothiazine derivative and atypical antipsychotic agent with sedative, antiemetic and antipsychotic activities. Propiomazine binds to a variety of receptors, including alpha1, dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors. Propiomazine exerts its antiemetic and sedative effects through antagonism at histamine H1 receptors; Its antipsychotic effect is attributed to antagonistic activities at dopamine and 5-HT2 receptors. Propiomazine was used for the relief of restlessness and apprehension, preoperatively or during surgery. In addition it was used as an adjunct to analgesics for the relief of restlessness and apprehension during labor. However, this drug was discontinued. phenothiazine antipsychotic drug (Code: CHEBI:37930) dopaminergic antagonist (Code: CHEBI:48561) serotonergic antagonist (Code: CHEBI:48279) muscarinic antagonist (Code: CHEBI:48876) histamine antagonist (Code: CHEBI:37956) sedative (Code: CHEBI:35717) 1960-12-05 FDA
Click to view lucanthone DNA-(apurinic or apyrimidinic site) lyase (Organism: Homo sapiens, class: Enzyme, accessions: P27695, gene: APEX1, swissprot: APEX1_HUMAN One of the SCHISTOSOMICIDES, it has been replaced largely by HYCANTHONE and more recently PRAZIQUANTEL. (From Martindale The Extrapharmacopoeia, 30th ed., p46) Anthelmintics (Code: D000871) schistosomicide drug (Code: CHEBI:38941) antineoplastic agent (Code: CHEBI:35610) photosensitizing agent (Code: CHEBI:47868) prodrug (Code: CHEBI:50266) adjuvant (Code: CHEBI:60809) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Schistosomicides (Code: D012556)
Click to view medrogestone 6,17-Dimethylpregna-4,6-diene-3,20-dione. A synthetic progestational hormone with actions similar to those of progesterone. It is used in the treatment of menstrual irregularities and has also been employed in the treatment of prostatic hypertrophy and endometrial carcinoma. Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931)
Click to view dimethisterone A synthetic progestational hormone without significant estrogenic or androgenic properties. It was formerly used as the progestational component in oral sequential contraceptives. Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102)
Click to view penthienate
Click to view docosanoic acid Peroxisome proliferator-activated receptor delta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q03181, gene: PPARD, swissprot: PPARD_HUMAN Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN
Click to view propanol Propanol (propyl alcohol) is a colorless liquid made by oxidation of aliphatic hydrocarbons that is used as a solvent and chemical intermediate. It is used as a solvent in the pharmaceutical industry, and for resins and cellulose esters. It is formed naturally in small amounts during many fermentation processes and small amounts are produced by gut microflora. protic solvent (Code: CHEBI:48356) 1994-02-15 Austrian Medicines and Medical Devices Agency POL
Click to view nitroxazepine has pronounced sedative properties, but otherwise resembles imipramine; minor descriptor (77-84); on-line & Index Medicus search DIBENZOXAZEPINES (77-84); RN given refers to mono-HCl
Click to view thebacon
Click to view naltrexone Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021897s042lbl.pdf) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021897s042lbl.pdf) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021897s042lbl.pdf) Naltrexone is a noroxymorphone derivative with competitive opioid antagonistic property. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence. central nervous system depressant (Code: CHEBI:35488) antidote to opioid poisoning (Code: CHEBI:90755) Central Nervous System Agents (Code: D002491) Narcotic Antagonists (Code: D009292) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Opioid Antagonist (Code: N0000175691) Opioid Antagonists (Code: N0000000154) 1984-11-20 FDA
Click to view diseptal B Diseptal B is a monomethyl derivative. It was developed as an anti-streptococcal agent.
Click to view fenetylline Fenetylline is a codrug of amphetamine and theophylline. Fenetylline after oral administration is metabolized into 24.5% Amphetamine and 13.7% Theophylline. It was formerly used to treat conditions such as attention deficit hyperactivity disorder, narcolepsy, and depression, but its use has been banned because of the potential for abuse. (See: amphetamine) (See: theophylline) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697)
Click to view sulpiride D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21495689) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21495689) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686894) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686894) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15686894) Carbonic anhydrase (Organism: Helicobacter pylori (strain ATCC 700392 / 26695), class: Enzyme, accessions: O24855, gene: cynT, swissprot: CYNT_HELPY) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16539401) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17251018) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19193158) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19193158) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23867389) Delta carbonic anhydrase (Organism: Thalassiosira weissflogii, class: Unclassified, accessions: Q5U9J1, gene: ca1, swissprot: Q5U9J1_THAWE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24314394) Sulpiride is a dopamine antagonist. Sulpiride is more selective and acts primarily as a dopamine D2 antagonist. It has a role as an antidepressant, an antiemetic and an antipsychotic agent. Levosulpiride or (S)-(-)-sulpiride is an optically active form of the racemic drug. It is used for the treatment the treatment of psychosis associated with schizophrenia and major depressive disorder. antidepressant (Code: CHEBI:35469) antiemetic (Code: CHEBI:50919) antipsychotic agent (Code: CHEBI:35476) dopaminergic antagonist (Code: CHEBI:48561) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1977-02-09 Italian Medicines Agency (AIFA)
Click to view cyclacillin Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor (Source: ) A cyclohexylamido analog of PENICILLANIC ACID. antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1979-09-13 FDA
Click to view propafenone Potassium voltage-gated channel subfamily A member 5 (Organism: Homo sapiens, class: Ion channel, accessions: P22460, gene: KCNA5, swissprot: KCNA5_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019151s015lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019151s015lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019151s015lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019151s015lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019151s015lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019151s015lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12618228) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15900513) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21955244) Sulfonylurea receptor 2, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: O60706|Q14654, gene: ABCC9|KCNJ11, swissprot: ABCC9_HUMAN|KCJ11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21955244) Potassium channel subfamily K member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O95069, gene: KCNK2, swissprot: KCNK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26588045) Potassium channel subfamily K member 3 (Organism: Homo sapiens, class: Ion channel, accessions: O14649, gene: KCNK3, swissprot: KCNK3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26588045) Propafenone is a Class 1C antiarrhythmic drug with local anesthetic effects and a direct stabilizing action on myocardial membranes. The electrophysiological effect of propafenone manifests itself in a reduction of upstroke velocity (Phase 0) of the monophasic action potential. In Purkinje fibers, and, to a lesser extent, myocardial fibers, propafenone reduces the fast inward current carried by sodium ions. Diastolic excitability threshold is increased and effective refractory period prolonged. Propafenone reduces spontaneous automaticity and depresses triggered activity. Propafenone is indicated to prolong the time to recurrence of symptomatic atrial fibrillation, prolong the time to recurrence of paroxysmal supraventricular tachycardia associated with disabling symptoms and for the treatment life-threatening ventricular arrhythmias. Antiarrhythmic (Code: N0000175426) Anti-Arrhythmia Agents (Code: D000889) anti-arrhythmia drug (Code: CHEBI:38070) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1989-11-27 FDA
Click to view clobenztropine Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT
Click to view maltose A dextrodisaccharide from malt and starch. It is used as a sweetening agent and fermentable intermediate in brewing. (Grant & Hackh's Chemical Dictionary, 5th ed) sweetening agent (Code: CHEBI:50505) Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Sweetening Agents (Code: D013549) MAL
N9S
Click to view lactulose A synthetic disaccharide used in the treatment of constipation and hepatic encephalopathy. It has also been used in the diagnosis of gastrointestinal disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p887) laxative (Code: CHEBI:50503) gastrointestinal drug (Code: CHEBI:55324) Gastrointestinal Agents (Code: D005765) Osmotic Laxative (Code: N0000175811) Osmotic Activity (Code: N0000010288) Acidifying Activity (Code: N0000175833) Stimulation Large Intestine Fluid/Electrolyte Secretion (Code: N0000009871) 1976-03-25 FDA
Click to view lactose A disaccharide of GLUCOSE and GALACTOSE in human and cow milk. It is used in pharmacy for tablets, in medicine as a nutrient, and in industry. Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Sweetening Agents (Code: D013549) LBT
LAT
Click to view siccanin antifungal drug (Code: CHEBI:86327)
Click to view megestrol acetate Megestrol Acetate is the acetate salt form of megestrol, a synthetic derivative of the naturally occurring female sex hormone progesterone with potential anti-estrogenic and antineoplastic activity. Mimicking the action of progesterone, megestrol acetate binds to and activates nuclear progesterone receptors in the reproductive system, and causes the ligand-receptor complex to be translocated to the nucleus where it binds to and promotes expression of target genes. Several investigators have reported on the appetite enhancing property of megestrol acetate and its possible use in cachexia. The precise mechanism by which megestrol acetate produces effects in anorexia and cachexia is unknown at the present time. Megestrol acetate is indicated for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Appetite Stimulants (Code: D019167) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102) Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) 1971-08-18 FDA
Click to view flutoprazepam Flunitrazepam is a short-acting benzodiazepine with general properties similar to diazepam.
Click to view etizolam Etizolam is a thienodiazepine derivative, with high affinity for the benzodiazepine site in GABAA receptors. It has also been shown that it possesses mainly anxiolytic effects but not sedative effects probably due to its lower intrinsic activity at alpha1subunit-containing GABAA receptors when compared to diazepam and alprazolam. Etizolam is indicated for treating generalized anxiety and other psychiatric pathologies. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1988-02-18 Italian Medicines Agency (AIFA) H4C
Click to view triazolam Platelet-activating factor receptor (Organism: Homo sapiens, class: GPCR, accessions: P25105, gene: PTAFR, swissprot: PTAFR_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) GABA-A receptor alpha-5/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P28472|P31644, gene: GABRA5|GABRB3|GABRG2, swissprot: GBRA5_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source:) GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source:) GABA-A receptor alpha-1/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P28472, gene: GABRA1|GABRB3|GABRG2, swissprot: GBRA1_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source:) GABA-A receptor alpha-2/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P28472|P47869, gene: GABRA2|GABRB3|GABRG2, swissprot: GBRA2_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source:) GABA A receptor alpha-3/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P34903|P47870, gene: GABRA3|GABRB2|GABRG2, swissprot: GBRA3_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source:) GABA-A receptor alpha-3/beta-3/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P28472|P34903, gene: GABRA3|GABRB3|GABRG2, swissprot: GBRA3_HUMAN|GBRB3_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source:) GABA A receptor alpha-3/beta-2/gamma-3 (Organism: Homo sapiens, class: Ion channel, accessions: P34903|P47870|Q99928, gene: GABRA3|GABRB2|GABRG3, swissprot: GBRA3_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN) positive allosteric modulator (Source:) GABA-A receptor alpha-1/beta-2/gamma-3 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47870|Q99928, gene: GABRA1|GABRB2|GABRG3, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN) positive allosteric modulator (Source:) GABA A receptor alpha-5/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P31644|P47870, gene: GABRA5|GABRB2|GABRG2, swissprot: GBRA5_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator (Source:) GABA A receptor alpha-5/beta-2/gamma-3 (Organism: Homo sapiens, class: Ion channel, accessions: P31644|P47870|Q99928, gene: GABRA5|GABRB2|GABRG3, swissprot: GBRA5_HUMAN|GBRB2_HUMAN|GBRG3_HUMAN) positive allosteric modulator (Source:) A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Adjuvants, Anesthesia (Code: D000759) Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1982-11-15 FDA
Click to view acetyldihydrocodeine Acetyldihydrocodeine is an opiate derivative. Acetyldihydrocodeine is a 6-acetyl derivative of dihydrocodeine and is metabolised in the liver by demethylation and deacetylation to produce dihydromorphine. (See: dihydrocodeine)
Click to view cinchocaine Sodium channel protein type 10 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y5Y9, gene: SCN10A, swissprot: SCNAA_HUMAN) blocker Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN A local anesthetic of the amide type now generally used for surface anesthesia. It is one of the most potent and toxic of the long-acting local anesthetics and its parenteral use is restricted to spinal anesthesia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1006) Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) topical anaesthetic (Code: CHEBI:48425) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) FDA
Click to view clotiapine D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT) antagonist (Source: https://pubmed.ncbi.nlm.nih.gov/7907148/) Clothiapine is a dibenzothiazepine. It has a high affinity for D2 dopamine and 5-HT2 receptors. Clothiapine is used for the treatment of psychoses, chizophrenia and anxiety. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1968-09-23 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view clemastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/6449094) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19934256) a first generation antihistamine that is used for symptoms of allergic rhinitis and the common cold. Clemastine has not been linked to instances of clinically apparent acute liver injury. Anti-Allergic Agents (Code: D018926) H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) muscarinic antagonist (Code: CHEBI:48876) antipruritic drug (Code: CHEBI:59683) Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1977-02-25 FDA
Click to view bromopride Bromopride is a substituted benzamide with prokinetic and antiemetic properties. Bromopride is a dopamine antagonist used as an antiemetic. Its prokinetic properties are similar to those of metoclopramide. Bromopride is indicated in the treatment of nausea and vomiting, including postoperative nausea and vomiting and as preparation for endoscopy and radiographic studies of the gastrointestinal tract. Also bromopride is used in psychosomatic digestive disorders, such as dyskinesia, nausea and vomiting, loss of appetite. Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) 1977 Italian Medicines Agency (AIFA)
Click to view lactitol Lactitol is a disaccharide consisting of beta-D-galactopyranose and D-glucitol joined by a 1->4 glycosidic bond. It is used as a laxative, as an excipient, and as replacement bulk sweetener in some low-calorie foods. It has a role as a laxative, an excipient and a cathartic. excipient (Code: CHEBI:75324) laxative (Code: CHEBI:50503) Cathartics (Code: D002400) Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Gastrointestinal Agents (Code: D005765) Sweetening Agents (Code: D013549) 2007-10-01 Ministry of Health of the Russian Federation
Click to view sultosilic acid Sultosilic acid is a benzenesulfonate ester. Sultosilic acid has been shown to be a hypolipidaemic drug. Sultosilic acid was used as a piperazine salt. 1982 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view formoterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/20831s2lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/20831s2lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/20831s2lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/20831s2lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/20831s2lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2001/20831s2lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021912s032lbl.pdf) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14730417) Formoterol is a long-acting selective beta2-adrenergic receptor agonist (beta2-agonist). Inhaled formoterol fumarate acts locally in the lung as a bronchodilator. Arformoterol, the (R,R)-enantiomer of formoterol, is a selective long-acting beta2adrenergic receptor agonist (beta2-agonist) that has two-fold greater potency than racemic formoterol (which contains both the (S,S) and (R,R)-enantiomers). Formoterol and arformoterol are used for long-term maintenance treatment of asthma in patients with reversible obstructive airways disease, for the prevention of exercise-induced bronchospasm, as well as long-term treatment of bronchospasm associated with COPD, including chronic bronchitis and emphysema. Not indicated for asthma that can be successfully managed with occasional use of an inhaled, short-acting beta2-adrenergic agonist. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) anti-asthmatic drug (Code: CHEBI:49167) beta-adrenergic agonist (Code: CHEBI:35522) bronchodilator agent (Code: CHEBI:35523) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Adrenergic beta2-Agonists (Code: N0000009922) beta2-Adrenergic Agonist (Code: N0000175779) 2001-02-16 FDA FVN
H98
Click to view piketoprofen Piketoprofen is a nonsteroidal anti-inflammatory drug. It is the 4-picolineamide of the NSAID ketoprofen. Piketoprofen is indicated for topical use in form of a cream. 1983-08-08 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view formebolone
Click to view oxyphencyclimine Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist cholinergic blocking agent used as an adjunct in the treatment of peptic ulcer FDA
Click to view medrysone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1969-11-28 FDA
Click to view medroxyprogesterone Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17013809) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15601807) 3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2 (Organism: Homo sapiens, class: Enzyme, accessions: P26439, gene: HSD3B2, swissprot: 3BHS2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10372718) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16645869) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16645869) A synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms. Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) contraceptive drug (Code: CHEBI:49323) synthetic oral contraceptive (Code: CHEBI:49326) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptive Agents, Male (Code: D003272) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102) 1959-06-18 FDA
Click to view tribromometacresol Tribromometacresol is a hydroxytoluene, wich has antifungal properties. Tribromometacresol was indicated for the topical treatment of mycosis.
Click to view clotrimazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991846) Nuclear receptor subfamily 1 group I member 3 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q14994, gene: NR1I3, swissprot: NR1I3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10748001) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9770465) Hydroxycarboxylic acid receptor 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q8TDS4, gene: HCAR2, swissprot: HCAR2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12799447) Intermediate conductance calcium-activated potassium channel protein 4 (Organism: Homo sapiens, class: Ion channel, accessions: O15554, gene: KCNN4, swissprot: KCNN4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8636434) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11136296) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15135088) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15135088) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15135088) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15135088) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17101742) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12699389) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27000539) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18321482) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/18321482) Potassium voltage-gated channel subfamily A member 3 (Organism: Homo sapiens, class: Ion channel, accessions: P22001, gene: KCNA3, swissprot: KCNA3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19282171) Indoleamine 2,3-dioxygenase 1 (Organism: Mus musculus, class: Enzyme, accessions: P28776, gene: Ido1, swissprot: I23O1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Indoleamine 2,3-dioxygenase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q8R0V5, gene: Ido2, swissprot: I23O2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) CX3C chemokine receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P49238, gene: CX3CR1, swissprot: CX3C1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23437772) Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23437772) Bile acid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q96RI1, gene: NR1H4, swissprot: NR1H4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23688559) An imidazole derivative with a broad spectrum of antimycotic activity. It inhibits biosynthesis of the sterol ergostol, an important component of fungal cell membranes. Its action leads to increased membrane permeability and apparent disruption of enzyme systems bound to the membrane. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) 14-alpha Demethylase Inhibitors (Code: D058888) antiinfective agent (Code: CHEBI:35441) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Antifungal Agents (Code: D000935) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) 1975-02-03 FDA CL6
Click to view trengestone
Click to view clorotepine 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Alpha-1B adrenergic receptor (Organism: Mesocricetus auratus, class: GPCR, accessions: P18841, gene: ADRA1B, swissprot: ADA1B_MESAU Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT D(3) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19020, gene: Drd3, swissprot: DRD3_RAT Serotonin 2 (5-HT2) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P30994, gene: Htr2a|Htr2b|Htr2c, swissprot: 5HT2A_RAT|5HT2B_RAT|5HT2C_RAT Dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901|P19020|P25115|P30729|P61169, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_RAT|DRD2_RAT|DRD3_RAT|DRD4_RAT|DRD5_RAT D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN Alpha-1A adrenergic receptor (Organism: Bos taurus, class: GPCR, accessions: P18130, gene: ADRA1A, swissprot: ADA1A_BOVIN 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN D(1A) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901, gene: Drd1, swissprot: DRD1_RAT Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT Trace amine-associated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q96RJ0, gene: TAAR1, swissprot: TAAR1_HUMAN) major tranquilizer with action similar to those of the phenothiazines; used in schizophrenic & manic psychoses; minor decriptor (77-86); on-line & INDEX MEDICUS search DIBENZOTHIEPINS (77-86); RN given refers to parent cpd without isomeric designation
Click to view niclofolan Proposed fasciolacide. Synonyms: Dertil; Bilevon; Bay 9015.
Click to view tretoquinol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901|P19020|P25115|P30729|P61169, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_RAT|DRD2_RAT|DRD3_RAT|DRD4_RAT|DRD5_RAT Adrenergic receptor alpha (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P19328|P22086|P22909|P23944|P43140, gene: Adra1a|Adra1b|Adra1d|Adra2a|Adra2b|Adra2c, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT|ADA2A_RAT|ADA2B_RAT|ADA2C_RAT Adrenergic receptor beta (Organism: Homo sapiens, class: GPCR, accessions: P07550|P08588|P13945, gene: ADRB1|ADRB2|ADRB3, swissprot: ADRB1_HUMAN|ADRB2_HUMAN|ADRB3_HUMAN Adrenergic receptor beta (Organism: Rattus norvegicus, class: GPCR, accessions: P10608|P18090|P26255, gene: Adrb1|Adrb2|Adrb3, swissprot: ADRB1_RAT|ADRB2_RAT|ADRB3_RAT Thromboxane A2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P21731, gene: TBXA2R, swissprot: TA2R_HUMAN Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) Beta-1 adrenergic receptor (Organism: Cavia porcellus, class: GPCR, accessions: B0FL73, gene: ADRB1, swissprot: B0FL73_CAVPO Beta-2 adrenergic receptor (Organism: Cavia porcellus, class: GPCR, accessions: Q8K4Z4, gene: Adrb2, swissprot: ADRB2_CAVPO An adrenergic beta-agonist used as a bronchodilator agent in asthma therapy. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sympathomimetics (Code: D013566)
Click to view omeprazole Potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P20648|P51164, gene: ATP4A|ATP4B, swissprot: ATP4A_HUMAN|ATP4B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019810s102,022056s019lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019810s102,022056s019lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019810s102,022056s019lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019810s102,022056s019lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/1280125) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/1280125) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15258107) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11770010) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11770010) Canalicular multispecific organic anion transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: O15438, gene: ABCC3, swissprot: MRP3_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12538803) Bombesin receptor subtype-3 (Organism: Homo sapiens, class: GPCR, accessions: P32247, gene: BRS3, swissprot: BRS3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18818070) Fatty acid synthase (Organism: Homo sapiens, class: Enzyme, accessions: P49327, gene: FASN, swissprot: FAS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25513712) Omeprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of the gastric parietal cell. Omeprazole is used for treatment of duodenal ulcer, gastric ulcer, Gastroesophageal Reflux Disease. Proton Pump Inhibitor (Code: N0000175525) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) anti-ulcer drug (Code: CHEBI:49201) anticonvulsant (Code: CHEBI:35623) Anti-Ulcer Agents (Code: D000897) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Proton Pump Inhibitors (Code: D054328) Omeprazole: 1989-09-14 FDA Esomeprazole: 2001-02-20 FDA
Click to view bevantolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist a beta-1 adrenoceptor antagonist that has been shown to be as effective as other beta blockers for the treatment of angina pectoris and hypertension Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) beta-adrenergic antagonist (Code: CHEBI:35530) antihypertensive agent (Code: CHEBI:35674) anti-arrhythmia drug (Code: CHEBI:38070) Neurotransmitter Agents (Code: D018377) 1987-01-01 YEAR INTRODUCED
Click to view clopamide A sulfamoylbenzamide piperidine. It is considered a thiazide-like diuretic. Diuretics (Code: D004232) Natriuretic Agents (Code: D045283)
Click to view metofoline Metofoline is an isoquinoline derivative and an opioid analgesic. Its (R)-enatiomer is approximately six times more potent than codeine, and (S)-enantiomer is inactive. Metofoline was withdrawn from the market for reasons of safety.
Click to view nifedipine Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9846638) Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Homo sapiens, class: Ion channel, accessions: Q01668, gene: CACNA1D, swissprot: CAC1D_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11160515) Potassium voltage-gated channel subfamily D member 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UK17, gene: KCND3, swissprot: KCND3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16414350) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16899990) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9890159) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9890159) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/14570758) Canalicular multispecific organic anion transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: O15438, gene: ABCC3, swissprot: MRP3_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/14570758) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/24014644) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8709132) Adenosine receptor A2a (Organism: Rattus norvegicus, class: GPCR, accessions: P30543, gene: Adora2a, swissprot: AA2AR_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8709132) Adenosine receptor A1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25099, gene: Adora1, swissprot: AA1R_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8709132) Potassium voltage-gated channel subfamily A member 5 (Organism: Homo sapiens, class: Ion channel, accessions: P22460, gene: KCNA5, swissprot: KCNA5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19004630) Transient receptor potential cation channel subfamily A member 1 (Organism: Mus musculus, class: Unclassified, accessions: Q8BLA8, gene: Trpa1, swissprot: TRPA1_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20356305) Glutathione reductase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P00390, gene: GSR, swissprot: GSHR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21795044) Indoleamine 2,3-dioxygenase 1 (Organism: Mus musculus, class: Enzyme, accessions: P28776, gene: Ido1, swissprot: I23O1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Indoleamine 2,3-dioxygenase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q8R0V5, gene: Ido2, swissprot: I23O2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Nifedipine is a dihydropyridine calcium channel blocking agent. Nifedipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. Nifedipine is indicated for the management of vasospastic angina, chronic stable angina (effort-associated angina). vasodilator agent (Code: CHEBI:35620) tocolytic agent (Code: CHEBI:66993) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Reproductive Control Agents (Code: D012102) Tocolytic Agents (Code: D015149) Vasodilator Agents (Code: D014665) Calcium Channel Antagonists (Code: N0000000069) Dihydropyridine Calcium Channel Blocker (Code: N0000175421) Dihydropyridines (Code: N0000007556) 1981-12-31 FDA C5U
Click to view beclobrate Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847)
Click to view adenosine phosphate Fructose-1,6-bisphosphatase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P09467, gene: FBP1, swissprot: F16P1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19348494) Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22738238) 5'-AMP-activated protein kinase subunit gamma-1 (Organism: Homo sapiens, class: Kinase, accessions: P54619, gene: PRKAG1, swissprot: AAKG1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16753576) Transient receptor potential cation channel subfamily M member 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q8TD43, gene: TRPM4, swissprot: TRPM4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14758478) Adenosine phosphate is a nucleotide, consisting of a phosphate group, the sugar ribose, and the nucleobase adenine. AMP is an activator of several enzymes in the tissues. In the glycolytic pathway, the enzyme phosphofructokinase is inhibited by ATP but the inhibition is reversed by AMP, the deciding factor for the reaction being the ratio between ATP and AMP. In medicine, AMP is used mainly as an alternative to adenosine for treatment of ischemia and as a tool compound to measure hyperresponsiveness of airways. nutraceutical (Code: CHEBI:50733) 1978-10-23 Ministry of Health of the Russian Federation AMP
Click to view arsthinol nanosuspensions of arsthinol could be used for treatment of acute promyelocytic leukaemia
Click to view nafamostat Serine protease hepsin (Organism: Homo sapiens, class: Enzyme, accessions: P05981, gene: HPN, swissprot: HEPS_HUMAN Hepatocyte growth factor activator (Organism: Homo sapiens, class: Enzyme, accessions: Q04756, gene: HGFAC, swissprot: HGFA_HUMAN Plasminogen (Organism: Homo sapiens, class: Enzyme, accessions: P00747, gene: PLG, swissprot: PLMN_HUMAN Prothrombin (Organism: Homo sapiens, class: Enzyme, accessions: P00734, gene: F2, swissprot: THRB_HUMAN Cationic trypsin (Organism: Bos taurus, class: Enzyme, accessions: P00760, gene: None, swissprot: TRY1_BOVIN Trypsin-1 (Organism: Homo sapiens, class: Enzyme, accessions: P07477, gene: PRSS1, swissprot: TRY1_HUMAN) inhibitor Complement C1r subcomponent (Organism: Homo sapiens, class: Enzyme, accessions: P00736, gene: C1R, swissprot: C1R_HUMAN) inhibitor Complement C1s subcomponent (Organism: Homo sapiens, class: Enzyme, accessions: P09871, gene: C1S, swissprot: C1S_HUMAN Kallikrein-1 (Organism: Homo sapiens, class: Enzyme, accessions: P06870, gene: KLK1, swissprot: KLK1_HUMAN Coagulation factor X (Organism: Homo sapiens, class: Enzyme, accessions: P00742, gene: F10, swissprot: FA10_HUMAN Acid-sensing ion channel 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q16515, gene: ASIC2, swissprot: ASIC2_HUMAN) blocker (Source: ) Acid-sensing ion channel 1 (Organism: Homo sapiens, class: Ion channel, accessions: P78348, gene: ASIC1, swissprot: ASIC1_HUMAN) blocker (Source: ) Acid-sensing ion channel 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UHC3, gene: ASIC3, swissprot: ASIC3_HUMAN) blocker (Source: ) Tryptase alpha/beta-1 (Organism: Homo sapiens, class: Enzyme, accessions: Q15661, gene: TPSAB1, swissprot: TRYB1_HUMAN) inhibitor (Source: ) Suppressor of tumorigenicity 14 protein (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y5Y6, gene: ST14, swissprot: ST14_HUMAN inhibitor of trypsin, plasmin, pancreatic kallikrein, plasma kallikrein & thrombin; strongly inhibits esterolytic activities of C1r & C1 esterase complement-mediated hemolysis; antineoplastic; RN given refers to parent cpd Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anticoagulants (Code: D000925) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Complement Inactivating Agents (Code: D051056) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Peripheral Nervous System Agents (Code: D018373) Protease Inhibitors (Code: D011480) Sensory System Agents (Code: D018689) Serine Proteinase Inhibitors (Code: D015842) Trypsin Inhibitors (Code: D014361) PMDA
Click to view sulbactam pivoxyl Sulbactam Pivoxil is the pivoxil prodrug form of sulbactam, a semi-synthetic beta-lactamase inhibitor, with beta-lactam antibiotic adjuvant activity. After oral administration of sulbactam pivoxil, the ester bond is cleaved, releasing active sulbactam. The beta-lactam ring of sulbactam irreversibly binds to beta-lactamase at or near its active site, thereby blocking enzyme activity and preventing metabolism of other beta-lactam antibiotics by the enzyme. (See: sulbactam)
Click to view cefalexin Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17142565) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8956326) Solute carrier family 22 member 8 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9R1U7, gene: Slc22a8, swissprot: S22A8_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12005172) Cefalexin is a semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of cephaloridine or cephalothin, but somewhat less potent. It is effective against: Staphylococcus aureus (methicillin-susceptible isolates only), Streptococcus pneumoniae (penicillin-susceptible isolates), Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Proteus mirabilis. Cefalexin is used for the treatment of respiratory tract infections (due to S. pneumoniae and S. pyogenes), otitis media (due to S. pneumoniae, H. influenzae, S. aureus, S. pyogenes, and M. catarrhalis), skin and skin structure infections (due to S. aureus and S. pyogenes), bone infections (due to S. aureus and P. mirabilis), genitourinary tract infections (due to E. coli, P. mirabilis, and K. pneumoniae). Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1971-01-04 FDA
Click to view fedrilate
Click to view benzpiperylone spelled benzopiperylone in title
Click to view repirinast Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Neurotransmitter Agents (Code: D018377)
Click to view indoramin D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P19328|P22086|P22909, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT Alpha-1A adrenergic receptor (Organism: Bos taurus, class: GPCR, accessions: P18130, gene: ADRA1A, swissprot: ADA1A_BOVIN Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent. Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 1981-01-01 YEAR INTRODUCED
Click to view clanobutin Clanobutin is a choleretic drug and an appetite stimulant. It increases the secretion of bile by hepatocytes. Now it is used for treating digestive upsets in animals.
Click to view embramine Embramine or mebrophenhydramine is an antiallergic agent. Embramine is a histamine H1-receptor antagonist exerting anticholinergic activity. It may inhibit stimulated platelet functions by inhibiting phospholipase A2. Embramine selectively binds to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. It is prescribed in allergic conditions. Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377)
Click to view succisulfone Succisulfone is a sulfonamide antibiotic. It was used in the treatment of leprosy.
Click to view enalaprilat Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/018998s083lbl.pdf) The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion. Antihypertensive Heart failure treatment Angiotensin-converting enzyme inhibitor 1988-02-09 FDA EAL
Click to view torsemide Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020136s027lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020136s027lbl.pdf) Cytochrome P450 2C18 (Organism: Homo sapiens, class: Enzyme, accessions: P33260, gene: CYP2C18, swissprot: CP2CI_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020136s027lbl.pdf) Heat shock protein HSP 90-alpha (Organism: Homo sapiens, class: Cytosolic other, accessions: P07900, gene: HSP90AA1, swissprot: HS90A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21190426) Torsemide acts from within the lumen of the thick ascending portion of the loop of Henle, where it inhibits the Na+/K+/2Cl–-carrier system. Torsemide increases the urinary excretion of sodium, chloride, and water, but it does not significantly alter glomerular filtration rate, renal plasma flow, or acid-base balance. Torsemide is indicated for the treatment of edema associated with heart failure, renal disease or hepatic disease and for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. Increased Diuresis at Loop of Henle (Code: N0000175366) antihypertensive agent (Code: CHEBI:35674) loop diuretic (Code: CHEBI:77608) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Potassium Chloride Symporter Inhibitors (Code: D049994) 1993-08-23 FDA
Click to view acrivastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/019806s013lbl.pdf) Acrivastine is an analog of triprolidine hydrochloride classified as an alkylamine antihistamine. Acrivastine is indicated for relief of symptoms associated with seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion. Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Antagonist (Code: N0000175587) H1-receptor antagonist (Code: CHEBI:37955) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Neurotransmitter Agents (Code: D018377) 1994-03-25 FDA
Click to view intoplicine DNA topoisomerase I, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q969P6, gene: TOP1MT, swissprot: TOP1M_HUMAN) DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) DNA topoisomerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P11387, gene: TOP1, swissprot: TOP1_HUMAN)
Click to view bexarotene Retinoic acid receptor RXR-alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P19793, gene: RXRA, swissprot: RXRA_HUMAN) agonist Retinoic acid receptor RXR-beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P28702, gene: RXRB, swissprot: RXRB_HUMAN) agonist Retinoic acid receptor RXR-gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P48443, gene: RXRG, swissprot: RXRG_HUMAN) agonist Retinoic acid receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10826, gene: RARB, swissprot: RARB_HUMAN Retinoic acid receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10276, gene: RARA, swissprot: RARA_HUMAN Retinoic acid receptor RXR-gamma (Organism: Mus musculus, class: Transcription factor, accessions: P28705, gene: Rxrg, swissprot: RXRG_MOUSE Retinoic acid receptor RXR-alpha (Organism: Mus musculus, class: Transcription factor, accessions: P28700, gene: Rxra, swissprot: RXRA_MOUSE Retinoic acid receptor RXR-alpha (Organism: Rattus norvegicus, class: Unclassified, accessions: Q05343, gene: Rxra, swissprot: RXRA_RAT Retinoic acid receptor RXR-beta (Organism: Mus musculus, class: Transcription factor, accessions: P28704, gene: Rxrb, swissprot: RXRB_MOUSE Retinoic acid receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P13631, gene: RARG, swissprot: RARG_HUMAN Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) antagonist (Source: ) a retinoid X receptor (RXR) selective agonist antineoplastic agent (Code: CHEBI:35610) Anticarcinogenic Agents (Code: D016588) Antineoplastic Agents (Code: D000970) Protective Agents (Code: D020011) Retinoid (Code: N0000175607) Retinoids (Code: N0000007700) 1999-12-29 FDA 9RA
Click to view leiopyrrole spasmolytic leioplegil is the HCl of leiopyrrole; RN given refers to leiopyrrole; no RN available for HCl; structure
Click to view oxyphenonium Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist A quaternary ammonium anticholinergic agent with peripheral side effects similar to those of ATROPINE. It is used as an adjunct in the treatment of gastric and duodenal ulcer, and to relieve visceral spasms. The drug has also been used in the form of eye drops for mydriatic effect. Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Mydriatics (Code: D009184) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) FDA
Click to view ethyl dibunate
Click to view doxefazepam Doxefazepam is a benzodiazepine derivative with putative hypnotic, anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. The potency of action was estimated to be equivalent to diazepam. Doxefazepam was used as a tranquilizer. Italian Medicines Agency (AIFA)
Click to view halocarban Halocarban (cloflucarban) is a synthetic, carbanilide compound with antiseptic activity. Halocarban is used as disinfectant and is found in antimicrobial soaps and deodorants.
Click to view sorivudine Thymidine kinase 2, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: O00142, gene: TK2, swissprot: KITM_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17324575) Thymidine kinase (Organism: Human herpesvirus 1, class: Kinase, accessions: Q9QNF7, gene: TK, swissprot: KITH_HHV1) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17324575) Sorivudine is an antiviral agent. Antiviral action of sorivudine against varicella-zoster virus and herpes simplex virus type 1 is based on the inhibition of DNA synthesis in herpesvirus-infected cells. It was withdrawn from the market within a month due to its fatal interaction with 5-FU. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 1993 PMDA
Click to view cloxazolam analog of oxazolam; structure
Click to view voriconazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021630s034,021266s045,021267s055lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021630s034,021266s045,021267s055lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021630s034,021266s045,021267s055lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021630s034,021266s045,021267s055lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021630s034,021266s045,021267s055lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021630s034,021266s045,021267s055lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021630s034,021266s045,021267s055lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19029318) Voriconazole is an azole antifungal agent. The primary mode of action of voriconazole is the inhibition of fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylation, an essential step in fungal ergosterol biosynthesis. The accumulation of 14 alpha-methyl sterols correlates with the subsequent loss of ergosterol in the fungal cell wall and may be responsible for the antifungal activity of voriconazole. Voriconazole has been shown to be active against Aspergillus fumigatus, Aspergillus flavus, Aspergillus niger, Aspergillus terreus, Candida albicans, Candida glabrata, Candida krusei, Candida parapsilosis, Candida tropicalis, Fusarium spp. including Fusarium solani, Scedosporium apiospermum. Voriconazole is indicated for the treatment of invasive apergillosis ( due to Aspergillus fumigatus), candidemia in non-neutropenic patients and (disseminated infections in skin and infections in abdomen, kidney, bladder wall, and wounds), esophageal candidiasis and serious fungal infections caused by Scedosporium apiospermum (asexual form of Pseudallescheria boydii) and Fusarium spp. including Fusarium solani. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) 14-alpha Demethylase Inhibitors (Code: D058888) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Cytochrome P-450 CYP3A Inhibitors (Code: D065692) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) 2002-05-24 FDA VOR
Click to view cinmetacin Cinmetacin is a synthetic non-steroidal anti-inflammatory agent. The anti-inflammatory activity of cinmetacin is attributed to the inhibition of the enzyme prostaglandin synthetase. Cinmetacin is indicated in the management of pain and inflammatory in conditions such as rheumatoid arthritis, ankylosing spondylitis and acute gout. 2015-03-20 China Food and Drug Administration (CFDA)
Click to view cefradine Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) Matrix metalloproteinase-9 (Organism: Homo sapiens, class: Enzyme, accessions: P14780, gene: MMP9, swissprot: MMP9_HUMAN) Somatostatin receptor type 4 (Organism: Homo sapiens, class: GPCR, accessions: P31391, gene: SSTR4, swissprot: SSR4_HUMAN) Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor (Source: ) A semi-synthetic cephalosporin antibiotic. antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1974-08-19 FDA
Click to view ampicillin Penicillin-binding protein 1A (Organism: Streptococcus pneumoniae (strain ATCC BAA-255 / R6), class: Enzyme, accessions: Q8DR59, gene: pbpA, swissprot: PBPA_STRR6) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7447421) Penicillin-binding protein 2B (Organism: Streptococcus pneumoniae (strain ATCC BAA-255 / R6), class: Enzyme, accessions: P0A3M6, gene: penA, swissprot: PBP2_STRR6) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7447421) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10636865) Ampicillin is a penicillin beta-lactam antibiotic. The following gram-negative and gram-positive bacteria have been shown in in vitro studies to be susceptible to ampicillin: Hemolytic and nonhemolytic streptococci, Streptococcus pneumoniae, Nonpenicillinase-producing staphylococci, Clostridium spp., B. anthracis, Listeria monocytogenes, most strains of enterococci, H. influenzae, N. gonorrhoeae, N. meningitidis, Proteus mirabilis, many strains of Salmonella, Shigella, and E. coli. Ampicillin is indicated in the treatment of bacterial meningitis, septicemia, endocarditis, urinary tract, gastrointestinal, respiratory tract infections caused by susceptible strains of the designated organisms. Penicillin-class Antibacterial (Code: N0000175497) Penicillins (Code: N0000011281) antibacterial drug (Code: CHEBI:36047) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1965-12-17 FDA AIC
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Click to view dipipanone piperidyl analog of methadone where piperidino group replaces dimethylamino group; RN given refers to parent cpd without isomeric designation; structure
Click to view cetiedil Antisickling Agents (Code: D000986) Cardiovascular Agents (Code: D002317) Hematologic Agents (Code: D006401) Vasodilator Agents (Code: D014665)
Click to view loracarbef Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor (Source: ) 1-carbacephem antibiotic; has a broad spectrum of antimicrobial activity; structure given in first source; carbacephems differ from cephalosporins in the substitution of a sulfur atom in the dihydrothiazine ring with a methylene group to form a tetrahydropyridine ring Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1991-12-31 FDA
Click to view azasetron 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/19967488) a selective 5-HT3 receptor antagonist; structure given in first source Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702)
Click to view phenoxymethylpenicillin Solute carrier family 22 member 8 (Organism: Mus musculus, class: Transporter, accessions: O88909, gene: Slc22a8, swissprot: S22A8_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23344796) Penicillin V exerts a bactericidal action against penicillin sensitive microorganisms during the stage of active multiplication through inhibition of biosynthesis of cell wall mucopeptides. It is not active against the penicillinase producing bacteria, which include many strains of staphylococci. Sensitive organisms include the following: • Gram-positive cocci, e.g. Streptococci (groups A,C,G,H,L and M), and non-penicillinase producing Staphylococcus pyogenes; Gram-positive bacilli, e.g. Clostridium tetani, Cl. Perfrigens, Corynebacterium diphtheriae and Bacillus anthracis; Gram-negative bacteria, both Neisseria meningitidis and N. gonorrhoeae are sensitive to a degree but Haemophilus influenzae is moderately resistant and other aerobic Gram-negative bacilli are highly resistant; Treponema pallidum is sensitive, but treatment of syphilis with oral penicillins is not recommended. Penicillin-class Antibacterial (Code: N0000175497) Penicillins (Code: N0000011281) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1958-01-13 FDA PNV
Click to view biapenem Biapenem is a carbapenem antibiotic. It has in vitro activity against anaerobes. Biapenem suppresses bacterial growth by inhibiting the enzymes responsible for bacterial cell wall synthesis, and shows broad-spectrum antibacterial activity both against gram-positive bacteria and gram-negative bacteria. Biapenem is stable to dehaloperoxidase-I (DHP-I) and can not be administered together with DHP-I inhibitor. Biapenem is stable to most beta-lactamases (including AmpC and extended-spectrum beta-lactamases). This product is applicable to the treatment of a variety of infections caused by sensitive bacteria: septicemia, pneumonia, lung abscess, secondary infections resulting from chronic respiratory disease, cystitis, pyelonephritis, peritonitis, appendagitis, etc. antibacterial drug (Code: CHEBI:36047) Anti-Infective Agents (Code: D000890) 2002-03-01 PMDA
Click to view disofenin
Click to view vinpocetine Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C (Organism: Homo sapiens, class: Enzyme, accessions: Q14123, gene: PDE1C, swissprot: PDE1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9216839) Vinpocetine is a synthetic derivative of the vinca alkaloid vincamine. Vinpocetine has been reported to have cerebral blood-flow enhancing and neuroprotective effects, and has been used as a drug in Eastern Europe for the treatment of cerebrovascular disorders and age-related memory impairment. Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Neuroprotective Agents (Code: D018696) Nootropic Agents (Code: D018697) Phosphodiesterase Inhibitors (Code: D010726) Protective Agents (Code: D020011) Vasodilator Agents (Code: D014665) 1977-01-01 Hungary National Institute of Pharmacy and Nutrition
Click to view loretin Loretin (iodo-oxyquinolin sulphonic acid) is an iodine compound. Loretin is a powerful microbicide. It was used as antiseptic and as a substitute for iodoform in the end of XIX centry.
Click to view menthyl salicylate Menthyl salicylate is an ester of menthol and salicylic acid. It was used in a sunscreen lotions. Now it is used in combination with menthol as a non-steroidal anti-inflammatory agent for the temporary relief of minor aches and pains of muscles and joints associated with simple backache, arthritis, strains and sprains, bruises. 1989-12-31 Health Canada
Click to view lomefloxacin DNA gyrase subunit A (Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd), class: Enzyme, accessions: P43700, gene: gyrA, swissprot: GYRA_HAEIN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/20013s015lbl.pdf) DNA gyrase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES4|P0AES6, gene: gyrA|gyrB, swissprot: GYRA_ECOLI|GYRB_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/20013s015lbl.pdf) A synthetic broad-spectrum fluoroquinolone with antibacterial activity. Lomefloxacin inhibits DNA gyrase, a type II topoisomerase involved in the induction or relaxation of supercoiling during DNA replication. This inhibition leads to a decrease in DNA synthesis during bacterial replication, resulting in cell growth inhibition and eventually cell lysis. photosensitizing agent (Code: CHEBI:47868) antitubercular agent (Code: CHEBI:33231) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1992-02-21 FDA
Click to view benfluorex Anti-Obesity Agents (Code: D019440) Antimetabolites (Code: D000963) Appetite Depressants (Code: D001067) Central Nervous System Agents (Code: D002491) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847)
Click to view moquizone
Click to view meloxicam Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020938s026lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020938s026lbl.pdf) 6-phosphogluconate dehydrogenase, decarboxylating (Organism: Homo sapiens, class: Enzyme, accessions: P52209, gene: PGD, swissprot: 6PGD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20235752) Meloxicam is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of meloxicam, like that of other NSAIDs, may be related to prostaglandin synthetase (cyclo-oxygenase) inhibition. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antirheumatic drug (Code: CHEBI:35842) analgesic (Code: CHEBI:35480) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) 2000-04-13 FDA MXM
Click to view pirenzepine Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19478135) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19478135) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19478135) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19478135) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19478135) Pirenzepine is an antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. Pirenzepine is indicated for the treatment of gastric and duodenal ulcer. anti-ulcer drug (Code: CHEBI:49201) muscarinic antagonist (Code: CHEBI:48876) antispasmodic drug (Code: CHEBI:53784) Anti-Ulcer Agents (Code: D000897) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Gastrointestinal Agents (Code: D005765) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) 1984-12-31 Health Canada
Click to view epicillin semisynthetic penicillin type antibiotic; minor descriptor (75-85); on-line & Index Medicus search AMPICILLIN/AA (75-85); RN given refers to (2s(2alpha,5alpha,6beta(S*)))-isomer Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view dipivefrine Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist used in treatment of both primary & open angle glaucoma; RN given refers to (+-)-isomer Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) prodrug (Code: CHEBI:50266) adrenergic agonist (Code: CHEBI:37886) sympathomimetic agent (Code: CHEBI:35524) antiglaucoma drug (Code: CHEBI:39456) ophthalmology drug (Code: CHEBI:66981) Neurotransmitter Agents (Code: D018377) Adrenergic Receptor Agonist (Code: N0000175883) 1980-05-02 FDA
Click to view tamibarotene Retinoic acid receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10276, gene: RARA, swissprot: RARA_HUMAN Retinoic acid receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10826, gene: RARB, swissprot: RARB_HUMAN) agonist (Source: ) Retinoic acid receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P13631, gene: RARG, swissprot: RARG_HUMAN) agonist (Source: ) has retinoid-binding activity antineoplastic agent (Code: CHEBI:35610) retinoic acid receptor alpha/beta agonist (Code: CHEBI:50741) 2005-04-11 PMDA A80
Click to view pipoxolan synonyms BR-18 & rowapraxin refer to HCl; structure
Click to view tazarotene Retinoic acid receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10826, gene: RARB, swissprot: RARB_HUMAN) agonist Retinoic acid receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10276, gene: RARA, swissprot: RARA_HUMAN) agonist Retinoic acid receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P13631, gene: RARG, swissprot: RARG_HUMAN) agonist a topical acetylenic retinoid; a topical kerytolytic Retinoid (Code: N0000175607) Retinoids (Code: N0000007700) keratolytic drug (Code: CHEBI:50176) prodrug (Code: CHEBI:50266) Dermatologic Agents (Code: D003879) Keratolytic Agents (Code: D007641) Noxae (Code: D009676) Teratogens (Code: D013723) 1997-06-13 FDA
Click to view phenadoxone
Click to view adinazolam Translocator protein (Organism: Homo sapiens, class: Transporter, accessions: P30536, gene: TSPO, swissprot: TSPO_HUMAN) GABA-A receptor (Organism: Homo sapiens, class: Ion channel, accessions: O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|Q16445|Q8N1C3|Q99928, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRG1|GABRG2|GABRG3, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN) positive allosteric modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/6148400) antidepressant (Code: CHEBI:35469) sedative (Code: CHEBI:35717) anxiolytic drug (Code: CHEBI:35474) anticonvulsant (Code: CHEBI:35623) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619)
Click to view sulmarin -
Click to view triflupromazine 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: ) Trypanothione reductase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P28593, gene: TPR, swissprot: TYTR_TRYCR Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN Pleiotropic ABC efflux transporter of multiple drugs (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Transporter, accessions: P33302, gene: PDR5, swissprot: PDR5_YEAST Cholinesterase (Organism: Equus caballus, class: Enzyme, accessions: P81908, gene: BCHE, swissprot: CHLE_HORSE A phenothiazine used as an antipsychotic agent and as an antiemetic. dopaminergic antagonist (Code: CHEBI:48561) antiemetic (Code: CHEBI:50919) first generation antipsychotic (Code: CHEBI:65190) Antiemetics (Code: D000932) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1957-09-16 FDA
Click to view posatirelin stimulates oxygen consumption
Click to view clidinium Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist a synthetic anticholinergic agent that has antispasmodic and antisecretory effect on the gastrointestinal tract Anticholinergic (Code: N0000175574) Decreased Parasympathetic Acetylcholine Activity (Code: N0000008779) GI Motility Alteration (Code: N0000009048) Digestive/GI System Activity Alteration (Code: N0000009022) Cholinergic Antagonists (Code: N0000175370) parasympatholytic (Code: CHEBI:50370) antispasmodic drug (Code: CHEBI:53784) anti-arrhythmia drug (Code: CHEBI:38070) Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) FDA
Click to view epoprostenol Prostacyclin receptor (Organism: Homo sapiens, class: GPCR, accessions: P43119, gene: PTGIR, swissprot: PI2R_HUMAN) agonist (Source: ) Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) agonist (Source: ) Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN) agonist (Source: ) P2Y purinoceptor 12 (Organism: Homo sapiens, class: GPCR, accessions: Q9H244, gene: P2RY12, swissprot: P2Y12_HUMAN) A prostaglandin that is a powerful vasodilator and inhibits platelet aggregation. It is biosynthesized enzymatically from PROSTAGLANDIN ENDOPEROXIDES in human vascular tissue. The sodium salt has been also used to treat primary pulmonary hypertension (HYPERTENSION, PULMONARY). Prostacycline Vasodilator (Code: N0000175416) Prostaglandins I (Code: N0000011280) Vasodilation (Code: N0000009909) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) 1995-09-20 FDA
Click to view dinoprostone Prostaglandin D2 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q13258, gene: PTGDR, swissprot: PD2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Thromboxane A2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P21731, gene: TBXA2R, swissprot: TA2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP2 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43116, gene: PTGER2, swissprot: PE2R2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) The most common and most biologically active of the mammalian prostaglandins. It exhibits most biological activities characteristic of prostaglandins and has been used extensively as an oxytocic agent. The compound also displays a protective effect on the intestinal mucosa. Prostaglandin Analog (Code: N0000175454) Prostaglandins (Code: N0000007706) oxytocic (Code: CHEBI:36063) Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102) 1977-08-23 FDA P2E
Click to view betoxycaine
Click to view encainide Sodium channel subunit beta-4 (Organism: Homo sapiens, class: Ion channel, accessions: Q8IWT1, gene: SCN4B, swissprot: SCN4B_HUMAN) Sodium channel subunit beta-3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NY72, gene: SCN3B, swissprot: SCN3B_HUMAN) Sodium channel subunit beta-2 (Organism: Homo sapiens, class: Ion channel, accessions: O60939, gene: SCN2B, swissprot: SCN2B_HUMAN) Sodium channel subunit beta-1 (Organism: Homo sapiens, class: Ion channel, accessions: Q07699, gene: SCN1B, swissprot: SCN1B_HUMAN) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) One of the ANTI-ARRHYTHMIA AGENTS, it blocks VOLTAGE-GATED SODIUM CHANNELS and slows conduction within the His-Purkinje system and MYOCARDIUM. Anti-Arrhythmia Agents (Code: D000889) anti-arrhythmia drug (Code: CHEBI:38070) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 1987-01-01 YEAR INTRODUCED
Click to view anileridine Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist minor descriptor (64-86); on line & INDEX MEDICUS search ISONIPECOTIC ACIDS (68-86); RN given refers to parent cpd opioid receptor agonist (Code: CHEBI:60606) opioid analgesic (Code: CHEBI:35482) FDA
Click to view quinbolone
Click to view griseofulvin Griseofulvin is a mycotoxic metabolic product of Penicillium spp. Griseofulvin is fungistatic with in vitro activity against various species of Microsporum Epidermophyton, and Trichophyton. The exact mechanism by which it inhibits the growth of dermatophytes is not clear. It is thought to inhibit fungal cell mitosis and nuclear acid synthesis. It also binds to and interferes with the function of spindle and cytoplasmic microtubules by binding to alpha and beta tubulin. It binds to keratin in human cells, then once it reaches the fungal site of action, it binds to fungal microtubes thus altering the fungal process of mitosis. Griseofulvin is used for the treatment of ringworm infections of the skin, hair, and nails, namely: tinea corporis, tinea pedis, tinea cruris, tinea barbae, cradle cap or other conditions caused by Trichophyton or Microsporum fungi. Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Decreased Mitosis (Code: N0000008732) Microtubule Inhibition (Code: N0000175085) Tubulin Inhibiting Agent (Code: N0000175848) 1962-08-22 FDA
Click to view acenocoumarol Vitamin K epoxide reductase complex subunit 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BQB6, gene: VKORC1, swissprot: VKOR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17275317) Acenocoumarol is a 4-hydroxycoumarin derivative, reduces the concentration of prothrombin in blood and increases the prothrombin time by inhibiting the formation of prothrombin in the liver. The drug also interferes with the production of coagulation factors VII, IX, X, as well as protein C, so their concentration in the blood is lowered during therapy. Acenocoumarol is indicated for the prophylaxis and treatment of venous thrombosis and its extension, for the treatment of atrial fibrillation with embolization, for the prophylaxis and treatment of pulmonary embolism, and as an adjunct in the treatment of coronary occlusion and transient cerebral ischemic attacks. anticoagulant (Code: CHEBI:50249) Anticoagulants (Code: D000925) Hematologic Agents (Code: D006401) 1962-12-31 Health Canada
Click to view dioxaphetyl butyrate
Click to view methysergide 5-hydroxytryptamine receptor 5A (Organism: Mus musculus, class: Unclassified, accessions: P30966, gene: Htr5a, swissprot: 5HT5A_MOUSE) antagonist (Source: ) 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: ) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) antagonist (Source: ) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) partial agonist Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT Serotonin 2 (5-HT2) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P30994, gene: Htr2a|Htr2b|Htr2c, swissprot: 5HT2A_RAT|5HT2B_RAT|5HT2C_RAT Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/15322733) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/15322733) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/15322733) Induced myeloid leukemia cell differentiation protein Mcl-1 (Organism: Homo sapiens, class: Cytosolic other, accessions: Q07820, gene: MCL1, swissprot: MCL1_HUMAN Bcl-2-like protein 1 (Organism: Homo sapiens, class: Cytosolic other, accessions: Q07817, gene: BCL2L1, swissprot: B2CL1_HUMAN Cytoplasmic zinc-finger protein (Organism: Caenorhabditis elegans, class: Unclassified, accessions: G5EF15, gene: pos-1, swissprot: G5EF15_CAEEL 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Zinc finger protein mex-5 (Organism: Caenorhabditis elegans, class: Cytosolic other, accessions: Q9XUB2, gene: mex-5, swissprot: MEX5_CAEEL 5-hydroxytryptamine receptor 1F (Organism: Rattus norvegicus, class: Unclassified, accessions: P30940, gene: Htr1f, swissprot: 5HT1F_RAT) antagonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Mus musculus, class: GPCR, accessions: P32304, gene: Htr7, swissprot: 5HT7R_MOUSE) antagonist (Source: ) 5-hydroxytryptamine receptor 5A (Organism: Rattus norvegicus, class: Unclassified, accessions: P35364, gene: Htr5a, swissprot: 5HT5A_RAT) antagonist (Source: ) An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome. sympatholytic agent (Code: CHEBI:66991) vasoconstrictor agent (Code: CHEBI:50514) serotonergic antagonist (Code: CHEBI:48279) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Vasoconstrictor Agents (Code: D014662) 1962-02-12 FDA
Click to view motretinide exerts a therapeutic influence on chemically induced papillomas & carcinomas of the skin in mice; RN given refers to cpd without isomeric designation; structure
Click to view acetylmethadol Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15911273) Acetylmethadol (methadyl acetate) is a synthetic opioid analgesic and a long-acting methadone analoge.It is a racemic mixture of levomethadyl acetate (LAAM; L-alpha-acetylmethadol), D-alpha-acetylmethadol, L-beta-acetylmethadol, and D-beta-acetylmethadol. The dextro isomer is more potent but shorter acting. The levo isomer is also less toxic. Beta-methadyl acetate also exists, however it is more toxic and less active than levomethadyl acetate and has no current medical use. Levomethadyl acetate was used as a second-line treatment for the treatment and management of opioid dependence if patients fail to respond to drugs like methadone or buprenorphine. Levomethadyl acetate was removed from the market due to reports of severe cardiac-related adverse events. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1993-07-09 FDA
Click to view isopropamide Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist 1957-10-09 FDA
Click to view butizide 3-isobutyl analog of hydrochlorothiazide; structure Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Natriuretic Agents (Code: D045283)
Click to view idoxuridine Idoxuridine is an iodinated analogue of deoxyuridine, with antiviral activity against herpes simplex virus (HSV) and potential radiosensitizing activities. Upon ocular administration, idoxuridine (IUdR) is converted to its mono-, di-, and triphosphate forms, is incorporated into DNA and disrupts viral replication. Upon oral administration of the idoxuridine prodrug ropidoxuridine and hepatic conversion by aldehyde oxidase into idoxuridine, this agent incorporates into DNA and sensitizes cells to ionizing radiation by increasing DNA strand breaks. It was used for the treatment of keratitis caused by the virus of herpes simplex. Nucleoside Analog (Code: N0000175459) Nucleoside Analog Antiviral (Code: N0000175466) antiviral drug (Code: CHEBI:36044) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) 1963-06-11 FDA ID2
Click to view quinfamide Quinfamide is a member of quinolines. The details of the mechanism of action are not known, but the overall effect is intraluminal immobilization of the Entamoeba. Quinafimide is used in trials for the treatment of Amoebiasis and Helminthiasis.
Click to view aceclofenac Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source:http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1573190969348.pdf) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source:http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1573190969348.pdf) Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) analog of Diclofenac. Aceclofenac blocks the action of cyclo-oxygenase. Aceclofenac is the glycolic acid ester of diclofenac. The incidence of gastric ulcerogenicity of aceclofenac has been reported to be significantly lower than that of other frequently prescribed NSAIDs. It is used for the relief of pain and inflammation in rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1996-06-03 Italian Medicines Agency (AIFA)
Click to view sultopride D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) amino group of sulpiride on SO2 group is replaced by an ethyl group; structure; RN given refers to parent cpd Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view valganciclovir Valganciclovir is an L-valyl ester and a prodrug of ganciclovir that exists as a mixture of two diastereomers. After oral administration, both diastereomers are rapidly converted to ganciclovir by intestinal and hepatic esterases. (See: ganciclovir) Valganciclovir is indicated for the treatment of cytomegalovirus (CMV) retinitis in patients with acquired immunodeficiency syndrome and for prevention of CMV disease in kidney, heart, and kidney-pancreas transplant patients at high risk. Cytomegalovirus Nucleoside Analog DNA Polymerase Inhibitor (Code: N0000175461) DNA Polymerase Inhibitors (Code: N0000020060) Nucleoside Analog (Code: N0000175459) prodrug (Code: CHEBI:50266) antiviral drug (Code: CHEBI:36044) Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) 2001-03-29 FDA F9E
Click to view phenolsulfonphthalein Red dye, pH indicator, and diagnostic aid for determination of renal function. It is used also for studies of the gastrointestinal and other systems. two-colour indicator (Code: CHEBI:50412) acid-base indicator (Code: CHEBI:50407) diagnostic agent (Code: CHEBI:33295) Coloring Agents (Code: D004396) Indicators and Reagents (Code: D007202)
Click to view isofezolac
Click to view seratrodast Thromboxane A2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P21731, gene: TBXA2R, swissprot: TA2R_HUMAN has thromboxane A2 & prostaglandin H2 receptor antagonistic action Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Asthmatic Agents (Code: D018927) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Peripheral Nervous System Agents (Code: D018373) Prostaglandin Antagonists (Code: D011448) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689)
Click to view yohimbine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10611634) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10611634) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10611634) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10611634) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10611634) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10611634) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10611634) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10611634) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10455251) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8380639) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8380639) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8226867) 5-hydroxytryptamine receptor 5A (Organism: Mus musculus, class: Unclassified, accessions: P30966, gene: Htr5a, swissprot: 5HT5A_MOUSE) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7988681) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7988681) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16250647) A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of erectile dysfunction. Adrenergic Agents (Code: D018663) Adrenergic alpha-2 Receptor Antagonists (Code: D058669) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) alpha-adrenergic antagonist (Code: CHEBI:37890) serotonergic antagonist (Code: CHEBI:48279) Autonomic Agents (Code: D001337) Mydriatics (Code: D009184) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Urological Agents (Code: D064804)
Click to view vincamine Vincamine is the major alkaloid of Vinca minor. Vincamine is a peripheral vasodilator that increases blood flow to the brain. Vincamine may be used as a dietary nootropic supplement. antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1982-02-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view hexamidine Prothrombin (Organism: Homo sapiens, class: Enzyme, accessions: P00734, gene: F2, swissprot: THRB_HUMAN Urokinase-type plasminogen activator (Organism: Homo sapiens, class: Enzyme, accessions: P00749, gene: PLAU, swissprot: UROK_HUMAN Trypsin-1 (Organism: Homo sapiens, class: Enzyme, accessions: P07477, gene: PRSS1, swissprot: TRY1_HUMAN Suppressor of tumorigenicity 14 protein (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y5Y6, gene: ST14, swissprot: ST14_HUMAN Anti-Infective Agents (Code: D000890) antiseptic drug (Code: CHEBI:48218) DID
Click to view bevonium Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view pipenzolate
Click to view phentetramine Phentetramine is an oxopurine. Phentetramine was used hypotension but later was replaced by phenylephrine.
Click to view benzilonium
Click to view dinoprost Prostaglandin E2 receptor EP2 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43116, gene: PTGER2, swissprot: PE2R2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin D2 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q13258, gene: PTGDR, swissprot: PD2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Thromboxane A2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P21731, gene: TBXA2R, swissprot: TA2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10952683) A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions. Abortifacient Agents (Code: D000019) Abortifacient Agents, Nonsteroidal (Code: D000020) Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102) 1976-05-18 FDA
Click to view alprostadil Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020379s034lbl.pdf) Prostaglandin E2 receptor EP2 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43116, gene: PTGER2, swissprot: PE2R2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020379s034lbl.pdf) Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020379s034lbl.pdf) Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020379s034lbl.pdf) Alprostadil is a synthetic form of prostaglandin E1 with a wide variety of pharmacological actions including vasodilation and inhibition of platelet aggregation. Alprostadil induces erection by relaxation of trabecular smooth muscle and by dilation of cavernosal arteries by binding to its receptors and increasing intracellular cyclic adenosine monophosphate (cAMP) levels via modulation of adenylate cyclase. Alprostadil also attenuates presynaptic noradrenaline release in the corpus cavernosum. Alprostadil is indicated for the treatment of erectile dysfunction and as an adjunct to other diagnostic tests in the diagnosis of erectile dysfunction. Genitourinary Arterial Vasodilation (Code: N0000009059) Prostaglandin Analog (Code: N0000175454) Prostaglandin E1 Agonist (Code: N0000180189) Prostaglandin Receptor Agonists (Code: N0000000106) Prostaglandins (Code: N0000007706) Venous Vasodilation (Code: N0000009911) Cardiovascular Agents (Code: D002317) Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) Urological Agents (Code: D064804) Vasodilator Agents (Code: D014665) vasodilator agent (Code: CHEBI:35620) platelet aggregation inhibitor (Code: CHEBI:50427) anticoagulant (Code: CHEBI:50249) 1981-10-16 FDA XPG
Click to view etretinate Retinoic acid receptor RXR-gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P48443, gene: RXRG, swissprot: RXRG_HUMAN) agonist Retinoic acid receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10276, gene: RARA, swissprot: RARA_HUMAN) agonist An oral retinoid used in the treatment of keratotic genodermatosis, lichen planus, and psoriasis. Beneficial effects have also been claimed in the prophylaxis of epithelial neoplasia. The compound may be teratogenic. Dermatologic Agents (Code: D003879) Keratolytic Agents (Code: D007641) keratolytic drug (Code: CHEBI:50176) 1986-09-30 FDA
Click to view eprozinol
Click to view rioprostil Prostaglandin E2 receptor EP2 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43116, gene: PTGER2, swissprot: PE2R2_HUMAN) agonist (Source: http://www.kegg.jp/entry/D05732) A synthetic methylprostaglandin E1 analog that reduces gastric acid secretion and enhances the gastric mucus-bicarbonate barrier. It is effective in the therapy of gastric ulcers and gives significant protection against NSAID-induced gastric mucosal damage. The drug also prevents cyclosporin A-induced damage to endocrine and exocrine pancreatic secretions. It shows a low order of acute toxicity and there is no evidence of embryotoxicity, fetotoxicity, teratogenicity, or mutagenicity in animal studies. Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765)
Click to view xipamide A sulfamoylbenzamide analog of CLOPAMIDE. It is diuretic and saluretic with antihypertensive activity. It is bound to PLASMA PROTEINS, thus has a delayed onset and prolonged action. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Natriuretic Agents (Code: D045283)
Click to view succinylsulfathiazole intestinal antimicrobial agent; structure
Click to view moperone D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN)
Click to view benzomethamine
Click to view tinofedrine improves cerebral and peripheral blood flow
Click to view plafibride morpholino-methylurea analog of clofibric acid Antimetabolites (Code: D000963) Hematologic Agents (Code: D006401) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Platelet Aggregation Inhibitors (Code: D010975)
Click to view tiaramide NTA-194, solantal, FK 1160 refer to mono-HCl salt; RN given refers to parent cpd; structure Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Asthmatic Agents (Code: D018927) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689)
Click to view amodiaquine Heparanase (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y251, gene: HPSE, swissprot: HPSE_HUMAN Histamine N-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P50135, gene: HNMT, swissprot: HNMT_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN A 4-aminoquinoline compound with anti-inflammatory properties. Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) antimalarial (Code: CHEBI:38068) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) drug allergen (Code: CHEBI:88188) prodrug (Code: CHEBI:50266) FDA CQA
Click to view bithionol Potassium channel subfamily T member 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q5JUK3, gene: KCNT1, swissprot: KCNT1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16876206) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Bithionol is an aryl sulfide. It is a fungicide and anthelmintic, it was used in various topical drug products for the treatment of trematode and cestode infestations, but withdrawn after being shown to be a potent photosensitizer with the potential to cause serious skin disorders. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) antifungal agrochemical (Code: CHEBI:86328) antiplatyhelmintic drug (Code: CHEBI:35684) B1T
Click to view pipobroman An antineoplastic agent that acts by alkylation. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) 1966-07-01 FDA
Click to view thiamphenicol Thiamphenicol is a broad-spectrum antibiotic, which is active against gram-positive and gram-negative organisms. Thiamphenicol inhibits the protein synthesis in bacterias by binding to 23S ribosomal subunit. Thiamphenicol is active against Streptococcus pneumoniae, Staphylococcus spp., Haemophilus influenzae, Klebsiella spp. Thiamphenicol is used in glycinate acetylcysteinate form for the treatment of urinary tract infections, respiratory tract infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) immunosuppressive agent (Code: CHEBI:35705) 1962-02-20 Italian Medicines Agency (AIFA) TH8
Click to view sulindac Aldose reductase (Organism: Rattus norvegicus, class: Enzyme, accessions: P07943, gene: Akr1b1, swissprot: ALDR_RAT) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor 72 kDa type IV collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P08253, gene: MMP2, swissprot: MMP2_HUMAN) Retinoic acid receptor RXR-alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P19793, gene: RXRA, swissprot: RXRA_HUMAN Prostaglandin E synthase (Organism: Homo sapiens, class: Enzyme, accessions: O14684, gene: PTGES, swissprot: PTGES_HUMAN Lactoylglutathione lyase (Organism: Homo sapiens, class: Enzyme, accessions: Q04760, gene: GLO1, swissprot: LGUL_HUMAN Aldose reductase (Organism: Homo sapiens, class: Enzyme, accessions: P15121, gene: AKR1B1, swissprot: ALDR_HUMAN Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antineoplastic Agents (Code: D000970) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) antineoplastic agent (Code: CHEBI:35610) non-narcotic analgesic (Code: CHEBI:35481) analgesic (Code: CHEBI:35480) antipyretic (Code: CHEBI:35493) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) prodrug (Code: CHEBI:50266) tocolytic agent (Code: CHEBI:66993) 1978-09-27 FDA SUZ
Click to view niaprazine selective brain catecholamine depletor; RN given refers to parent cpd; structure
Click to view pioglitazone Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021073s049lbl.pdf) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021073s049lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021073s049lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021073s049lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14977862) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14977862) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20650633) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) Pioglitazone is a thiazolidinedione that depends on the presence of insulin for its mechanism of action. Pioglitazone decreases insulin resistance in the periphery and in the liver resulting in increased insulin-dependent glucose disposal and decreased hepatic glucose output. Pioglitazone is not an insulin secretagogue. Pioglitazone is an agonist for peroxisome proliferator-activated receptor-gamma (PPAR-gamma). PPAR receptors are found in tissues important for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma nuclear receptors modulates the transcription of a number of insulin responsive genes involved in the control of glucose and lipid metabolism. Pioglitazone is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus in multiple clinical settings. Hypoglycemic Agents (Code: D007004) insulin-sensitizing drug (Code: CHEBI:50864) Peroxisome Proliferator Receptor alpha Agonist (Code: N0000175596) Peroxisome Proliferator Receptor gamma Agonist (Code: N0000180186) Peroxisome Proliferator-activated Receptor Activity (Code: N0000175374) PPAR alpha (Code: N0000170118) PPAR gamma (Code: N0000170119) Thiazolidinedione (Code: N0000180190) Thiazolidinediones (Code: N0000011272) 1999-07-15 FDA 8N6
P1B
Click to view hycanthone Potentially toxic, but effective antischistosomal agent, it is a metabolite of LUCANTHONE. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Schistosomicides (Code: D012556) schistosomicide drug (Code: CHEBI:38941)
Click to view quinestradol
Click to view estradiol valerate Estradiol valerate is a long-acting estrogen. Estradiol Valerate is a pro-drug ester of estradiol, a naturally occurring hormone that circulates endogenously within the human body. (See: estradiol) Estradiol valerate is commercially available as an intramuscular injection and is indicated for the treatment of moderate to severe vasomotor symptoms and vulvovaginal atrophy due to menopause, for the treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure, and for the treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only), for the prevention of pregnancy and for the treatment of heavy menstrual bleeding. Contraceptive Agents (Code: D003270) Reproductive Control Agents (Code: D012102) 1954-07-15 FDA
Click to view dopexamine D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Cardiovascular Agents (Code: D002317) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) 1989-01-01 YEAR INTRODUCED
Click to view tevenel sulfamoyl analog of D-threo-chloramphenicol; structure
Click to view balsalazide Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN) inhibitor Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) prodrug (Code: CHEBI:50266) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) anti-ulcer drug (Code: CHEBI:49201) gastrointestinal drug (Code: CHEBI:55324) Aminosalicylate (Code: N0000175781) Aminosalicylic Acids (Code: N0000005760) 2000-07-18 FDA
Click to view droxicam Droxicam is an oxicam non-steroidal anti-inflammatory drug and a prodrug of Piroxicam. It was used to reduce pain and inflammation in musculoskeletal disorders such as rheumatoid arthritis and osteoarthritis. Droxicam was withdrawn due to its hepatotoxicity. (See: piroxicam) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) platelet aggregation inhibitor (Code: CHEBI:50427) prodrug (Code: CHEBI:50266) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) 1990 YEAR INTRODUCED
Click to view tolrestat Aldo-keto reductase family 1 member B10 (Organism: Homo sapiens, class: Enzyme, accessions: O60218, gene: AKR1B10, swissprot: AK1BA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20304656) Aldose reductase (Organism: Homo sapiens, class: Enzyme, accessions: P15121, gene: AKR1B1, swissprot: ALDR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10737739) Alcohol dehydrogenase [NADP(+)] (Organism: Homo sapiens, class: Enzyme, accessions: P14550, gene: AKR1A1, swissprot: AK1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15857120) Aldo-keto reductase family 1 member C21 (Organism: Mus musculus, class: Enzyme, accessions: Q91WR5, gene: Akr1c21, swissprot: AK1CL_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18165015) Tolrestat is an aldose-reductase inhibitor. It was indicated in the treatment of complications of serious diabetes such as neuropathy, retinopathy and nephropathy. The manufacturer withdrew tolrestat from the market worldwide following reports of two additional deaths from hepatic necrosis associated with the use of tolrestat. Enzyme Inhibitors (Code: D004791) 1989-01-01 YEAR INTRODUCED TOL
Click to view etersalate
Click to view cafedrine Cafedrine (norephedrinoethyltheophylline) is a chemical linkage of norephedrine and theophylline and is a cardiac stimulant. The effects of cafedrine on cardiac output are believed to be mediated via ?- adrenoceptors. Cafedrine has a positive inotropic effect in humans, and this can be abolished by administration of the non-selective ?-adrenoceptor antagonist propranolol. A combination of cafedrine and theodrenaline was used for the treatment of hypotension in adults that occurs during emergency situations, general anesthesia, and regional anesthesia, especially during cesarean sections. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view cinacalcet Extracellular calcium-sensing receptor (Organism: Homo sapiens, class: GPCR, accessions: P41180, gene: CASR, swissprot: CASR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021688s025s026lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021688s025s026lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021688s025s026lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021688s025s026lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021688s025s026lbl.pdf) Cinacalcet is a naphthalene derivative and calcimimetic agent that increases the sensitivity of the calcium-sensing receptor to activation by extracellular calcium. Cinacalcet directly lowers PTH levels by increasing the sensitivity of the calcium-sensing receptor to extracellular calcium. Cinacalcet is used for the treatment of secondary hyperparathyroidism in adult patients with chronic kidney disease on dialysis, for the treatment of hypercalcemia in adult patients with parathyroid carcinoma and primary hyperparathyroidism in patient, who are unable to undergo parathyroidectomy. Calcimimetic Agents (Code: D057966) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) calcimimetic (Code: CHEBI:48525) Calcium-sensing Receptor Agonist (Code: N0000175902) Increased Calcium-sensing Receptor Sensitivity (Code: N0000020081) 2004-03-08 FDA
Click to view rosiglitazone Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021071s052lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021071s052lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021071s052lbl.pdf) Long-chain-fatty-acid--CoA ligase 4 (Organism: Homo sapiens, class: Enzyme, accessions: O60488, gene: ACSL4, swissprot: ACSL4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17259370) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12642470) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21861202) Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15177462) Peroxisome proliferator-activated receptor delta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q03181, gene: PPARD, swissprot: PPARD_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15177462) Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22282722) Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22282722) Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22282722) Amine oxidase [flavin-containing] A (Organism: Rattus norvegicus, class: Enzyme, accessions: P21396, gene: Maoa, swissprot: AOFA_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22282722) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) Free fatty acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: O14842, gene: FFAR1, swissprot: FFAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12565875) Transient receptor potential cation channel subfamily M member 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9HCF6, gene: TRPM3, swissprot: TRPM3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21406603) Short transient receptor potential channel 5 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UL62, gene: TRPC5, swissprot: TRPC5_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/21406603) Rosiglitazone, a member of the thiazolidinedione class of antidiabetic agents, improves glycemic control by improving insulin sensitivity. Rosiglitazone is a highly selective and potent agonist for the peroxisome proliferator-activated receptor-gamma, a ligand-activated transcription factor, thereby inducing cell differentiation and inhibiting cell growth and angiogenesis. This agent also modulates the transcription of insulin-responsive genes, inhibits macrophage and monocyte activation, and stimulates adipocyte differentiation. Rosiglitazone is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Peroxisome Proliferator Receptor gamma Agonist (Code: N0000180186) Peroxisome Proliferator-activated Receptor Activity (Code: N0000175374) PPAR gamma (Code: N0000170119) Thiazolidinedione (Code: N0000180190) Thiazolidinediones (Code: N0000011272) Hypoglycemic Agents (Code: D007004) insulin-sensitizing drug (Code: CHEBI:50864) 1999-05-25 FDA BRL
RGZ
Click to view nalbuphine Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018024s041lbl.pdf) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018024s041lbl.pdf) Nalbuphine is a synthetic mixed opioid agonist-antagonist with analgesic properties. Nalbuphine is an agonist at kappa opioid receptors and an antagonist at mu opioid receptors. Compared to other opioid agents that stimulate mu receptors, nalbuphine antagonizes mu receptors, thereby potentially producing less intense respiratory depression. Nalbuphine is a narcotic used as a pain medication. Competitive Opioid Antagonists (Code: N0000175686) Opioid Agonist/Antagonist (Code: N0000175692) Partial Opioid Agonists (Code: N0000175685) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotic Antagonists (Code: D009292) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) opioid analgesic (Code: CHEBI:35482) 1979-05-15 FDA
Click to view oxybutynin Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021351s017s018lbl.pdf) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16275087) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22243489) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22243489) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22243489) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021351s017s018lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26721703) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9584328) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9584328) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9584328) Oxybutynin acts as a competitive antagonist of acetylcholine at post-ganglionic muscarinic receptors, resulting in relaxation of bladder smooth muscle. Oxybutynin is a racemic (50:50) mixture of R- and S-isomers. Antimuscarinic activity resides predominantly in the R-isomer. The R-isomer of oxybutynin shows greater selectivity for the M1 and M3 muscarinic subtypes (predominant in bladder detrusor muscle and parotid gland) compared to the M2 subtype (predominant in cardiac tissue). Oxybutynin is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Cholinergic Muscarinic Antagonist (Code: N0000175700) Cholinergic Muscarinic Antagonists (Code: N0000000125) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Urological Agents (Code: D064804) parasympatholytic (Code: CHEBI:50370) antispasmodic drug (Code: CHEBI:53784) muscle relaxant (Code: CHEBI:51371) muscarinic antagonist (Code: CHEBI:48876) 1975-07-16 FDA
Click to view grepafloxacin Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/11370709/) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://pubmed.ncbi.nlm.nih.gov/10991972/) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/9827570/) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/12089365/) DNA gyrase (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: P0A4L9|P72524, gene: gyrA|gyrB, swissprot: GYRA_STRPN|GYRB_STRPN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/11796384/) DNA topoisomerase 4 (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: P72525|Q59961, gene: parC|parE, swissprot: PARC_STRPN|PARE_STRPN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/11796384/) Grepafloxacin is a monofluorinated quinolone. Grepafloxacin exerts its antibacterial activity by inhibiting bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, essential enzymes for duplication, transcription, and repair of bacterial DNA. Grepafloxacin is active against Staphylococcus aureus, Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, Chlamydia trachomatis, Mycoplasma pneumoniae, Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus pyogenes, Acinetobacter calcoaceticus, Citrobacter diversus, Citrobacter freundii, Enterobacter aerogenes, Enterobacter agglomerans, Enterobacter cloacae, Escherichia coli, Klebsiella oxytoca, Klebsiella pneumoniae, Morganella morganii, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Chlamydia pneumoniae, Legionella pneumophilia, Mycoplasma hominis, Mycobacterium tuberculosis. Due to the QTc-prolonging potential, as indicated by the changes in the QT interval on the electrocardiogram, and the risk for cardiovascular adverse events, grepafloxacin was withdrawn Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1997-11-06 FDA
Click to view cinolazepam Cinolazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Cinolazepam binds to central benzodiazepine receptors, which interact allosterically with GABA receptors. Cinolazepam is indicated for the treatment of severe insomnia. anticonvulsant (Code: CHEBI:35623) sedative (Code: CHEBI:35717) 1991-03-19 Hungary National Institute of Pharmacy and Nutrition
Click to view indomethacin Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018332s037s038lbl.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/018332s037s038lbl.pdf) Prostaglandin D2 receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5Y4, gene: PTGDR2, swissprot: PD2R2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12466225) Prostaglandin D2 receptor 2 (Organism: Mus musculus, class: Unclassified, accessions: Q9Z2J6, gene: Ptgdr2, swissprot: PD2R2_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12721327) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11301062) Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19007764) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12835412) Multidrug resistance-associated protein 6 (Organism: Homo sapiens, class: Transporter, accessions: O95255, gene: ABCC6, swissprot: MRP6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11880368) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21861202) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12130730) ATP-binding cassette sub-family C member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q96J66, gene: ABCC11, swissprot: ABCCB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15537867) Nitric oxide synthase, inducible (Organism: Mus musculus, class: Enzyme, accessions: P29477, gene: Nos2, swissprot: NOS2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22633833) Aldo-keto reductase family 1 member C4 (Organism: Homo sapiens, class: Enzyme, accessions: P17516, gene: AKR1C4, swissprot: AK1C4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17346963) A non-steroidal anti-inflammatory agent (NSAID) that inhibits the enzyme cyclooxygenase necessary for the formation of prostaglandins and other autacoids. It also inhibits the motility of polymorphonuclear leukocytes. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cardiovascular Agents (Code: D002317) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Gout Suppressants (Code: D006074) Peripheral Nervous System Agents (Code: D018373) Reproductive Control Agents (Code: D012102) Sensory System Agents (Code: D018689) Tocolytic Agents (Code: D015149) analgesic (Code: CHEBI:35480) gout suppressant (Code: CHEBI:35845) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) 1965-06-10 FDA IMN
Click to view clometacin Prostaglandin-H2 D-isomerase (Organism: Mus musculus, class: Enzyme, accessions: O09114, gene: Ptgds, swissprot: PTGDS_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1900533) Clometacin is an indometacin derivative and an analgesic. All preparations containing clometacin were withdrawn in 1987 due to their hepatotoxicity. Analgesics (Code: D000700) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view setastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/1982751)
Click to view carbon tetrachloride Carbon Tetrachloride is a clear, colorless, volatile and very stable chlorinated hydrocarbon. Carbon Tetrachloride is used as a solvent for oils and fats, as a refrigerant and as a dry-cleaning agent. Inhalation of its vapors can depress central nervous system activity and cause degeneration of the liver and kidneys. Carbon Tetrachloride is reasonably anticipated to be a human carcinogen based on evidence of carcinogenicity in experimental animals. refrigerant (Code: CHEBI:78433)
Click to view bendamustine DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) alkylating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022249Orig1s019lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205580s006lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205580s006lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205580s006lbl.pdf) Bendamustine is an alkylating agent and a nitrogen mustard compound. Bendamustine is a bifunctional mechlorethamine derivative containing a purine-like benzimidazole ring. Mechlorethamine and its derivatives form electrophilic alkyl groups. These groups form covalent bonds with electron-rich nucleophilic moieties, resulting in interstrand DNA crosslinks. The bifunctional covalent linkage can lead to cell death via several pathways. Bendamustine is active against both quiescent and dividing cells. The exact mechanism of action of bendamustine remains unknown. Bendamustine is indicated for the treatment of patients with chronic lymphocytic leukemia or indolent B-cell non-Hodgkin lymphoma. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) 2008-03-20 FDA
Click to view prednisone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202020s000lbl.pdf) Prednisone is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. It is biologically inert and converted to prednisolone in the liver. Prednison is indicated as an anti-inflammatory or immunosuppressive agent for certain allergic, dermatologic, gastrointestinal, hematologic, ophthalmologic, nervous system, renal, respiratory, rheumatologic, specific infectious diseases or conditions and organ transplantation, for the treatment of certain endocrine conditions, for palliation of certain neoplastic conditions. Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) prodrug (Code: CHEBI:50266) anti-inflammatory drug (Code: CHEBI:35472) antineoplastic agent (Code: CHEBI:35610) adrenergic agent (Code: CHEBI:37962) immunosuppressive agent (Code: CHEBI:35705) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) 1955-02-21 FDA
Click to view itopride Acetylcholinesterase (Organism: Electrophorus electricus, class: Enzyme, accessions: O42275, gene: ache, swissprot: ACES_ELEEL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7869618) D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1831229) Itopride inhibit dopamine and acetylcholine esterase enzyme and have a gastrokinetic effect. It is used for the treatment of gastrointestinal symptoms caused by reduced gastrointestinal motility. 1995 PMDA
Click to view cimetropium Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view cilastatin Dipeptidase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P16444, gene: DPEP1, swissprot: DPEP1_HUMAN) inhibitor (Source: ) Dipeptidase 1 (Organism: Sus scrofa, class: Enzyme, accessions: P22412, gene: DPEP1, swissprot: DPEP1_PIG) A renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4. Dipeptidase Inhibitors (Code: N0000175513) Renal Dehydropeptidase Inhibitor (Code: N0000175514) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 1985-11-26 FDA CIL
Click to view dimethoxanate
Click to view potassium canrenoate A synthetic pregnadiene derivative with anti-aldosterone activity. Diuretics (Code: D004232) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Mineralocorticoid Receptor Antagonists (Code: D000451) Natriuretic Agents (Code: D045283)
Click to view feclemine
Click to view etoricoxib Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1573192315087.pdf) Sulfotransferase 1E1 (Organism: Homo sapiens, class: Enzyme, accessions: P49888, gene: SULT1E1, swissprot: ST1E1_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1573192315087.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1573192315087.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1573192315087.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1573192315087.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1573192315087.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1573192315087.pdf) Etoricoxib is a member of the class of bipyridines. Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme to reduce the generation of prostaglandins from arachidonic acid. Etoricoxib is indicated in the symptomatic relief of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and the pain and signs of inflammation associated with acute gouty arthritis. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase 2 Inhibitors (Code: D052246) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) 2002-10-24 New Zealand Medicines and Medical Devices Safety Authority 5CH
Click to view capecitabine Thymidylate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P04818, gene: TYMS, swissprot: TYSY_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10631692) Capecitabine is a deoxycytidine derivative and fluorouracil prodrug that is used as an antineoplastic antimetabolite in the treatment of colon cancer; breast cancer and gastric cancer. Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Noxae (Code: D009676) prodrug (Code: CHEBI:50266) antineoplastic agent (Code: CHEBI:35610) 1998-04-30 FDA
Click to view adicillin Adicillin (Penicillin N) is a penicillin derivative produced by Cephalosporium acremonium. Adicillin is active against Sarcina lutea, Proteus vulgaris, Salmonella typhimurium, Diplococcus pneumoniae.
Click to view rabeprazole Potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P20648|P51164, gene: ATP4A|ATP4B, swissprot: ATP4A_HUMAN|ATP4B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020973s039lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020973s039lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020973s039lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19076159) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15258107) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15258107) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15258107) Fatty acid synthase (Organism: Homo sapiens, class: Enzyme, accessions: P49327, gene: FASN, swissprot: FAS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25513712) Rabeprazole belongs to a class of antisecretory compounds that suppress gastric acid secretion by inhibiting the gastric H+, K+ATPase at the secretory surface of the gastric parietal cell. Because this enzyme is regarded as the acid (proton) pump within the parietal cell, rabeprazole has been characterized as a gastric proton-pump inhibitor. Rabeprazole blocks the final step of gastric acid secretion. Rabeprazole sodium has been shown to be active against most strains of Helicobacter pylori in vitro and in clinical infections. Rabeprazole is a racemic mixture of two enantiomers, R(+)-enantiomer and S(-)-enantiomer in 1:1 proportion. Dexrabeprazole is the chirally pure R(+)-enantiomer which is more effective than the racemate and S(-)-rabeprazole in inhibiting acid-related gastric lesions. Rabeprazole is used for the treatment of Erosive or Ulcerative Gastroesophageal Reflux Disease (GERD), Duodenal Ulcers and pathological hypersecretory conditions such as Zollinger-Ellison Syndrome. Anti-Ulcer Agents (Code: D000897) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Proton Pump Inhibitors (Code: D054328) anti-ulcer drug (Code: CHEBI:49201) Proton Pump Inhibitor (Code: N0000175525) rabeprazole: 1999-08-19 FDA dexrabeprazole: 2007-06-13 CDSCO (INDIA) RZX
Click to view cyclomethycaine Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN
Click to view captodiame Captodiamine represents an interesting strategy for achieving benzodiazepine substitution with a low risk of dependence or impairment of cognitive function
Click to view triclabendazole Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Dimethylaniline monooxygenase [N-oxide-forming] 3 (Organism: Homo sapiens, class: Enzyme, accessions: P31513, gene: FMO3, swissprot: FMO3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208711s000lbl.pdf) Cruzipain (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P25779, gene: None, swissprot: CYSP_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20426472) Triclabendazole is an orally administered anthelmintic for immediate release. Triclabendazole is designated chemically as benzimidazole derivative. The mechanism by which triclabendazole exhibits its effect against Fasciola species is not fully elucidated. Studies in vitro and/or in infected animals suggest that triclabendazole and its active metabolites (sulfoxide and sulfone) are absorbed by the tegument of the immature and mature worms, leading to a decrease of the resting membrane potential, inhibition of tubulin function as well as protein and enzyme synthesis. These metabolic disturbances are associated with inhibition of motility, disruption of the surface as well as ultrastructure that includes inhibition of spermatogenesis and vitelline cells. Triclabendazole and its metabolites are active against the immature and mature worms of Fasciola hepatica and Fasciola gigantica. Triclabendazole is indicated for the treatment of fascioliasis. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) 2019-02-13 FDA
Click to view methyclothiazide Methyclothiazide is a benzothiadiazine-sulfonamide derivative belonging to the class of the thiazide diuretics. Methyclothiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule. Methyclothiazide was used in the management of hypertension either as the sole therapeutic agent or to enhance the effect of other antihypertensive drugs in the more severe forms of hypertension. Also it was used as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Increased Diuresis (Code: N0000175359) Thiazide Diuretic (Code: N0000175419) Thiazides (Code: N0000166469) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) 1960-10-21 FDA
Click to view nitrendipine Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Homo sapiens, class: Ion channel, accessions: Q01668, gene: CACNA1D, swissprot: CAC1D_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19029287) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18974361) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12128170) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/24014644) Adenosine receptor A2a (Organism: Rattus norvegicus, class: GPCR, accessions: P30543, gene: Adora2a, swissprot: AA2AR_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8709132) Adenosine receptor A1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25099, gene: Adora1, swissprot: AA1R_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8709132) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8709132) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12873512) Transient receptor potential cation channel subfamily A member 1 (Organism: Mus musculus, class: Unclassified, accessions: Q8BLA8, gene: Trpa1, swissprot: TRPA1_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20356305) Nitrendipine is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive. Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) 1988-10-28 Italian Medicines Agency (AIFA)
Click to view nadifloxacin (R)-isomer does not induce chromosomal aberrations, unlike (S)-isomer; structure given in first source Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antibacterial drug (Code: CHEBI:36047)
Click to view prednisolone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25965047) Solute carrier organic anion transporter family member 1B2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9QZX8, gene: Slco1b2, swissprot: SO1B2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8786566) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14661924) Prednisolone is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states. Prednisolone is used for the treatment of primary or secondary adrenocortical insufficiency, psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis, bursitis, acute gouty arthritis, epicondylitis, systemic lupus erythematosus, pemphigus and acute rhematic carditis. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) adrenergic agent (Code: CHEBI:37962) anti-inflammatory drug (Code: CHEBI:35472) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) 1955-06-21 FDA
Click to view cortisone acetate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=73673e2d-8d33-4719-92ce-ab619de343b0&type=display) Cortisone Acetate is the acetate salt form of cortisone, a synthetic or semisynthetic analog of the naturally occurring cortisone hormone produced by the adrenal glands with anti-inflammatory and immunomodulating properties. Cortisone acetate diffuses through the cell membrane and binds to nuclear glucocorticoid receptors. The receptor-ligand complex binds to promotor regions of certain genes and initiates RNA transcription. This results in an induction of synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Anti-Inflammatory Agents (Code: D000893) 1950-06-13 FDA
Click to view aldosterone Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN Mineralocorticoid receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P22199, gene: Nr3c2, swissprot: MCR_RAT Corticosteroid-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P08185, gene: SERPINA6, swissprot: CBG_HUMAN A hormone secreted by the ADRENAL CORTEX that regulates electrolyte and water balance by increasing the renal retention of sodium and the excretion of potassium. AS4
Click to view tetrachloroethylene Tetrachloroethylene is a colorless, volatile, nonflammable, liquid, chlorinated hydrocarbon with an ether-like odor that may emit toxic fumes of phosgene when exposed to sunlight or flames. Tetrachloroethylene is mainly used as a cleaning solvent in dry cleaning and textile processing and in the manufacture of fluorocarbons. Exposure to this substance irritates the upper respiratory tract and eyes and causes neurological effects as well as kidney and liver damage. Tetrachloroethylene is reasonably anticipated to be a human carcinogen and may be linked to an increased risk of developing skin, colon, lung, esophageal, and urogenital tract cancer as well as lymphosarcoma and leukemia. Carcinogens (Code: D002273) Environmental Pollutants (Code: D004785) Noxae (Code: D009676) Solvents (Code: D012997)
Click to view iloprost Prostacyclin receptor (Organism: Homo sapiens, class: GPCR, accessions: P43119, gene: PTGIR, swissprot: PI2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostacyclin receptor (Organism: Mus musculus, class: Unclassified, accessions: P43252, gene: Ptgir, swissprot: PI2R_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9313928) Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP2 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43116, gene: PTGER2, swissprot: PE2R2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin D2 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q13258, gene: PTGDR, swissprot: PD2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Thromboxane A2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P21731, gene: TBXA2R, swissprot: TA2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP3 subtype (Organism: Mus musculus, class: GPCR, accessions: P30557, gene: Ptger3, swissprot: PE2R3_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9313928) Prostaglandin E2 receptor EP4 subtype (Organism: Mus musculus, class: GPCR, accessions: P32240, gene: Ptger4, swissprot: PE2R4_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9313928) Prostaglandin E2 receptor EP1 subtype (Organism: Mus musculus, class: GPCR, accessions: P35375, gene: Ptger1, swissprot: PE2R1_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9313928) Prostaglandin E2 receptor EP2 subtype (Organism: Mus musculus, class: GPCR, accessions: Q62053, gene: Ptger2, swissprot: PE2R2_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9313928) Prostaglandin E2 receptor EP3 subtype (Organism: Rattus norvegicus, class: Unclassified, accessions: P34980, gene: Ptger3, swissprot: PE2R3_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9537820) Prostaglandin E2 receptor EP1 subtype (Organism: Rattus norvegicus, class: Unclassified, accessions: P70597, gene: Ptger1, swissprot: PE2R1_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9537820) Prostaglandin E2 receptor EP2 subtype (Organism: Rattus norvegicus, class: GPCR, accessions: Q62928, gene: Ptger2, swissprot: PE2R2_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9537820) An eicosanoid, derived from the cyclooxygenase pathway of arachidonic acid metabolism. It is a stable and synthetic analog of epoprostenol, but with a longer half-life than the parent compound. Its actions are similar to prostacyclin. Iloprost produces vasodilation and inhibits platelet aggregation. Prostacycline (Code: N0000175603) Prostaglandins I (Code: N0000011280) Cardiovascular Agents (Code: D002317) Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) Vasodilator Agents (Code: D014665) platelet aggregation inhibitor (Code: CHEBI:50427) vasodilator agent (Code: CHEBI:35620) 2004-12-29 FDA IL2
Click to view drostanolone propionate Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist synthetic anabolic androgenic steroid used to lower plasma cholesterol & as antineoplastic agent in advanced breast neoplasms; major descriptor (66-86); on-line search ANDROSTANOLS (80-86); ANDROSTANES (68-86); INDEX MEDICUS search DROMOSTANOLONE (66-86); RN given refers to (2alpha,5alpha,17beta)-isomer antineoplastic agent (Code: CHEBI:35610) FDA
Click to view ethyl loflazepate Ethyl loflazepate is a prodrug for descarboxyloflazepate (desalkylflurazepam), its active metabolite. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. The main metabolites of ethyl loflazepate are desalkylflurazepam, loflazepate and 3-ydroxydescarbethoxyloflazepate which are the benzodiazepine receptor agonists. Ethyl loflazeplate is indicated for the treatment of anxiety, tension, depression, sleep disorders in neurosis and psychosomatic disorders. Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1989-01-01 PMDA
Click to view fenofibrate Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/12904063) Fenofibrate is a fibric acid derivative, a prodrug comprising fenofibric acid linked to an isopropyl ester. Fenofibrate is rapidly hydrolyzed after oral ingestion to its pharmacologically active form, fenofibric acid. Fenofibric acid lowers lipid levels by activating peroxisome proliferator-activated receptor alpha (PPAR?). Through this mechanism, fenofibrate increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III (an inhibitor of lipoprotein lipase activity). The resulting decrease in triglycerides produces an alteration in the size and composition of LDL from small, dense particles (which are thought to be atherogenic due to their susceptibility to oxidation), to large buoyant particles. These larger particles have a greater affinity for cholesterol receptors and are catabolized rapidly. Activation of PPAR? also induces an increase in the synthesis of apolipoproteins AI, AII and HDL cholesterol. Fenofibrate is used as adjunctive therapy to diet to reduce elevated LDL-C, Total-C,Triglycerides and Apo B, and to increase HDL-C in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Fredrickson Types IIa and IIb). Peroxisome Proliferator Receptor alpha Agonist (Code: N0000175596) Peroxisome Proliferator-activated Receptor alpha Agonists (Code: N0000175375) PPAR alpha (Code: N0000170118) Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) antilipemic drug (Code: CHEBI:35679) 1993-12-31 FDA
Click to view haletazole
Click to view ofloxacin DNA gyrase (Organism: Staphylococcus aureus subsp. aureus, class: Enzyme, accessions: P20831|P0A0K8, gene: gyrA|gyrB, swissprot: GYRA_STAAU|GYRB_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019921s021lbl.pdf) DNA gyrase (Organism: Staphylococcus epidermidis (strain ATCC 35984 / RP62A), class: Enzyme, accessions: Q5HK04|Q5HK03, gene: gyrA|gyrB, swissprot: GYRA_STAEQ|GYRB_STAEQ) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019921s021lbl.pdf) DNA gyrase (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: P72524|P0A4L9, gene: gyrA|gyrB, swissprot: GYRA_STRPN|GYRB_STRPN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019921s021lbl.pdf) DNA gyrase (Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd), class: Enzyme, accessions: P43700|P43701, gene: gyrA|gyrB, swissprot: GYRA_HAEIN|GYRB_HAEIN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019921s021lbl.pdf) DNA gyrase (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: P48372|Q9I7C2, gene: gyrA|gyrB, swissprot: GYRA_PSEAE|GYRB_PSEAE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019921s021lbl.pdf) DNA gyrase subunit B (Organism: Proteus mirabilis, class: Enzyme, accessions: P22840, gene: gyrB, swissprot: GYRB_PROMI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019921s021lbl.pdf) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10525100) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10817732) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10817732) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10411577) Solute carrier family 22 member 4 (Organism: Homo sapiens, class: Transporter, accessions: Q9H015, gene: SLC22A4, swissprot: S22A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10215651) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) weak inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24014644) DNA gyrase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES4|P0AES6, gene: gyrA|gyrB, swissprot: GYRA_ECOLI|GYRB_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18426901) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19707748) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12089365) Ofloxacin is a second generation fluoroquinolone. Ofloxacin diffuses through the bacterial cell wall and acts by inhibiting DNA gyrase (bacterial topoisomerase II), an enzyme required for DNA replication, RNA transcription, and repair of bacterial DNA. Inhibition of DNA gyrase activity leads to blockage of bacterial cell growth. It is used for the treatment of infections (respiratory tract, kidney, skin, soft tissue, UTI), urethral and cervical gonorrhoea. Optically active L-isomer of ofloxacin with antibacterial activity is levofloxacin. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Antineoplastic Agents (Code: D000970) Cytochrome P-450 CYP1A2 Inhibitors (Code: D065609) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Metabolic Side Effects of Drugs and Substances (Code: D065606) Renal Agents (Code: D012076) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antiinfective agent (Code: CHEBI:35441) antibacterial drug (Code: CHEBI:36047) Quinolone Antimicrobial (Code: N0000175937) Quinolones (Code: N0000007606) ofloxacin: 1990-12-28 FDA levofloxacin: 1996-12-20 FDA LFX
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Click to view bisacodyl Bisacodyl is a stimulant laxative pro-drug. After oral administration, bisacodyl is metabolized on the inner surface of the intestine to produce the active metabolite, 4,4'-dihydroxydiphenyl-(2-pyridyl) methane, which induces intestinal contraction and peristalsis and increases intestinal mucosal secretion. Bisacodyl is typically prescribed for relief of constipation and for the management of neurogenic bowel dysfunction as well as part of bowel preparation before medical examinations, such as for a colonoscopy. Increased Large Intestinal Motility (Code: N0000009371) Stimulant Laxative (Code: N0000175812) Stimulation Large Intestine Fluid/Electrolyte Secretion (Code: N0000009871) Cathartics (Code: D002400) Gastrointestinal Agents (Code: D005765) Laxatives (Code: D054368) 2004-05-10 FDA
Click to view haloprogin UDP-glucose 4-epimerase (Organism: Homo sapiens, class: Enzyme, accessions: Q14376, gene: GALE, swissprot: GALE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16962325) UDP-glucose 4-epimerase (Organism: Trypanosoma brucei, class: Enzyme, accessions: Q8T8E9, gene: galE, swissprot: Q8T8E9_9TRYP) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16962325) Haloprogin is an active synthetic antifungal and antimonilial agent that was effective in the treatment of superficial fungal and monilial infections of the skin. Haloprogin was especially useful in the treatment of infections when the identity of the specific causative organism had not been established or is being determined. Studies in-vitro demonstrated antifungal, antimonilial and antibacterial activity. It was shown to demonstrate marked in-vitro activity against Staphylococcus and Streptococcus. Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 1971-08-06 FDA
Click to view metampicillin Metampicillin is a penicillin prepared by the reaction of ampicillin with formaldehyde. Metampicillin has a spectrum and level of activity similar to that of ampicillin in vitro, and it's inactive against penicillinase-producing strains of bacteria. Metampicillin is a prodrug of ampicillin. (See: ampicillin)
Click to view carbocromen A coronary vasodilator agent. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view octocrylene ingredient in sunscreens and cosmetics 2006-07-21 FDA
Click to view prenoxdiazine Prenoxdiazine is a cough suppressant and antitussive for non productive cough. It is used for treatment and prevention of acute respiratory viral infection, bronchitis, pharyngitis, asthma. It has some local anesthetic characteristics as well. 1990-07-01 CDSCO (INDIA)
Click to view bezafibrate Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) agonist (Source: ) Lipoprotein lipase (Organism: Homo sapiens, class: Enzyme, accessions: P06858, gene: LPL, swissprot: LIPL_HUMAN) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) Fatty acid-binding protein, liver (Organism: Rattus norvegicus, class: Unclassified, accessions: P02692, gene: Fabp1, swissprot: FABPL_RAT Peroxisome proliferator-activated receptor delta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q03181, gene: PPARD, swissprot: PPARD_HUMAN Fatty acid-binding protein, intestinal (Organism: Homo sapiens, class: Cytosolic other, accessions: P12104, gene: FABP2, swissprot: FABPI_HUMAN 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Organism: Homo sapiens, class: Enzyme, accessions: P04035, gene: HMGCR, swissprot: HMDH_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/2907502) An antilipemic agent that lowers CHOLESTEROL and TRIGLYCERIDES. It decreases LOW DENSITY LIPOPROTEINS and increases HIGH DENSITY LIPOPROTEINS. Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) antilipemic drug (Code: CHEBI:35679) 1978-01-01 YEAR INTRODUCED PEM
Click to view fosphenytoin Fosphenytoin is hydantoin derivative. Fosphenytoin is a prodrug intended for parenteral administration, its active metabolite is phenytoin. Fosphenytoin is indicated for the treatment of generalized tonic-clonic status epilepticus and prevention and treatment of seizures occurring during neurosurgery. Fosphenytoin can also be substituted, as short-term use, for oral phenytoin. Fosphenytoin should be used only when oral phenytoin administration is not possible. (See: phenytoin) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) 1996-08-05 FDA
Click to view phthalylsulfacetamide Phthalylsulfacetamide is a sulfonamide antibiotic used for topical application to the skin and the conjunctiva.
Click to view protirelin Thyrotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P34981, gene: TRHR, swissprot: TRFR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17035026) Protirelin is the synthetic analogue of the endogenous peptide thyrotropin-releasing hormone (TRH). TRH is a tri-peptide tropic hormone, released by the hypothalamus, which stimulates the release of Thyroid Stimulating Hormone and prolactin from the anterior pituitary. Protirelin is indicated as an adjunctive agent in the diagnostic assessment of thyroid function. Protirelin is indicated as an adjunct to evaluate the effectiveness of thyrotropin suppression with a particular dose of T4 in patients with nodular or diffuse goiter. Protirelin may be used, adjunctively, for adjustment of thyroid hormone dosage given to patients with primary hypothyroidism. 1976-11-05 FDA
Click to view piretanide Solute carrier family 12 member 1 (Organism: Homo sapiens, class: Transporter, accessions: Q13621, gene: SLC12A1, swissprot: S12A1_HUMAN) inhibitor Solute carrier family 12 member 2 (Organism: Homo sapiens, class: Transporter, accessions: P55011, gene: SLC12A2, swissprot: S12A2_HUMAN) inhibitor (Source: ) potent inhibitor of chloride transport; structure Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Potassium Chloride Symporter Inhibitors (Code: D049994) 1980-01-01 YEAR INTRODUCED
Click to view revaprazan Potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P20648|P51164, gene: ATP4A|ATP4B, swissprot: ATP4A_HUMAN|ATP4B_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/14681344) proton pump inhibitor 2005-09-15 Korean Food and Drug Administration (KFDA)
Click to view hydrocortisone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8282004) Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8282004) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/10772626) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8274418) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/1360010) Hydrocortisone is a glucocorticoid. Naturally occurring hydrocortisone, which also have salt-retaining properties, are used as replacement therapy in adrenocortical deficiency states. Hydrocortisone binds to the cytosolic glucocorticoid receptor. The formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids induce lipocortin-1 (annexin-1) synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. This leads to diminished eicosanoid production. The cyclooxygenase (both COX-1 and COX-2) expression is also suppressed, potentiating the effect. Hydrocortisone is used for the treatment of endocrine disorders (primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, non suppurative thyroiditis, hypercalcemia associated with cancer), rheumatic disorders, collagen diseases, dermatologic diseases, allergic states, phthalmic diseases, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, gastrointestinal diseases, nervous system, tuberculous meningitis, and trichinosis with neurologic or myocardial involvement. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Anti-Inflammatory Agents (Code: D000893) anti-inflammatory drug (Code: CHEBI:35472) anti-allergic agent (Code: CHEBI:50857) anti-asthmatic drug (Code: CHEBI:49167) 1952-08-05 FDA HCY
Click to view solifenacin Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021518s018lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021518s018lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily KQT member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O43526, gene: KCNQ2, swissprot: KCNQ2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily D member 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UK17, gene: KCND3, swissprot: KCND3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Solifenacin is a quinuclidine and tetrahydroisoquinoline derivative and muscarinic antagonist. Solifenacin is indicated to treat an overactive bladder with urinary incontinence, urgency, and frequency. Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Urological Agents (Code: D064804) Cholinergic Muscarinic Antagonist (Code: N0000175700) Cholinergic Muscarinic Antagonists (Code: N0000000125) 2004-11-19 FDA
Click to view dexetimide Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor (Organism: Mus musculus, class: GPCR, accessions: P12657|P32211|Q920H4|Q9ERZ3|Q9ERZ4, gene: Chrm1|Chrm2|Chrm3|Chrm4|Chrm5, swissprot: ACM1_MOUSE|ACM2_MOUSE|ACM3_MOUSE|ACM4_MOUSE|ACM5_MOUSE Muscarinic acetylcholine receptor M2 (Organism: Rattus norvegicus, class: GPCR, accessions: P10980, gene: Chrm2, swissprot: ACM2_RAT) antagonist (Source: ) A muscarinic antagonist that has been used to treat neuroleptic-induced parkinsonism. Benzetimide is the (-)-enantimorph of dexetimide. Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view viminol proposed as antitussive or analgesic; occurs as six stereoisomer with differing action; minor descriptor (75-86); on-line & INDEX MEDICUS search ETHANOLAMINES (75-86); RN given refers to parent cpd without isomeric designation
Click to view mexazolam Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.info.pmda.go.jp/go/pack/1124025C1030_1_09/) Mexazolam is a benzodiazepine. Mexazolam's structure is similar to that of other benzodiazepines such as oxazolam and cloxazolam. Mexazolam is rapidly metabolized to the active metabolites delorazepam and lorazepam. Mexazolam is indicated for the management of anxiety, nervousness, depression, fatigue, sleep disorders in neurosis. 1984-04-01 PMDA
Click to view cefadroxil Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor (Source: ) Long-acting, broad-spectrum, water-soluble, CEPHALEXIN derivative. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1978-02-17 FDA
Click to view rufloxacin DNA gyrase (Organism: Micrococcus luteus, class: Enzyme, accessions: C5C7X9|C5C7X8, gene: gyrA|gyrB, swissprot: GYRA_MICLC|GYRB_MICLC) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1653205) Rufloxacin is a quinolone antibiotic. It acts as a DNA gyrase inhibitor. Rufloxacin shows in vitro antibacterial activity against E. coli, Salmonella, Klebsiella, Proteus and Staphylococcus spp. Lower in vitro activity was observed with Pseudomonas, Serratia, Enterobacter and the streptococci group D. Rufloxacin is indicated for the treatment of lower respiratory tract and urinary tract infections caused by germs sensitive to rufloxacin. Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1992-06-16 Italian Medicines Agency (AIFA)
Click to view talinolol Talinolol is a cardioselective beta1-receptor blocker displaying lipophilic properties without intrinsic activity. Talinolol is used for the treatment of various cardiovascular diseases and in tachyarrhythmias. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 2004-02-09 Ministry of Health of the Russian Federation G3Q
Click to view opipramol 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Organism: Homo sapiens, class: Enzyme, accessions: Q15125, gene: EBP, swissprot: EBP_HUMAN Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN C-8 sterol isomerase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P32352, gene: ERG2, swissprot: ERG2_YEAST A tricyclic antidepressant with actions similar to AMITRIPTYLINE. Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619)
Click to view lapyrium chloride FDA
Click to view etofibrate analog of clofibrate with nicotinic acid substituted on the 2-carbon of the ethyl ester group; structure; RN given refers to parent cpd Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847)
Click to view diaziquone Diaziquone is a synthetic aziridinylbenzoquinone with potential antineoplastic activity. Diaziquone is rapidly and extensively metabolized by the liver. Diaziquone is a potent marrow suppressive agent inducing significant degrees of leukopenia, granulocytopenia, and thrombocytopenia in humans. Diaziquone alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis. This agent can also form free radicals, thereby initiating DNA damage via DNA strand breaks. Diaziquone readily crosses the blood brain barrier. In phase I and preliminary phase II trials, diaziquone has demonstrated activity against primary brain tumors. Antineoplastic Agents (Code: D000970) Cross-Linking Reagents (Code: D003432) Indicators and Reagents (Code: D007202) antineoplastic agent (Code: CHEBI:35610)
Click to view pheneticillin pheneticillin (feneticillin) is an oral acid resistant penicillin analogous to penicillin V with a range of antimicrob activity similar to penicillin G Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view bumetanide Sodium/potassium-transporting ATPase subunit alpha-1 (Organism: Homo sapiens, class: Transporter, accessions: P05023, gene: ATP1A1, swissprot: AT1A1_HUMAN) Solute carrier family 12 member 1 (Organism: Homo sapiens, class: Transporter, accessions: Q13621, gene: SLC12A1, swissprot: S12A1_HUMAN) inhibitor Solute carrier family 12 member 2 (Organism: Homo sapiens, class: Transporter, accessions: P55011, gene: SLC12A2, swissprot: S12A2_HUMAN) inhibitor (Source: ) G-protein coupled receptor 35 (Organism: Homo sapiens, class: GPCR, accessions: Q9HC97, gene: GPR35, swissprot: GPR35_HUMAN) agonist (Source: ) A sulfamyl diuretic. Increased Diuresis at Loop of Henle (Code: N0000175366) Loop Diuretic (Code: N0000175590) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Potassium Chloride Symporter Inhibitors (Code: D049994) diuretic (Code: CHEBI:35498) 1983-02-28 FDA
Click to view cyclofenil A gonadal stimulant and inducer of ovulation. It is used in the treatment of infertility and amenorrhea, but is thought to be less effective than CLOMIPHENE. Fertility Agents (Code: D005299) Fertility Agents, Female (Code: D005300) Reproductive Control Agents (Code: D012102)
Click to view piminodine
Click to view tribuzone antirheumatic, anti-inflammatory agent with analgesic properties; minor descriptor (75-85); on-line search PHENYLBUTAZONE/AA (75-85); Index Medicus search PYRAZOLES (75-80), PHENYLBUTAZONE/AA (81-85)
Click to view quinestrol Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist The 3-cyclopentyl ether of ETHINYL ESTRADIOL. After gastrointestinal absorption, it is stored in ADIPOSE TISSUE, slowly released, and metabolized principally to the parent compound. It has been used in ESTROGEN REPLACEMENT THERAPY. (From AMA Drug Evaluations Annual, 1992, p1011) Estrogens (Code: D004967) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) xenoestrogen (Code: CHEBI:76988) FDA
Click to view benzoxonium chloride
Click to view suclofenide Suclofenide is a benzenesulfonamide derivative. It was developed as anticonvulsant and antiepileptic agent.
Click to view clostebol acetate
Click to view fludarabine phosphate Fludarabine-triphosphate: DNA polymerase alpha catalytic subunit (Organism: Homo sapiens, class: Enzyme, accessions: P09884, gene: POLA1, swissprot: DPOLA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022137s003lbl.pdf) Ribonucleoside-diphosphate reductase subunit M2 (Organism: Homo sapiens, class: Enzyme, accessions: P31350, gene: RRM2, swissprot: RIR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022137s003lbl.pdf) Ribonucleoside-diphosphate reductase large subunit (Organism: Homo sapiens, class: Enzyme, accessions: P23921, gene: RRM1, swissprot: RIR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022137s003lbl.pdf) DNA primase large subunit (Organism: Homo sapiens, class: Enzyme, accessions: P49643, gene: PRIM2, swissprot: PRI2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022137s003lbl.pdf) DNA primase small subunit (Organism: Homo sapiens, class: Enzyme, accessions: P49642, gene: PRIM1, swissprot: PRI1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022137s003lbl.pdf) Fludarabine Phosphate is the phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth. For the treatment of adult patients with B-cell chronic lymphocytic leukemia (CLL) who have not responded to or whose disease has progressed during treatment with at least one standard alkylating-agent containing regimen. Nucleic Acid Synthesis Inhibitors (Code: N0000000233) Nucleoside Metabolic Inhibitor (Code: N0000175595) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Noxae (Code: D009676) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) prodrug (Code: CHEBI:50266) 1991-04-18 FDA Fluda
Click to view clofoctol
Click to view cefroxadine orally active, broad spectrum cephalosporin
Click to view amoxicillin Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10411577) Amoxicillin is an analog of ampicillin, derived from the basic penicillin nucleus, 6-aminopenicillanic acid. Amoxicillin is a semisynthetic antibiotic with in vitro bactericidal activity against Gram-positive and Gram-negative bacteria. It acts through the inhibition of cell wall biosynthesis that leads to the death of the bacteria. Amoxicillin has been shown to be active against Streptococcus spp. (Group B, C, and G; Beta-hemolytic). Amoxicillin is indicated for the treatment of tonsillitis and/or pharyngitis. Also amoxicillin is indicated for the treatment oflower respiratory tract infections, acute bacterial otitis media, sinusitis, skin and skin structure infections and urinary tract infections in combinations with clavulanate. Penicillin-class Antibacterial (Code: N0000175497) Penicillins (Code: N0000011281) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1974-12-09 FDA Bound
Click to view alkofanone
Click to view caroverine a muscle-relaxing drug used to relieve spasms in smooth muscles Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Excitatory Amino Acid Agents (Code: D018683) Excitatory Amino Acid Antagonists (Code: D018691) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) 1964-07-03 None
Click to view periciazine Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17606915) Acetylcholinesterase (Organism: Bos taurus, class: Enzyme, accessions: P23795, gene: ACHE, swissprot: ACES_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21459491) Cholinesterase (Organism: Bos taurus, class: Enzyme, accessions: P32749, gene: BCHE, swissprot: CHLE_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21459491) Periciazine is a phenothiazine with a piperidine side chain. It has similar antipsychotic action to other phenothiazines but produces more sedation. It also has adrenolytic, anticholinergic and extrapyramidal effects. Periciazine is undicated for the short-term treatment of severe anxiety or tension and in the maintenance treatment of psychotic disorders such as schizophrenia. adrenergic antagonist (Code: CHEBI:37887) sedative (Code: CHEBI:35717) first generation antipsychotic (Code: CHEBI:65190) 1966-10-31 Italian Medicines Agency (AIFA)
Click to view trimetaphan Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P30926|P32297, gene: CHRNA3|CHRNB4, swissprot: ACHA3_HUMAN|ACHB4_HUMAN) antagonist Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN) Neuronal acetylcholine receptor subunit alpha-10 (Organism: Homo sapiens, class: Ion channel, accessions: Q9GZZ6, gene: CHRNA10, swissprot: ACH10_HUMAN) Nicotinic acetylcholine receptor alpha 5 subunit (Organism: Musca domestica, class: Ion channel, accessions: A9XFY4, gene: nAChRalpha5, swissprot: A9XFY4_MUSDO Acetylcholine receptor subunit alpha (Organism: Torpedo californica, class: Ion channel, accessions: P02710, gene: CHRNA1, swissprot: ACHA_TORCA A nicotinic antagonist that has been used as a ganglionic blocker in hypertension, as an adjunct to anesthesia, and to induce hypotension during surgery. Adjuvants, Anesthesia (Code: D000759) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Ganglionic Blockers (Code: D005730) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) Vasodilator Agents (Code: D014665) anaesthesia adjuvant (Code: CHEBI:60807) vasodilator agent (Code: CHEBI:35620) antihypertensive agent (Code: CHEBI:35674) nicotinic antagonist (Code: CHEBI:48878) FDA
Click to view clinafloxacin DNA gyrase (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: P72524|P0A4L9, gene: gyrA|gyrB, swissprot: GYRA_STRPN|GYRB_STRPN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10223925) Clinafloxacin is a fluoroquinolone antibacterial. Clinafloxacin displays broad-spectrum antibacterial activity against Gram-positive, Gram-negative, and anaerobic pathogens by inhibiting the bacterial regulatory enzyme DNA gyrase and topoisomerase IV. It was developed for the treatment of respiratory diseases. However, its approval and release have been halted due to the presence of serious side effects. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) NFX
Click to view propiverine anticholinergic used for overactive bladder syndrome Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Urological Agents (Code: D064804)
Click to view metolazone Solute carrier family 12 member 1 (Organism: Homo sapiens, class: Transporter, accessions: Q13621, gene: SLC12A1, swissprot: S12A1_HUMAN) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) Solute carrier family 12 member 3 (Organism: Homo sapiens, class: Transporter, accessions: P55017, gene: SLC12A3, swissprot: S12A3_HUMAN) inhibitor (Source: ) Metolazone is a quinazoline diuretic, with properties generally similar to the thiazide diuretics. The actions of metolazone result from interference with the renal tubular mechanism of electrolyte reabsorption. Metolazone acts primarily to inhibit sodium reabsorption at the cortical diluting site and to a lesser extent in the proximal convoluted tubule. Sodium and chloride ions are excreted in approximately equivalent amounts. The increased delivery of sodium to the distal tubular exchange site results in increased potassium excretion. Metolazone does not inhibit carbonic anhydrase. A proximal action of metolazone has been shown in humans by increased excretion of phosphate and magnesium ions and by a markedly increased fractional excretion of sodium in patients with severely compromised glomerular filtration. This action has been demonstrated in animals by micropuncture studies. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) diuretic (Code: CHEBI:35498) antihypertensive agent (Code: CHEBI:35674) Increased Diuresis (Code: N0000175359) Thiazide-like Diuretic (Code: N0000175420) 1973-11-27 FDA
Click to view indapamide Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18374572) Solute carrier family 12 member 3 (Organism: Homo sapiens, class: Transporter, accessions: P55017, gene: SLC12A3, swissprot: S12A3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/018538s028lbl.pdf) Indapamide is the first of a new class of antihypertensive/diuretics, the indolines.Lozol is indicated for the treatment of hypertension, alone or in combination with otherantihypertensive drugs. Lozol is also indicated for the treatment of salt and fluid retention associated with congestive heart failure. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) antihypertensive agent (Code: CHEBI:35674) diuretic (Code: CHEBI:35498) Increased Diuresis (Code: N0000175359) Thiazide-like Diuretic (Code: N0000175420) 1983-07-06 FDA BL1
Click to view cyclovalone Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q7ZJM1, gene: pol, swissprot: Q7ZJM1_9HIV1 is a synthetic curcumin derivative
Click to view ilaprazole Potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P20648|P51164, gene: ATP4A|ATP4B, swissprot: ATP4A_HUMAN|ATP4B_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/11304936) Ilaprazole is a proton pump inhibitor. Ilaprazole revealed the characteristics as a strong proton pump inhibitor, and its potency against gastric acid secretion was superior to that of the reference drug, omeprazole. Ilaprazole is used for the treatment of gastric ulcer, duodenal ulcer, erosive esophagitis, H.pylori eradication. 2008-10-28 Korean Food and Drug Administration (KFDA)
Click to view glibornuride Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/2445740) Sulfonylurea receptor 2, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: O60706|Q14654, gene: ABCC9|KCNJ11, swissprot: ABCC9_HUMAN|KCJ11_HUMAN) blocker was MH 1975-92 (see under SULFONYLUREA COMPOUNDS 1975-90); use SULFONYLUREA COMPOUNDS to search GLIBORNURIDE 1975-92; an oral, sulfonylurea hypoglycemic agent which stimulates insulin secretion Hypoglycemic Agents (Code: D007004) 1969-01-01 YEAR INTRODUCED
Click to view drospirenone Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) antagonist Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) a progestational compound with antimineralocorticoid and antiandrogenic activity; structure given in first source Progestin (Code: N0000175602) Progesterone Congeners (Code: N0000011301) Diuretics (Code: D004232) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Mineralocorticoid Receptor Antagonists (Code: D000451) Natriuretic Agents (Code: D045283) contraceptive drug (Code: CHEBI:49323) 2001-05-11 FDA
Click to view bepridil Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/1281221) Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Homo sapiens, class: Ion channel, accessions: Q01668, gene: CACNA1D, swissprot: CAC1D_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/1281221) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) blocker Voltage-dependent P/Q-type calcium channel subunit alpha-1A (Organism: Homo sapiens, class: Ion channel, accessions: O00555, gene: CACNA1A, swissprot: CAC1A_HUMAN) blocker Potassium voltage-gated channel subfamily KQT member 4 (Organism: Homo sapiens, class: Ion channel, accessions: P56696, gene: KCNQ4, swissprot: KCNQ4_HUMAN) blocker (Source: ) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y3Q4, gene: HCN4, swissprot: HCN4_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Oryctolagus cuniculus, class: Ion channel, accessions: P15381, gene: CACNA1C, swissprot: CAC1C_RABIT Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Lethal factor (Organism: Bacillus anthracis, class: Enzyme, accessions: P15917, gene: lef, swissprot: LEF_BACAN Potassium channel subfamily T member 1 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q9Z258, gene: Kcnt1, swissprot: KCNT1_RAT) gating inhibitor (Source: ) A long-acting calcium-blocking agent with significant anti-anginal activity. The drug produces significant coronary vasodilation and modest peripheral effects. It has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) vasodilator agent (Code: CHEBI:35620) anti-arrhythmia drug (Code: CHEBI:38070) antihypertensive agent (Code: CHEBI:35674) 1990-12-28 FDA BEP
CQN
Click to view phenoperidine A narcotic analgesic partly metabolized to meperidine in the liver. It is similar to morphine in action and used for neuroleptanalgesia, usually with droperidol. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view atovaquone Ubiquinol-cytochrome-c reductase complex core protein I, mitochondrial (Organism: Euglena gracilis, class: Enzyme, accessions: P43264, gene: None, swissprot: QCR1_EUGGR) Dihydroorotate dehydrogenase (quinone), mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q02127, gene: DHODH, swissprot: PYRD_HUMAN) Dihydroorotate dehydrogenase (quinone), mitochondrial (Organism: Rattus norvegicus, class: Enzyme, accessions: Q63707, gene: Dhodh, swissprot: PYRD_RAT Cytochrome b (Organism: Plasmodium falciparum, class: Enzyme, accessions: Q02768, gene: MT-CYB, swissprot: CYB_PLAFA) inhibitor Dihydroorotate dehydrogenase (Organism: Plasmodium falciparum, class: Unclassified, accessions: Q54A96, gene: dhod, swissprot: Q54A96_PLAFA A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols. Antiprotozoal (Code: N0000175485) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Enzyme Inhibitors (Code: D004791) antimalarial (Code: CHEBI:38068) 1992-11-25 FDA AOQ
Click to view pitofenone Acetylcholinesterase (Organism: Bos taurus, class: Enzyme, accessions: P23795, gene: ACHE, swissprot: ACES_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1777122) Acetylcholinesterase (Organism: Electrophorus electricus, class: Enzyme, accessions: O42275, gene: ache, swissprot: ACES_ELEEL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1777122) Pitofenone is an antispasmodic drug. Pitofenone is indicated to relieve pain and spasms of smooth muscles of the stomach, intestines, urinary tract, biliary tract, uterus and for the treatment of back pain and sprains. 2003-08-05 Bulgarian Drug Agency (BDA)
Click to view dioxyline Methionine aminopeptidase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P50579, gene: METAP2, swissprot: MAP2_HUMAN Methionine aminopeptidase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P53582, gene: METAP1, swissprot: MAP11_HUMAN
Click to view bambuterol Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: ) selective inhibitor of butyrylcholinesterase & acetylcholinesterase Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) tocolytic agent (Code: CHEBI:66993) sympathomimetic agent (Code: CHEBI:35524) beta-adrenergic agonist (Code: CHEBI:35522) prodrug (Code: CHEBI:50266) bronchodilator agent (Code: CHEBI:35523) anti-asthmatic drug (Code: CHEBI:49167) 1990-01-01 YEAR INTRODUCED
Click to view tiracizine Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619)
Click to view fenbutrazate
Click to view blonanserin Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/15686911) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/15686911) 2008-01-25 PMDA
Click to view cefaclor Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16434549) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16434549) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16434549) Cefaclor is a semisynthetic cephalosporin antibiotic derivative of cephalexin. Cefaclor has been shown to be active against: Staphylococcus aureus (methicillin susceptible only), Coagulase negative staphylococci (methicillin susceptible only), Streptococcus pneumoniae, Streptococcus pyogenes (group A -hemolytic streptococci), Escherichia coli, Haemophilus influenzae (excluding -lactamase-negative, ampicillin-resistant strains), Klebsiella spp. and Proteus mirabilis. Cefaclor is indicated in the treatment of the otitis media (due to S. pneumoniae, H. influenzae, staphylococci, and S. pyogenes), Lower respiratory tract infections (due to S. pneumoniae, Haemophilus influenzae, and S. pyogenes), Pharyngitis and Tonsillitis (due to S. pyogenes), Urinary tract infections, including pyelonephritis and cystitis (due to E. coli, P. mirabilis, Klebsiella spp., and coagulase-negative staphylococci), Skin and skin structure infections (due to S. aureus and S. pyogenes). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) drug allergen (Code: CHEBI:88188) 1979-04-04 FDA
Click to view prucalopride 5-hydroxytryptamine receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q13639, gene: HTR4, swissprot: 5HT4R_HUMAN) agonist (Source: https://www.ema.europa.eu/documents/product-information/resolor-epar-product-information_en.pdf) D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT) antagonist (Source: https://www.ema.europa.eu/documents/product-information/resolor-epar-product-information_en.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/resolor-epar-product-information_en.pdf) Prucalopride is a dihydrobenzofurancarboxamide with gastrointestinal prokinetic activities. Prucalopride is a selective, high affinity serotonin (5-HT4) receptor agonist, which is likely to explain its prokinetic effects. In rats, prucalopride in vivo induced hyperprolactinaemia caused by an antagonistic action at the D2 receptor. Prucalopride is indicated for symptomatic treatment of chronic constipation in adults in whom laxatives fail to provide adequate relief. Gastrointestinal Agents (Code: D005765) Laxatives (Code: D054368) Neurotransmitter Agents (Code: D018377) Serotonin 5-HT4 Receptor Agonists (Code: D058828) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) 2009-10-15 EMA
Click to view diacerein Rhein: Cytochrome P450 2E1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P05182, gene: Cyp2e1, swissprot: CP2E1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18814214) Cytochrome P450 3A (Organism: Rattus norvegicus, class: Enzyme, accessions: P04800|P05183|P51538|Q64581, gene: Cyp3a1|Cyp3a2|Cyp3a9|Cyp3a18, swissprot: CP3A1_RAT|CP3A2_RAT|CP3A9_RAT|CP3AI_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18814214) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24568372) Diacerein is a prodrug which is metabolized to rhein. Rhein dose-dependently inhibits superoxide anion production, chemotaxis and phagocytic activity of neutrophils, and macrophage migration and phagocytosis. In addition, rhein exerts its anticancer effects via the modulation of processes of cellular proliferation, apoptosis, migration, and invasion. It is currently approved for the treatment of osteoarthritis. Anti-Inflammatory Agents (Code: D000893) 1992-08-12 ANSM (French National Agency for Medicines and Health Products Safety) Rhein
Click to view cyclarbamate
Click to view perindopril Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Perindopril, a pro-drug, is hydrolyzed to perindoprilat, which inhibits angiotensin converting enzyme. Perindopril is indicated for the treatment of hypertension to lower blood pressure. Angiotensin Converting Enzyme Inhibitor (Code: N0000175562) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor (Code: CHEBI:35457) antihypertensive agent (Code: CHEBI:35674) 1993-12-30 FDA
Click to view etofenamate Etofenamate is a non-steroidal anti-inflammatory agent with analgesic properties. Etofenamate is used to treat muscle and joint paint. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1980-02-28 Italian Medicines Agency (AIFA)
Click to view pyritinol Pyritinol is a neurotropic agent which reduces permeability of blood-brain barrier to phosphate. Pyritinol is a nootropic, used in the treatment of various cerebrovascular and mental function disorders. 1974-04-09 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view prasterone sulfate Steryl-sulfatase (Organism: Homo sapiens, class: Enzyme, accessions: P08842, gene: STS, swissprot: STS_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11087571) Solute carrier family 22 member 9 (Organism: Homo sapiens, class: Transporter, accessions: Q8IVM8, gene: SLC22A9, swissprot: S22A9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10660625) Solute carrier family 22 member 9 (Organism: Homo sapiens, class: Transporter, accessions: Q8IVM8, gene: SLC22A9, swissprot: S22A9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10660625) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9539145) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11134001) ATP-binding cassette sub-family C member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q96J66, gene: ABCC11, swissprot: ABCCB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15537867) Prasterone sulfate (dehydroepiandrosterone sulfate) is 19-carbon steroid originating principally from the zona reticularis of the human adrenal cortex. Tissue sulfatases rapidly interconvert dehydroepiandrosterone sulfate to dehydroepiandrosterone, which has a higher clearance rate and shorter halflife. (See: prasterone)
Click to view propantheline Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: ) A muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking. Anticholinergic (Code: N0000175574) Anti-Ulcer Agents (Code: D000897) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Gastrointestinal Agents (Code: D005765) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) 1953-04-02 FDA
Click to view carboprost Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist A nonsteroidal abortifacient agent that is effective in both the first and second trimesters of PREGNANCY. Prostaglandin Analog (Code: N0000175454) Prostaglandins (Code: N0000007706) Abortifacient Agents (Code: D000019) Abortifacient Agents, Nonsteroidal (Code: D000020) Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102) oxytocic (Code: CHEBI:36063) abortifacient (Code: CHEBI:50691) 1979-01-09 FDA
Click to view cinnarizine Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Cavia porcellus, class: Ion channel, accessions: O35505, gene: CACNA1C, swissprot: CAC1C_CAVPO) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/1281221) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8323546) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8951176) Cinnarizine is a piperazine derivative with antihistaminic, antiserotonergic, antidopaminergic, and calcium channel-blocking activities. Cinnarizine has been shown to be a non-competitive antagonist of the smooth muscle contractions caused by various vasoactive agents including histamine. It acts on smooth muscle by selectively inhibiting the transport of calcium ions across cell membranes into depolarised cells, therefore reducing the availability of free Ca+ ions for the induction and maintenance of contraction. It is currently used for the treatment of nausea, vomiting, and vertigo caused by Meniere’s disease and other vestibular disorders. Cinnarizine is also used for prevention and treatment of motion sickness. Chronic use of cinnarizine may induce Parkinsonian disorders. Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) antiemetic (Code: CHEBI:50919) histamine antagonist (Code: CHEBI:37956) muscarinic antagonist (Code: CHEBI:48876) anti-allergic agent (Code: CHEBI:50857) H1-receptor antagonist (Code: CHEBI:37955) 1970-03-01 Italian Medicines Agency (AIFA)
Click to view cethexonium Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Surface-Active Agents (Code: D013501)
Click to view ketazolam Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view fleroxacin DNA gyrase subunit A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES4, gene: gyrA, swissprot: GYRA_ECOLI) A broad-spectrum antimicrobial fluoroquinolone. The drug strongly inhibits the DNA-supercoiling activity of DNA GYRASE. Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antibacterial drug (Code: CHEBI:36047) 1992-01-01 YEAR INTRODUCED
Click to view lansoprazole Potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P20648|P51164, gene: ATP4A|ATP4B, swissprot: ATP4A_HUMAN|ATP4B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/21-428lbl.pdf) Indoleamine 2,3-dioxygenase 1 (Organism: Mus musculus, class: Enzyme, accessions: P28776, gene: Ido1, swissprot: I23O1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Indoleamine 2,3-dioxygenase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q8R0V5, gene: Ido2, swissprot: I23O2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Fatty acid synthase (Organism: Homo sapiens, class: Enzyme, accessions: P49327, gene: FASN, swissprot: FAS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25513712) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224780) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224780) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9224780) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22328583) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22328583) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22328583) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19076159) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11770010) olute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/29353278) Lansoprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but that suppress gastric acid secretion by specific inhibition of the (H+,K+)-ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the parietal cell, lansoprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus. The R-enantiomer is known as dexlansoprazole. Although the R and S isomers appeared to exhibit similar in vitro pharmacological properties, in vivo studies indicated that the gastric acid secretion inhibition activity of racemic lansoprazole was mainly from dexlansoprazole. Proton Pump Inhibitor (Code: N0000175525) Inhibition Gastric Acid Secretion (Code: N0000009724) Anti-Ulcer Agents (Code: D000897) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Proton Pump Inhibitors (Code: D054328) anti-ulcer drug (Code: CHEBI:49201) lansoprazole: 1995-05-10 FDA dexansoprazole: 2009-01-30 FDA
Click to view sulfadiasulfone Sulfadiasulfone is a sulfonamide and an antibacterial agent. It was used in the treatment of leprosy. Also it was used for the treatment of sarcoidosis. FDA
Click to view trimetrexate Folylpolyglutamate synthase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q05932, gene: FPGS, swissprot: FOLC_HUMAN) Dihydrofolate reductase (Organism: Rattus norvegicus, class: Enzyme, accessions: Q920D2, gene: Dhfr, swissprot: DYR_RAT Dihydrofolate reductase (Organism: Pneumocystis carinii, class: Enzyme, accessions: P16184, gene: None, swissprot: DYR_PNECA) inhibitor Dihydrofolate reductase (Organism: Lactobacillus casei, class: Enzyme, accessions: P00381, gene: folA, swissprot: DYR_LACCA Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN Dihydrofolate reductase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0ABQ4, gene: folA, swissprot: DYR_ECOLI Bifunctional dihydrofolate reductase-thymidylate synthase (Organism: Toxoplasma gondii, class: Enzyme, accessions: Q07422, gene: None, swissprot: DRTS_TOXGO Dihydrofolate reductase (Organism: Mus musculus, class: Enzyme, accessions: P00375, gene: Dhfr, swissprot: DYR_MOUSE Dihydrofolate reductase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P07807, gene: DFR1, swissprot: DYR_YEAST Bifunctional dihydrofolate reductase-thymidylate synthase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: Q27793, gene: None, swissprot: DRTS_TRYCR Dihydrofolate reductase (Organism: Candida albicans, class: Enzyme, accessions: P22906, gene: DFR1, swissprot: DYR_CANAX Dihydrofolate reductase (Organism: Mycobacterium avium, class: Enzyme, accessions: O30463, gene: folA, swissprot: O30463_MYCAV Dihydrofolate reductase (Organism: Escherichia coli, class: Unclassified, accessions: B0BL08, gene: dfrA17, swissprot: B0BL08_ECOLX A nonclassical folic acid inhibitor through its inhibition of the enzyme dihydrofolate reductase. It is being tested for efficacy as an antineoplastic agent and as an antiparasitic agent against PNEUMOCYSTIS PNEUMONIA in AIDS patients. Myelosuppression is its dose-limiting toxic effect. Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) Noxae (Code: D009676) antifungal drug (Code: CHEBI:86327) 1993-12-17 FDA TMQ
Click to view bulaquine
Click to view cilostazol cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Organism: Homo sapiens, class: Enzyme, accessions: Q14432, gene: PDE3A, swissprot: PDE3A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020863s024lbl.pdf) cGMP-inhibited 3',5'-cyclic phosphodiesterase B (Organism: Homo sapiens, class: Enzyme, accessions: Q13370, gene: PDE3B, swissprot: PDE3B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020863s024lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020863s024lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020863s024lbl.pdf) Cilostazol is a quinolinone derivative that inhibits cellular phosphodiesterase (more specific for phosphodiesterase III). Cilostazol and several of its metabolites inhibit phosphodiesterase III activity and suppress cAMP degradation with a resultant increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation, respectively. Cilostazol is indicated for the reduction of symptoms of intermittent claudication. Phosphodiesterase 3 Inhibitor (Code: N0000175598) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Fibrin Modulating Agents (Code: D050299) Fibrinolytic Agents (Code: D005343) Hematologic Agents (Code: D006401) Neuroprotective Agents (Code: D018696) Peripheral Nervous System Agents (Code: D018373) Phosphodiesterase 3 Inhibitors (Code: D058987) Phosphodiesterase Inhibitors (Code: D010726) Platelet Aggregation Inhibitors (Code: D010975) Protective Agents (Code: D020011) Respiratory System Agents (Code: D019141) Vasodilator Agents (Code: D014665) anticoagulant (Code: CHEBI:50249) neuroprotective agent (Code: CHEBI:63726) bronchodilator agent (Code: CHEBI:35523) vasodilator agent (Code: CHEBI:35620) fibrin modulating drug (Code: CHEBI:48676) platelet aggregation inhibitor (Code: CHEBI:50427) 1999-01-15 FDA
Click to view amisulpride D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.medsafe.govt.nz/profs/Datasheet/s/sulprixtab.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.medsafe.govt.nz/profs/Datasheet/s/sulprixtab.pdf) Amisulpride is a member of the class of benzamides. It is a potent, selective dopamine D2 and D3 receptor antagonist. It is an atypical antipsychotic/antischizophrenic agent with limited extrapyrimidal side effects. Unlike classical and atypical neuroleptics, amisulpride has no affinity for serotonin, alpha-adrenergic, histamine H1 and cholinergic receptors. In addition, amisulpride does not bind to sigma sites. Amisulpride is indicated for the treatment of acute and chronic schizophrenic disorders, in which positive symptoms (such as delusions, hallucinations, thought disorders) and/or negative symptoms (such as blunted affect, emotional and social withdrawal) are prominent, including patients characterised by predominant negative symptoms. second generation antipsychotic (Code: CHEBI:65191) 1986-01-20 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view norgestimate Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist Progesterone Congeners (Code: N0000011301) Progestin (Code: N0000175602) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102) contraceptive drug (Code: CHEBI:49323) synthetic oral contraceptive (Code: CHEBI:49326) 1989-12-29 FDA
Click to view diprafenone Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317)
Click to view prajmalium Prajmalium is an antiarrhythmic agent and a derivative of the rauwolfia alkaloid ajmaline. Prajmaline is a class Ia antiarrhythmic agent. It is an anti-arrhythmia agent, but may cause liver damage. It is used for the treatment of angina pectoris, Wolff–Parkinson–White Syndrome, paroxysmal atrial fibrillation, atrioventricular tachycardia and coronary artery disease. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317)
Click to view tripamide Tripamide is a diuretic derived from a sulfonamide nucleus that has both antihypertensive and natriuretic properties. It is Na-K-Cl cotransporter inhibitor. The antihypertensive mechanism of tripamide is considered to be based on a mild saluretic action and a peripheral vasodilation action. Tripamide is indicated for the treatment of essential hypertension. Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Potassium Chloride Symporter Inhibitors (Code: D049994) 1982-03-01 PMDA
Click to view flavodic acid capillary protective agent; RN given refers to parent cpd; structure
Click to view parecoxib Parecoxib is a prodrug of valdecoxib. Valdecoxib is a selective COX-2 inhibitor. Parecoxib is indicated for the short-term treatment of postoperative pain in adults. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase 2 Inhibitors (Code: D052246) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) non-narcotic analgesic (Code: CHEBI:35481) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) prodrug (Code: CHEBI:50266) 2002-03-22 EMA PXB
Click to view thioridazine 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7898773) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7898773) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12747773) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12747773) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1826762) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1826762) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12629531) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12629531) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12629531) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12629531) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Thioridazine is a phenothiazine antipsychotic used in the management of psychoses, including schizophrenia, and in the control of severely disturbed or agitated behavior. Thioridazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; blocks alpha-adrenergic effect depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis. Thioridazine was withdrawn worldwide in 2005 due to it's association with cardiac arrythmias. Phenothiazine (Code: N0000175746) Phenothiazines (Code: N0000007544) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) first generation antipsychotic (Code: CHEBI:65190) serotonergic antagonist (Code: CHEBI:48279) H1-receptor antagonist (Code: CHEBI:37955) alpha-adrenergic antagonist (Code: CHEBI:37890) dopaminergic antagonist (Code: CHEBI:48561) 1962-03-15 FDA LZU
RTZ
Click to view fusidic acid Elongation factor G (Organism: Staphylococcus aureus, class: Other, accessions: P68790, gene: fusA, swissprot: EFG_STAAU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20718859) Canalicular multispecific organic anion transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63120, gene: Abcc2, swissprot: MRP2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12106615) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27458210) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27458210) Fusidic Acid is a bacteriostatic antibiotic derived from the fungus Fusidium coccineum and used as a topical medication to treat skin infections. Fusidic acid acts as a bacterial protein synthesis inhibitor by preventing the turnover of elongation factor G (EF-G) from the ribosome. Fusidic acid is a narrow-spectrum antibiotic. Fusidic acid has potent antibacterial activity toward Grampositive bacteria and Neisseria species. Fusidic acid is most notable for its activity against Staphylococci, whether coagulase-positive or negative, and regardless of resistance to methicillin and related penicillins. Fusidic acid is active against Haemophilus sp. but has almost no antibacterial activity against other Gram-negative organisms such as E. Coli, Proteus, Klebsiella and Salmonella. Fungi are also insensitive to fusidic acid. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) 1987-03-09 ANSM (French National Agency for Medicines and Health Products Safety) FUA
Click to view hydroxyestrone diacetate
Click to view elcometrine Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Reproductive Control Agents (Code: D012102)
Click to view nomegestrol acetate Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: https://www.ema.europa.eu/documents/product-information/ioa-epar-product-information_en.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/ioa-epar-product-information_en.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/ioa-epar-product-information_en.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/ioa-epar-product-information_en.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/ioa-epar-product-information_en.pdf) Nomegestrol acetate is a highly selective progestogen derived from the naturally occurring steroid hormone, progesterone. Nomegestrol acetate has a strong affinity for the human progesterone receptor and has an anti-gonadotropic activity, a progesterone receptor-mediated anti-estrogenic activity, a moderate anti-androgenic activity, and is devoid of any estrogenic, androgenic, glucocorticoid or mineralocorticoid activity. Nomegestrol acetate is used with estradiol for the oral contraception. Also nomegestrol acetate has been used successfully for the treatment of some gynaecological disorders (menstrual disturbances, dysmenorrhoea, premenstrual syndrome) and as a component of hormone replacement therapy in combination with estradiol for the relief of menopausal symptoms 1983-11-18 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view oxypendyl
Click to view rimexolone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Rimexolone is a corticosteroids indicated for the treatment of postoperative inflammation following ocular surgery and in the treatment of anterior uveitis. Corticosteroids suppress the inflammatory response to a variety of inciting agents of a mechanical, chemical, or immunological nature. They inhibit edema, cellular infiltration, capillary dilatation, fibroblastic proliferation, deposition of collagen and scar formation associated with inflammation. Placebo-controlled clinical studies demonstrated that rimexolone ophthalmic suspension is efficacious for the treatment of anterior chamber inflammation following cataract surgery. Adrenal Cortex Hormones (Code: D000305) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) 1994-12-30 FDA
Click to view penmesterol
Click to view rebamipide Cholecystokinin receptor type A (Organism: Rattus norvegicus, class: GPCR, accessions: P30551, gene: Cckar, swissprot: CCKAR_RAT) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15556137) Prostaglandin G/H synthase 2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P35355, gene: Ptgs2, swissprot: PGH2_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/11046075) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14738594) Prostaglandin E2 receptor EP4 subtype (Organism: Rattus norvegicus, class: GPCR, accessions: P43114, gene: Ptger4, swissprot: PE2R4_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/10882227) Pro-epidermal growth factor (Organism: Rattus norvegicus, class: Unclassified, accessions: P07522, gene: Egf, swissprot: EGF_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/9753233) Vascular endothelial growth factor A (Organism: Rattus norvegicus, class: Secreted, accessions: P16612, gene: Vegfa, swissprot: VEGFA_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/15104358) Proheparin-binding EGF-like growth factor (Organism: Rattus norvegicus, class: Secreted, accessions: Q06175, gene: Hbegf, swissprot: HBEGF_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/15104358) Insulin-like growth factor I (Organism: Rattus norvegicus, class: Secreted, accessions: P08025, gene: Igf1, swissprot: IGF1_RAT) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/15104358) Rebamipide, an amino acid derivative of 2(1H)-quinolinone, has been used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. Rebamipide induces cyclooxygenase 2 (COX2) synthesis which results in an increase in endogenous prostaglandin synthesis in the gastric mucosa. Rebamipide is used for the treatment of gastric ulcers, gastric mucosal lesions (erosion, bleeding, redness, and edema), acute gastritis and acute exacerbation of chronic gastritis. Anti-Ulcer Agents (Code: D000897) Antioxidants (Code: D000975) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Protective Agents (Code: D020011) 2004-07-29 CDSCO (INDIA)
Click to view azosemide Azosemide is a monosulfamyl belonging to the class of loop diuretics. Azosemide inhibits sodium and chloride reabsorption throughout the thick ascending limb of the loop of Henle. The exact mechanism of action is not fully understood. Azosemide is indicated for cardiac-induced oedema (congestive cardiac failure), renal-induced oedema, and hepatic-induced oedema. Diuretics (Code: D004232) Natriuretic Agents (Code: D045283) loop diuretic (Code: CHEBI:77608) PMDA
Click to view lorcainide Sodium channel subunit beta-4 (Organism: Homo sapiens, class: Ion channel, accessions: Q8IWT1, gene: SCN4B, swissprot: SCN4B_HUMAN) Sodium channel subunit beta-3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NY72, gene: SCN3B, swissprot: SCN3B_HUMAN) Sodium channel subunit beta-2 (Organism: Homo sapiens, class: Ion channel, accessions: O60939, gene: SCN2B, swissprot: SCN2B_HUMAN) Sodium channel subunit beta-1 (Organism: Homo sapiens, class: Ion channel, accessions: Q07699, gene: SCN1B, swissprot: SCN1B_HUMAN) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317)
Click to view remoxipride 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901|P19020|P25115|P30729|P61169, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_RAT|DRD2_RAT|DRD3_RAT|DRD4_RAT|DRD5_RAT) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: ) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) D(3) dopamine receptor (Organism: Chlorocebus aethiops, class: GPCR, accessions: P52703, gene: DRD3, swissprot: DRD3_CHLAE) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) D(2) dopamine receptor (Organism: Chlorocebus aethiops, class: GPCR, accessions: P52702, gene: DRD2, swissprot: DRD2_CHLAE) D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) An antipsychotic agent that is specific for dopamine D2 receptors. It has been shown to be effective in the treatment of schizophrenia. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1990-01-01 YEAR INTRODUCED
Click to view azaribine pyrimidine analogue; anti-metabolite used in psoriasis & mycosis fungoides Dermatologic Agents (Code: D003879) antipsoriatic (Code: CHEBI:50748) prodrug (Code: CHEBI:50266)
Click to view nedocromil fMet-Leu-Phe receptor (Organism: Homo sapiens, class: GPCR, accessions: P21462, gene: FPR1, swissprot: FPR1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1326878) G-protein coupled receptor 35 (Organism: Homo sapiens, class: GPCR, accessions: Q9HC97, gene: GPR35, swissprot: GPR35_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/24113750) Nedocromil is a mast cell stabilizer that inhibits activation of inflammatory cells which are associated with asthma, including eosinophils, neutrophils, macrophages, mast cells, monocytes, and platelets. Decreased Histamine Release (Code: N0000175628) Mast Cell Stabilizer (Code: N0000175630) Anti-Allergic Agents (Code: D018926) Anti-Asthmatic Agents (Code: D018927) Anti-Inflammatory Agents (Code: D000893) Respiratory System Agents (Code: D019141) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) anti-asthmatic drug (Code: CHEBI:49167) anti-allergic agent (Code: CHEBI:50857) 1992-12-30 FDA
Click to view isradipine Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Homo sapiens, class: Ion channel, accessions: Q01668, gene: CACNA1D, swissprot: CAC1D_HUMAN) gating inhibitor (Source: ) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) blocker Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Oryctolagus cuniculus, class: Ion channel, accessions: P15381, gene: CACNA1C, swissprot: CAC1C_RABIT Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Rattus norvegicus, class: Ion channel, accessions: P27732, gene: Cacna1d, swissprot: CAC1D_RAT Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Mus musculus, class: Ion channel, accessions: Q01815, gene: Cacna1c, swissprot: CAC1C_MOUSE) gating inhibitor (Source: ) Voltage-dependent L-type calcium channel subunit alpha-1F (Organism: Mus musculus, class: Unclassified, accessions: Q9JIS7, gene: Cacna1f, swissprot: CAC1F_MOUSE) gating inhibitor (Source: ) A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure. Calcium Channel Antagonists (Code: N0000000069) Dihydropyridine Calcium Channel Blocker (Code: N0000175421) Dihydropyridines (Code: N0000007556) Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) 1990-12-20 FDA
Click to view amocarzine Amocarzine is an antifilarial antihelminthic drug, derived from amoscanate, that is active against the adult worms of Onchocerca volvulus. It was used for the treatment of onchocerciasis. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Filaricides (Code: D005369) antinematodal drug (Code: CHEBI:35444)
Click to view tamoxifen Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist/antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021807s006lbl.pdf) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) agonist/antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021807s006lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021807s006lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021807s006lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021807s006lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021807s006lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021807s006lbl.pdf) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021807s006lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021807s006lbl.pdf) Sulfotransferase 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P50225, gene: SULT1A1, swissprot: ST1A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021807s006lbl.pdf) 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Organism: Homo sapiens, class: Enzyme, accessions: Q15125, gene: EBP, swissprot: EBP_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9618436) Dimethylaniline monooxygenase [N-oxide-forming] 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q01740, gene: FMO1, swissprot: FMO1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16684653) Dimethylaniline monooxygenase [N-oxide-forming] 3 (Organism: Homo sapiens, class: Enzyme, accessions: P31513, gene: FMO3, swissprot: FMO3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16684653) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12124303) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12124303) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12124303) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15601807) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8293548) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8293548) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15386482) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12739759) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12739759) Tamoxifen is a selective estrogen receptor modulator with tissue-specific activities. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the endometrium. Tamoxifen is indicated for treatment estrogen receptor-positive metastatic breast cancer, to reduce risk of invasive breast cancer following breast surgery and radiation in adult women with ductal carcinoma in situ and to reduce the incidence of breast cancer in adult women at high risk. Estrogen Agonist/Antagonist (Code: N0000175826) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Bone Density Conservation Agents (Code: D050071) Estrogen Antagonists (Code: D004965) Estrogen Receptor Modulators (Code: D020847) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Selective Estrogen Receptor Modulators (Code: D020845) estrogen antagonist (Code: CHEBI:50837) estrogen receptor modulator (Code: CHEBI:50739) bone density conservation agent (Code: CHEBI:50646) estrogen receptor antagonist (Code: CHEBI:50792) angiogenesis inhibitor (Code: CHEBI:48422) antineoplastic agent (Code: CHEBI:35610) 1977-12-30 FDA CTX
Click to view arotinolol Arotinolol is a thiopropanolamine with a tertiary butyl moiety. Arotinolol binds to the beta1-, beta2- and alpha1- adrenergic receptor sites with a very high affinity. Radioligand studies have shown that arotinolol presents a higher affinity to the beta-receptor compared to the alpha-receptor. The elucidated mechanism of action seems to be the result of a reduction in the cardiac output via the beta-blockade and an additional inhibition of the counter-regulatory increase in peripheral resistance mediated by the alpha-blockade. It is used in the treatment of high blood pressure and essential tremor. Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Neurotransmitter Agents (Code: D018377) 1985 PMDA
Click to view camazepam
Click to view lornoxicam Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10450786) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10450786) Glutathione reductase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P00390, gene: GSR, swissprot: GSHR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18608753) Lornoxicam is a non-steroidal anti-inflammatory drug (NSAID), with analgesic, anti-pyretic, anti-thrombotic and anti-inflammatory activities. Upon oral administration, lornoxicam binds to and inhibits the activity of the cyclooxygenase enzymes (COX) type 1 (COX-1) and type 2 (COX-2). Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) 2000-03 Italian Medicines Agency (AIFA)
Click to view trazodone Trazodone is a synthetic triazolopyridine derivative, antidepressant and sedative Trazodone acts as a serotonin uptake inhibitor. Preclinical studies have shown that trazodone selectively inhibits neuronal reuptake of serotonin and acts as an antagonist at 5-HT-2A/2C serotonin receptors. Trazodone is not a monoamine oxidase inhibitor and, unlike amphetamine-type drugs, does not stimulate the central nervous system. Trazodone antagonizes alpha 1-adrenergic receptors, a property which may be associated with postural hypotension. Trazodone is indicated for the treatment of major depressive disorder. A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309) Serotonin Reuptake Inhibitor (Code: N0000175696) Anti-Anxiety Agents (Code: D014151) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Uptake Inhibitors (Code: D017367) Tranquilizing Agents (Code: D014149) antidepressant (Code: CHEBI:35469) sedative (Code: CHEBI:35717) adrenergic antagonist (Code: CHEBI:37887) H1-receptor antagonist (Code: CHEBI:37955) serotonin uptake inhibitor (Code: CHEBI:50949) anxiolytic drug (Code: CHEBI:35474) 1981-12-24 FDA
Click to view exisulind Endothelin-1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25101, gene: EDNRA, swissprot: EDNRA_HUMAN) Aldose reductase (Organism: Rattus norvegicus, class: Enzyme, accessions: P07943, gene: Akr1b1, swissprot: ALDR_RAT) Mitogen-activated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P28482, gene: MAPK1, swissprot: MK01_HUMAN) inhibits K-ras-dependent cyclooxygenase-2; sulfated analog of indomethacin;; CP248 is an antineoplastic agent that fosters microtubule depolymerization Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Anticarcinogenic Agents (Code: D016588) Antineoplastic Agents (Code: D000970) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sensory System Agents (Code: D018689) SLO
Click to view medroxalol Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377)
Click to view aminoquinuride Matrix metalloproteinase-9 (Organism: Homo sapiens, class: Enzyme, accessions: P14780, gene: MMP9, swissprot: MMP9_HUMAN Botulinum neurotoxin type A (Organism: Clostridium botulinum, class: Enzyme, accessions: P10845, gene: botA, swissprot: BXA1_CLOBO Interstitial collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P03956, gene: MMP1, swissprot: MMP1_HUMAN Lethal factor (Organism: Bacillus anthracis, class: Enzyme, accessions: P15917, gene: lef, swissprot: LEF_BACAN NSC
Click to view prednylidene
Click to view meprednisone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist 1978-01-26 FDA
Click to view desoxycorticosterone acetate Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) agonist The 21-acetate derivative of desoxycorticosterone. Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Mineralocorticoids (Code: D008901) 1939-08-17 FDA
Click to view nabilone Cannabinoid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: P34972, gene: CNR2, swissprot: CNR2_HUMAN Cannabinoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P21554, gene: CNR1, swissprot: CNR1_HUMAN) agonist Cannabinoid receptor 1 (Organism: Rattus norvegicus, class: GPCR, accessions: P20272, gene: Cnr1, swissprot: CNR1_RAT Cannabinoid receptor 2 (Organism: Mus musculus, class: GPCR, accessions: P47936, gene: Cnr2, swissprot: CNR2_MOUSE cannabinol deriv; RN given refers to cpd without isomeric designation; structure Cannabinoid (Code: N0000175782) Cannabinoids (Code: N0000008010) Anti-Anxiety Agents (Code: D014151) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1985-12-26 FDA
Click to view anagestone acetate
Click to view finasteride 3-oxo-5-alpha-steroid 4-dehydrogenase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P31213, gene: SRD5A2, swissprot: S5A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020788s024lbl.pdf) 3-oxo-5-alpha-steroid 4-dehydrogenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P18405, gene: SRD5A1, swissprot: S5A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020788s024lbl.pdf) Aldo-keto reductase family 1 member D1 (Organism: Homo sapiens, class: Enzyme, accessions: P51857, gene: AKR1D1, swissprot: AK1D1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19515843) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020788s024lbl.pdf) Finasteride is a synthetic 4-azasteroid compound. Finasteride competitively binds to and inhibits steroid type II 5-alpha-reductase in the prostate, seminal vesicles, epididymides, and hair follicles as well as liver, thereby interfering with the enzymatic conversion of testosterone to 5-dihydrotestosterone (DHT) and reducing serum DHT levels. The reduction in serum DHT levels results in diminished stimulation of androgen receptors in the nuclei of prostate cells and, so, diminished prostate cell proliferation. 5-alpha Reductase Inhibitor (Code: N0000175836) 5-alpha Reductase Inhibitors (Code: D058891) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Steroid Synthesis Inhibitors (Code: D065088) Urological Agents (Code: D064804) antihyperplasia drug (Code: CHEBI:59844) androgen antagonist (Code: CHEBI:35497) 1992-06-19 FDA FIT
Click to view oxametacin Arachidonate 5-lipoxygenase (Organism: Rattus norvegicus, class: Enzyme, accessions: P12527, gene: Alox5, swissprot: LOX5_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2115586) Cyclooxygenase (Organism: Rattus norvegicus, class: Enzyme, accessions: P35355|Q63921, gene: Ptgs1|Ptgs2, swissprot: PGH1_RAT|PGH2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2115586) Oxametacin is a non-steroidal anti-inflammatory drug. Oxametacin has anti-inflammatory, analgesic and antipyretic properties comparable to those of indomethacin. The mechanism of action of oxametacin is to be related to its inhibitory activity on prostaglandin biosynthesis. Oxametacin is used in the treatment of rheumatoid arthritis, ankylosing spondyliti and gout. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) Italian Medicines Agency (AIFA)
Click to view glafenine Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT An anthranilic acid derivative with analgesic properties used for the relief of all types of pain. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) non-narcotic analgesic (Code: CHEBI:35481) non-steroidal anti-inflammatory drug (Code: CHEBI:35475)
Click to view deferasirox iron (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021882s021lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021882s030lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021882s030lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021882s030lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021882s030lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021882s030lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021882s030lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021882s030lbl.pdf) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021882s030lbl.pdf) Deferasirox is an iron chelating agent that is selective for iron (as Fe3+). It is a tridentate ligand that binds iron with high affinity in a 2:1 ratio. Although deferasirox has very low affinity for zinc and copper there are variable decreases in the serum concentration of these trace metals after the administration of deferasirox. The clinical significance of these decreases is uncertain. Deferasirox is indicated for the treatment of chronic iron overload due to blood transfusions or with non-transfusion-dependent thalassemia syndromes. Iron Chelating Activity (Code: N0000000144) Iron Chelator (Code: N0000175522) Cytochrome P450 3A4 Inducers (Code: N0000185506) Cytochrome P450 2C8 Inhibitors (Code: N0000187062) Cytochrome P450 1A2 Inhibitors (Code: N0000182138) Chelating Agents (Code: D002614) Iron Chelating Agents (Code: D007502) Sequestering Agents (Code: D064449) 2005-11-02 FDA
Click to view prasugrel P2Y purinoceptor 12 (Organism: Homo sapiens, class: GPCR, accessions: Q9H244, gene: P2RY12, swissprot: P2Y12_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022307s016lbl.pdf) Prasugrel, a thienopyridine derivative. Prasugrel is a prodrug and is rapidly metabolized to a pharmacologically active metabolite. Prasugrel is used in combination with acetylsalicylic acid to decrease the risk of myocardial infarction and stroke in patients with acute coronary syndromes. Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) platelet glycoprotein-IIb/IIIa receptor antagonist (Code: CHEBI:50433) cardiovascular drug (Code: CHEBI:35554) prodrug (Code: CHEBI:50266) Decreased Platelet Aggregation (Code: N0000008832) P2Y12 Platelet Inhibitor (Code: N0000182142) P2Y12 Receptor Antagonists (Code: N0000182143) 2009-07-10 FDA
Click to view bunazosin Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist Ribosyldihydronicotinamide dehydrogenase [quinone] (Organism: Homo sapiens, class: Enzyme, accessions: P16083, gene: NQO2, swissprot: NQO2_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Neurotransmitter Agents (Code: D018377)
Click to view clebopride D(1A) dopamine receptor (Organism: Bos taurus, class: GPCR, accessions: Q95136, gene: DRD1, swissprot: DRD1_BOVIN 5-hydroxytryptamine receptor 4 (Organism: Cavia porcellus, class: GPCR, accessions: O70528, gene: HTR4, swissprot: 5HT4R_CAVPO Serotonin 2 (5-HT2) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P30994, gene: Htr2a|Htr2b|Htr2c, swissprot: 5HT2A_RAT|5HT2B_RAT|5HT2C_RAT D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P19328|P22086|P22909, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN 5-hydroxytryptamine receptor 4 (Organism: Rattus norvegicus, class: GPCR, accessions: Q62758, gene: Htr4, swissprot: 5HT4R_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT antidopaminergic; RN given refers to parent cpd; structure Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373)
Click to view prochlorperazine 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) 5-hydroxytryptamine receptor 4 (Organism: Cavia porcellus, class: GPCR, accessions: O70528, gene: HTR4, swissprot: 5HT4R_CAVPO) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) Membrane-associated progesterone receptor component 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: P70580, gene: Pgrmc1, swissprot: PGRC1_RAT) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Pleiotropic ABC efflux transporter of multiple drugs (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Transporter, accessions: P33302, gene: PDR5, swissprot: PDR5_YEAST 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT A phenothiazine antipsychotic used principally in the treatment of NAUSEA; VOMITING; and VERTIGO. It is more likely than CHLORPROMAZINE to cause EXTRAPYRAMIDAL DISORDERS. (From Martindale, The Extra Pharmacopoeia, 30th ed, p612) Phenothiazine (Code: N0000175746) Phenothiazines (Code: N0000007544) Antiemetics (Code: D000932) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) antiemetic (Code: CHEBI:50919) dopaminergic antagonist (Code: CHEBI:48561) alpha-adrenergic antagonist (Code: CHEBI:37890) cholinergic antagonist (Code: CHEBI:48873) first generation antipsychotic (Code: CHEBI:65190) 1956-10-23 FDA P77
Click to view trospectomycin active against Neisseria gonorrhoeae; RN refers to 2R-(2alpha,4abeta,5abeta,6beta,7beta,8beta,9beta,9alpha,9aalpha,10abeta)-(9CI)-isomer
Click to view methylprednisolone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/011153s075lbl.pdf) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15329590) Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone is used in endocrine disorders (primary or secondary adrenocortical insufficiency, congenital adrenal hyperplasia, nonsuppurative thyroiditis, hypercalcemia associated with cancer), rheumatic disorders (rheumatoid arthritis, ankylosing spondylitis, bursitis, synovitis of osteoarthritis, tenosynovitis, osteoarthritis, epicondylitis, gouty arthritis), collagen diseases (systemic lupus erythematosus, systemic dermatomyositis (polymyositis), acute rheumatic carditis), dermatologic diseases (bullous dermatitis herpetiformis, erythema multiforme (Stevens-Johnson syndrome), seborrheic dermatitis, exfoliative dermatitis, mycosis fungoides, pemphigus, psoriasis), allergic states (allergic rhinitis, drug hypersensitivity reactions, serum sickness, contact dermatitis, bronchial asthma, atopic dermatitis), ophthalmic diseases (allergic corneal marginal ulcers, herpes zoster ophthalmicus, keratitis, optic neuritis, allergic conjunctivitis), respiratory diseases (sarcoidosis, berylliosis, Loeffler’s syndrome, pulmonary tuberculosis, aspiration pneumonitis), hematologic disorders ( idiopathic thrombocytopenic purpura, secondary thrombocytopenia, hemolytic anemia, erythroblastopenia, congenital (erythroid) hypoplastic anemia), neoplastic diseases (leukemias and lymphomas), edematous states, gastrointestinal diseases (ulcerative colitis, regional enteritis), acute exacerbations of multiple sclerosis, tuberculous meningitis with subarachnoid block or impending block, trichinosis with neurologic or myocardial involvement. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Neuroprotective Agents (Code: D018696) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) anti-inflammatory drug (Code: CHEBI:35472) neuroprotective agent (Code: CHEBI:63726) adrenergic agent (Code: CHEBI:37962) antiemetic (Code: CHEBI:50919) 1957-10-24 FDA
Click to view cicaprost Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) Prostacyclin receptor (Organism: Homo sapiens, class: GPCR, accessions: P43119, gene: PTGIR, swissprot: PI2R_HUMAN) Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN) Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN) Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) Prostaglandin D2 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q13258, gene: PTGDR, swissprot: PD2R_HUMAN) Prostaglandin E2 receptor EP3 subtype (Organism: Mus musculus, class: GPCR, accessions: P30557, gene: Ptger3, swissprot: PE2R3_MOUSE) agonist (Source: ) Prostacyclin receptor (Organism: Mus musculus, class: Unclassified, accessions: P43252, gene: Ptgir, swissprot: PI2R_MOUSE) agonist (Source: ) Prostaglandin E2 receptor EP2 subtype (Organism: Mus musculus, class: GPCR, accessions: Q62053, gene: Ptger2, swissprot: PE2R2_MOUSE) agonist (Source: ) Antineoplastic Agents (Code: D000970)
Click to view artisone acetate
Click to view cyproterone acetate Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1557461367867.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1557461367867.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1557461367867.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1557461367867.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1557461367867.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1557461367867.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1557461367867.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1557461367867.pdf) Cyproterone acetate acts as an antiandrogen by blocking androgen receptors. It also has progestogenic activity. It shows competitive binding with dihydrotestosterone at androgen receptor sites. It is used in the treatment of hypersexuality in males, as a palliative in prostatic carcinoma, and, in combination with estrogen, for the therapy of severe acne and hirsutism in females. Also cyproterone acetate is widely used as a contraceptive, however its usage is associated with liver toxicity and clots formation. Androgen Antagonists (Code: D000726) Antineoplastic Agents (Code: D000970) Contraceptive Agents (Code: D003270) Contraceptive Agents, Male (Code: D003272) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Reproductive Control Agents (Code: D012102) androgen antagonist (Code: CHEBI:35497) 1974-01-01 YEAR INTRODUCED CA4
Click to view bromhexine Bromhexine is a synthetic derivative of the herbal active ingredient vasicine. Bromhexine is used as a mucolytic to break down mucus and help clear the chest in conditions accompanied by excessive mucus secretions, such as in the common cold, influenza, infections of the respiratory tract or in other conditions where excess mucus is produced. Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) mucolytic (Code: CHEBI:77034) 1966-08-26 Austrian Medicines and Medical Devices Agency
Click to view hydroxyzine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11809864) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00046272.PDF) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00046272.PDF) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9616188) Hydroxyzine is a piperazine antihistamine. Hydroxyzine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. Hydroxyzine is used to treat histamine-mediated pruritus or pruritus due to allergy, nausea and vomiting, and, in combination with an opiate agonist, anxiolytic pain. Hydroxyzine is also used as a perioperative sedative and anxiolytic and to manage acute alcohol withdrawal. Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) H1-receptor antagonist (Code: CHEBI:37955) anxiolytic drug (Code: CHEBI:35474) dermatologic drug (Code: CHEBI:50177) antipruritic drug (Code: CHEBI:59683) Antihistamine (Code: N0000175750) Histamine Receptor Antagonists (Code: N0000000207) 1956-04-12 FDA
Click to view theodrenaline Theodrenaline is a theophylline derivative. It is used in combination with cafedrinefor the treatment of hypotensive states during anesthesia and in emergency medicine. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317)
Click to view gatifloxacin DNA topoisomerase 4 subunit A (Organism: Staphylococcus aureus, class: Enzyme, accessions: P0C1U9, gene: parC, swissprot: PARC_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021493s011lbl.pdf) DNA gyrase (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: P0A4L9|P72524, gene: gyrA|gyrB, swissprot: GYRA_STRPN|GYRB_STRPN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021493s011lbl.pdf) DNA topoisomerase 4 (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: P72525|Q59961, gene: parC|parE, swissprot: PARC_STRPN|PARE_STRPN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021493s011lbl.pdf) DNA gyrase (Organism: Staphylococcus epidermidis (strain ATCC 35984 / RP62A), class: Enzyme, accessions: Q5HK04|Q5HK03, gene: gyrA|gyrB, swissprot: GYRA_STAEQ|GYRB_STAEQ) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021493s011lbl.pdf) Gatifloxacin is a quinolone antimicrobial topical ophthalmic solution for the treatment of bacterial conjunctivitis. Gatifloxacin is an 8-methoxyfluoroquinolone with a 3-methylpiperazinyl substituent at C7. The antibacterial action of gatifloxacin results from inhibition of DNA gyrase and topoisomerase IV. Gatifloxacin has been shown to be active against Corynebacterium propinquum, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus mitis group, Streptococcus pneumoniae, and Haemophilus influenzae. Quinolone Antimicrobial (Code: N0000175937) Quinolones (Code: N0000007606) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antiinfective agent (Code: CHEBI:35441) 2003-03-28 FDA GFN
Click to view azidocillin antibiotic similir to ampicillin; minor descriptor (75-86); on line & INDEX MEDICUS search PENICILLIN G/AA (75-86); RN given refers to (2S-(2alpha,5alpha,6beta(S*))-isomer)
Click to view pipamperone 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: ) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Tranquilizing Agents (Code: D014149) serotonergic antagonist (Code: CHEBI:48279) dopaminergic antagonist (Code: CHEBI:48561) first generation antipsychotic (Code: CHEBI:65190)
Click to view tiagabine Sodium- and chloride-dependent GABA transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P23978, gene: Slc6a1, swissprot: SC6A1_RAT Sodium- and chloride-dependent GABA transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P30531, gene: SLC6A1, swissprot: SC6A1_HUMAN) inhibitor Sodium- and chloride-dependent GABA transporter 1 (Organism: Mus musculus, class: Transporter, accessions: P31648, gene: Slc6a1, swissprot: SC6A1_MOUSE Sodium- and chloride-dependent betaine transporter (Organism: Mus musculus, class: Unclassified, accessions: P31651, gene: Slc6a12, swissprot: S6A12_MOUSE The precise mechanism by which tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to block GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells. Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) GABA Agents (Code: D018682) GABA Agonists (Code: D018755) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) GABA reuptake inhibitor (Code: CHEBI:85384) anticonvulsant (Code: CHEBI:35623) 1997-09-30 FDA
Click to view haloperidol D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23332346) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14611858) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25126833) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18448342) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22028316) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22028316) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22028316) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Potassium voltage-gated channel subfamily H member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O95259, gene: KCNH1, swissprot: KCNH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12522086) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9298538) Kir3.1/Kir3.2 (Organism: Homo sapiens, class: Ion channel, accessions: P48549|P48051, gene: KCNJ3|KCNJ6, swissprot: KCNJ3_HUMAN|KCNJ6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10780978) Kir3.1/Kir3.4 (Organism: Homo sapiens, class: Ion channel, accessions: P48549|P48544, gene: KCNJ3|KCNJ5, swissprot: KCNJ3_HUMAN|KCNJ5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10780978) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9067310) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1826762) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1826762) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15102927) Glutamate receptor ionotropic, NMDA 2B (Organism: Homo sapiens, class: Ion channel, accessions: Q13224, gene: GRIN2B, swissprot: NMDE2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17588330) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9140699) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9140699) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11717183) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11717183) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11717183) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11717183) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11717183) Haloperidol is a butyrophenone derivative with antipsychotic properties that has been considered particularly effective in the management of hyperactivity, agitation, and mania. Haloperidol is an effective neuroleptic and also possesses antiemetic properties; it has a marked tendency to provoke extrapyramidal effects and has relatively weak alphaadrenolytic properties. It may also exhibit hypothermic and anorexiant effects and potentiates the reaction of barbiturates, general anesthetics and other CNS depressant drugs. The mechanism of action of haloperidol has not been entirely elucidated, but has been attributed to the inhibition of the transport mechanism of cerebral monoamines, particularly by blocking the impulse transmission in dopaminergic neurons. Haloperidol is indicated in the management of manifestations of acute and chronic psychosis (including schizophrenia and manic states) and aggressive and agitated behavior in patients with chronic brain syndrome and mental retardation and in the symptomatic control Tourette’s syndrome. Typical Antipsychotic (Code: N0000180182) Anti-Dyskinesia Agents (Code: D018726) Antiemetics (Code: D000932) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) dopaminergic antagonist (Code: CHEBI:48561) antidyskinesia agent (Code: CHEBI:66956) antiemetic (Code: CHEBI:50919) first generation antipsychotic (Code: CHEBI:65190) serotonergic antagonist (Code: CHEBI:48279) 1967-04-12 FDA GMJ
Click to view riboflavin Riboflavin kinase (Organism: Homo sapiens, class: Kinase, accessions: Q969G6, gene: RFK, swissprot: RIFK_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21308351) Riboflavin (vitamin B2) is an essential human nutrient that is a heat-stable and water-soluble flavin belonging to the vitamin B family. Riboflavin is a precursor of the coenzymes flavin mononucleotide (FMN) and flavin adenine dinucleotide (FAD). These coenzymes are of vital importance in normal tissue respiration, pyridoxine activation, tryptophan to niacin conversion, fat, carbohydrate, and protein metabolism, and glutathione reductase mediated detoxification. Riboflavin may also be involved in maintaining erythrocyte integrity. This vitamin is essential for healthy skin, nails, and hair. Dermatologic Agents (Code: D003879) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) photosensitizing agent (Code: CHEBI:47868) food colouring (Code: CHEBI:77182) B vitamin (Code: CHEBI:75769) 1953-02-20 FDA RBF
Click to view picotamide Picotamide is an antiplatelet drug with dual mechanism of action it inhibits thromboxane A2 synthase and antagonizes the pharmacological responses mediated by thromboxane A2 receptor. Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975)
Click to view remifentanil Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist Remifentanil is a mu-opioid agonist with rapid onset and peak effect, and short duration of action. Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) mu-opioid receptor agonist (Code: CHEBI:55322) opioid analgesic (Code: CHEBI:35482) intravenous anaesthetic (Code: CHEBI:38877) sedative (Code: CHEBI:35717) 1996-07-12 FDA
Click to view enalapril Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10052994) Solute carrier family 22 member 6 (Organism: Mus musculus, class: Transporter, accessions: Q8VC69, gene: Slc22a6, swissprot: S22A6_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9880528) Solute carrier family 22 member 8 (Organism: Mus musculus, class: Transporter, accessions: O88909, gene: Slc22a8, swissprot: S22A8_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15100168) Solute carrier family 22 member 7 (Organism: Mus musculus, class: Transporter, accessions: Q91WU2, gene: Slc22a7, swissprot: S22A7_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9650585) Solute carrier organic anion transporter family member 1A1 (Organism: Rattus norvegicus, class: Transporter, accessions: P46720, gene: Slco1a1, swissprot: SO1A1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9794920) Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2544729) Enalapril, after hydrolysis to enalaprilat, inhibits angiotensin-converting enzyme (ACE) in human subjects and animals. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex. Inhibition of ACE results in decreased plasma angiotensin II, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Antihypertensive Heart failure treatment Angiotensin-converting enzyme inhibitor Intestinal peptide-proton cotransporter inhibitor 1985-12-24 FDA
Click to view fluorometholone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) A glucocorticoid employed, usually as eye drops, in the treatment of allergic and inflammatory conditions of the eye. It has also been used topically in the treatment of various skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p732) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Allergic Agents (Code: D018926) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) anti-inflammatory drug (Code: CHEBI:35472) 1972-01-12 FDA
Click to view fluocortolone A glucocorticoid with anti-inflammatory activity used topically for various skin disorders. Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view desoximetasone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Annexin A1 (Organism: Homo sapiens, class: Cytosolic other, accessions: P04083, gene: ANXA1, swissprot: ANXA1_HUMAN) A topical anti-inflammatory glucocorticoid used in DERMATOSES, skin allergies, PSORIASIS, etc. Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) anti-inflammatory drug (Code: CHEBI:35472) antipruritic drug (Code: CHEBI:59683) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) 1977-02-28 FDA
Click to view estradiol benzoate Estradiol benzoate is a pro-drug ester of Estradiol, a naturally occurring hormone that circulates endogenously within the human body. (See: estradiol) xenoestrogen (Code: CHEBI:76988) 1997-05-06 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view hexcarbacholine
Click to view lauroguadine
Click to view flutazolam
Click to view haloxazolam Haloxazolam is a GABA-A receptor agonist. It is used for the treatment of insomnia. 1981-01-01 PMDA
Click to view pentolonium Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P30926|P32297, gene: CHRNA3|CHRNB4, swissprot: ACHA3_HUMAN|ACHB4_HUMAN) antagonist (Source: ) Neuronal acetylcholine receptor subunit alpha-10 (Organism: Homo sapiens, class: Ion channel, accessions: Q9GZZ6, gene: CHRNA10, swissprot: ACH10_HUMAN) A nicotinic antagonist that has been used as a ganglionic blocking agent in hypertension. Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Ganglionic Blockers (Code: D005730) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) FDA
Click to view morazone
Click to view sulfinalol
Click to view domitroban Thromboxane A2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P21731, gene: TBXA2R, swissprot: TA2R_HUMAN) antagonist (Source: ) Thromboxane A2 receptor (Organism: Mus musculus, class: Unclassified, accessions: P30987, gene: Tbxa2r, swissprot: TA2R_MOUSE) antagonist (Source: )
Click to view famprofazone Nuclear receptor subfamily 2 group E member 1 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q9Y466, gene: NR2E1, swissprot: NR2E1_HUMAN)
Click to view ronifibrate
Click to view etoperidone Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN)
Click to view ambroxol Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10659952) Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. The substance is a mucoactive drug with several properties including secretolytic and secretomotoric actions that restore the physiological clearance mechanisms of the respiratory tract which play an important role in the body’s natural defence mechanisms. It stimulates synthesis and release of surfactant by type II pneumocytes. Surfactants acts as an anti-glue factor by reducing the adhesion of mucus to the bronchial wall, in improving its transport and in providing protection against infection and irritating agents. Ambroxol is indicated for the treatment of all forms of tracheobronchitis, emphysema with bronchitis pneumoconiosis, chronic inflammatory pulmonary conditions, bronchiectasis, bronchitis with bronchospasm asthma. Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) 1982-03-03 Italian Medicines Agency (AIFA)
Click to view mefloquine Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18406614) Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18406614) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3878759) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3878759) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22328583) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22328583) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11561091) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27045516) Voltage-dependent calcium channel gamma-1 subunit (Organism: Homo sapiens, class: Ion channel, accessions: Q06432, gene: CACNG1, swissprot: CCG1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/29208420) Mefloquine is a quinoline derivative used for the prevention and therapy of P. falciparum malaria. Mefloquine is a chiral molecule. According to some research, the (+) enantiomer is more effective in treating malaria, and the (-) enantiomer specifically binds to adenosine receptors in the central nervous system, which may explain some of its psychotropic effects. Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) antimalarial (Code: CHEBI:38068) 1989-05-02 FDA
Click to view carbenicillin Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10411577) Peptidoglycan D,D-transpeptidase FtsI (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: G3XD46, gene: ftsI, swissprot: FTSI_PSEAE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20974151) Broad-spectrum semisynthetic penicillin derivative used parenterally. It is susceptible to gastric juice and penicillinase and may damage platelet function. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) Penicillin-class Antibacterial (Code: N0000175497) Penicillins (Code: N0000011281) FDA
Click to view fluprednisolone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist A synthetic glucocorticoid with anti-inflammatory properties. Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1982-12-07 FDA
Click to view propicillin major descriptor (64-84); on-line search PENICILLIN, PHENOXYMETHYL/AA (64-84); Index Medicus search PROPICILLIN (64-84); RN given refers to parent cpd(2S-(2alpha,5alpha,6beta))-isomer Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view doxapram Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Potassium channel subfamily K member 3 (Organism: Homo sapiens, class: Ion channel, accessions: O14649, gene: KCNK3, swissprot: KCNK3_HUMAN) blocker Potassium channel subfamily K member 9 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NPC2, gene: KCNK9, swissprot: KCNK9_HUMAN) blocker A central respiratory stimulant with a brief duration of action. (From Martindale, The Extra Pharmocopoeia, 30th ed, p1225) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Respiratory System Agents (Code: D019141) central nervous system stimulant (Code: CHEBI:35337) Increased Medullary Respiratory Drive (Code: N0000009393) Respiratory Stimulant (Code: N0000175716) 1965-06-23 FDA
Click to view cyclopenthiazide Thiazide diuretic also used as an antihypertensive agent. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993)
Click to view scarlet red Coloring Agents (Code: D004396)
Click to view droperidol D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2527092) A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593) Dopamine D2 Antagonists (Code: N0000175799) Dopamine-2 Receptor Antagonist (Code: N0000175800) Adjuvants, Anesthesia (Code: D000759) Antiemetics (Code: D000932) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Dopamine D2 Receptor Antagonists (Code: D065127) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) antiemetic (Code: CHEBI:50919) dopaminergic antagonist (Code: CHEBI:48561) anaesthesia adjuvant (Code: CHEBI:60807) first generation antipsychotic (Code: CHEBI:65190) 1970-06-11 FDA
Click to view donepezil Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020690s042,021720s014,022568s011lbl.pdf) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25257911) is the hydrochloride salt of a piperidine derivative with neurocognitive-enhancing activity. Donepezil reversibly inhibits acetylcholinesterase, thereby blocking the hydrolysis of the neurotransmitter acetylcholine and, consequently, increasing its activity. This agent may improve neurocognitive function in Alzheimer's disease, reduce sedation associated with opioid treatment of cancer pain, and improve neurocognitive function in patients who have received radiation therapy for primary brain tumors or brain metastases. Cholinesterase Inhibitor (Code: N0000175723) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Nootropic Agents (Code: D018697) nootropic agent (Code: CHEBI:66980) 1996-11-25 FDA E20
Click to view celiprolol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT A cardioselective beta-1 adrenergic antagonist that has intrinsic symopathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566) Vasodilator Agents (Code: D014665) 1982-01-01 YEAR INTRODUCED
Click to view etomidoline has myolytic activity on extravascular smooth muscle
Click to view oxypertine
Click to view coumetarol
Click to view meticillin Beta-lactam-inducible penicillin-binding protein (Organism: Staphylococcus aureus, class: Enzyme, accessions: P07944, gene: pbp, swissprot: PBP_STAAU) NH(3)-dependent NAD(+) synthetase (Organism: Escherichia coli (strain K12), class: Unclassified, accessions: P18843, gene: nadE, swissprot: NADE_ECOLI) Penicillin-binding protein (Organism: Staphylococcus aureus, class: Enzyme, accessions: P72355|Q53707|Q53725|Q53729|Q9XDB3, gene: PBP2|mecA|pbp4|pbpA|pbpF, swissprot: P72355_STAAU|Q53707_STAAU|Q53725_STAAU|Q53729_STAAU|Q9XDB3_STAAU) inhibitor One of the PENICILLINS which is resistant to PENICILLINASE but susceptible to a penicillin-binding protein. It is inactivated by gastric acid so administered by injection. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) FDA MII
Click to view fludrocortisone acetate Fludrocortisone acetate is the acetate salt of a synthetic fluorinated corticosteroid with antiinflammatory and antiallergic activities. (See: fludrocortisone) Anti-Inflammatory Agents (Code: D000893) 1955-08-18 FDA
Click to view amosulalol Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377)
Click to view bopindolol 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Neurotransmitter Agents (Code: D018377) 1985-01-01 YEAR INTRODUCED
Click to view ecabet Anti-Infective Agents (Code: D000890) Anti-Ulcer Agents (Code: D000897) Anticarcinogenic Agents (Code: D016588) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Protease Inhibitors (Code: D011480) Protective Agents (Code: D020011)
Click to view limaprost Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN) agonist (Source: http://www.kegg.jp/entry/D02722) Limaprost exerts potent effects on vasodilation, increase of blood flow and inhibition of platelet aggregation, and thereby has proven clinical effects on various ischemic symptoms such as ulcer, pain and feeling of coldness associated with thromboangiitis obliterans. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) PMDA
Click to view eprazinone Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) mucolytic (Code: CHEBI:77034)
Click to view trichlormethiazide Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Thiopurine S-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P51580, gene: TPMT, swissprot: TPMT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8866635) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14610216) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14610216) Trichloromethiazide is belong to the class of thiazides which promote water loss from the body. Trichlormethiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule. This results in excretion of sodium, chloride, and water and, hence, diuresis. Trichloromethiazide is indicated as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy. Trichloromethiazide has also been found useful in edema due to various forms of renal dysfunction such as nephrotic syndrome, acute glomer-ulonephritis, and chronic renal failure. Trichloromethiazide is also indicated in the management of hypertension either as the sole therapeutic agent or to enhance the effectiveness of other antihypertensive drugs in the more severe forms of hypertension. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) diuretic (Code: CHEBI:35498) antihypertensive agent (Code: CHEBI:35674) 1960-03-09 FDA TRU
Click to view chlorotrianisene Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) modulator A powerful synthetic, non-steroidal estrogen. Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Estrogens (Code: D004967) Estrogens, Non-Steroidal (Code: D004968) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) estrogen receptor modulator (Code: CHEBI:50739) antineoplastic agent (Code: CHEBI:35610) xenoestrogen (Code: CHEBI:76988) FDA
Click to view celecoxib Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020998s033,021156s003lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020998s033,021156s003lbl.pdf) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20605094) Carbonic anhydrase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P53615, gene: NCE103, swissprot: CAN_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19124253) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase (Organism: Methanosarcina thermophila, class: Enzyme, accessions: P40881, gene: None, swissprot: CAH_METTE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15546717) [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial (Organism: Homo sapiens, class: Kinase, accessions: Q15118, gene: PDK1, swissprot: PDK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15205346) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19846301) Delta carbonic anhydrase (Organism: Thalassiosira weissflogii, class: Unclassified, accessions: Q5U9J1, gene: ca1, swissprot: Q5U9J1_THAWE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24314394) Celecoxib is a nonsteroidal anti-inflammatory drug that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of celecoxib is believed to be due to inhibition of prostaglandin synthesis, primarily via inhibition of cyclooxygenase-2, and at therapeutic concentrations in humans, celecoxib does not inhibit the cyclooxygenase-1 isoenzyme. In animal colon tumor models, celecoxib reduced the incidence and multiplicity of tumors. Celecoxib is indicated for the treatment osteoarthritis, rheumatoid arthritis, juvenile rheumatoid arthritis, ankylosing spondylitis, acute pain and primary dysmenorrhea. Celecoxib has been linked to rare instances of idiosyncratic drug induced liver disease. Nonsteroidal Anti-inflammatory Compounds (Code: N0000175721) Nonsteroidal Anti-inflammatory Drug (Code: N0000175722) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase 2 Inhibitors (Code: D052246) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) non-narcotic analgesic (Code: CHEBI:35481) 1998-12-31 FDA CEL
Click to view fendosal Plasminogen activator inhibitor 1 (Organism: Homo sapiens, class: Secreted, accessions: P05121, gene: SERPINE1, swissprot: PAI1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/12152654) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481)
Click to view benperidol Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) A butyrophenone with general properties similar to those of HALOPERIDOL. It has been used in the treatment of aberrant sexual behavior. (From Martindale, The Extra Pharmacopoeia, 30th ed, p567) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1965-01-01 YEAR INTRODUCED
Click to view micinicate
Click to view econazole Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Cannabinoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P21554, gene: CNR1, swissprot: CNR1_HUMAN) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Adenosine receptor A1 (Organism: Homo sapiens, class: GPCR, accessions: P30542, gene: ADORA1, swissprot: AA1R_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) Receptor tyrosine-protein kinase erbB-2 (Organism: Homo sapiens, class: Kinase, accessions: P04626, gene: ERBB2, swissprot: ERBB2_HUMAN) Thromboxane-A synthase (Organism: Homo sapiens, class: Enzyme, accessions: P24557, gene: TBXAS1, swissprot: THAS_HUMAN) Matrix metalloproteinase-9 (Organism: Homo sapiens, class: Enzyme, accessions: P14780, gene: MMP9, swissprot: MMP9_HUMAN) Substance-K receptor (Organism: Homo sapiens, class: GPCR, accessions: P21452, gene: TACR2, swissprot: NK2R_HUMAN) Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) Melanocortin receptor 5 (Organism: Homo sapiens, class: GPCR, accessions: P33032, gene: MC5R, swissprot: MC5R_HUMAN) Melanocortin receptor 3 (Organism: Homo sapiens, class: GPCR, accessions: P41968, gene: MC3R, swissprot: MC3R_HUMAN) Neuropeptide Y receptor type 2 (Organism: Homo sapiens, class: GPCR, accessions: P49146, gene: NPY2R, swissprot: NPY2R_HUMAN) Membrane-associated progesterone receptor component 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: P70580, gene: Pgrmc1, swissprot: PGRC1_RAT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Beta-lactamase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P00811, gene: ampC, swissprot: AMPC_ECOLI Lanosterol 14-alpha demethylase (Organism: Homo sapiens, class: Enzyme, accessions: Q16850, gene: CYP51A1, swissprot: CP51A_HUMAN Lanosterol 14-alpha demethylase (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPP9, gene: cyp51, swissprot: CP51_MYCTU Malate dehydrogenase cytoplasmic (Organism: Homo sapiens, class: Enzyme, accessions: P40925, gene: MDH1, swissprot: MDHC_HUMAN Indoleamine 2,3-dioxygenase 1 (Organism: Mus musculus, class: Enzyme, accessions: P28776, gene: Ido1, swissprot: I23O1_MOUSE Steroid 17-alpha-hydroxylase/17,20 lyase (Organism: Homo sapiens, class: Enzyme, accessions: P05093, gene: CYP17A1, swissprot: CP17A_HUMAN Indoleamine 2,3-dioxygenase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q8R0V5, gene: Ido2, swissprot: I23O2_MOUSE Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor Indoleamine 2,3-dioxygenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P14902, gene: IDO1, swissprot: I23O1_HUMAN 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT An imidazole derivative that is commonly used as a topical antifungal agent. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) 14-alpha Demethylase Inhibitors (Code: D058888) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) 1982-12-23 FDA ECL
ECN
Click to view azelastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020114s028lbl.pdf) Phospholipase A2 (Organism: Homo sapiens, class: Enzyme, accessions: P04054, gene: PLA2G1B, swissprot: PA21B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8630722) Leukotriene C4 synthase (Organism: Homo sapiens, class: Enzyme, accessions: Q16873, gene: LTC4S, swissprot: LTC4S_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8630722) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10570018) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10570018) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10570018) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10383922) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10383922) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10383922) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11231118) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22985961) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22985961) Histamine H3 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5N1, gene: HRH3, swissprot: HRH3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22985961) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22985961) Azelastine hydrochloride, a phthalazinone derivative, exhibits histamine H1-receptor antagonist activity in isolated tissues, animal models, and humans. Azelastine Hydrochloride is administered as a racemic mixture with no difference in pharmacologic activity noted between the enantiomers in in vitro studies. The major metabolite, desmethylazelastine, also possesses H1-receptor antagonist activity. Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Antagonist (Code: N0000175587) Anti-Allergic Agents (Code: D018926) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Enzyme Inhibitors (Code: D004791) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Lipoxygenase Inhibitors (Code: D016859) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) anti-asthmatic drug (Code: CHEBI:49167) bronchodilator agent (Code: CHEBI:35523) platelet aggregation inhibitor (Code: CHEBI:50427) 1996-11-01 FDA
Click to view mebutizide Mebutizide is a benzothiadiazinesulfonamide derivative belonging to the class of the thiazide diuretics.
Click to view tofisopam cGMP-dependent 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O00408, gene: PDE2A, swissprot: PDE2A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20967473) cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Organism: Homo sapiens, class: Enzyme, accessions: Q14432, gene: PDE3A, swissprot: PDE3A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20967473) cGMP-inhibited 3',5'-cyclic phosphodiesterase B (Organism: Homo sapiens, class: Enzyme, accessions: Q13370, gene: PDE3B, swissprot: PDE3B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20967473) cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20967473) cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y233, gene: PDE10A, swissprot: PDE10_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20967473) Tofisopam is a benzodiazepine derivative. In contrast to classical 1,4-benzodiazepines, the compound does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor and its psychopharmacological profile differs from such compounds. Tofisopam is used for for the treatment of anxiety disorders. Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1988-11-29 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view tetrofosmin Tetrofosmin is a diagnostic agent used to assess areas of reversible myocardial ischemia in the presence or absence of infracted myocardium and is also used to assess ventricular function. When Tetrofosmin is reconstituted with Tc99m pertechnetate, a complex of Tc99m Tetrofosmin is formed and is the active ingredient of the reconstituted product. When administered intravenously, Tc99m Tetrofosmin shows rapid myocardial uptake and its distribution follows a linear relationship with coronary blood flow. Tc99m Tetrofosmin is a lipophilic agent that is taken up by the mitochondria of myocardial cells by passive diffusion and appears to accumulate in viable myocardial tissue. FDA
Click to view alpiropride Alpiropride is a sulpiride-like dopamine antagonist. Alpiropride was used for the treatment of migraine.
Click to view eletriptan 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021016s021s023s024s027lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12814962) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12814962) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12814962) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12814962) Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors. Migraines are likely due to local cranial vasodilatation and/or to the release of sensory neuropeptides (vasoactive intestinal peptide, substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of Eletriptan for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. Serotonin 1b Receptor Agonists (Code: N0000175763) Serotonin 1d Receptor Agonists (Code: N0000175764) Serotonin-1b and Serotonin-1d Receptor Agonist (Code: N0000175765) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) serotonergic agonist (Code: CHEBI:35941) vasoconstrictor agent (Code: CHEBI:50514) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) 2002-12-26 FDA
Click to view pyrvinium Casein kinase I isoform alpha (Organism: Homo sapiens, class: Kinase, accessions: P48729, gene: CSNK1A1, swissprot: KC1A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20890287) Pyrvinium (Viprynium) is an anthelmintic effective for pinworms. Pyrvinium has being shown to be a potent inhibitor of Wnt signaling.Several forms of pyrvinium have been prepared with variable counter anions, such as halides, tosylate, triflate and pamoate. Pyrvinium is used in the treatment of enterobiasis caused by Enterobius vermicularis (pinworm). Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) 1956 FDA
Click to view teflurane Teflurane is a halogenated ethane and has a structural formula which is very similar to halothane. Teflurane is a non-flammable anaesthetic. Teflurane is not available today because it produce cardiac arrhytmias in therapeutic concentration.
Click to view misoprostol Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Prostaglandin E2 receptor EP2 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43116, gene: PTGER2, swissprot: PE2R2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10634944) Misoprostol is a synthetic analog of natural prostaglandin E1. It produces a dose-related inhibition of gastric acid and pepsin secretion, and enhances mucosal resistance to injury. It is an effective anti-ulcer agent and also has oxytocic properties. Abortifacient Agents (Code: D000019) Abortifacient Agents, Nonsteroidal (Code: D000020) Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102) anti-ulcer drug (Code: CHEBI:49201) oxytocic (Code: CHEBI:36063) abortifacient (Code: CHEBI:50691) Prostaglandin E1 Analog (Code: N0000175785) Prostaglandins E, Synthetic (Code: N0000007710) 1988-12-27 FDA
Click to view mefruside A benzene-sulfonamide-furan. It is used as a diuretic that affects the concentrating ability of the KIDNEY, increases SODIUM CHLORIDE excretion, but may not spare POTASSIUM. It inhibits CARBONIC ANHYDRASES and may increase the blood URIC ACID level. Diuretics (Code: D004232) Natriuretic Agents (Code: D045283)
Click to view loratadine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2000/20641s7lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15601807) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11502723) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11502723) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11454724) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12873512) Bile acid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q96RI1, gene: NR1H4, swissprot: NR1H4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23688559) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23688559) Sodium-dependent neutral amino acid transporter B(0)AT2 (Organism: Homo sapiens, class: Transporter, accessions: Q9H2J7, gene: SLC6A15, swissprot: S6A15_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25318072) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23812503) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23812503) Loratadine is a piperidine histamine H1-receptor antagonist with anti-allergic properties and without sedative effects. Loratadine blocks the H1 histamine receptor and prevents the symptoms that are caused by histamine activity on capillaries, bronchial smooth muscle, and gastrointestinal smooth muscle, including vasodilatation, increased capillary permeability, bronchoconstriction, and spasmodic contraction of gastrointestinal smooth muscle. Anti-Allergic Agents (Code: D018926) Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Neurotransmitter Agents (Code: D018377) 1993-04-12 FDA
Click to view pantoprazole Potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P20648|P51164, gene: ATP4A|ATP4B, swissprot: ATP4A_HUMAN|ATP4B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020987s050,022020s012lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020987s050,022020s012lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020987s050,022020s012lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020987s050,022020s012lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020987s050,022020s012lbl.pdf) N(G),N(G)-dimethylarginine dimethylaminohydrolase 1 (Organism: Homo sapiens, class: Enzyme, accessions: O94760, gene: DDAH1, swissprot: DDAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28588208) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11770010) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11770010) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25239859) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19076159) ATP-binding cassette sub-family G member 2 (Organism: Mus musculus, class: Transporter, accessions: Q7TMS5, gene: Abcg2, swissprot: ABCG2_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15313923) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Indoleamine 2,3-dioxygenase 1 (Organism: Mus musculus, class: Enzyme, accessions: P28776, gene: Ido1, swissprot: I23O1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Indoleamine 2,3-dioxygenase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q8R0V5, gene: Ido2, swissprot: I23O2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Pantoprazole is a proton pump inhibitor that suppresses the final step in gastric acid production by covalently binding to the (H+, K+)-ATPase enzyme system at the secretory surface of the gastric parietal cell. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. The binding to the (H+, K+)-ATPase results in a duration of antisecretory effect that persists longer than 24 hours. Pantoprazole is used for the treatment of gastroesophageal reflux disease, for gastric protection to prevent recurrence of stomach ulcers or gastric damage from chronic use of NSAIDs, for the treatment of pathological hypersecretory conditions including Zollinger-Ellison Syndrome and also in combination with antibiotics to treat ulcers caused by Helicobacter pylori. Anti-Ulcer Agents (Code: D000897) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Proton Pump Inhibitors (Code: D054328) anti-ulcer drug (Code: CHEBI:49201) Proton Pump Inhibitor (Code: N0000175525) 2000-02-02 FDA
Click to view ceftizoxime Penicillin-binding protein 1A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918, gene: mrcA, swissprot: PBPA_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7018389) Peptidoglycan D,D-transpeptidase FtsI (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD68, gene: ftsI, swissprot: FTSI_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7018389) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15618677) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16098483) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16098483) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17344354) Ceftizoxime is a semisynthetic, broad-spectrum, beta-lactamase-resistant, third-generation cephalosporin with antibacterial activity. The bactericidal action of ceftizoxime results from inhibition of cell­wall synthesis. Ceftizoxime is highly resistant to a broad spectrum of beta­lactamases (penicillinase and cephalosporinase), including Richmond types I, II, III, TEM, and IV, produced by both aerobic and anaerobic gram­positive and gram­negative organisms. Ceftizoxime has been shown to be active against Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Enterobacter spp., Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Morganella morganii, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Pseudomonas aeruginosa, Serratia marcescens, Bacteroides spp., Peptococcus spp., Peptostreptococcus spp. Ceftizoxime is usually inactive against most strains of Enterococcus faecalis. Ceftizoxime is used for the treatment of Lower Respiratory Tract Infections, Urinary Tract Infections, Gonorrhea, Gynecological Infections, Intra­Abdominal Infections, Septicemia, Skin and Skin Structure Infections, Bone and Joint Infections, Meningitis. Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1983-09-15 FDA
Click to view veralipride used in treatment of menopausal disorders; RN given refers to parent cpd Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view meropenem Penicillin-binding protein 2 (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD65, gene: mrdA, swissprot: PBP2_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050706s041lbl.pdf) Peptidoglycan D,D-transpeptidase FtsI (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD68, gene: ftsI, swissprot: FTSI_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050706s041lbl.pdf) D-alanyl-D-alanine carboxypeptidase DacB (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P24228, gene: dacB, swissprot: DACB_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050706s041lbl.pdf) Peptidoglycan D,D-transpeptidase FtsI (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: G3XD46, gene: ftsI, swissprot: FTSI_PSEAE) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050706s041lbl.pdf) The bactericidal activity of meropenem results from the inhibition of cell wall synthesis. Meropenem penetrates the cell wall of most gram-positive and gram-negative bacteria to bind penicillin-binding-protein (PBP) targets. Meropenem binds to PBPs 2, 3 and 4 of Escherichia coli and Pseudomonas aeruginosa; and PBPs 1, 2 and 4 of Staphylococcus aureus. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) drug allergen (Code: CHEBI:88188) antibacterial drug (Code: CHEBI:36047) 1996-06-21 FDA MEM
Click to view tandospirone 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Tranquilizing Agents (Code: D014149)
Click to view quetiapine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8935801) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8935801) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8935801) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18059438) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020639s060s063lbl.pdf) Quetiapine is a dibenzothiazepine and antipsychotic agent that targets the serotonin 5-ht2 receptor; histamine h1 receptor, adrenergic alpha1 and alpha2 receptors, as well as the dopamine d1 receptor and dopamine d2 receptor. It is used in the treatment of schizophrenia; bipolar disorder and depressive disorder. Atypical Antipsychotic (Code: N0000175430) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) serotonergic antagonist (Code: CHEBI:48279) dopaminergic antagonist (Code: CHEBI:48561) histamine antagonist (Code: CHEBI:37956) adrenergic antagonist (Code: CHEBI:37887) second generation antipsychotic (Code: CHEBI:65191) 1997-09-26 FDA
Click to view brinzolamide Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020816s019lbl.pdf) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase (Organism: Helicobacter pylori (strain ATCC 700392 / 26695), class: Enzyme, accessions: O24855, gene: cynT, swissprot: CYNT_HELPY) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540563) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Brinzolamide is a carbonic anhydrase inhibitor. brinzolamide inhibits aqueous humor formation and reduces elevated intraocular pressure. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss. Brinzolamide is indicated for in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. Carbonic Anhydrase Inhibitor (Code: N0000175517) Carbonic Anhydrase Inhibitors (Code: D002257) Enzyme Inhibitors (Code: D004791) antiglaucoma drug (Code: CHEBI:39456) 1998-04-01 FDA BZ1
Click to view mebrofenin 99mTc-mebrofenin: Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21163547) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21163547) Mebrofenin is an iminodiacetic acid (HIDA) derivative with no known pharmacologic action at the recommended doses. Mebrofenin, which is bound to 99mTechnetium, is used as a diagnostic radiopharmaceutical composed for imaging of the liver and gallbladder. Liver and gallbladder imaging is enabled through attachment to mebrofenin as this molecule has high hepatic uptake and fast biliary excretion, resulting in improved hepatic imaging. 1987-01-21 FDA
Click to view naftidrofuryl 5-hydroxytryptamine receptor 2C (Organism: Mus musculus, class: GPCR, accessions: P34968, gene: Htr2c, swissprot: 5HT2C_MOUSE) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1478263) 5-hydroxytryptamine receptor 2A (Organism: Mus musculus, class: GPCR, accessions: P35363, gene: Htr2a, swissprot: 5HT2A_MOUSE) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1478263) 5-hydroxytryptamine receptor 2B (Organism: Mus musculus, class: GPCR, accessions: Q02152, gene: Htr2b, swissprot: 5HT2B_MOUSE) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1478263) Naftidrofuryl is a vasodilator used in the management of peripheral and cerebral vascular disorders. The drug act as a selective antagonist of 5-HT2 receptors. However, the drug has also been shown to activate intracellular aerobic metabolism as demonstrated by a reduction in the level of lactic acid level and an increased level of ATP. It is claimed that this action protects cells against the metabolic effects of ischaemia. Furthermore, naftidrofuryl oxalate is a powerful spasmolytic agent. Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Vasodilator Agents (Code: D014665) 1972-09-11 Italian Medicines Agency (AIFA)
Click to view denaverine
Click to view melinamide
Click to view altizide Altizide is a thiazide diuretic with antihypertensive activity. It is used in combination with spironolactone for the treatment of hypertension and edemas associated with liver cirrhosis, congestive heart failure and nephrotic syndrome. 1975-09-01 Spanish Agency of Medicines and Medical Products (AEMPS) B4D
Click to view bortezomib Proteasome subunit beta type-1 (Organism: Homo sapiens, class: Enzyme, accessions: P20618, gene: PSMB1, swissprot: PSB1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16286248) Proteasome subunit beta type-5 (Organism: Homo sapiens, class: Enzyme, accessions: P28074, gene: PSMB5, swissprot: PSB5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16286248) Proteasome subunit beta type-2 (Organism: Homo sapiens, class: Enzyme, accessions: P49721, gene: PSMB2, swissprot: PSB2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16286248) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021602s044lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021602s044lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021602s044lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021602s044lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021602s044lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021602s044lbl.pdf) Prothrombin (Organism: Homo sapiens, class: Enzyme, accessions: P00734, gene: F2, swissprot: THRB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871680) Cathepsin G (Organism: Homo sapiens, class: Enzyme, accessions: P08311, gene: CTSG, swissprot: CATG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871680) Chymotrypsinogen B (Organism: Homo sapiens, class: Enzyme, accessions: P17538, gene: CTRB1, swissprot: CTRB1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871680) Neutrophil elastase (Organism: Homo sapiens, class: Enzyme, accessions: P08246, gene: ELANE, swissprot: ELNE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871680) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27469982) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27469982) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27469982) Bortezomib is a modified dipeptidyl boronic acid. Bortezomib is an antineoplastic agent which acts as a reversible inhibitor of the chymotrypsin-like activity of the 26S proteasome in mammalian cells. Bortezomib is indicated for the treatment of adult patients with multiple myeloma or with mantle cell lymphoma. Proteasome Inhibitors (Code: N0000175075) Antineoplastic Agents (Code: D000970) antineoplastic agent (Code: CHEBI:35610) antiprotozoal drug (Code: CHEBI:35820) proteasome inhibitor (Code: CHEBI:52726) 2003-05-13 FDA BO2
Click to view felodipine Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Homo sapiens, class: Ion channel, accessions: Q01668, gene: CACNA1D, swissprot: CAC1D_HUMAN) blocker Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) blocker Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Bile acid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q96RI1, gene: NR1H4, swissprot: NR1H4_HUMAN Cystic fibrosis transmembrane conductance regulator (Organism: Homo sapiens, class: Ion channel, accessions: P13569, gene: CFTR, swissprot: CFTR_HUMAN) activator (Source: ) Felodipine is a dihydropyridine calcium channel blocker that reduces the influx of Ca++ by an effect on the voltage dependent L-channels in vascular smooth muscle and atrial cells, and blocks potassium-induced contracture of the portal vein. Felodipine is used for the treatment of mild to moderate essential hypertension. Calcium Channel Antagonists (Code: N0000000069) Dihydropyridine Calcium Channel Blocker (Code: N0000175421) Dihydropyridines (Code: N0000007556) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) anti-arrhythmia drug (Code: CHEBI:38070) 1991-07-25 FDA 225
Click to view artesunate Amebicides (Code: D000563) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) antimalarial (Code: CHEBI:38068)
Click to view ticarcillin An antibiotic derived from penicillin similar to CARBENICILLIN in action. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) Penicillin-class Antibacterial (Code: N0000175497) Penicillins (Code: N0000011281) 1976-11-09 FDA
Click to view bufogenin respiratory stimulant; from toad; structure Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Protective Agents (Code: D020011)
Click to view estradiol dipropionate Estradiol dipropionate is an estradiol ester and a prodrug of estradiol. (See: estradiol)
Click to view zipeprol Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141)
Click to view perimetazine
Click to view estradiol enanthate Estradiol enanthate is an estrogen ester and a long-lasting prodrug of estradiol. (See: estradiol) Estrogens (Code: D004967) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view ibutilide Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) blocker Antiarrhythmic (Code: N0000175426) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) 1995-12-28 FDA
Click to view nilvadipine Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/7898101) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.info.pmda.go.jp/go/pack/2149022F1079_1_06/) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/12128170/) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) activator (Source: https://pubmed.ncbi.nlm.nih.gov/20966043/) Nilvadipine is a L-type calcium channel blocker. It inhibits the influx of extracellular calcium through myocardial and vascular membrane pores by physically plugging the channel. It is used for treatment of hypertension. Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) 1994-08-16 Austrian Medicines and Medical Devices Agency
Click to view perflutren Perflutren lipid microspheres exhibit lower acoustic impedance than blood and enhance the intrinsic backscatter of blood. These physical acoustic properties of activated perflutren provide contrast enhancement of the left ventricular chamber and aid delineation of the left ventricular endocardial border during echocardiography. Contrast Agent for Ultrasound Imaging (Code: N0000175864) Ultrasound Contrast Activity (Code: N0000010259) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 2001-07-31 FDA
Click to view bamifylline Analgesics (Code: D000700) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689) Vasodilator Agents (Code: D014665)
Click to view racecadotril Racecadotril is a prodrug that needs to be hydrolysed to its active metabolite thiorphan, which is an inhibitor of enkephalinase, a cell membrane peptidase located in various tissues, notably the epithelium of the small intestine. This enzyme contributes both to the hydrolysis of exogenous peptides and to the breakdown of endogenous peptides such as enkephalins. Racecadotril protects enkephalins from enzymatic degradation thereby prolonging their action at enkephalinergic synapses in the small intestine and reducing hypersecretion. Racecadotril is used for the treatment of Diarrhea, Acute Diarrhea, and Acute Gastroenteritis. Antidiarrheals (Code: D000930) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Protease Inhibitors (Code: D011480) 1993-01-01 YEAR INTRODUCED
Click to view buspirone 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19147349) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Buspirone is an antianxiety agent that is not chemically or pharmacologically related to the benzodiazepines, barbiturates, or other sedative/anxiolytic drugs. The mechanism of action of buspirone is unknown. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. In vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models. Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems. Buspirone is indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety. Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Tranquilizing Agents (Code: D014149) serotonergic agonist (Code: CHEBI:35941) sedative (Code: CHEBI:35717) anxiolytic drug (Code: CHEBI:35474) 1986-09-29 FDA
Click to view fosfluconazole fluconazole: Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf) Lanosterol 14-alpha demethylase (Organism: Candida tropicalis , class: Enzyme, accessions: P14263, gene: ERG11, swissprot: CP51_CANTR) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019949s065,020090s047lbl.pdf) Fosfluconazole is a phosphate prodrug of fluconazole that has been developed to reduce the volume of fluid required to administer fluconazole by the intravenous route. Fosfluconazole is hydrolyzed by alkaline phosphatase to fluconazole and phosphoric acid. Fluconazole preferentially inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols, the loss of normal fungal sterols, and fungistatic activity. Fosfluconazole is indicated for the treatment of the Candida or Cryptococcus infections, fungemia, respiratory mycosis, fungal peritonitis, gastrointestinal mycosis, urinary tract mycosis, fungal meningitis. 14-alpha Demethylase Inhibitors (Code: D058888) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) prodrug (Code: CHEBI:50266) 2003-10-16 PMDA
Click to view piposulfan Piposulfan is an alkyl sulfonate with potential antineoplastic activity. Piposulfan alkylates DNA, thereby producing DNA interstrand crosslinks and DNA strand breaks and inhibiting DNA replication.
Click to view anecortave Plasminogen activator inhibitor 1 (Organism: Homo sapiens, class: Secreted, accessions: P05121, gene: SERPINE1, swissprot: PAI1_HUMAN) Angiogenesis Inhibitors (Code: D020533) Angiogenesis Modulating Agents (Code: D043924) Antineoplastic Agents (Code: D000970) Growth Inhibitors (Code: D006131) Growth Substances (Code: D006133) 2006-01-01 YEAR INTRODUCED
Click to view medibazine
Click to view sufentanil Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT Mu-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33535, gene: Oprm1, swissprot: OPRM_RAT An opioid analgesic that is used as an adjunct in anesthesia, in balanced anesthesia, and as a primary anesthetic agent. Adjuvants, Anesthesia (Code: D000759) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322) anaesthesia adjuvant (Code: CHEBI:60807) intravenous anaesthetic (Code: CHEBI:38877) Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) 1984-05-04 FDA
Click to view mesoridazine 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: ) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: ) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: ) A phenothiazine antipsychotic with effects similar to CHLORPROMAZINE. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) dopaminergic antagonist (Code: CHEBI:48561) first generation antipsychotic (Code: CHEBI:65190) Phenothiazine (Code: N0000175746) Phenothiazines (Code: N0000007544) 1970-02-27 FDA
Click to view quazepam Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15801544) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15801544) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15801544) Dimethylaniline monooxygenase [N-oxide-forming] 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q01740, gene: FMO1 swissprot: FMO1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15801544) Quazepam is a trifluoroethyl benzodiazepine hypnotic agent and a gamma-aminobutyric (GABAA ) agonist. Quazepam, like other central nervous system agents of the 1,4-benzodiazepine class, presumably exerts its effects by binding to stereo-specific receptors at several sites within the central nervous system. The exact mechanism of action is unknown. All metabolites of quazepam show central nervous system depressant activity. Quazepam, like halazepam, binds to GABA-A receptors in lamina IV of the cerebral cortex, the zona incerta, substantia nigra and the cerebellum. Quazepam is indicated for the treatment of insomnia characterized by difficulty falling asleep, frequent nocturnal awakenings, and/or early morning awakenings. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1985-12-27 FDA
Click to view terazosin Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9379432) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9379432) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9379432) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Terazosin is a quinazoline derivative alpha-1-selective adrenergic blocking agent. Terazosin is selective for alpha-1-adrenoceptors but not their individual subtypes. Inhibition of these alpha-1-adrenoceptors results in relaxation of smooth muscle in blood vessels and the prostate, lowering blood pressure and improving urinary flow. Terazosin is indicated for use in treating symptomatic benign prostatic hyperplasia and hypertension. Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Neurotransmitter Agents (Code: D018377) Urological Agents (Code: D064804) antineoplastic agent (Code: CHEBI:35610) antihypertensive agent (Code: CHEBI:35674) alpha-adrenergic antagonist (Code: CHEBI:37890) alpha-Adrenergic Blocker (Code: N0000175553) 1987-08-07 FDA TZN
Click to view trimebutine Trimebutine is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu opioid agonist effects. It is marketed for the treatment of irritable bowel syndrome (IBS) and lower gastrointestinal tract motility disorders. It is used to restore normal bowel function and is commonly present in pharmaceutical mixtures as trimebutine maleate salt form. Autonomic Agents (Code: D001337) Gastrointestinal Agents (Code: D005765) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) 1983-12-31 Health Canada
Click to view urapidil Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_002936_040135_RCP.pdf&retry=0&sys=m0b1l3) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_002936_040135_RCP.pdf&retry=0&sys=m0b1l3) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_002936_040135_RCP.pdf&retry=0&sys=m0b1l3) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/3207999) Urapidil is a peripheral postsynaptic alpha 1-adrenoceptor antagonist with central agonistic action at serotonin 5-HT1A receptors. Urapidil reduces blood pressure without altering heart rate. Urapidil is used for the treatment of mild to moderate hypertension and as an intravenous injection for the treatment of hypertensive crises, severe or treatment-resistant hypertension, perioperative or postoperative hypertension and pre-eclampsia. Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Vasodilator Agents (Code: D014665) 1987-07-30 Italian Medicines Agency (AIFA)
Click to view gusperimus synthesized by chemical modification of spergualin; in combination with cyclosporin A prevents diabetes in predisposed NOD mice; structure given in first source; RN given refers to (-)-isomer trihydrochloride Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Hypoglycemic Agents (Code: D007004) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837)
Click to view teclothiazide Teclothiazide is a benzothiadiazine sulfonamide derivative belonging to the class of the thiazide diuretics.
Click to view tioconazole Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11854151) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11854151) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11854151) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11854151) Tioconazole is an antifungal medication of the Imidazole class used to treat infections caused by a fungus or yeast. Tioconazole interacts with 14-alpha demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol, an essential component of the yeast membrane. In this way, tioconazole inhibits ergosterol synthesis, resulting in increased cellular permeability. Tioconazole exhibits fungicidal activity in vitro against Candida albicans, other species of the genus Candida, and against Torulopsis glabrata. Tioconazole is used for the treatment of vaginal yeast infections, jock itch, athlete's foot, and tinea versicolor or 'sun fungus'. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) 14-alpha Demethylase Inhibitors (Code: D058888) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) antiinfective agent (Code: CHEBI:35441) 1983-02-18 FDA FJQ
Click to view benzylhydrochlorothiazide Benzylhydrochlorothiazide is a thiazide diuretic used as a blood pressure-lowering agent. 1961-02-27 PMDA
Click to view flurazepam Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) positive allosteric modulator A benzodiazepine derivative used mainly as a hypnotic. Benzodiazepine (Code: N0000175694) Benzodiazepines (Code: N0000007542) Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) GABA Agents (Code: D018682) GABA Modulators (Code: D018757) Hypnotics and Sedatives (Code: D006993) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1970-04-07 FDA FL7
Click to view nemonapride D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: ) D(3) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19020, gene: Drd3, swissprot: DRD3_RAT D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT an atypical antipsychotic approved in Japan for the treatment of schizophrenia Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) dopaminergic antagonist (Code: CHEBI:48561) serotonergic agonist (Code: CHEBI:35941) second generation antipsychotic (Code: CHEBI:65191) AQD
Click to view oxantel oxyphenyl analog of pyrantel; RN given refers to (E)-isomer; synonym CP-14,445-16 refers to oxantel pamoate Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977)
Click to view aranidipine Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: )
Click to view visnadine
Click to view nisoldipine Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Mus musculus, class: Ion channel, accessions: Q01815, gene: Cacna1c, swissprot: CAC1C_MOUSE) gating inhibitor (Source: ) Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Mus musculus, class: Ion channel, accessions: Q99246, gene: Cacna1d, swissprot: CAC1D_MOUSE) gating inhibitor (Source: ) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) gating inhibitor (Source: ) Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Homo sapiens, class: Ion channel, accessions: Q01668, gene: CACNA1D, swissprot: CAC1D_HUMAN) blocker Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Voltage-dependent P/Q-type calcium channel subunit alpha-1A (Organism: Homo sapiens, class: Ion channel, accessions: O00555, gene: CACNA1A, swissprot: CAC1A_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina. Dihydropyridine Calcium Channel Blocker (Code: N0000175421) Dihydropyridines (Code: N0000007556) Calcium Channel Antagonists (Code: N0000000069) Decreased Blood Pressure (Code: N0000178477) Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) platelet aggregation inhibitor (Code: CHEBI:50427) cardiovascular drug (Code: CHEBI:35554) 1995-02-02 FDA
Click to view trimethobenzamide major descriptor (64-84); on-line search BENZAMIDES (64-84); Index Medicus search TRIMETHOBENZAMIDE (64-84); RN given refers to parent cpd Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373) antiemetic (Code: CHEBI:50919) Emesis Suppression (Code: N0000009034) 1974-07-12 FDA
Click to view zopiclone Gamma-aminobutyric acid receptor subunit alpha-5 (Organism: Homo sapiens, class: Ion channel, accessions: P31644, gene: GABRA5, swissprot: GBRA5_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/1897328) Gamma-aminobutyric acid receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: P47869, gene: GABRA2, swissprot: GBRA2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/1897328) Gamma-aminobutyric acid receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P14867, gene: GABRA1, swissprot: GBRA1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/1897328) Gamma-aminobutyric acid receptor subunit alpha-3 (Organism: Homo sapiens, class: Ion channel, accessions: P34903, gene: GABRA3, swissprot: GBRA3_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/1897328) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021476s038lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021476s038lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00046512.PDF)RA5, swissprot: GBRA5_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/1897328) Gamma-aminobutyric acid receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: P47869, gene: GABRA2, swissprot: GBRA2_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/1897328) Gamma-aminobutyric acid receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P14867, gene: GABRA1, swissprot: GBRA1_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/1897328) Gamma-aminobutyric acid receptor subunit alpha-3 (Organism: Homo sapiens, class: Ion channel, accessions: P34903, gene: GABRA3, swissprot: GBRA3_HUMAN) positive allosteric modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/1897328) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021476s038lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021476s038lbl.pdf) Zopiclone is a nonbenzodiazepine hypnotic agent. The therapeutic pharmacological properties of zopiclone include hypnotic, anxiolytic, anticonvulsant, and myorelaxant properties. The metabolite of zopiclone called desmethylzopiclone is also pharmacologically active, although it has predominately anxiolytic properties. Eszopiclone is the (5S)- (active) enantiomer of zopiclone. Although the exact mechanism of action remains to be fully elucidated, eszopiclone is able to bind to and activate the omega-1 subtype of the alpha subunit of the gamma-aminobutyric acid-benzodiazepine GABA receptor complex (GABA-A), a chloride ionophore complex in the central nervous system (CNS). This leads to the opening of chloride channels, causing hyperpolarization, inhibition of neuronal firing, and enhancement of the inhibitory effect of GABA. Zopiclone is used in the treatment of insomnia. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) central nervous system depressant (Code: CHEBI:35488) sedative (Code: CHEBI:35717) 2004-12-15 FDA ZPC
Click to view fipexide regulates dopaminergic systems at macromolecular level
Click to view cetirizine Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27123426) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14502547) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12873512) Cetirizine is a potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects. Levocetirizine is the active enantiomer of cetirizine. Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Antagonist (Code: N0000175587) Anti-Allergic Agents (Code: D018926) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Neurotransmitter Agents (Code: D018377) H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) Cetirizine: 1995-12-08 FDA Levocetirizine: 2007-05-25 FDA CZE
LCR
Click to view bepotastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Histamine-1 Receptor Antagonist (Code: N0000175587) Anti-Allergic Agents (Code: D018926) H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) 2009-09-08 FDA
Click to view gemifloxacin DNA topoisomerase 4 (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: P72525|Q59961, gene: parC|parE, swissprot: PARC_STRPN|PARE_STRPN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021158s026lbl.pdf) DNA gyrase subunit A (Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd), class: Enzyme, accessions: P43700, gene: gyrA, swissprot: GYRA_HAEIN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021158s026lbl.pdf) Gemifloxacin is a synthetic antibacterial agent. Gemifloxacin related to the fluoroquinolone class of antibiotics. Gemifloxacin acts by inhibiting DNA synthesis through the inhibition of both DNA gyrase and topoisomerase IV (TOPO IV), which are essential for bacterial growth. Gemifloxacin has been shown to be active against Streptococcus pneumoniae (including multi-drug resistant strains), Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Chlamydia pneumoniae, Mycoplasma pneumoniae. Gemifloxacin is used for the treatment of acute bacterial exacerbation of chronic bronchitis (caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, or Moraxella catarrhalis) and of community-acquired pneumonia (caused by Streptococcus pneumonia, Haemophilus influenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, Chlamydia pneumoniae, or Klebsiella pneumoniae). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antibacterial drug (Code: CHEBI:36047) Quinolone Antimicrobial (Code: N0000175937) Quinolones (Code: N0000007606) 2002-12-27 Korean Food and Drug Administration (KFDA)
Click to view tadalafil cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022332s009lbl.pdf) Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HCR9, gene: PDE11A, swissprot: PDE11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022332s009lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022332s009lbl.pdf) Phosphodiesterase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P16499|P35913|P51160|O43924|P18545|Q13956, gene: PDE6A|PDE6B|PDE6C|PDE6D|PDE6G|PDE6H, swissprot: PDE6A_HUMAN|PDE6B_HUMAN|PDE6C_HUMAN|PDE6D_HUMAN|CNRG_HUMAN|CNCG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15837326) Tadalafil is a carboline-based compound with vasodilatory activity. Tadalafil is a selective inhibitor of phosphodiesterase type 5 (PDE5) and is used as therapy of erectile dysfunction and pulmonary hypertension. Phosphodiesterase 5 Inhibitor (Code: N0000175599) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Phosphodiesterase 5 Inhibitors (Code: D058986) Phosphodiesterase Inhibitors (Code: D010726) Urological Agents (Code: D064804) Vasodilator Agents (Code: D014665) vasodilator agent (Code: CHEBI:35620) 2003-11-21 FDA CIA
Click to view reproterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10364735) Reproterol is a short-acting beta2 adrenoreceptor agonist. Reproterol increases the generation of cAMP in isolated peripheral blood monocytes in vitro more effectively than does orciprenaline. It was used in combination with cromoglycate as a symptomatic drug for the treatment of asthma. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141)
Click to view balofloxacin Balofloxacin is a broad spectrum fluoroquinolone derivative notable for its activity against Gram-positive cocci. Mechanism of action is a type II DNA topoisomerase inhibition. It is used for the treatment of urinary tract infections due to E.coli and S.pneumoniae. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 2001-12-31 Korean Food and Drug Administration (KFDA)
Click to view cefprozil Cefprozil is a semi-synthetic broad-spectrum cephalosporin antibiotic. Cefprozil's effect is dependent on its binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane. Cefprozil has been shown to be active against Staphylococcus aureus, Haemophilus influenzae, Moraxella catarrhalis (including beta lactamase-producing strains), Streptococcus pneumoniae, Streptococcus pyogenes. Cefprozil is indicated for the treatment of upper and lower respiratory tract infections (pharyngitis/tonsillitis, otitis media, acute Sinusitis, acute bacterial exacerbation of chronic bronchitis) and for the treatment of skin and skin structure infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) 1991-12-23 FDA
Click to view alfuzosin Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021287s021lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021287s021lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021287s021lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021287s021lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Alfuzosin is a selective antagonist of post-synaptic alpha1-adrenoreceptors, which are located in the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra. Alfuzosin is indicated for the treatment of signs and symptoms of benign prostatic hyperplasia. alpha-Adrenergic Blocker (Code: N0000175553) Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Neurotransmitter Agents (Code: D018377) Urological Agents (Code: D064804) antineoplastic agent (Code: CHEBI:35610) antihypertensive agent (Code: CHEBI:35674) alpha-adrenergic antagonist (Code: CHEBI:37890) 2003-06-12 FDA
Click to view hetacillin Hetacillin is a semi-synthetic penicillin compound with bactericidal properties. Hetacillin is a prodrug that is converted to ampicillin via esterases. Hetacillin has been withdrawn from the market since it has been discovered that it has no therapeutic advantage compared to non-ester derivatives like ampicillin. (See: ampicillin) antibacterial drug (Code: CHEBI:36047)
Click to view cyclothiazide Glutamate receptor 2 (Organism: Homo sapiens, class: Ion channel, accessions: P42262, gene: GRIA2, swissprot: GRIA2_HUMAN) Glutamate receptor ionotropic, AMPA (Organism: Rattus norvegicus, class: Ion channel, accessions: P19490|P19491|P19492|P19493, gene: Gria1|Gria2|Gria3|Gria4, swissprot: GRIA1_RAT|GRIA2_RAT|GRIA3_RAT|GRIA4_RAT) Glutamate receptor 1 (Organism: Homo sapiens, class: Ion channel, accessions: P42261, gene: GRIA1, swissprot: GRIA1_HUMAN) Solute carrier family 12 member 3 (Organism: Homo sapiens, class: Transporter, accessions: P55017, gene: SLC12A3, swissprot: S12A3_HUMAN) inhibitor (Source: ) Glutamate receptor 3 (Organism: Homo sapiens, class: Ion channel, accessions: P42263, gene: GRIA3, swissprot: GRIA3_HUMAN) allosteric modulator (Source: ) Glutamate receptor 4 (Organism: Homo sapiens, class: Ion channel, accessions: P48058, gene: GRIA4, swissprot: GRIA4_HUMAN) allosteric modulator (Source: ) Cyclothiazide belongs to the class of thiazide diuretics, exerts its action by inhibitin sodium reabsorption in the renal tubules. Cyclothiazide was used for the treatment of hypertension. In 1993 it was discovered that cyclothiazide stimulates AMPA receptors and may induce seizures activity. Cyclothiazide was also found to inhibit gamma-aminobutyric acid (GABA)-A receptors. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Natriuretic Agents (Code: D045283) antihypertensive agent (Code: CHEBI:35674) diuretic (Code: CHEBI:35498) 1982-06-08 FDA CYZ
Click to view regadenoson Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022161s015lbl.pdf) Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator. Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor. This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors. Regadenoson is used as a pharmacologic stress agent which is indicated for radionuclide myocardial perfusion imaging (MPI) in patients unable to undergo adequate exercise stress. Adenosine A2 Receptor Agonists (Code: D058908) Neurotransmitter Agents (Code: D018377) Purinergic Agents (Code: D058905) Purinergic Agonists (Code: D058913) Purinergic P1 Receptor Agonists (Code: D058906) Adenosine Receptor Agonist (Code: N0000178375) Adenosine Receptor Agonists (Code: N0000175788) 2008-04-10 FDA
Click to view treprostinil Prostacyclin receptor (Organism: Homo sapiens, class: GPCR, accessions: P43119, gene: PTGIR, swissprot: PI2R_HUMAN) agonist (Source: ) Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN) agonist (Source: ) Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) agonist (Source: ) Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN) agonist (Source: ) Prostaglandin E2 receptor EP2 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43116, gene: PTGER2, swissprot: PE2R2_HUMAN) agonist (Source: ) Prostaglandin D2 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q13258, gene: PTGDR, swissprot: PD2R_HUMAN) agonist (Source: ) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) platelet aggregation inhibitor (Code: CHEBI:50427) vasodilator agent (Code: CHEBI:35620) antihypertensive agent (Code: CHEBI:35674) cardiovascular drug (Code: CHEBI:35554) Prostacycline Vasodilator (Code: N0000175416) Prostaglandins I (Code: N0000011280) Vasodilation (Code: N0000009909) 2002-05-21 FDA
Click to view oxamarin
Click to view meclozine Nuclear receptor subfamily 1 group I member 3 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q14994, gene: NR1I3, swissprot: NR1I3_HUMAN) antagonist (Source: ) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Constitutive androstane receptor (Organism: Mus musculus, class: Unclassified, accessions: O35627, gene: Nr1i3, swissprot: NR1I3_MOUSE) agonist (Source: ) A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. Antiemetic (Code: N0000178372) Emesis Suppression (Code: N0000009034) Anti-Allergic Agents (Code: D018926) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) 1957-02-14 FDA
Click to view flavoxate Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Phosphodiesterase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27815|Q07343|Q08493|Q08499, gene: PDE4A|PDE4B|PDE4C|PDE4D, swissprot: PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN) inhibitor Phosphodiesterase 7 (Organism: Homo sapiens, class: Enzyme, accessions: Q13946|Q9NP56, gene: PDE7A|PDE7B, swissprot: PDE7A_HUMAN|PDE7B_HUMAN) inhibitor Phosphodiesterase 8 (Organism: Homo sapiens, class: Enzyme, accessions: O60658|O95263, gene: PDE8A|PDE8B, swissprot: PDE8A_HUMAN|PDE8B_HUMAN) inhibitor A drug that has been used in various urinary syndromes and as an antispasmodic. Its therapeutic usefulness and its mechanism of action are not clear. It may have local anesthetic activity and direct relaxing effects on smooth muscle as well as some activity as a muscarinic antagonist. Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Urological Agents (Code: D064804) parasympatholytic (Code: CHEBI:50370) muscarinic antagonist (Code: CHEBI:48876) antispasmodic drug (Code: CHEBI:53784) Cholinergic Muscarinic Antagonist (Code: N0000175700) Cholinergic Muscarinic Antagonists (Code: N0000000125) 1970-01-15 FDA
Click to view biriperone D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT D(1A) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901, gene: Drd1, swissprot: DRD1_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT
Click to view dimetotiazine has considerable antiemetic & serotonin antagonistic action used mainly in allergic skin conditions; minor descriptor (75-84); on-line & Index Medicus search PHENOTHIAZINES (75-84); RN given refers to parent cpd Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377)
Click to view dithiazanine 3-Ethyl-2-(5-(3-ethyl-2-benzothiazolinylidene)-1,3- pentadienyl)benzothiazolium. A benzothiazole that was formerly used as an antinematodal agent and is currently used as a fluorescent dye. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Coloring Agents (Code: D004396) Fluorescent Dyes (Code: D005456) Indicators and Reagents (Code: D007202) Luminescent Agents (Code: D049408) fluorochrome (Code: CHEBI:51217) anthelminthic drug (Code: CHEBI:35443)
Click to view sparfloxacin DNA gyrase (Organism: Staphylococcus aureus subsp. aureus, class: Enzyme, accessions: P20831|P0A0K8, gene: gyrA|gyrB, swissprot: GYRA_STAAU|GYRB_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2003/020677s006lbl.pdf) DNA gyrase subunit A (Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd), class: Enzyme, accessions: P43700, gene: gyrA, swissprot: GYRA_HAEIN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2003/020677s006lbl.pdf) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10525100) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9756763) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12190308) Sparfloxacin has in vitro activity against a wide range of gramnegative and gram-positive microorganisms. Sparfloxacin exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. Sparfloxacin is used for the treatment of community-acquired pneumonia (caused by Chlamydia pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, or Streptococcus pneumoniae) and acute bacterial exacerbations of chronic bronchitis (caused by Chlamydia pneumoniae, Enterobacter cloacae, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Staphylococcus aureus, or Streptococcus pneumoniae). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Antitubercular Agents (Code: D000995) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1996-12-19 FDA
Click to view cinepazet
Click to view paramethasone acetate A glucocorticoid with the general properties of corticosteroids. It has been used by mouth in the treatment of all conditions in which corticosteroid therapy is indicated except adrenal-deficiency states for which its lack of sodium-retaining properties makes it less suitable than HYDROCORTISONE with supplementary FLUDROCORTISONE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p737) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) FDA
Click to view dexamethasone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10611474) Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10611474) Nuclear receptor subfamily 1 group I member 2 (Organism: Mus musculus, class: Nuclear hormone receptor, accessions: O54915, gene: Nr1i2, swissprot: NR1I2_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9489701) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14661924) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211379s000lbl.pdf) Dexamethasone (Betamethasone) is a glucocorticoid receptor agonist. The beta- and dexa- forms of these molecules are epimers with identical chemical structures except that the orientation of the methyl group at the C-16 position is in the opposite direction from the plane. Betamethasone has a longer half-life than dexamethasone. Dexamethasone and betamethasone are indicated to control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment in asthma, atopic dermatitis, contact dermatitis, drug hypersensitivity reactions, perennial or seasonal allergic rhinitis, serum sickness. It also indicated for the treatment of dermatologic diseases ( Bullous dermatitis herpetiformis, exfoliative erythroderma, mycosis fungoides, pemphigus, Stevens-Johnson syndrome), endocrine disorders (congenital adrenal hyperplasia, hypercalcemia associated with cancer, nonsuppurative thyroiditis), gastrointestinal diseases:, hematologic disorders (acquired (autoimmune) hemolytic anemia, Diamond-Blackfan anemia, idiopathic thrombocytopenic purpura in adults, pure red cell aplasia, selected cases of secondary thrombocytopenia), trichinosis with neurologic or myocardial involvement, tuberculous meningitis with subarachnoid block or impending block when used with appropriate antituberculous chemotherapy, for the palliative management of leukemias and lymphomas, acute exacerbations of multiple sclerosis; cerebral edema associated with primary or metastatic brain tumor, craniotomy, or head injury, sympathetic ophthalmia, temporal arteritis, uveitis and ocular inflammatory conditions, to induce diuresis or remission of proteinuria in idiopathic nephrotic syndrome or that due to lupus erythematosus, to treat berylliosis, fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy, idiopathic eosinophilic pneumonias, symptomatic sarcoidosis and as adjunctive therapy for short-term administration in acute gouty arthritis; acute rheumatic carditis; ankylosing spondylitis; psoriatic arthritis; rheumatoid arthritis, including juvenile rheumatoid arthritis, for the treatment of dermatomyositis, polymyositis, and systemic lupus erythematosus. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Antiemetics (Code: D000932) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Peripheral Nervous System Agents (Code: D018373) antiemetic (Code: CHEBI:50919) adrenergic agent (Code: CHEBI:37962) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) anti-inflammatory drug (Code: CHEBI:35472) Betamethasone: 1961-04-17 FDA Dexamethasone: 1958-10-30 FDA DEX
Click to view naftopidil Beta-2 adrenergic receptor (Organism: Canis familiaris, class: GPCR, accessions: P54833, gene: ADRB2, swissprot: ADRB2_CANFA Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P19328|P22086|P22909, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10976457) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10976457) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10976457) Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Hematologic Agents (Code: D006401) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Platelet Aggregation Inhibitors (Code: D010975) 1998-12-25 PMDA
Click to view trospium Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021595s009lbl.pdf) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021595s009lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10628907) Trospium is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Trospium antagonizes the effect of acetylcholine on muscarinic receptors in cholinergically innervated organs including the bladder. Its parasympatholytic action reduces the tonus of smooth muscle in the bladder. Trospium is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Cholinergic Muscarinic Antagonist (Code: N0000175700) Cholinergic Muscarinic Antagonists (Code: N0000000125) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Urological Agents (Code: D064804)
Click to view tiotropium bromide Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021395s048lbl.pdf) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021395s048lbl.pdf) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021395s048lbl.pdf) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021395s048lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021395s048lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021395s048lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021395s048lbl.pdf) Solute carrier family 22 member 4 (Organism: Homo sapiens, class: Transporter, accessions: Q9H015, gene: SLC22A4, swissprot: S22A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20020740) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20020740) Tiotropium is a synthetic anticholinergic agent that is used as an inhalant for treatment of acute bronchospasm due to chronic bronchitis or emphysema. Tiotropium is an antagonist of muscarinic receptors M1 to M5. Inhibition of the M3 receptor in the smooth muscle of the lungs leads to relaxation of smooth muscle and bronchodilation. Anticholinergic (Code: N0000175574) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) muscarinic antagonist (Code: CHEBI:48876) bronchodilator agent (Code: CHEBI:35523) 2004-01-30 FDA 0HK
Click to view halopropane Halopropane is a fluorinated hydrocarbon possessing the desirable anesthetic attributes of noninflammability, appropriate volatility, chemical stability and low toxicity. But later its clinical development was terminated due to a high incidence of cardiac arrhythmias. anaesthetic (Code: CHEBI:38867) General Anesthesia (Code: N0000175975) General Anesthetic (Code: N0000175681) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492)
Click to view dextromoramide An opioid analgesic structurally related to METHADONE and used in the treatment of severe pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1070) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) opioid analgesic (Code: CHEBI:35482)
Click to view iocetamic acid was MH 1975-92 (see under IODOBENZENES 1975-90); use IODOBENZENES to search IOCETAMIC ACID 1975-92 FDA
Click to view ursodiol G-protein coupled bile acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDU6, gene: GPBAR1, swissprot: GPBAR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18307294) Bile acid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q96RI1, gene: NR1H4, swissprot: NR1H4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17292610) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: Q9QY30, gene: Abcb11, swissprot: ABCBB_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10607905) Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15297262) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7557095) Sodium/bile acid cotransporter (Organism: Rattus norvegicus, class: Transporter, accessions: P26435, gene: Slc10a1, swissprot: NTCP_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12842829) Ileal sodium/bile acid cotransporter (Organism: Homo sapiens, class: Transporter, accessions: Q12908, gene: SLC10A2, swissprot: NTCP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9458785) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18583509) Ursodiol (ursodeoxycholic acid) and chenodiol (chenodeoxycholic acid) are diastereomeric naturally occuring bile acids and widely used as anticholelithogenic agents. Both agents have been found effective in dissolving radiolucent gall- bladder stones, but chenodiol treatment was associated with frequent serum transaminase elevations and diarrhea, whereas ursodiol was found to cause no elevation of serum transaminases. Ursodiol is present as a minor fraction of the total human bile acid pool (app. 5%). Chenodiol is indicated for patients with radiolucent stones in well-opacifying gallbladders, in whom selective surgery would be undertaken except for the presence of increased surgical risk due to systemic disease or age. Chenodiol will not dissolve calcified (radiopaque) or radiolucent bile pigment stones. Ursodiol is indicated for the treatment of patients with primary biliary cirrhosis. Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765) Bile Acid (Code: N0000175802) Bile Acids and Salts (Code: N0000006801) ursodiol: 1987-12-31 FDA chenodiol: 1983-07-28 FDA IU5
JN3
Click to view chloroprednisone
Click to view cloprednol relative anti-inflammatory potency twice prednisolone; synthetic glucocorticoid; structure
Click to view perflubutane Perflubutane has been used in trials studying the diagnostic of liver mass, liver diseases, liver metastasis, portal hypertension, and peripheral artery disease. Perflubutane is used as a gas component for newer generation microbubble ultrasound contrast agents. It is a cardiovascular drug designed to enable ultrasound to compete more effectively with nuclear stress testing. Currently it is used in the leading procedure for detecting coronary heart disease. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 2007-01-01 PMDA
Click to view pentetic acid lead (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021749s008lbl.pdf) An iron chelating agent with properties like EDETIC ACID. DTPA has also been used as a chelator for other metals, such as plutonium. Lead Chelating Activity (Code: N0000175962) Lead Chelator (Code: N0000175963) Antidotes (Code: D000931) Chelating Agents (Code: D002614) Iron Chelating Agents (Code: D007502) Protective Agents (Code: D020011) Sequestering Agents (Code: D064449) FDA
Click to view rubitecan Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase I Inhibitors (Code: D059004) Topoisomerase Inhibitors (Code: D059003) antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266)
Click to view sulfaloxic acid Sulfaloxic acid is a member of benzamides. It was developed as an antibacterial agent.
Click to view erlotinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021743s025lbl.pdf) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021743s025lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021743s025lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021743s025lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24713129) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19733976) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19733976) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/19733976) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/19733976) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19493273) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18723475) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18723475) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23434139) Erlotinib is a quinazoline derivative with antineoplastic properties. Competing with adenosine triphosphate, erlotinib reversibly binds to the intracellular catalytic domain of epidermal growth factor receptor (EGFR) tyrosine kinase, thereby reversibly inhibiting EGFR phosphorylation and blocking the signal transduction events and tumorigenic effects associated with EGFR activation. Erlotinib is indicated for the treatment of patients with metastatic non-small cell lung cancer whose tumors have epidermal growth factor receptor exon 19 deletions or exon 21 (L858R) substitution mutations and for the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine. Kinase Inhibitor (Code: N0000175605) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) antineoplastic agent (Code: CHEBI:35610) 2004-11-18 FDA AQ4
Click to view amsacrine DNA topoisomerase I, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q969P6, gene: TOP1MT, swissprot: TOP1M_HUMAN) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN DNA topoisomerase 2-beta (Organism: Homo sapiens, class: Enzyme, accessions: Q02880, gene: TOP2B, swissprot: TOP2B_HUMAN DNA topoisomerase II (Organism: Homo sapiens, class: Enzyme, accessions: P11388|Q02880, gene: TOP2A|TOP2B, swissprot: TOP2A_HUMAN|TOP2B_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) DNA topoisomerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P11387, gene: TOP1, swissprot: TOP1_HUMAN) An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent. Antineoplastic Agents (Code: D000970) Indicators and Reagents (Code: D007202) Intercalating Agents (Code: D007364) antineoplastic agent (Code: CHEBI:35610) 1987-01-01 YEAR INTRODUCED ASW
Click to view brotizolam Platelet-activating factor receptor (Organism: Homo sapiens, class: GPCR, accessions: P25105, gene: PTAFR, swissprot: PTAFR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2016721) Brotizolam is a sedative-hypnotic thienotriazolodiazepine drug which is a benzodiazepine analog. It possesses anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties, and is considered to be similar in effect to short-acting benzodiazepines such as triazolam. It is used in the short-term treatment of severe or debilitating insomnia and as a premedication prior to surgery. Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993) 1985-06-18 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view metaclazepam Metaclazepam is a benzodiazepine with properties similar to those of diazepam. It was used for the treatment of anxiety. It is no longer available.
Click to view besifloxacin Topoisomerase IV (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AFI2|P20083, gene: parC|parE, swissprot: PARC_ECOLI|PARE_ECOLI) inhibitor DNA gyrase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES4|P0AES6, gene: gyrA|gyrB, swissprot: GYRA_ECOLI|GYRB_ECOLI) inhibitor Besifloxacin is an 8-chloro fluoroquinolone with a N-1 cyclopropyl group. The compound has activity against Gram-positive and Gram-negative bacteria due to the inhibition of both bacterial DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme required for replication, transcription and repair of bacterial DNA. Topoisomerase IV is an essential enzyme required for partitioning of the chromosomal DNA during bacterial cell division. Quinolone Antimicrobial (Code: N0000175937) Quinolones (Code: N0000007606) 2009-05-28 FDA
Click to view ambuside Ambuside is a benzenesulfonamide-based diuretic. Ambuside is structurally similar to thiazide type diuretics and acts in a similar manner. It is no longer available. 1970 YEAR INTRODUCED
Click to view triamcinolone Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Triamcinolone is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B. Triamcinolone is indicated for the treatment of alopecia areata, discoid lupus erythematosus, keloids, and necrobiosis lipoidica diabeticorum, localized hypertrophic infiltrated inflammatory lesions of granuloma annulare, lichen planus, lichen simplex chronicus, psoriatic plaques and inflammatory and pruritic manifestations of corticosteroid responsive dermatoses. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) anti-allergic agent (Code: CHEBI:50857) anti-inflammatory drug (Code: CHEBI:35472) 1957-12-03 FDA
Click to view diflucortolone A topical glucocorticoid used in various DERMATOSES. It is absorbed through the skin, bound to plasma albumin, and may cause adrenal suppression. It is also administered as the valerate. Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view fluacizine Russian drug; 2-trifluoromethyl analog of chloracizine; RN given refers to parent cpd
Click to view gemeprost used for preoperative dilation of cervix before surgical abortion; RN given refers to (2E,11alpha,13E,15R)-isomer Abortifacient Agents (Code: D000019) Abortifacient Agents, Nonsteroidal (Code: D000020) Reproductive Control Agents (Code: D012102)
Click to view cefdinir Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9092716) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9092716) Cefdinir is an extended-spectrum, semisynthetic cephalosporin, for oral administration. Bactericidal activity of cefdinir results from inhibition of cell wall synthesis. Cefdinir is stable in the presence of some, but not all, beta-lactamase enzymes. Cefdinir has been shown to be active against Staphylococcus aureus (including beta-lactamase producing strains), Streptococcus pneumoniae (penicillin-susceptible strains only), Streptococcus pyogenes, Haemophilus influenzae (including beta-lactamase producing strains), Haemophilus parainfluenzae (including beta-lactamase producing strains), Moraxella catarrhalis (including beta-lactamase producing strains). Cefdinir is indicated for the treatment of community-acquired pneumonia, acute exacerbations of chronic bronchitis, acute maxillary sinusitis, pharyngitis/tonsillitis, uncomplicated skin and skin structure infections, acute bacterial otitis media. Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1997-12-04 FDA
Click to view cloricromen Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975)
Click to view timiperone Antiemetics (Code: D000932) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view ketanserin 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT) antagonist (Source: ) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: ) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: ) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: ) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: ) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) antagonist (Source: ) Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT Serotonin 2 (5-HT2) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P30994, gene: Htr2a|Htr2b|Htr2c, swissprot: 5HT2A_RAT|5HT2B_RAT|5HT2C_RAT 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT 5-hydroxytryptamine receptor 2C (Organism: Rattus norvegicus, class: GPCR, accessions: P08909, gene: Htr2c, swissprot: 5HT2C_RAT 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: ) Chromaffin granule amine transporter (Organism: Homo sapiens, class: Transporter, accessions: P54219, gene: SLC18A1, swissprot: VMAT1_HUMAN) inhibitor (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1B (Organism: Mus musculus, class: Unclassified, accessions: P28334, gene: Htr1b, swissprot: 5HT1B_MOUSE) antagonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Mus musculus, class: GPCR, accessions: P32304, gene: Htr7, swissprot: 5HT7R_MOUSE) antagonist (Source: ) A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Hematologic Agents (Code: D006401) Neurotransmitter Agents (Code: D018377) Platelet Aggregation Inhibitors (Code: D010975) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) antihypertensive agent (Code: CHEBI:35674) cardiovascular drug (Code: CHEBI:35554) alpha-adrenergic antagonist (Code: CHEBI:37890) serotonergic antagonist (Code: CHEBI:48279) 1985-01-01 YEAR INTRODUCED
Click to view vesnarinone cGMP-inhibited 3',5'-cyclic phosphodiesterase A (Organism: Homo sapiens, class: Enzyme, accessions: Q14432, gene: PDE3A, swissprot: PDE3A_HUMAN cGMP-inhibited 3',5'-cyclic phosphodiesterase B (Organism: Homo sapiens, class: Enzyme, accessions: Q13370, gene: PDE3B, swissprot: PDE3B_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Phosphodiesterase 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q13370|Q14432, gene: PDE3A|PDE3B, swissprot: PDE3A_HUMAN|PDE3B_HUMAN Transitional endoplasmic reticulum ATPase (Organism: Homo sapiens, class: Enzyme, accessions: P55072, gene: VCP, swissprot: TERA_HUMAN) Adjuvants, Immunologic (Code: D000276) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Antiviral Agents (Code: D000998) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Immunologic Factors (Code: D007155) Phosphodiesterase Inhibitors (Code: D010726) Protective Agents (Code: D020011)
Click to view spiperone Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) antagonist (Source: ) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: ) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: ) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Mus musculus, class: GPCR, accessions: P32304, gene: Htr7, swissprot: 5HT7R_MOUSE Dopamine receptor (Organism: Mus musculus, class: Unclassified, accessions: P30728|P51436|P61168|Q61616|Q8BLD9, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_MOUSE|DRD2_MOUSE|DRD3_MOUSE|DRD4_MOUSE|DRD5_MOUSE 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT Muscarinic acetylcholine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08482|P08483|P08485|P08911|P10980, gene: Chrm1|Chrm2|Chrm3|Chrm4|Chrm5, swissprot: ACM1_RAT|ACM2_RAT|ACM3_RAT|ACM4_RAT|ACM5_RAT 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Vesicular acetylcholine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q62666, gene: Slc18a3, swissprot: VACHT_RAT 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN Serotonin 2 (5-HT2) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P30994, gene: Htr2a|Htr2b|Htr2c, swissprot: 5HT2A_RAT|5HT2B_RAT|5HT2C_RAT 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN Dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901|P19020|P25115|P30729|P61169, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_RAT|DRD2_RAT|DRD3_RAT|DRD4_RAT|DRD5_RAT D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Serotonin 1 (5-HT1) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19327|P28564|P28565|P30940, gene: Htr1a|Htr1b|Htr1d|Htr1f, swissprot: 5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT 5-hydroxytryptamine receptor 2C (Organism: Rattus norvegicus, class: GPCR, accessions: P08909, gene: Htr2c, swissprot: 5HT2C_RAT 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT Beta-casein (Organism: Rattus norvegicus, class: Unclassified, accessions: P02665, gene: Csn2, swissprot: CASB_RAT Alpha-1A adrenergic receptor (Organism: Bos taurus, class: GPCR, accessions: P18130, gene: ADRA1A, swissprot: ADA1A_BOVIN Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT 5-hydroxytryptamine receptor 1B (Organism: Mus musculus, class: Unclassified, accessions: P28334, gene: Htr1b, swissprot: 5HT1B_MOUSE) antagonist (Source: ) 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: ) A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) psychotropic drug (Code: CHEBI:35471) dopaminergic antagonist (Code: CHEBI:48561) serotonergic antagonist (Code: CHEBI:48279) alpha-adrenergic antagonist (Code: CHEBI:37890) antipsychotic agent (Code: CHEBI:35476) 1969-01-01 YEAR INTRODUCED
Click to view ethaverine tetraethyl homolog of papaverine; smooth muscle relaxant; RN given refers to parent cpd; structure Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view quinagolide D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://pdf.hres.ca/dpd_pm/00022550.PDF) Quinagolide is a non-ergot-derived selective dopamine D2 receptor agonist used for the treatment of elevated levels of prolactin or hyperprolactinaemia. Hyperprolalctinaemia is associated with gonadal dysfunction, including infertility and reduced libido, as well as long-term complications such as osteoporosis. Quinagolide exists as a racemate and its relevant clinical activity is mediated predominantly by the (-) enantiomer. Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) 1995-02-23 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view cefalotin Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12650826) Cephalothin is a first generation, semisynthetic analogue of natural cephalosporin antibiotic. It kills susceptible bacterial cells by inhibiting cell wall synthesis. Cephalothin is indicated for the treatment of Respiratory tract infections (due to S. pneumonia, staphylococcus spp., Group A beta-hemolytic streptococcus spp., Klebsiella spp., and H.influenzae), Skin and soft tissue infections, including peritonitis (due to staphylococcus spp., Group A beta-hemolytic streptococcus spp., E. coli, P.mirabilis, and Klebsiella spp.), Genitourinary tract infections (due to E. coli, P.mirabilis, and Klebsiella spp.), Septicemia, including endocarditis, (due to S.pneumoniae, staphylococcus spp., Group A beta-hemolytic streptococcus spp., S.viridans, E. coli, P.mirabilis, and Klebsiella spp.), Meningitis (due to S.pneumoniae, Group A beta-hemolytic streptococcus spp. and staphylococcus spp., Bone and joint infections (due to staphylococcus spp.). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1974-12-18 FDA CLS
Click to view estradiol cypionate Estradiol cypionate is a pro-drug ester of Estradiol, a naturally occurring hormone that circulates endogenously within the human body. Estradiol cypionate is used for the treatment of moderate to severe vasomotor symptoms associated with menopause and for the treatment of hypoestrogenism due to hypogonadism. (See: estradiol) 1979-08-15 FDA
Click to view ergocalciferol Vitamin D 25-hydroxylase (Organism: Homo sapiens, class: Enzyme, accessions: Q6VVX0, gene: CYP2R1, swissprot: CP2R1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15465040) Ergocalciferol is a form of Vitamin D, also called vitamin D2. It is created from viosterol, which in turn is created when ultraviolet light activates ergosterol. Vitamin D2, a fat-soluble vitamin important for many biochemical processes including the absorption and metabolism of calcium and phosphorus. In vivo, ergocalciferol is formed after sun (ultraviolet) irradiation of plant-derived ergosterol, another form of vitamin D. Ergocalciferol is used in the treatment of hypcalcemia and in dialysis-dependent renal failure. Ergocalciferols (Code: N0000006337) Provitamin D2 Compound (Code: N0000175909) nutraceutical (Code: CHEBI:50733) bone density conservation agent (Code: CHEBI:50646) rodenticide (Code: CHEBI:33288) 1941-01-11 FDA D2V
Click to view diiodohydroxyquinoline Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/817025) Diiodohydroxyquinoline (uidoquinol) is one of the halogenated 8-quinolinols widely used as an intestinal antiseptic, especially as an antiamebic agent. It is also used topically in other infections and may cause CNS and eye damage. The exact mechanism of action is unknown. Amebicides (Code: D000563) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981)
Click to view pancuronium Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P17787|P43681, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) Acetylcholine receptor (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN) antagonist Acetylcholine receptor; alpha1/beta1/delta/gamma (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P07510|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND|CHRNG, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN|ACHG_HUMAN A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release. Neuromuscular Nondepolarizing Blockade (Code: N0000175732) Nondepolarizing Neuromuscular Blocker (Code: N0000175720) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) nicotinic antagonist (Code: CHEBI:48878) cholinergic antagonist (Code: CHEBI:48873) muscle relaxant (Code: CHEBI:51371) 1972-10-24 FDA
Click to view cefetamet Cefetamet is a semisynthetic, beta-lactamase-stable, third-generation cephalosporin with antibacterial activity. Cefetamet binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Cefetamet has in vitro activity against the major respiratory pathogens Streptococcus pneumoniae, Haemophilus influenzae, Moraxella (Branhamella) catarrhalis and group A beta-haemolytic streptococci; it is active against beta-lactamase-producing strains of H. influenzae and M. catarrhalis, but has poor activity against penicillin-resistant S. pneumoniae. Cefetamet has marked activity against Neisseria gonorrhoeae and possesses a broad spectrum of activity against Enterobacteriaceae. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view diperodon Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN
Click to view drotaverine Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12823389) cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20554370) an antispasmodic drug, structurally related to papaverine. Drotaverine is a selective inhibitor of phosphodiesterase 4, and has no anticholinergic effects. Drotaverine has been shown to possess dose-dependant analgesic effects in animal models. One small study has shown drotaverine to be eliminated mainly non-renally. Overdosage may cause vomiting and seizures with associated cardiac toxicity Analgesics (Code: D000700) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Vasodilator Agents (Code: D014665) 1996-07-09 Ministry of Health of the Russian Federation
Click to view sulconazole Indoleamine 2,3-dioxygenase 1 (Organism: Mus musculus, class: Enzyme, accessions: P28776, gene: Ido1, swissprot: I23O1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Indoleamine 2,3-dioxygenase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q8R0V5, gene: Ido2, swissprot: I23O2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Sulconazole is an imidazole derivative and a broad-spectrum antifungal agent intended for topical application. Sulconazole inhibits the growth of the common pathogenic dermatophytes including Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis. It also inhibits the organism responsible for tinea versicolor, Malassezia furfur, and certain gram positive bacteria. Sulconazole is indicated for the treatment of tinea cruris and tinea corporis, tinea versicolor. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 1985-08-30 FDA
Click to view melarsoprol Arsenical used in trypanosomiases. It may cause fatal encephalopathy and other undesirable side effects. Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Trypanocidal Agents (Code: D014344)
Click to view sulfasalazine ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19541926) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19541926) Proton-coupled folate transporter (Organism: Homo sapiens, class: Transporter, accessions: Q96NT5, gene: SLC46A1, swissprot: PCFT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17475902) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18819808) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18819808) Sulfasalazine is a synthetic salicylic acid derivative with affinity for connective tissues containing elastin. The mode of action of sulfasalazine (SSZ) or its metabolites, 5-aminosalicylic acid (5ASA) and sulfapyridine (SP), is still under investigation, but may be related to the anti-inflammatory and/or immunomodulatory properties. In ulcerative colitis, clinical studies utilizing rectal administration of SSZ, SP, and 5-ASA have indicated that the major therapeutic action may reside in the 5-ASA moiety. Sulfasalazine is indicated for the treatment of ulcerative colitis and rheumatoid arthritis. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Infective Agents (Code: D000890) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antiinfective agent (Code: CHEBI:35441) gastrointestinal drug (Code: CHEBI:55324) Aminosalicylate (Code: N0000175781) Aminosalicylic Acids (Code: N0000005760) 1950-06-20 FDA SAS
Click to view camostat Prothrombin (Organism: Homo sapiens, class: Enzyme, accessions: P00734, gene: F2, swissprot: THRB_HUMAN Trypsin-1 (Organism: Homo sapiens, class: Enzyme, accessions: P07477, gene: PRSS1, swissprot: TRY1_HUMAN) inhibitor Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN Plasminogen (Organism: Rattus norvegicus, class: Enzyme, accessions: Q01177, gene: Plg, swissprot: PLMN_RAT Kallikrein-1 (Organism: Homo sapiens, class: Enzyme, accessions: P06870, gene: KLK1, swissprot: KLK1_HUMAN Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN Hepatocyte growth factor activator (Organism: Homo sapiens, class: Enzyme, accessions: Q04756, gene: HGFAC, swissprot: HGFA_HUMAN Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) Trypsin Inhibitors (Code: D014361)
Click to view bisantrene NAD(P)H dehydrogenase [quinone] 1 (Organism: Homo sapiens, class: Enzyme, accessions: P15559, gene: NQO1, swissprot: NQO1_HUMAN Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) antineoplastic agent (Code: CHEBI:35610)
Click to view sunitinib Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021938s036lbl.pdf) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021938s036lbl.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021938s036lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021938s036lbl.pdf) Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021938s036lbl.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021938s036lbl.pdf) Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021938s036lbl.pdf) Macrophage colony-stimulating factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P07333, gene: CSF1R, swissprot: CSF1R_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021938s036lbl.pdf) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021938s036lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021938s036lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19773380) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19773380) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19773380) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19773380) ALK tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: Q9UM73, gene: ALK, swissprot: ALK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20117004) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24890652) Leucine-rich repeat serine/threonine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q5S007, gene: LRRK2, swissprot: LRRK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23768909) Serine/threonine-protein kinase Chk1 (Organism: Homo sapiens, class: Kinase, accessions: O14757, gene: CHEK1, swissprot: CHK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21794960 ) Serine/threonine-protein kinase Chk2 (Organism: Homo sapiens, class: Kinase, accessions: O96017, gene: CHEK2, swissprot: CHK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21794960 ) Ribosomal protein S6 kinase alpha-1 (Organism: Homo sapiens, class: Kinase, accessions: Q15418, gene: RPS6KA1, swissprot: KS6A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21794960 ) Ribosomal protein S6 kinase alpha-3 (Organism: Homo sapiens, class: Kinase, accessions: P51812, gene: RPS6KA3, swissprot: KS6A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21794960 ) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21794960 ) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21794960 ) Aurora kinase B (Organism: Homo sapiens, class: Kinase, accessions: Q96GD4, gene: AURKB, swissprot: AURKB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22560627) Focal adhesion kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q05397, gene: PTK2, swissprot: FAK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22560627) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Tyrosine-protein kinase receptor UFO (Organism: Homo sapiens, class: Kinase, accessions: P30530, gene: AXL, swissprot: UFO_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26555154) Sunitinib is an indolinone derivative and tyrosine kinase inhibitor with potential antineoplastic activity. Sunitinib inhibits multiple receptor tyrosine kinases (RTKs), some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Sunitinib is indicated for the treatment of gastrointestinal stromal tumor, advanced renal cell carcinoma, progressive, well-differentiated pancreatic neuroendocrine tumors. Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) Angiogenesis Inhibitors (Code: D020533) Angiogenesis Modulating Agents (Code: D043924) Antineoplastic Agents (Code: D000970) Growth Inhibitors (Code: D006131) Growth Substances (Code: D006133) angiogenesis inhibitor (Code: CHEBI:48422) antineoplastic agent (Code: CHEBI:35610) immunomodulator (Code: CHEBI:50846) neuroprotective agent (Code: CHEBI:63726) 2006-01-26 FDA B49
Click to view bemetizide Bemetizide is a benzothiadiazine sulfonamide derivative belonging to the class of the thiazide diuretics. It was used in combination with triamterene for the treatment of hypertension, chronic heart failure and edema.
Click to view flutropium
Click to view beraprost Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) agonist (Source: ) Prostacyclin receptor (Organism: Homo sapiens, class: GPCR, accessions: P43119, gene: PTGIR, swissprot: PI2R_HUMAN) agonist Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN) agonist (Source: ) Prostacyclin receptor (Organism: Mus musculus, class: Unclassified, accessions: P43252, gene: Ptgir, swissprot: PI2R_MOUSE) agonist (Source: ) Prostacyclin receptor (Organism: Rattus norvegicus, class: Unclassified, accessions: P43253, gene: Ptgir, swissprot: PI2R_RAT) agonist (Source: ) stable prostacyclin analog; structure given in first source Cardiovascular Agents (Code: D002317) Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) Vasodilator Agents (Code: D014665) 1992-01-01 YEAR INTRODUCED
Click to view pholcodine Analgesics (Code: D000700) Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689) antitussive (Code: CHEBI:51177) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322)
Click to view dimorpholamine analeptic properties; minor descriptor (75-83); on-line & Index Medicus search MORPHOLINES (75-83); structure PMDA
Click to view pipazetate Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141)
Click to view pentagestrone
Click to view dihydrotachysterol Vitamin D3 receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11473, gene: VDR, swissprot: VDR_HUMAN) (Source: https://www.ncbi.nlm.nih.gov/pubmed/8380156) A VITAMIN D that can be regarded as a reduction product of vitamin D2. Bone Density Conservation Agents (Code: D050071) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) bone density conservation agent (Code: CHEBI:50646) 2006-07-14 Ministry of Health of the Russian Federation
Click to view colchicine Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) Glycine receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: P23416, gene: GLRA2, swissprot: GLRA2_HUMAN) Tubulin beta-4B chain (Organism: Homo sapiens, class: Structural, accessions: P68371, gene: TUBB4B, swissprot: TBB4B_HUMAN) Tubulin (Organism: Sus scrofa, class: Structural, accessions: P02550|P02554, gene: TUBA1A, swissprot: TBA1A_PIG|TBB_PIG Tubulin alpha-1A chain (Organism: Sus scrofa, class: Structural, accessions: P02550, gene: TUBA1A, swissprot: TBA1A_PIG Tubulin beta-2B chain (Organism: Bos taurus, class: Structural, accessions: Q6B856, gene: TUBB2B, swissprot: TBB2B_BOVIN Tubulin (Organism: Bos taurus, class: Structural, accessions: Q6B856|Q862F3|Q862L2, gene: TUBB2B, swissprot: Q862F3_BOVIN|Q862L2_BOVIN|TBB2B_BOVIN Tubulin polymerization-promoting protein (Organism: Bos taurus, class: Unclassified, accessions: Q27957, gene: TPPP, swissprot: TPPP_BOVIN Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Tubulin beta chain (Organism: Homo sapiens, class: Structural, accessions: P07437, gene: TUBB, swissprot: TBB5_HUMAN) inhibitor A major alkaloid from Colchicum autumnale L. and found also in other Colchicum species. Its primary therapeutic use is in the treatment of gout, but it has been used also in the therapy of familial Mediterranean fever (PERIODIC DISEASE). Cytochrome P450 3A4 Inhibitors (Code: N0000182141) P-Glycoprotein Interactions (Code: N0000000239) Antimitotic Agents (Code: D050256) Antirheumatic Agents (Code: D018501) Gout Suppressants (Code: D006074) Mitosis Modulators (Code: D050258) Tubulin Modulators (Code: D050257) 1961-07-27 FDA LOC
Click to view ademetionine Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21846718) Adenosylmethionine is a methyl donor and a cofactor for enzyme-catalyzed methylations, including catechol O-methyltransferase and DNA methyltransferases. Although present in all cells, it is concentrated in liver where 85% of all methylation reactions occur. Adenosylmethionine is anti-apoptotic in normal hepatocytes and normal colon epithelial cells but pro-apoptotic in liver human hepatocellular carcinoma, HepG2 cells and colon cancer cells. Adenosylmethionine is used for the treatment of depression and for other medical conditions such as osteoarthritis, fibromyalgia, liver disease and migraine headaches. 2006-10-27 Ministry of Health of the Russian Federation SAM
Click to view thiethylperazine Pleiotropic ABC efflux transporter of multiple drugs (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Transporter, accessions: P33302, gene: PDR5, swissprot: PDR5_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19188399) Thiethylperazine is a piperazine phenothiazine derivative and a dopamine antagonist used as antiemetic. Thiethylperazine blocks postsynaptic dopamine 2 (D2) receptors in the medullary chemoreceptor trigger zone (CTZ), thereby decreasing stimulation of the vomiting center in the brain. Peripherally, thiethylperazine blocks the vagus nerve in the gastrointestinal tract. In addition, this agent also shows antagonistic activities mediated through muscarinic receptors, H1-receptors, and alpha(1)-receptors. Thiethylperazine is used for the treatment of the nausea and vomiting associated with anesthesia, mildly emetic cancer chemotherapy agents, radiation therapy, and toxins. Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) phenothiazine antipsychotic drug (Code: CHEBI:37930) histamine antagonist (Code: CHEBI:37956) muscarinic antagonist (Code: CHEBI:48876) serotonergic antagonist (Code: CHEBI:48279) dopaminergic antagonist (Code: CHEBI:48561) antiemetic (Code: CHEBI:50919) 1961-07-18 FDA
Click to view mepacrine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) Trypanothione reductase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P28593, gene: TPR, swissprot: TYTR_TRYCR Bacterial DNA-directed RNA polymerase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A7Z4|P0A800|P0A8T7|P0A8V2, gene: rpoA|rpoB|rpoC|rpoZ, swissprot: RPOA_ECOLI|RPOB_ECOLI|RPOC_ECOLI|RPOZ_ECOLI Major prion protein (Organism: Homo sapiens, class: Surface antigen, accessions: P04156, gene: PRNP, swissprot: PRIO_HUMAN Phospholipase A2 group 1B (Organism: Rattus norvegicus, class: Unclassified, accessions: P04055, gene: Pla2g1b, swissprot: PA21B_RAT Phospholipase A2 group 1B (Organism: Sus scrofa, class: Enzyme, accessions: P00592, gene: PLA2G1B, swissprot: PA21B_PIG Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Cholinesterase (Organism: Equus caballus, class: Enzyme, accessions: P81908, gene: BCHE, swissprot: CHLE_HORSE Riboflavin-binding protein (Organism: Gallus gallus, class: Unclassified, accessions: P02752, gene: None, swissprot: RBP_CHICK Cyclooxygenase (Organism: Bos taurus, class: Enzyme, accessions: O62664|O62698, gene: PTGS1|PTGS2, swissprot: PGH1_BOVIN|PGH2_BOVIN An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Anticestodal Agents (Code: D000923) Antimalarials (Code: D000962) Antinematodal Agents (Code: D000969) Antineoplastic Agents (Code: D000970) Antiparasitic Agents (Code: D000977) Antiplatyhelmintic Agents (Code: D000980) Antiprotozoal Agents (Code: D000981) Enzyme Inhibitors (Code: D004791) antimalarial (Code: CHEBI:38068) 1933-01-01 YEAR INTRODUCED QUN
Click to view enprostil Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) agonist (Source: ) Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: ) Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN) Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN) Prostacyclin receptor (Organism: Homo sapiens, class: GPCR, accessions: P43119, gene: PTGIR, swissprot: PI2R_HUMAN) Prostaglandin E2 receptor EP3 subtype (Organism: Rattus norvegicus, class: Unclassified, accessions: P34980, gene: Ptger3, swissprot: PE2R3_RAT) agonist (Source: ) Prostaglandin E2 receptor EP1 subtype (Organism: Rattus norvegicus, class: Unclassified, accessions: P70597, gene: Ptger1, swissprot: PE2R1_RAT) agonist (Source: ) A synthetic PGE2 analog that has an inhibitory effect on gastric acid secretion, a mucoprotective effect, and a postprandial lowering effect on gastrin. It has been shown to be efficient and safe in the treatment of gastroduodenal ulcers. Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) 1985-01-01 YEAR INTRODUCED
Click to view fominoben was MH 1975-92 (see under MORPHOLINES 1975-90); use MORPHOLINES to search FOMINOBEN 1975-92 Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141)
Click to view fursultiamine Compound used for therapy of thiamine deficiency. It has also been suggested for several non-deficiency disorders but has not yet proven useful. Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) Vitamin B Complex (Code: D014803)
Click to view beta-Ergocryptine
Click to view tiocarlide Epoxide hydrolase EphE; Hydrolase, alpha/beta hydrolase fold family (Organism: Mycobacterium tuberculosis (strain CDC 1551 / Oshkosh), class: Enzyme, accessions: O69638, gene: None, swissprot: O69638_MYCTO major descriptor (68-85); on-line search PHENYLTHIOUREA/AA (68-85); Index Medicus search THIOCARLIDE (68-85); Antitubercular Agent Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antitubercular Agents (Code: D000995)
Click to view gefarnate A water insoluble terpene fatty acid used in the treatment of gastrointestinal ulcers; it facilitates the healing and function of mucosal tissue. Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765)
Click to view calcifediol Vitamin D3 receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11473, gene: VDR, swissprot: VDR_HUMAN) agonist The major circulating metabolite of VITAMIN D3. It is produced in the LIVER and is the best indicator of the body's vitamin D stores. It is effective in the treatment of RICKETS and OSTEOMALACIA, both in azotemic and non-azotemic patients. Calcifediol also has mineralizing properties. Bone Density Conservation Agents (Code: D050071) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) bone density conservation agent (Code: CHEBI:50646) nutraceutical (Code: CHEBI:50733) 1980-08-05 FDA VDY
Click to view alfacalcidol Alfacalcidol is a synthetic vitamin D analogue. Alfacalcidol is a pro-drug that exerts its action after it has been metabolised to calcitriol, mainly in the liver. (See: calcitriol) Alfacalcidol is indicated in all conditions where there is a disturbance of calcium metabolism due to impaired 1-? hydroxylation such as when there is reduced renal function. The main indications are renal osteodystrophy, hyperparathyroidism (with bone disease), hypoparathyroidism, neonatal hypocalcaemia, nutritional and malabsorptive rickets and osteomalacia, pseudo-deficiency (D-dependent) rickets and osteomalacia, hypophosphataemic vitamin D resistant rickets and osteomalacia. Bone Density Conservation Agents (Code: D050071) bone density conservation agent (Code: CHEBI:50646) 1978-08-04 Ministry of Health, Welfare and Sport (Netherlands)
Click to view mometasone furoate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9793625) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15601807) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209310s001lbl.pdf) Mometasone furoate is a corticosteroid demonstrating anti-inflammatory, antipruritic, and vasoconstrictive properties. The precise mechanism of corticosteroid action is not known. Mometasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor. Mometasone furoate is indicated for the maintenance treatment of asthma as prophylactic therapy and allergic rhinitis. It is also used as a topical treatment for skin disorders. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Anti-Allergic Agents (Code: D018926) Anti-Inflammatory Agents (Code: D000893) Dermatologic Agents (Code: D003879) anti-inflammatory drug (Code: CHEBI:35472) anti-allergic agent (Code: CHEBI:50857) 1987-04-30 FDA MOF
Click to view oxyphenisatine acetate A laxative that undergoes enterohepatic circulation. It may cause jaundice. Cathartics (Code: D002400) Gastrointestinal Agents (Code: D005765)
Click to view moxifloxacin DNA topoisomerase 4 subunit A (Organism: Staphylococcus aureus, class: Enzyme, accessions: P0C1U9, gene: parC, swissprot: PARC_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022428s009lbl.pdf) DNA gyrase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES4|P0AES6, gene: gyrA|gyrB, swissprot: GYRA_ECOLI|GYRB_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022428s009lbl.pdf) Topoisomerase IV (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AFI2|P20083, gene: parC|parE, swissprot: PARC_ECOLI|PARE_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022428s009lbl.pdf) DNA gyrase subunit A (Organism: Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd), class: Enzyme, accessions: P43700, gene: gyrA, swissprot: GYRA_HAEIN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022428s009lbl.pdf) DNA gyrase subunit A (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WG47, gene: gyrA, swissprot: GYRA_MYCTU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022428s009lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily KQT member 1 (Organism: Homo sapiens, class: Ion channel, accessions: P51787, gene: KCNQ1, swissprot: KCNQ1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Moxifloxacin is a member of the fluoroquinolone class of anti-infective drugs. The antibacterial action of moxifloxacin results from inhibition of the topoisomerase II (DNA gyrase) and topoisomerase IV. Moxifloxacin has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections: Aerococcus viridans, Corynebacterium macginleyi, Enterococcus faecalis, Micrococcus luteus, Staphylococcus arlettae, Staphylococcus aureus, Staphylococcus capitis, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus, Staphylococcus warneri, Streptococcus mitis, Streptococcus pneumoniae, Streptococcus parasanguinis, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Propionibacterium acnes and Chlamydia trachomatis. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antibacterial drug (Code: CHEBI:36047) Quinolone Antimicrobial (Code: N0000175937) Quinolones (Code: N0000007606) 1999-12-10 FDA MFX
Click to view oxacillin Penicillin-binding protein 2B (Organism: Streptococcus pneumoniae (strain ATCC BAA-255 / R6), class: Enzyme, accessions: P0A3M6, gene: penA, swissprot: PBP2_STRR6) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7447421) Penicillin-binding protein 1A (Organism: Streptococcus pneumoniae (strain ATCC BAA-255 / R6), class: Enzyme, accessions: Q8DR59, gene: pbpA, swissprot: PBPA_STRR6) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7447421) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 15 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63424, gene: Slc15a2, swissprot: S15A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Oxacillin is a semisynthetic penicillinase-resistant and acid-stable penicillin with an antimicrobial activity. Oxacillin binds to penicillin-binding proteins in the bacterial cell wall, thereby blocking the synthesis of peptidoglycan, a critical component of the bacterial cell wall. This leads to inhibition of cell growth and causes cell lysis. Oxacillin is used in the treatment of resistant staphylococci infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) Penicillin-class Antibacterial (Code: N0000175497) Penicillins (Code: N0000011281) 1971-04-08 FDA
Click to view amperozide 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Fatty-acid amide hydrolase 1 (Organism: Homo sapiens, class: Enzyme, accessions: O00519, gene: FAAH, swissprot: FAAH1_HUMAN Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Tranquilizing Agents (Code: D014149)
Click to view pipamazine D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) Membrane-associated progesterone receptor component 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: P70580, gene: Pgrmc1, swissprot: PGRC1_RAT) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT
Click to view prednisolone acetate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Anti-Inflammatory Agents (Code: D000893) 1955-05-22 FDA
Click to view cinitapride Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765)
Click to view dehydrocholic acid A semisynthetic bile acid made from cholic acid. It is used as a cholagogue, hydrocholeretic, diuretic, and as a diagnostic aid. Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765) gastrointestinal drug (Code: CHEBI:55324)
Click to view ethinylestradiol sulfonate
Click to view sulforidazine D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Antidepressive Agents (Code: D000928) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view metergoline 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: ) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) antagonist (Source: ) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) Substance-K receptor (Organism: Homo sapiens, class: GPCR, accessions: P21452, gene: TACR2, swissprot: NK2R_HUMAN) 5-hydroxytryptamine receptor 4 (Organism: Cavia porcellus, class: GPCR, accessions: O70528, gene: HTR4, swissprot: 5HT4R_CAVPO) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN Serotonin 2 (5-HT2) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P30994, gene: Htr2a|Htr2b|Htr2c, swissprot: 5HT2A_RAT|5HT2B_RAT|5HT2C_RAT 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN Serotonin 1 (5-HT1) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19327|P28564|P28565|P30940, gene: Htr1a|Htr1b|Htr1d|Htr1f, swissprot: 5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT 5-hydroxytryptamine receptor 7 (Organism: Mus musculus, class: GPCR, accessions: P32304, gene: Htr7, swissprot: 5HT7R_MOUSE) antagonist (Source: ) A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy. Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) serotonergic antagonist (Code: CHEBI:48279) dopamine agonist (Code: CHEBI:51065)
Click to view tipranavir Pol polyprotein (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72874, gene: pol, swissprot: Q72874_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022292s010lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022292s010lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022292s010lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022292s010lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21861202) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20507927) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Tipranavir is a sulfonamide-containing dyhydropyrone and a nonpeptidic protease inhibitor that targets the HIV protease. Tipranavir and ritonavir are coadministered to treat HIV. Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) antiviral drug (Code: CHEBI:36044) HIV Protease Inhibitors (Code: N0000000246) Protease Inhibitor (Code: N0000175889) 2005-06-22 FDA TPV
Click to view delmadinone acetate Androgen Antagonists (Code: D000726) Hormone Antagonists (Code: D006727) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Progestins (Code: D011372)
Click to view lorajmine A monochloroacetyl derivative of ajmaline. It is a class Ia antiarrhythmic agent that is rapidly hydrolyzed to ajmaline by plasma and tissue esterases. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317)
Click to view clocinizine
Click to view roflumilast Phosphodiesterase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27815|Q07343|Q08493|Q08499, gene: PDE4A|PDE4B|PDE4C|PDE4D, swissprot: PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022522s009lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022522s009lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022522s009lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) weak inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022522s009lbl.pdf) Roflumilast is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3',5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling. cAMP prevents phosphorylation of spleen tyrosine kinase (SYK) and abrogates activation of the PI3K/AKT/mTOR signaling pathway, which may result in the induction of apoptosis. PDE4, a member of the PDE superfamily that hydrolyses cAMP and 3',5'-cyclic guanosine monophosphate (cGMP) to their inactive 5' monophosphates, is upregulated in a variety of cancers and may contribute to chemoresistance; it also plays a key role in inflammation, especially in inflammatory airway diseases. Roflumilast is used to treat and prevent exacerbations of chronic obstructive pulmonary disease. anti-asthmatic drug (Code: CHEBI:49167) Phosphodiesterase 4 Inhibitor (Code: N0000182961) Phosphodiesterase 4 Inhibitors (Code: N0000182960) 2011-02-28 FDA ROF
Click to view phthalylsulfathiazole Phthalylsulfathiazole is a sulfonamide antibiotic which is used for the treatment of dysentery, diarrhea and other intestinal fluxes. It inhibits dihydropteroate synthetase activity of bacteria. Phthalylsulfadiazine is effective against S. enteritidis and the Hiss, Flexner and Sonne strains of Shigella and Shiga strain. Sulfonamide (Code: N0000175880) Sulfonamides (Code: N0000008048) antibacterial drug (Code: CHEBI:36047) 1964-04-30 Ministry of Health of the Russian Federation
Click to view aminoxytriphene
Click to view perphenazine D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23675993) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20853847) Pleiotropic ABC efflux transporter of multiple drugs (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Transporter, accessions: P33302, gene: PDR5, swissprot: PDR5_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19188399) Pleiotropic ABC efflux transporter of multiple drugs CDR1 (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Transporter, accessions: Q5ANA3, gene: CDR1, swissprot: CDR1_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19188399) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Perphenazine is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties. Perphenazine is used for the management of the manifestations of psychotic disorders and for the control of severe nausea and vomiting in adults. Phenothiazine (Code: N0000175746) Phenothiazines (Code: N0000007544) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) dopaminergic antagonist (Code: CHEBI:48561) antiemetic (Code: CHEBI:50919) phenothiazine antipsychotic drug (Code: CHEBI:37930) 1957-02-27 FDA
Click to view alpidem Translocator protein (Organism: Rattus norvegicus, class: Membrane receptor, accessions: P16257, gene: Tspo, swissprot: TSPO_RAT GABA-A receptor; anion channel (Organism: Rattus norvegicus, class: Ion channel, accessions: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14, gene: Gabra1|Gabra2|Gabra3|Gabra4|Gabra5|Gabra6|Gabrb1|Gabrb2|Gabrb3|Gabrd|Gabre|Gabrg1|Gabrg2|Gabrg3|Gabrp|Gabrq, swissprot: GBRA1_RAT|GBRA2_RAT|GBRA3_RAT|GBRA4_RAT|GBRA5_RAT|GBRA6_RAT|GBRB1_RAT|GBRB2_RAT|GBRB3_RAT|GBRD_RAT|GBRE_RAT|GBRG1_RAT|GBRG2_RAT|GBRG3_RAT|GBRP_RAT|Q91ZM7_RAT Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1991-01-01 YEAR INTRODUCED
Click to view tosufloxacin quinolone anti-infective agent; structure given in first source antiinfective agent (Code: CHEBI:35441)
Click to view bentiromide chymotrypsin labile peptide used diagnostically as an index of exocrine pancreas function Indicators and Reagents (Code: D007202) reagent (Code: CHEBI:33893) indicator (Code: CHEBI:47867) diagnostic agent (Code: CHEBI:33295) 1983-12-29 FDA
Click to view nicocodine
Click to view aldesulfone Aldesulfone (sulfoxone) is a water-soluble sulfone used as an antileprosy drug. Sulfoxone is a competitive inhibitor of bacterial enzyme dihydropteroate synthetase. The normal substrate for the enzyme, para-aminobenzoic acid (PABA) cannot bind as usual. The inhibited reaction is necessary in these organisms for the synthesis of folic acid. Aldesulfone was used as an antileprosy drug, for treatment of dermatitis herpetiformis, and to treat pulmonary tuberculosis. Presently, usage of aldesulfone has been discontinued. 1974-05-24 FDA
Click to view sulfinpyrazone fMet-Leu-Phe receptor (Organism: Homo sapiens, class: GPCR, accessions: P21462, gene: FPR1, swissprot: FPR1_HUMAN) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) Solute carrier family 22 member 12 (Organism: Homo sapiens, class: Transporter, accessions: Q96S37, gene: SLC22A12, swissprot: S22AC_HUMAN) inhibitor A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties. Antirheumatic Agents (Code: D018501) Gout Suppressants (Code: D006074) Renal Agents (Code: D012076) Uricosuric Agents (Code: D014528) uricosuric drug (Code: CHEBI:35841) 1959-05-13 FDA
Click to view flunarizine Cannabinoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P21554, gene: CNR1, swissprot: CNR1_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Membrane-associated progesterone receptor component 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: P70580, gene: Pgrmc1, swissprot: PGRC1_RAT) Sodium channel protein type 1 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35498, gene: SCN1A, swissprot: SCN1A_HUMAN) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) blocker Voltage-dependent T-type calcium channel subunit alpha-1I (Organism: Homo sapiens, class: Ion channel, accessions: Q9P0X4, gene: CACNA1I, swissprot: CAC1I_HUMAN) blocker Voltage-dependent T-type calcium channel subunit alpha-1G (Organism: Homo sapiens, class: Ion channel, accessions: O43497, gene: CACNA1G, swissprot: CAC1G_HUMAN) blocker Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Rattus norvegicus, class: Ion channel, accessions: P04774|P04775|P08104, gene: Scn1a|Scn2a|Scn3a, swissprot: SCN1A_RAT|SCN2A_RAT|SCN3A_RAT Voltage-dependent N-type calcium channel subunit alpha-1B (Organism: Homo sapiens, class: Ion channel, accessions: Q00975, gene: CACNA1B, swissprot: CAC1B_HUMAN D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT Sodium channel protein type 2 subunit alpha (Organism: Rattus norvegicus, class: Ion channel, accessions: P04775, gene: Scn2a, swissprot: SCN2A_RAT CAAX prenyl protease 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y256, gene: RCE1, swissprot: FACE2_HUMAN 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT CAAX prenyl protease 2 (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Unclassified, accessions: Q03530, gene: RCE1, swissprot: RCE1_YEAST Flunarizine is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy. Anticonvulsants (Code: D000927) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665)
Click to view benzquinamide Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: ) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: ) antiemetic (Code: CHEBI:50919) sedative (Code: CHEBI:35717) H1-receptor antagonist (Code: CHEBI:37955) muscarinic antagonist (Code: CHEBI:48876) antipsychotic agent (Code: CHEBI:35476) 1974-03-12 FDA
Click to view lovastatin 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Organism: Homo sapiens, class: Enzyme, accessions: P04035, gene: HMGCR, swissprot: HMDH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021316s035lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15601807) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11474784) Solute carrier organic anion transporter family member 1A4 (Organism: Rattus norvegicus, class: Transporter, accessions: O35913, gene: Slco1a4, swissprot: SO1A4_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10601278) Acyl-CoA:cholesterol acyltransferase (Organism: Oryctolagus cuniculus, class: Unclassified, accessions: Q95214, gene: ACAT, swissprot: Q95214_RABIT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17275297) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15616150) Histone deacetylase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBN7, gene: HDAC6, swissprot: HDAC6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23570542) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23570542) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23570542) A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver. HMG-CoA Reductase Inhibitor (Code: N0000175589) Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Hydroxymethylglutaryl-CoA Reductase Inhibitors (Code: D019161) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) prodrug (Code: CHEBI:50266) anticholesteremic drug (Code: CHEBI:35821) antineoplastic agent (Code: CHEBI:35610) 1987-08-31 FDA 803
Click to view mepitiostane orally active anti-estrogenic steroid; RN refers to (2alpha,3alpha,5alpha,17beta)-isomer; structure Anabolic Agents (Code: D045930) Antineoplastic Agents (Code: D000970) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view chlormadinone Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Sodium/potassium-transporting ATPase subunit alpha-2 (Organism: Sus scrofa, class: Ion channel, accessions: D2WKD8, gene: ATP1A2, swissprot: AT1A2_PIG) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) An orally active synthetic progestational hormone used often in combinations as an oral contraceptive. Androgen Antagonists (Code: D000726) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Reproductive Control Agents (Code: D012102)
Click to view taltirelin Thyrotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P34981, gene: TRHR, swissprot: TRFR_HUMAN) agonist (Source: https://pubmed.ncbi.nlm.nih.gov/23087672/) Taltirelin is a synthetic thyrotropin-releasing hormone (TRH) analog. Taltirelin mimics the physiological actions of TRH, but with a much longer half-life and duration of effects, and little development of tolerance following prolonged dosing. Taltirelin has nootropic, neuroprotective and analgesic effects. It is used for the treatment of ataxia in neurodegenerative diseases. Central Nervous System Agents (Code: D002491) Nootropic Agents (Code: D018697) 2000-09-01 PMDA
Click to view cefaloglycin Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor A cephalorsporin antibiotic. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1970-06-12 FDA
Click to view nebivolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021742s022lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20095790) Potassium channel subfamily E member 1 (Organism: Homo sapiens, class: Ion channel, accessions: P15382, gene: KCNE1, swissprot: KCNE1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily KQT member 1 (Organism: Homo sapiens, class: Ion channel, accessions: P51787, gene: KCNQ1, swissprot: KCNQ1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Nebivolol is a beta-1 adrenergic receptor antagonist with antihypertensive and vasodilatory activity. Nebivolol is indicated for the treatment of hypertension. Adrenergic beta-Antagonists (Code: N0000000161) beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-1 Receptor Agonists (Code: D058665) Adrenergic beta-Agonists (Code: D000318) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) beta-adrenergic antagonist (Code: CHEBI:35530) vasodilator agent (Code: CHEBI:35620) antihypertensive agent (Code: CHEBI:35674) 2007-12-17 FDA
Click to view hexachlorophene Hexachlorophene is an organochlorine compound that was once widely used as a disinfectant. Exact mechanism of action unknown, but at low concentrations appears to interrupt bacterial electron transport and inhibit membrane-bound enzymes. Higher concentrations rupture bacterial membranes. It induces leakage, causes protoplast lysis, and inhibits respiration. In medicine, hexachlorophene is a useful as a topical anti-infective, anti-bacterial agent, often used in soaps and toothpaste. It is also used in agriculture as a soil fungicide, plant bactericide, and acaricide. Antiseptic (Code: N0000175486) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) antiseptic drug (Code: CHEBI:48218) acaricide (Code: CHEBI:22153) antifungal agrochemical (Code: CHEBI:86328) 1949-04-19 FDA H3P
Click to view imidapril Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 1993-01-01 YEAR INTRODUCED
Click to view febarbamate
Click to view nifekalant Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317)
Click to view lisinopril Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019777s076lbl.pdf) One of the angiotensin-converting enzyme inhibitors, orally active, that has been used in the treatment of hypertension and congestive heart failure. Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) Protective Agents (Code: D020011) antihypertensive agent (Code: CHEBI:35674) 1987-12-29 FDA LPR
Click to view astromicin Astromicin is an aminoglycoside antibiotic isolated from Micromonospora olivasterospora with antibacterial activity. It is effective against major gram-negative bacterias such as Proteus, Serratia, Citrobacter, Enterobacter spp., Klebsiella, Escherichia coli and Staphylococcus aureus.
Click to view mazaticol
Click to view morclofone
Click to view toremifene Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020497s009lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020497s009lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020497s009lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/7914405) Metastatic Breast Cancer Estrogen Agonist/Antagonist (Code: N0000175826) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Bone Density Conservation Agents (Code: D050071) Estrogen Receptor Modulators (Code: D020847) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Selective Estrogen Receptor Modulators (Code: D020845) antineoplastic agent (Code: CHEBI:35610) estrogen antagonist (Code: CHEBI:50837) bone density conservation agent (Code: CHEBI:50646) estrogen receptor modulator (Code: CHEBI:50739) 1997-05-29 FDA T0R
Click to view clomifene Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20379036) Clomiphene is a triphenylethylene nonsteroidal ovulatory stimulant evaluated for antineoplastic activity against breast cancer. Clomiphene has both estrogenic and anti-estrogenic activities that compete with estrogen for binding at estrogen receptor sites in target tissues. This agent causes the release of the pituitary gonadotropins follicle stimulating hormone and luteinizing hormone, leading to ovulation. Estrogen Agonist/Antagonist (Code: N0000175826) Estrogen Antagonists (Code: D004965) Estrogen Receptor Modulators (Code: D020847) Fertility Agents (Code: D005299) Fertility Agents, Female (Code: D005300) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Reproductive Control Agents (Code: D012102) Selective Estrogen Receptor Modulators (Code: D020845) anti-estrogen (Code: CHEBI:50751) 1967-02-01 FDA
Click to view floctafenine Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/23755755) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/23755755) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view penamecillin antibacterial drug (Code: CHEBI:36047) prodrug (Code: CHEBI:50266)
Click to view carvedilol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15655528) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15655528) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15655528) NADH dehydrogenase [ubiquinone] 1 subunit C2 (Organism: Rattus norvegicus, class: Enzyme, accessions: Q5PQZ9, gene: Ndufc2, swissprot: Q5PQZ9_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10666308) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11164846) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15306222) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15306222) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15306222) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15306222) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15306222) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15306222) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15306222) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15306222) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10571255) Carvedilol is a synthetic antihypertensive methoxyphenoxy- 2-propanol derivative with no intrinsic sympathomimetic activity, Carvedilol acts as a nonselective beta-adrenoceptor blocking agent (S(-) enantiomer) and as an alpha 1-adrenoceptor blocker (R(+) and S(-) enantiomers). Its acts more strongly on beta-receptors than on alpha 1-receptors, reduces peripheral vascular resistance by vasodilation, and prevents reflex tachycardia (beta-blockade) so that heart rate is either unchanged or decreased. Carvedilol also reduces renin release through beta-blockade. Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) vasodilator agent (Code: CHEBI:35620) cardiovascular drug (Code: CHEBI:35554) beta-adrenergic antagonist (Code: CHEBI:35530) antihypertensive agent (Code: CHEBI:35674) alpha-adrenergic antagonist (Code: CHEBI:37890) Adrenergic beta1-Antagonists (Code: N0000009923) Adrenergic beta2-Antagonists (Code: N0000009924) alpha-Adrenergic Blocker (Code: N0000175553) beta-Adrenergic Blocker (Code: N0000175556) 1995-09-14 FDA CVD
Click to view alacepril Alacepril is a long-acting, sulfhydryl-containing angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, alacepril is rapidly metabolized to captopril; captopril competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. Alacepril is indicated for the treatment of essential and renal hypertension. (See: captopril) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor (Code: CHEBI:35457) 1988-06-01 PMDA
Click to view lincomycin 23S rRNA (Organism: Staphylococcus aureus, class: Ribosomal protein, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050317s183lbl.pdf) 23S rRNA (Organism: Streptococcus pneumoniae, class: Ribosomal protein, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050317s183lbl.pdf) An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) 1964-12-29 FDA 3QB
Click to view nandrolone phenpropionate Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) Anabolic Agents (Code: D045930) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1959-10-30 FDA
Click to view sitagliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021995s045lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021995s045lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021995s045lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021995s045lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021995s045lbl.pdf) Dipeptidyl peptidase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q6V1X1, gene: DPP8, swissprot: DPP8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17434732) Dipeptidyl peptidase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q86TI2, gene: DPP9, swissprot: DPP9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25164763) Prolyl endopeptidase FAP (Organism: Homo sapiens, class: Enzyme, accessions: Q12884, gene: FAP, swissprot: SEPR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25164763) Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses. Dipeptidyl Peptidase 4 Inhibitor (Code: N0000175913) Dipeptidyl Peptidase 4 Inhibitors (Code: N0000175912) Dipeptidyl-Peptidase IV Inhibitors (Code: D054873) Enzyme Inhibitors (Code: D004791) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Hypoglycemic Agents (Code: D007004) Incretins (Code: D054795) Protease Inhibitors (Code: D011480) hypoglycemic agent (Code: CHEBI:35526) 2006-10-16 FDA 715
Click to view trifluoperazine D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9015795) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1262953) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1262953) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1262953) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991983) Beta-glucuronidase (Organism: Rattus norvegicus, class: Enzyme, accessions: P06760, gene: Gusb, swissprot: BGLR_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15013012) Lysozyme C-1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P00697, gene: Lyz1, swissprot: LYSC1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15013012) Trypanothione reductase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P28593, gene: TPR, swissprot: TYTR_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9457238) Trifluoperazine is a phenothiazine derivative and a dopamine antagonist with antipsychotic and antiemetic activities. Trifluoperazine exerts its antipsychotic effect by blocking central dopamine receptors, thereby preventing effects such as delusions and hallucinations caused by an excess of dopamine. Trifluoperazine is indicated for the management of anxiety states, depressive symptoms secondary to anxiety, agitation and for the treatment of symptoms and prevention of relapse in schizophrenia and in other psychoses, especially of the paranoid type, but not in depressive psychoses. It is also indicated in the symptomatic treatment of nausea and vomiting. It may also be used as an adjunct in the short-term management of severe psychomotor agitation and of dangerously impulsive behaviour in, for example, mental subnormality. Phenothiazine (Code: N0000175746) Phenothiazines (Code: N0000007544) Antiemetics (Code: D000932) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) dopaminergic antagonist (Code: CHEBI:48561) antiemetic (Code: CHEBI:50919) phenothiazine antipsychotic drug (Code: CHEBI:37930) 1959-04-16 FDA TFP
Click to view bidisomide Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317)
Click to view ethyl biscoumacetate Vitamin K epoxide reductase complex subunit 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BQB6, gene: VKORC1, swissprot: VKOR1_HUMAN) A coumarin that is used as an anticoagulant. It has actions similar to those of WARFARIN. (From Martindale, The Extra Pharmacopoeia, 30th ed, p226) Anticoagulants (Code: D000925) Hematologic Agents (Code: D006401)
Click to view tamsulosin Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020579s033lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020579s033lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020579s033lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27709945) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27709945) Tamsulosin, an alpha1 adrenoceptor blocking agent, exhibits selectivity for alpha1 receptors in the human prostate. Tamsulosin is used for the treatment of prostatic hyperplasia, chronic prostatitis, urinary retention, and help with the passage of kidney stones. alpha-Adrenergic Blocker (Code: N0000175553) Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Neurotransmitter Agents (Code: D018377) Urological Agents (Code: D064804) antineoplastic agent (Code: CHEBI:35610) alpha-adrenergic antagonist (Code: CHEBI:37890) 1997-04-15 FDA
Click to view omapatrilat Angiotensin-converting enzyme (Organism: Oryctolagus cuniculus, class: Enzyme, accessions: P12822, gene: ACE, swissprot: ACE_RABIT Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN Neprilysin (Organism: Homo sapiens, class: Enzyme, accessions: P08473, gene: MME, swissprot: NEP_HUMAN Neprilysin (Organism: Rattus norvegicus, class: Enzyme, accessions: P07861, gene: Mme, swissprot: NEP_RAT Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) Vasopeptidase Inhibitors (Code: D000075563)
Click to view cholic acid G-protein coupled bile acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDU6, gene: GPBAR1, swissprot: GPBAR_HUMAN) agonist (Source: ) A major primary bile acid produced in the liver and usually conjugated with glycine or taurine. It facilitates fat absorption and cholesterol excretion. Bile Acid (Code: N0000175802) Bile Acids and Salts (Code: N0000006801) 2013-09-12 EMA
Click to view quingestanol acetate Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: http://www.kegg.jp/entry/D05679)
Click to view miltefosine RAC-alpha serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P31749, gene: AKT1, swissprot: AKT1_HUMAN Dual specificity phosphatase Cdc25A (Organism: Homo sapiens, class: Enzyme, accessions: P30304, gene: CDC25A, swissprot: MPIP1_HUMAN hexadecyl phosphocholine derivative of cisplatin; did not substantially activate HIV long terminal repeat; less toxic than cisplatin Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antineoplastic Agents (Code: D000970) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) immunomodulator (Code: CHEBI:50846) anti-inflammatory agent (Code: CHEBI:67079) antineoplastic agent (Code: CHEBI:35610) antiprotozoal drug (Code: CHEBI:35820) Antileishmanial (Code: N0000190851) 2014-03-19 FDA
Click to view amlodipine Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019787s062lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019787s062lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/24301608) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/24301608) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10805063) Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Levamlodipine (S-amlodipine) is a pharmacologically active enantiomer of amlodipine. As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity. Amlodipine is indicated for the treatment of hypertension, chronic stable angina, confirmed or suspected vasospastic angina as monotherapy or in combination with other antianginal agents. Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) Calcium Channel Antagonists (Code: N0000000069) Dihydropyridine Calcium Channel Blocker (Code: N0000175421) Dihydropyridines (Code: N0000007556) 1992-07-31 FDA 6UB
06X
Click to view beclometasone dipropionate Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202813s011lbl.pdf) Beclomethasone dipropionate is an anti-inflammatory steroid and a di-ester of beclomethasone (a synthetic corticosteroid chemically related to dexamethasone). Beclomethasone dipropionate is a prodrug. Beclomethasone-17-monopropionate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor. Beclomethasone dipropionate is indicated for the treatment of nasal symptoms associated with seasonal and perennial allergic rhinitis. (See: beclomethasone) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Asthmatic Agents (Code: D018927) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Respiratory System Agents (Code: D019141) anti-asthmatic drug (Code: CHEBI:49167) prodrug (Code: CHEBI:50266) anti-arrhythmia drug (Code: CHEBI:38070) anti-inflammatory drug (Code: CHEBI:35472) 1976-05-12 FDA
Click to view trifluperidol D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN C-8 sterol isomerase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P32352, gene: ERG2, swissprot: ERG2_YEAST 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Organism: Homo sapiens, class: Enzyme, accessions: Q15125, gene: EBP, swissprot: EBP_HUMAN Sigma non-opioid intracellular receptor 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: Q9R0C9, gene: Sigmar1, swissprot: SGMR1_RAT A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in the treatment of PSYCHOSES including MANIA and SCHIZOPHRENIA. (From Martindale, The Extra Pharmacopoeia, 30th ed, p621) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view ezetimibe Ezetimibe-glucuronide: Niemann-Pick C1-like protein 1 (Organism: Homo sapiens, class: Membrane other, accessions: Q9UHC9, gene: NPC1L1, swissprot: NPCL1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021445s033lbl.pdf) Ezetimibe: UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21368751) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21368751) Canalicular multispecific organic anion transporter 1 (Organism: Mus musculus, class: Transporter, accessions: Q8VI47, gene: Abcc2, swissprot: MRP2_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19443695) Canalicular multispecific organic anion transporter 2 (Organism: Mus musculus, class: Transporter, accessions: B2RX12, gene: Abcc3, swissprot: MRP3_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19443695) Broad substrate specificity ATP-binding cassette transporter ABCG2 (Organism: Homo sapiens, class: Transporter, accessions: Q7TMS5, gene: Abcg2, swissprot: ABCG2_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19443695) An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS. Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) anticholesteremic drug (Code: CHEBI:35821) antilipemic drug (Code: CHEBI:35679) Decreased Cholesterol Absorption (Code: N0000008553) Dietary Cholesterol Absorption Inhibitor (Code: N0000175911) 2002-10-25 FDA
Click to view benexate
Click to view butaperazine
Click to view flecainide Potassium voltage-gated channel subfamily A member 7 (Organism: Homo sapiens, class: Ion channel, accessions: Q96RP8, gene: KCNA7, swissprot: KCNA7_HUMAN) blocker (Source: ) Potassium voltage-gated channel subfamily A member 5 (Organism: Homo sapiens, class: Ion channel, accessions: P22460, gene: KCNA5, swissprot: KCNA5_HUMAN) blocker (Source: ) Sodium channel protein type 4 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35499, gene: SCN4A, swissprot: SCN4A_HUMAN) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y3Q4, gene: HCN4, swissprot: HCN4_HUMAN) Potassium voltage-gated channel subfamily D member 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q63881, gene: Kcnd2, swissprot: KCND2_RAT Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Potassium voltage-gated channel subfamily C member 1 (Organism: Mus musculus, class: Unclassified, accessions: P15388, gene: Kcnc1, swissprot: KCNC1_MOUSE) blocker (Source: ) A potent anti-arrhythmia agent, effective in a wide range of ventricular and atrial ARRHYTHMIAS and TACHYCARDIAS. Antiarrhythmic (Code: N0000175426) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) anti-arrhythmia drug (Code: CHEBI:38070) 1985-10-31 FDA
Click to view sitafloxacin DNA gyrase subunit B (Organism: Escherichia coli O157:H7, class: Enzyme, accessions: P0AES7, gene: gyrB, swissprot: GYRB_ECO57) DNA topoisomerase 4 subunit A (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: P72525, gene: parC, swissprot: PARC_STRPN) Sitafloxacin hydrate is a fluoroquinolone antibiotic. It is indicated for the treatment of various infections such as respiratory infection, urologic infection, gynecologic infection, otorhinological infections, and dental infection. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 2008-01-25 PMDA
Click to view ceftibuten Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12415572) Ceftibuten is a semisynthetic third-generation cephalosporin antibiotic. Ceftibuten exerts its bactericidal action by binding to essential target proteins of the bacterial cell wall. This binding leads to inhibition of cell-wall synthesis. Ceftibuten is stable in the presence of most plasmid-mediated beta-lactamases, but it is not stable in the presence of chromosomally-mediated cephalosporinases produced in organisms such as Bacteroides, Citrobacter, Enterobacter, Morganella, and Serratia. Ceftibuten has been shown to be active against Streptococcus pneumoniae (penicillin-susceptible strains only), Streptococcus pyogenes, Haemophilus influenzae, Moraxella catarrhalis. Ceftibuten is inactive in vitro against Acinetobacter, Bordetella, Campylobacter, Enterobacter, Enterococcus, Flavobacterium, Hafnia, Listeria, Pseudomonas, Staphylococcus, and Streptococcus (except pneumoniae and pyogenes) species. In addition, it shows little in vitro activity against most anaerobes, including most species of Bacteroides. Ceftibuten is used for the treatment of Acute Bacterial Exacerbations of Chronic Bronchitis, Acute Bacterial Otitis Media, Pharyngitis and Tonsillitis. Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1995-12-20 FDA
Click to view risperidone 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: ) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020272s082,020588s070,021444s056lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10048600) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9760039) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18448342) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23812503) Voltage-dependent calcium channel subunit alpha-2/delta-1 (Organism: Homo sapiens, class: Ion channel, accessions: P54289, gene: CACNA2D1, swissprot: CA2D1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23812503) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23812503) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15821958) Risperidone is a benzisoxazole derivative with antipsychotic property. Risperidone selectively antagonizes serotonin (5-HT) effects via cortical 5-HT2 receptor, and, to a lesser extent, competes with dopamine at the limbic dopamine D2 receptor. The antagonism leads to decreased psychotic effects, such as hallucinations and delusions. Risperidone is a monoaminergic antagonist with high affinity for the serotonin Type 2, dopamine Type 2, alpha1 and alpha2 adrenergic, and H1 histaminergic receptors. Risperidone showed low to moderate affinity for the serotonin 5HT1C, 5HT1D, and 5HT1A receptors, weak affinity for the dopamine D1 and haloperidol-sensitive sigma site, and no affinity for cholinergic muscarinic or alpha1 and alpha2 adrenergic receptors. Risperidone is indicated for the treatment of schizophrenia, as monotherapy or adjunctive therapy with lithium or valproate, for the treatment of acute manic or mixed episodes associated with Bipolar I Disorder and for the treatment of irritability associated with autistic disorder. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Tranquilizing Agents (Code: D014149) dopaminergic antagonist (Code: CHEBI:48561) psychotropic drug (Code: CHEBI:35471) second generation antipsychotic (Code: CHEBI:65191) serotonergic antagonist (Code: CHEBI:48279) alpha-adrenergic antagonist (Code: CHEBI:37890) H1-receptor antagonist (Code: CHEBI:37955) Atypical Antipsychotic (Code: N0000175430) 1993-12-29 FDA 8NU
Click to view cinepazide Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view ornoprostil
Click to view methestrol dipropionate
Click to view piperacetazine was MH 1975-91 (see under PHENOTHIAZINE TRANQUILIZERS 1975-90) 1969-02-03 FDA
Click to view norethindrone enanthate Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Reproductive Control Agents (Code: D012102)
Click to view iomazenil (123I) potential benzodiazepine receptor imaging tracer for SPECT; structure given in first source; RN given refers to 123I-labeled cpd; RN for unlabeled cpd not avail 10/90
Click to view tasosartan Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) antagonist Angiotensin II receptor (AT-1) type-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25095|P29089, gene: Agtr1|Agtr1b, swissprot: AGTRA_RAT|AGTRB_RAT angiotensin II antagonist; structure given in first source Angiotensin II Type 1 Receptor Blockers (Code: D047228) Angiotensin Receptor Antagonists (Code: D057911)
Click to view fluvastatin 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Organism: Homo sapiens, class: Enzyme, accessions: P04035, gene: HMGCR, swissprot: HMDH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020261s052,021192s026lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020261s052,021192s026lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020261s052,021192s026lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020261s052,021192s026lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10064574) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10064574) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10064574) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10064574) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10064574) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10064574) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18381445) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21861202) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16046661) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16046661) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16046661) Fluvastatin is a synthetic lipid-lowering agent with antilipidemic and potential antineoplastic properties. Fluvastatin competitively inhibits hepatic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses through the suppression of MHC II (major histocompatibility complex II) on interferon gamma-stimulated antigen-presenting cells such as human vascular endothelial cells. Fluvastatin is used as an adjunct to dietary therapy to prevent cardiovascular events. May be used as secondary prevention in patients with coronary heart disease (CHD) to reduce the risk of requiring coronary revascularization procedures, for reducing progression of coronary atherosclerosis in hypercholesterolemic patients with CHD, and for the treatment of primary hypercholesterolemia and mixed dyslidipidemia. HMG-CoA Reductase Inhibitor (Code: N0000175589) Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Hydroxymethylglutaryl-CoA Reductase Inhibitors (Code: D019161) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) anticholesteremic drug (Code: CHEBI:35821) 1993-12-31 FDA 115
Click to view acetophenazine D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT major descriptor (73-85); minor descriptor (64-72); on-line search PHENOTHIAZINES (64-85); Index Medicus search PHENOTHIAZINES (64-72); ACETOPHENAZINE (73-85); RN given refers to parent cpd phenothiazine antipsychotic drug (Code: CHEBI:37930) 1961-04-05 FDA
Click to view butoconazole Butoconazole is an imidazole derivative with antifungal activity. Like other imidazole derivatives, butoconazole nitrate presumably exerts its antifungal activity by altering cellular membranes, resulting in increased membrane permeability, secondary metabolic effects, and growth inhibition. Although the exact mechanism of action of butoconazole nitrate has not been fully determined, it has been suggested that the fungistatic activity of the drug may result from interference with ergosterol synthesis, probably via inhibition of C-14 demethylation of sterol intermediates. Like some other imidazole derivatives (e.g. miconazole), the fungicidal activity of butoconazole at high concentrations may result from a direct physicochemical effect of the drug on the fungal cell. This effect may involve hydrophobic interactions between the drug and unsaturated fatty acid components of the membrane. Butoconazole is indicated for the local treatment of vulvovaginal infections caused by Candida albicans. Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) 1995-12-21 FDA
Click to view reserpiline
Click to view adapalene Retinoic acid receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10276, gene: RARA, swissprot: RARA_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022502s003lbl.pdf) Retinoic acid receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P13631, gene: RARG, swissprot: RARG_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022502s003lbl.pdf) Retinoic acid receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10826, gene: RARB, swissprot: RARB_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022502s003lbl.pdf) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) potentiator (Source: https://www.ncbi.nlm.nih.gov/pubmed/25790278) Adapalene is a naphthoic acid derivative with retinoid-like properties. Adapalene binds to specific retinoic acid nuclear receptors but does not bind to cytosolic receptor protein. Biochemical and pharmacological profile studies have demonstrated that adapalene is a modulator of cellular differentiation, keratinization and inflammatory processes. However, the significance of these findings with regard to the mechanism of action of adapalene for the treatment of acne is unknown. Adapalene is indicated for the topical treatment of acne vulgaris in patients 12 years and older. Retinoid (Code: N0000175607) Retinoids (Code: N0000007700) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Dermatologic Agents (Code: D003879) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) dermatologic drug (Code: CHEBI:50177) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) 1996-05-31 FDA
Click to view cinalukast Cysteinyl leukotriene receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y271, gene: CYSLTR1, swissprot: CLTR1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/23859232) Cysteinyl leukotriene receptor 1 (Organism: Cavia porcellus, class: GPCR, accessions: Q2NNR5, gene: CYSLTR1, swissprot: CLTR1_CAVPO anti-arrhythmia drug (Code: CHEBI:38070) anti-asthmatic drug (Code: CHEBI:49167) leukotriene antagonist (Code: CHEBI:49159)
Click to view calcipotriene Vitamin D3 receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11473, gene: VDR, swissprot: VDR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020273s013,020554s012lbl.pdf) Calcipotriene (calcipotriol) is a synthetic vitamin D derivative usually formulated for topical dermatological use. It induces differentiation and suppresses proliferation of keratinocytes, reversing abnormal keratinocyte changes in psoriasis, and leads to normalization of epidermal growth. Dermatologic Agents (Code: D003879) antipsoriatic (Code: CHEBI:50748) Vitamin D (Code: N0000006277) Vitamin D Analog (Code: N0000175849) 1993-12-29 FDA MC9
Click to view benzethonium Benzethonium is a synthetic quaternary ammonium salt with surfactant, antiseptic, and broad spectrum antimicrobial properties. Its salt form, benzethonium chloride, is primarily used as a skin disinfectant at concentrations of 0.1-0.2 %. It is additionally found in cosmetics and toiletries such as mouthwashes and anti-itch ointments. It is shown to be effective in mediating its antimicrobial action against bacteria, fungi, mold and viruses. There is evidence that benzethonium acts as a spermatocide but may cause vaginal irritation. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) antiseptic drug (Code: CHEBI:48218) 1953-04-01 PMDA
Click to view bretylium Bretylium is a quaternary ammonium cation having 2-bromobenzyl, ethyl and two methyl groups attached to the nitrogen. It blocks noradrenaline release from the peripheral sympathetic nervous system, and is used in emergency medicine, cardiology, and other specialties for the acute management of ventricular tachycardia and ventricular fibrillation. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377)
Click to view talniflumate an anti-inflammatory molecule for the treatment of cystic fibrosis, chronic obstructive pulmonary disease and asthma
Click to view doxercalciferol Vitamin D3 receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11473, gene: VDR, swissprot: VDR_HUMAN) agonist decrease of bone density caused by prednisolone was prevented by above cpd; decreases number of osteoclast areas in normal rats; RN given refers to (1alpha,3beta,5Z,7E,22E)-isomer Ergocalciferols (Code: N0000006337) Vitamin D2 Analog (Code: N0000175907) bone density conservation agent (Code: CHEBI:50646) 1999-06-09 FDA V2H
Click to view nizofenone Nizofenone is a neuroprotective drug which protects neurons from death following cerebral anoxia (interruption of oxygen supply to the brain). It might thus be useful in the treatment of acute neurological conditions such as stroke. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Neuroprotective Agents (Code: D018696) Protective Agents (Code: D020011) PMDA
Click to view ziprasidone 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020825s059,020919s047lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020825s059,020919s047lbl.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020825s059,020919s047lbl.pdf) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020825s059,020919s047lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020825s059,020919s047lbl.pdf) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020825s059,020919s047lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020825s059,020919s047lbl.pdf) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonism (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020825s059,020919s047lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020825s059,020919s047lbl.pdf) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17848919) Ziprasidone is a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone Atypical Antipsychotic (Code: N0000175430) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Tranquilizing Agents (Code: D014149) psychotropic drug (Code: CHEBI:35471) histamine antagonist (Code: CHEBI:37956) muscarinic antagonist (Code: CHEBI:48876) serotonergic antagonist (Code: CHEBI:48279) dopaminergic antagonist (Code: CHEBI:48561) antipsychotic agent (Code: CHEBI:35476) 2001-02-05 FDA
Click to view thiamphenicol glycinate Thiamphenicol glycinate is a prodrug of thiamphenicol with better water solubility, developed for oral administration. thiamphenicol glycinate was presumably cleaved quickly by tissue esterase to release thiamphenicol. (See: thiamphenicol)
Click to view etodroxizine
Click to view dichlorisone Adrenal Cortex Hormones (Code: D000305) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view noscapine Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20233183) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20233183) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor Noscapine is a phthalide isoquinoline non-narcotic alkaloid derived from the opium poppy Papaver somniferum, with mild analgesic, antitussive, and potential antineoplastic activities. Noscapine has been used as a cough suppressant since the mid 1950’s, however the mechanism of its antitussive nature is largely unknown. This agent appears to exert its antimitotic effect by binding to tubulin, resulting in a disruption of microtubule assembly dynamics and subsequently, the inhibition of mitosis and tumor cell death. Antitussive Agents (Code: D000996) Central Nervous System Agents (Code: D002491) Respiratory System Agents (Code: D019141) antitussive (Code: CHEBI:51177) antineoplastic agent (Code: CHEBI:35610) 2005-12-23 Ministry of Health of the Russian Federation
Click to view desoxycorticosterone pivalate Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) agonist FDA
Click to view podophyllotoxin Tubulin (Organism: Homo sapiens, class: Structural, accessions: Q71U36|P68363|Q9BQE3|P0DPH7|P0DPH8|Q6PEY2|P68366|P07437|Q9H4B7|Q13885|Q9BVA1|Q13509|P04350|P68371|Q9BUF5|Q3ZCM7, gene: TUBA1A|TUBA1B|TUBA1C|TUBA3C|TUBA3D|TUBA3E|TUBA4A|TUBB|TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB6|TUBB8, swissprot: TBA1A_HUMAN|TBA1B_HUMAN|TBA1C_HUMAN|TBA3C_HUMAN|TUBA3D_HUMAN|TBA3E_HUMAN|TBA4A_HUMAN|TBB5_HUMAN|TBB1_HUMAN|TBB2A_HUMAN|TBB2B_HUMAN|TBB3_HUMAN|TBB4A_HUMAN|TBB4B_HUMAN|TBB6_HUMAN|TBB8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12852768) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22116286) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22116286) Podophyllotoxin is an antimitotic drug found in podophyllin resin from the roots of podophyllum plants. Podophyllotoxin is indicated for the treatment of external genital warts and keratoses. Podophyllotoxin may have antineoplastic properties. The exact mechanism of action is unknown, but is believed to exert its antimitotic effect by binding to tubulin. Decreased Mitosis (Code: N0000008732) Antimitotic Agents (Code: D050256) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Phytogenic (Code: D000972) Dermatologic Agents (Code: D003879) Keratolytic Agents (Code: D007641) Mitosis Modulators (Code: D050258) Tubulin Modulators (Code: D050257) antineoplastic agent (Code: CHEBI:35610) keratolytic drug (Code: CHEBI:50176) 1990-12-13 FDA POD
Click to view sancycline
Click to view sulbenicillin Semisynthetic penicillin-type antibiotic. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view temocillin beta-lactam antibiotic with unusual spectrum of antibacterial activity & exceptional stability to bacterial beta-lactamases; RN given refers to di-Na salt (2S-(2alpha,5alpha,6alpha))-isomer Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1984-01-01 YEAR INTRODUCED
Click to view mesulfen used in therapy of scabies; structure
Click to view nafcillin Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) Penicillin-binding protein (Organism: Staphylococcus aureus, class: Enzyme, accessions: P72355|Q53707|Q53725|Q53729|Q9XDB3, gene: PBP2|mecA|pbp4|pbpA|pbpF, swissprot: P72355_STAAU|Q53707_STAAU|Q53725_STAAU|Q53729_STAAU|Q9XDB3_STAAU) inhibitor A semi-synthetic antibiotic related to penicillin. Penicillin-class Antibacterial (Code: N0000175497) Penicillins (Code: N0000011281) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1965-10-11 FDA NFN
Click to view eplerenone Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) antagonist Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN Eplerenone is a selective aldosterone receptor antagonist. Eplerenone binds to the mineralocorticoid receptor and blocks the binding of aldosterone, thereby decreasing sodium resorption and subsequently increasing water outflow. This leads to a decrease in blood pressure. Eplerenone is used in the treatment of hypertension and congestive heart failure. Aldosterone Antagonist (Code: N0000175557) Aldosterone Antagonists (Code: N0000011310) Diuretics (Code: D004232) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Mineralocorticoid Receptor Antagonists (Code: D000451) Natriuretic Agents (Code: D045283) antihypertensive agent (Code: CHEBI:35674) 2002-09-27 FDA YNU
Click to view diltiazem Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020062s043lbl.pdf) Voltage-dependent calcium channel gamma-1 subunit (Organism: Homo sapiens, class: Ion channel, accessions: Q06432, gene: CACNG1, swissprot: CCG1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19929811) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/21505038) A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions. Calcium Channel Antagonists (Code: N0000000069) Calcium Channel Blocker (Code: N0000175566) Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) vasodilator agent (Code: CHEBI:35620) antihypertensive agent (Code: CHEBI:35674) 1982-11-05 FDA
Click to view gestonorone caproate Gestonorone caproate is a long-acting potent progestogen structurally related to progesterone. It is used for the treatment of benign prostatic hyperplasia and endometrial cancer. PMDA
Click to view cefpimizole semisynthetic cephalosporin Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view sitosterol Nuclear factor NF-kappa-B p105 subunit (Organism: Homo sapiens, class: Cytosolic other, accessions: P19838, gene: NFKB1, swissprot: NFKB1_HUMAN DNA polymerase beta (Organism: Homo sapiens, class: Enzyme, accessions: P06746, gene: POLB, swissprot: DPOLB_HUMAN Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN used as tranquillizer; sedative; or anticonvulsant; structure Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Indicators and Reagents (Code: D007202) Intercalating Agents (Code: D007364) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) anticholesteremic drug (Code: CHEBI:35821) FDA
Click to view salmeterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020692s047lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020692s047lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15601807) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19317397) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19317397) Salmeterol is a selective long acting beta2-adrenoceptor agonist. The precise function of these receptors has not been established, but their presence raises the possibility that even selective beta2-agonists may have cardiac effects. The pharmacologic effects of beta2-adrenoceptor agonist drugs, including salmeterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. In vitro tests show that salmeterol is a potent and long-lasting inhibitor of the release of mast cell mediators, such as histamine, leukotrienes, and prostaglandin D2, from human lung. Salmeterol inhibits histamine-induced plasma protein extravasation and inhibits platelet-activating factor-induced eosinophil accumulation in the lungs of guinea pigs when administered by the inhaled route. In humans, single doses of salmeterol administered via inhalation aerosol attenuate allergen-induced bronchial hyper-responsiveness. Salmeterol is indicated for the treatment of asthma, bronchospasm associated with chronic obstructive pulmonary disease and for the prevention of exercise-induced bronchospasm. Adrenergic beta2-Agonists (Code: N0000009922) beta2-Adrenergic Agonist (Code: N0000175779) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) bronchodilator agent (Code: CHEBI:35523) beta-adrenergic agonist (Code: CHEBI:35522) 1994-02-04 FDA K5Y
Click to view bimatoprost Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00048161.PDF) Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: https://pdf.hres.ca/dpd_pm/00048161.PDF) Bimatoprost is a synthetic structural analog of prostaglandin with ocular hypotensive activity. It selectively mimics the effects of naturally occurring substances, prostamides. Bimatoprost is believed to lower intraocular pressure (IOP) in humans by increasing outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes. Elevated IOP presents a major risk factor for glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss. Bimatoprost is indicated for the reduction of elevated intraocular pressure in patients with open angle glaucoma or ocular hypertension. Also bimatoprost is indicated to treat hypotrichosis of the eyelashes by increasing their growth including length, thickness and darkness. Prostaglandin Analog (Code: N0000175454) Prostaglandins (Code: N0000007706) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) antihypertensive agent (Code: CHEBI:35674) antiglaucoma drug (Code: CHEBI:39456) 2001-03-16 FDA 15M
Click to view acemetacin Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1556251583660.pdf) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1556251583660.pdf) Lactoylglutathione lyase (Organism: Homo sapiens, class: Enzyme, accessions: Q04760, gene: GLO1, swissprot: LGUL_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21237663) Acemetacin is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indomethacin. Acemetacin is a prodrug of indomethacin and acemetacin is only a relatively weak inhibitor of prostaglandin synthetase. (See: indomethacin) It is used for the treatment of osteoarthritis, rheumatoid arthritis, lower back pain, and relieving post-operative pain. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) non-narcotic analgesic (Code: CHEBI:35481) prodrug (Code: CHEBI:50266) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) 1984-01-12 Austrian Medicines and Medical Devices Agency
Click to view rupatadine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1562299496368.pdf) Platelet-activating factor receptor (Organism: Homo sapiens, class: GPCR, accessions: P25105, gene: PTAFR, swissprot: PTAFR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8996188) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1562299496368.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037668.PDF) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037668.PDF) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00037668.PDF) Rupatadine is a second-generation antihistamine, long-acting histamine antagonist with selective peripheral H1-receptor and platelet activating factor (PAF) antagonistic activities. Some of the metabolites (desloratadine and its hydroxylated metabolites) retain an antihistaminic activity and may partially contribute to the overall efficacy of the drug, maintaining activity for up to 24 hours. Rupatadine is indicated for the Symptomatic treatment of allergic rhinitis and urticaria. 2007-10-24 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view isoconazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876) (Yeast), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23574019) an azole antifungal drug that has similar effectiveness to clotrimazole in the treatment of foot and vaginal infections. Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) antibacterial drug (Code: CHEBI:36047) 2008-11-05 Ministry of Health of the Russian Federation
Click to view miconazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022404s003lbl.pdf) Nitric oxide synthase, inducible (Organism: Homo sapiens, class: Enzyme, accessions: P35228, gene: NOS2, swissprot: NOS2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9873034) Nitric oxide synthase, endothelial (Organism: Homo sapiens, class: Enzyme, accessions: P29474, gene: NOS3, swissprot: NOS3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9873034) Calcium-activated potassium channel subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: Q12791, gene: KCNMA1, swissprot: KCMA1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1376313) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15778703) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9143352) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9143352) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9143352) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11854151) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11854151) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11854151) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16141569) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16141569) Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15554355) Malate dehydrogenase cytoplasmic (Organism: Homo sapiens, class: Enzyme, accessions: P40925, gene: MDH1, swissprot: MDHC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14521410) Beta-lactamase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P00811, gene: ampC, swissprot: AMPC_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14521410) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12699389) Lanosterol 14-alpha demethylase (Organism: Homo sapiens, class: Enzyme, accessions: Q16850, gene: CYP51A1, swissprot: CP51A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17194716) Indoleamine 2,3-dioxygenase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q8R0V5, gene: Ido2, swissprot: I23O2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Indoleamine 2,3-dioxygenase 1 (Organism: Mus musculus, class: Enzyme, accessions: P28776, gene: Ido1, swissprot: I23O1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) Indoleamine 2,3-dioxygenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P14902, gene: IDO1, swissprot: I23O1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25036789) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22328583) Miconazole is an antifungal synthetic derivative of imidazole and used in the treatment of candidal skin infections. Miconazole inhibits 14-alpha-demethlyase, blocks formation of ergosterol and leads to the buildup of toxic methylated 14-a-sterols. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) 14-alpha Demethylase Inhibitors (Code: D058888) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Cytochrome P-450 CYP2C9 Inhibitors (Code: D065688) Cytochrome P-450 CYP3A Inhibitors (Code: D065692) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) antineoplastic agent (Code: CHEBI:35610) 1974-01-08 FDA X89
Click to view tenitramine Tenitramine is a vasodilator with general properties similar to those of glyceryl trinitrate. It was used for the treatment and prevention of angina pectoris.
Click to view trovafloxacin Trovafloxacin is a synthetic broad-spectrum antibacterial agent. Trovafloxacin is a fluoronaphthyridone related to the fluoroquinolones with activity against Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermitis, Streptococcus agalactiae, Streptococcus pneumonia, Streptococcus pyogenes, Escherichia coli, Cardnerella vaginalis, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Neisseria gonorrhoeae, Proteus mirabilis, Pseudomonas aeruginosa, Bacteriodes fragilis, Chlamidia pneumoniae, Chlamydia trachomatis, Legionella pneumophila and Mycoplasma pneumoniae. The bactericidal action of trovafloxacin results from inhibition of DNA gyrase and topoisomerase IV. Trovafloxacin was used for the treatment of nosocomial and community acquired pneumonia, acute bacterial exacerbation of chronic bronchitis, acute sinusitis, intra-abdominal infections, gynecologic and pelvic infections, skin and skin structure infections, urinary tract infections, chronic bacterial prostatitis, urethral, endocervical or rectal gonorrhea, cervicitis and for prophylaxis of infections associated with elective colorectal surgery, vaginal ans abdominal hysterectomy. Trovafloxacin was withdrawn from the market due to its hepatotoxic potential. Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antibacterial drug (Code: CHEBI:36047) 1997-12-18 FDA TR6
Click to view guaiacol phosphate Guaiacol phosphate is a phosphoric ester of guaiacol. It is less toxic than guaiacol. (See: guaiacol)
Click to view ramatroban Prostaglandin D2 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q13258, gene: PTGDR, swissprot: PD2R_HUMAN Prostaglandin D2 receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5Y4, gene: PTGDR2, swissprot: PD2R2_HUMAN Thromboxane A2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P21731, gene: TBXA2R, swissprot: TA2R_HUMAN) inverse agonist Prostaglandin D2 receptor 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q6XKD3, gene: Ptgdr2, swissprot: PD2R2_RAT) antagonist (Source: ) Prostaglandin D2 receptor 2 (Organism: Mus musculus, class: Unclassified, accessions: Q9Z2J6, gene: Ptgdr2, swissprot: PD2R2_MOUSE) antagonist (Source: ) thromboxane A2 receptor antagonist; BAY u 3405 & 3406 are enantiomers of each other Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975)
Click to view pyrinoline
Click to view cefaloridine A cephalosporin antibiotic. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047)
Click to view desonide Desonide is a topical glucocorticoid which was approved for the relief of the inflammatory and pruritic manifestations of corticosteroid responsive dermatoses. The exact mechanism of drug action is unknown. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Anti-Inflammatory Agents (Code: D000893) anti-inflammatory drug (Code: CHEBI:35472) 1972-01-04 FDA
Click to view methylprednisolone acetate Methylprednisolone acetate is a soluble prodrug of methylprednisolone. It is used in the endocrine disorders, rheumatic disorders, collagen diseases, dermatologic diseases, allergic states, ophthalmic diseases, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, gastrointestinal diseases, acute exacerbations of multiple sclerosis, tuberculous meningitis with subarachnoid block or impending block, trichinosis with neurologic or myocardial involvement. (See: methylprednisolone) Anti-Inflammatory Agents (Code: D000893) anti-inflammatory drug (Code: CHEBI:35472) 1959-05-27 FDA
Click to view ramipril Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019901s067lbl.pdf) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Solute carrier family 15 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63424, gene: Slc15a2, swissprot: S15A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Ramipril is a long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its metabolite ramiprilat, which has about 6 times the ACE inhibitory activity of ramipril. Ramipril is used in the therapy of hypertension and heart failure. Angiotensin Converting Enzyme Inhibitor (Code: N0000175562) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) prodrug (Code: CHEBI:50266) cardioprotective agent (Code: CHEBI:77307) EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor (Code: CHEBI:35457) 1991-01-28 FDA
Click to view distigmine Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: http://www.kegg.jp/entry/D01228) Distigmine is an anticholinergic drug and long-acting reversible carbamate cholinesterase inhibitor that binds directly and competitively to the agonist binding sites of muscurinic receptors. Distigmine is used for treatment of underactive detrusor and voiding dysfunction in the urinary tract where the active ingredient is distigmine bromide. Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) 1967-09-05 PMDA
Click to view iopronic acid Iopronic acid is a triiodide derivative of aminophenol. It was used as a contrast medium for oral cholecystography in 1980s.
Click to view alfentanil Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist Mu-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P97266, gene: OPRM1, swissprot: OPRM_CAVPO Opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533|P33535|P34975|Q9R0C9, gene: Oprd1|Oprk1|Oprm1|Sigmar1, swissprot: OPRD_RAT|OPRK_RAT|OPRM_RAT|SGMR1_RAT Mu-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33535, gene: Oprm1, swissprot: OPRM_RAT Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) A short-acting opioid anesthetic and analgesic derivative of FENTANYL. It produces an early peak analgesic effect and fast recovery of consciousness. Alfentanil is effective as an anesthetic during surgery, for supplementation of analgesia during surgical procedures, and as an analgesic for critically ill patients. Full Opioid Agonists (Code: N0000175684) Opioid Agonist (Code: N0000175690) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322) intravenous anaesthetic (Code: CHEBI:38877) central nervous system depressant (Code: CHEBI:35488) peripheral nervous system drug (Code: CHEBI:49110) 1986-12-29 FDA
Click to view spironolactone Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/012151s075lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15601807) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11743742) Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23777778) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23777778) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23777778) Spironolactone is a potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827) Aldosterone Antagonist (Code: N0000175557) Aldosterone Antagonists (Code: N0000011310) Diuretics (Code: D004232) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Mineralocorticoid Receptor Antagonists (Code: D000451) Natriuretic Agents (Code: D045283) diuretic (Code: CHEBI:35498) antihypertensive agent (Code: CHEBI:35674) 1960-01-21 FDA SNL
Click to view colecalciferol Vitamin D3 receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11473, gene: VDR, swissprot: VDR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021762s021lbl.pdf) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) modulator (Source: https://www.ncbi.nlm.nih.gov/pubmed/25790278) Cholecalciferol is a steroid hormone produced in the skin when exposed to ultraviolet light or obtained from dietary sources. The active form of cholecalciferol, calcitriol plays an important role in maintaining blood calcium and phosphorus levels and mineralization of bone. The activated form of cholecalciferol binds to vitamin D receptors and modulates gene expression. This leads to an increase in serum calcium concentrations by increasing intestinal absorption of phosphorus and calcium, promoting distal renal tubular reabsorption of calcium and increasing osteoclastic resorption. Vitamin D (Code: N0000006277) Bone Density Conservation Agents (Code: D050071) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) 2000-05-18 FDA VD3
Click to view secalciferol
Click to view diiodotyrosine Diiodotyrosine is a product from the iodination of monoiodotyrosine. In the biosynthesis of thyroid hormones, diiodotyrosine residues are coupled with other monoiodotyrosine or diiodotyrosine residues to form T4 or T3 thyroid hormones. TYI
Click to view paricalcitol Vitamin D3 receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11473, gene: VDR, swissprot: VDR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021606s016s017lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021606s016s017lbl.pdf) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021606s016s017lbl.pdf) 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q07973, gene: CYP24A1, swissprot: CP24A_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021606s016s017lbl.pdf) Paricalcitol is a synthetic, biologically active vitamin D2 analog of calcitriol. Paricalcitol's biological actions are mediated through binding of the VDR, which results in the selective activation of vitamin D responsive pathways. Paricalcitol have been shown to reduce parathyroid hormone levels by inhibiting PTH synthesis and secretion. Paricalcitol is indicated for the prevention and treatment of secondary hyperparathyroidism associated with chronic renal failure. Cholecalciferol (Code: N0000006996) Vitamin D3 Analog (Code: N0000175908) antiparathyroid drug (Code: CHEBI:50827) 1998-04-17 FDA
Click to view calcitriol Vitamin D3 receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11473, gene: VDR, swissprot: VDR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/018874s022lbl.pdf) The physiologically active form of vitamin D. It is formed primarily in the kidney by enzymatic hydroxylation of 25-hydroxycholecalciferol (CALCIFEDIOL). Its production is stimulated by low blood calcium levels and parathyroid hormone. Calcitriol increases intestinal absorption of calcium and phosphorus, and in concert with parathyroid hormone increases bone resorption. Cholecalciferol (Code: N0000006996) Vitamin D3 Analog (Code: N0000175908) Bone Density Conservation Agents (Code: D050071) Calcium Channel Agonists (Code: D002120) Cardiovascular Agents (Code: D002317) Growth Substances (Code: D006133) Membrane Transport Modulators (Code: D049990) Micronutrients (Code: D018977) Vasoconstrictor Agents (Code: D014662) Vitamins (Code: D014815) nutraceutical (Code: CHEBI:50733) antipsoriatic (Code: CHEBI:50748) immunomodulator (Code: CHEBI:50846) antineoplastic agent (Code: CHEBI:35610) bone density conservation agent (Code: CHEBI:50646) 1978-08-17 FDA VDX
Click to view temafloxacin Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antibacterial drug (Code: CHEBI:36047) antiinfective agent (Code: CHEBI:35441)
Click to view bisoxatin acetate
Click to view ibacitabine Ibacitabine is an iodinated analog of deoxycytidine. Ibacitabine is used topically as antiviral agent in the treatment of herpes labialis. 1995-04-12 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view cilazapril Cilazaprilat: Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00009932.PDF) Cilazapril: Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11895100) Cilazapril is a prodrug of cilazaprilat, an angiotensin converting enzyme (ACE) inhibitor. After absorption, cilazapril is hydrolysed to cilazaprilat, the active metabolite, which prevents the conversion of angiotensin I to angiotensin II by inhibition of ACE. Cilazapril is used in the treatment of hypertension and congestive heart failure. Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 1990-09-19 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view nimodipine Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Rattus norvegicus, class: Ion channel, accessions: P27732, gene: Cacna1d, swissprot: CAC1D_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11487617) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Rattus norvegicus, class: Ion channel, accessions: P22002, gene: Cacna1c, swissprot: CAC1C_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11487617) Adenosine receptor A2a (Organism: Rattus norvegicus, class: GPCR, accessions: P30543, gene: Adora2a, swissprot: AA2AR_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8709132) Adenosine receptor A1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25099, gene: Adora1, swissprot: AA1R_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8709132) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8709132) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/203340lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Aryl hydrocarbon receptor (Organism: Homo sapiens, class: Transcription factor, accessions: P35869, gene: AHR, swissprot: AHR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17327465) Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18250364) Nimodipine is a calcium channel blockader with preferential cerebrovascular activity. It has marked cerebrovascular dilating effects and lowers blood pressure. Nimodipine inhibits the transmembrane influx of calcium ions in response to depolarization in smooth muscle cells, thereby inhibiting vascular smooth muscle contraction and inducing vasodilatation. Nimodipine has a greater effect on cerebral arteries than on peripheral smooth muscle cells and myocardial cells, probably because this agent can cross the blood brain barrier due to its lipophilic nature. Nimodipine is used to as an adjunct to improve the neurologic outcome following subarachnoid hemorrhage from ruptured intracranial aneurysm. Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) antihypertensive agent (Code: CHEBI:35674) vasodilator agent (Code: CHEBI:35620) cardiovascular drug (Code: CHEBI:35554) Calcium Channel Antagonists (Code: N0000000069) Dihydropyridine Calcium Channel Blocker (Code: N0000175421) Dihydropyridines (Code: N0000007556) 1988-12-28 FDA 6U9
Click to view simvastatin Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/019766s092lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11474784) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15616150) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15616150) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22328583) Simvastatin is a prodrug and is hydrolyzed to its active ?-hydroxyacid form, simvastatin acid, after administration. Simvastatin acid is a specific inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. Simvastatin is used for the treatment of hypercholesterolemia and for the reduction in the risk of cardiac heart disease mortality and cardiovascular events. HMG-CoA Reductase Inhibitor (Code: N0000175589) Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Hydroxymethylglutaryl-CoA Reductase Inhibitors (Code: D019161) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) prodrug (Code: CHEBI:50266) 1991-12-23 FDA
Click to view maxacalcitol Vitamin D3 receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P13053, gene: Vdr, swissprot: VDR_RAT) agonist (Source: ) Anticarcinogenic Agents (Code: D016588) Antineoplastic Agents (Code: D000970) Dermatologic Agents (Code: D003879) Protective Agents (Code: D020011) MCZ
Click to view lofepramine D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE. Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) antidepressant (Code: CHEBI:35469) 1977-01-01 YEAR INTRODUCED
Click to view thyropropic acid Proliferating cell nuclear antigen (Organism: Homo sapiens, class: Unclassified, accessions: P12004, gene: PCNA, swissprot: PCNA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23395113) Thyroid hormone receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10827, gene: THRA, swissprot: THA_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17467994) Thyroid hormone receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10828, gene: THRB, swissprot: THB_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17467994) Thyropropic Acid is a hydrocinnamic acid derivative and naturally occurring thyroid analog with antigoitrogenic and anticholesteremic activity. Thyropropic Acid acts as potent antagonist of thyroid hormone receptors and may be useful in the therapy of resistance to thyroid hormone and corticosteroid-induced skin atrophy.
Click to view bromperidol Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) bromine-substituted for chlorine in haloperidol; RN given refers to unlabeled parent cpd; structure Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1973-01-01 YEAR INTRODUCED
Click to view amtolmetin guacil Amtolmetin guacil is a prodrug of non-steroidal anti-inflammatory drug tolmetin. (See: tolmetin) Amtolmetin guacyl has substantially lower incidence of gastrointestinal adverse events compared to traditional NSAIDs. 1993-06-01 Italian Medicines Agency (AIFA)
Click to view hexoprenaline Catechol O-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: P22734, gene: Comt, swissprot: COMT_RAT) substrate (Source: https://aspregister.basg.gv.at/document/servlet?action=show&zulnr=17687&type=DOTC_FACH_INFO) Hexoprenaline is a selective beta2-adrenoreceptor agonist indicated for use in the treatment of bronchospasm associated with obstructive airways diseases, including asthma, bronchitis and emphysema. Hexoprenaline also is used as an emergency measures for premature labor. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Reproductive Control Agents (Code: D012102) Respiratory System Agents (Code: D019141) Tocolytic Agents (Code: D015149) 1984-03-29 Austrian Medicines and Medical Devices Agency
Click to view levocabastine Neurotensin receptor type 2 (Organism: Homo sapiens, class: GPCR, accessions: O95665, gene: NTSR2, swissprot: NTR2_HUMAN) partial antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11723247) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8951676) Levocabastine is a synthetic piperidine derivative with antihistamine properties. Levocabastine is a second generation histamine-1 receptor antagonist. When applied locally into the eye as a topical solution, this agent reduces itching, rhinorrhea and symptoms of allergic rhinitis or conjunctivitis. Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Neurotransmitter Agents (Code: D018377) 1993-11-10 FDA
Click to view pipebuzone
Click to view etofylline clofibrate Etofylline clofibrate (theofibrate) is the clofibric acid ester of theophylline. Etofylline clofibrate increases lipoprotein lipase activity to promote the conversion of Very low-density lipoprotein (VLDL) to Low-density lipoprotein (LDL), and hence reduce the level of VLDL. Etophylline clofibrate substantially decreases platelet aggregability and plasma viscosity, properties which may be desirable in the prevention of coronary heart disease (CHD). Etofylline clofibrate is used in the treatment of hyperlipoproteinaemia. Antimetabolites (Code: D000963) Antioxidants (Code: D000975) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Protective Agents (Code: D020011) Radiation-Sensitizing Agents (Code: D011838)
Click to view bendroflumethiazide Solute carrier family 12 member 3 (Organism: Homo sapiens, class: Transporter, accessions: P55017, gene: SLC12A3, swissprot: S12A3_HUMAN) inhibitor Calcium-activated potassium channel subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: Q12791, gene: KCNMA1, swissprot: KCMA1_HUMAN) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) diuretic (Code: CHEBI:35498) antihypertensive agent (Code: CHEBI:35674) Increased Diuresis (Code: N0000175359) Thiazide Diuretic (Code: N0000175419) Thiazides (Code: N0000166469) 1959-12-07 FDA
Click to view pipecuronium Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/6248079) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/6248079) Pipecuronium is a piperazinyl androstane derivative which is a non-depolarizing neuromuscular blocking agent. It is used as a muscle relaxant during anesthesia and surgical procedures. Owing to its relatively long duration of action and to the residual postoperative neuromuscular block, the use of pipecuronium was discontinued in the United States and in several European countries. Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) 1990-06-26 FDA
Click to view topotecan DNA topoisomerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P11387, gene: TOP1, swissprot: TOP1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020981s008lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020981s008lbl.pdf)) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020981s008lbl.pdf)) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17509534) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) RAC-alpha serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P31749, gene: AKT1, swissprot: AKT1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21440338) Topotecan is a semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata. Topotecan inhibits topoisomerase I activity by stabilizing the topoisomerase I-DNA covalent complexes during S phase of cell cycle, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. Topotecan is indicated for the treatment of small cell lung cancer and ovarian neoplasms. Topoisomerase Inhibitor (Code: N0000175609) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase I Inhibitors (Code: D059004) Topoisomerase Inhibitors (Code: D059003) antineoplastic agent (Code: CHEBI:35610) 1996-05-28 FDA TTC
Click to view pitavastatin 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Organism: Homo sapiens, class: Enzyme, accessions: P04035, gene: HMGCR, swissprot: HMDH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022363s015lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022363s015lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022363s015lbl.pdf) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022363s015lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022363s015lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15159445) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15159445) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/24014644) Pitavastatin competitively inhibits HMG-CoA reductase, which is a rate-determining enzyme involved with biosynthesis of cholesterol. Pitavastatin is indicated for the treatment of adult patients with primary hyperlipidemia or mixed dyslipidemia to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol, apolipoprotein B, triglycerides, and to increase high-density lipoprotein cholesterol. It is also indicated for the treatment of pediatric patients aged 8 years and older with heterozygous familial hypercholesterolemia. Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Hydroxymethylglutaryl-CoA Reductase Inhibitors (Code: D019161) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) HMG-CoA Reductase Inhibitor (Code: N0000175589) 2003-07-01 PMDA
Click to view mopidamol A phosphodiesterase inhibitor which inhibits platelet aggregation. Formerly used as an antineoplastic. Antineoplastic Agents (Code: D000970)
Click to view pentacynium chloride
Click to view mosapride 5-hydroxytryptamine receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q13639, gene: HTR4, swissprot: 5HT4R_HUMAN) agonist (Source: ) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) 5-hydroxytryptamine receptor 4 (Organism: Cavia porcellus, class: GPCR, accessions: O70528, gene: HTR4, swissprot: 5HT4R_CAVPO Serotonin 3 (5-HT3) receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35563|Q9JJ16, gene: Htr3a|Htr3b, swissprot: 5HT3A_RAT|5HT3B_RAT Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Mosapride is a 5-HT4 receptor agonist which increases the release of acetylcholine and stimulates GI motility. Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) 1998-01-01 YEAR INTRODUCED
Click to view conivaptan Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) antagonist Vasopressin V1a receptor (Organism: Homo sapiens, class: GPCR, accessions: P37288, gene: AVPR1A, swissprot: V1AR_HUMAN) antagonist Antidiuretic Hormone Antagonists (Code: N0000009945) Vasopressin Antagonist (Code: N0000178376) Antidiuretic Hormone Receptor Antagonists (Code: D065092) Natriuretic Agents (Code: D045283) vasopressin receptor antagonist (Code: CHEBI:59680) Vasopressin Receptor Antagonists (Code: N0000020044) Cytochrome P450 3A Inhibitors (Code: N0000190114) 2005-12-29 FDA
Click to view nandrolone cyclotate
Click to view losartan Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11823761) cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Cavia porcellus, class: Enzyme, accessions: O89085, gene: PDE4A, swissprot: PDE4A_CAVPO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9154964) Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020386s062lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23571415) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23571415) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10049739) Losartan is an angiotensin II receptor blocker used in the therapy of hypertension and diabetic nephropathy. Angiotensin 2 Receptor Antagonists (Code: N0000000070) Angiotensin 2 Receptor Blocker (Code: N0000175561) Angiotensin II Type 1 Receptor Blockers (Code: D047228) Angiotensin Receptor Antagonists (Code: D057911) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) antihypertensive agent (Code: CHEBI:35674) anti-arrhythmia drug (Code: CHEBI:38070) angiotensin receptor antagonist (Code: CHEBI:61016) endothelin receptor antagonist (Code: CHEBI:51451) 1995-04-14 FDA LSN
Click to view cefapirin Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) Interstitial collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P03956, gene: MMP1, swissprot: MMP1_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) Substance-K receptor (Organism: Homo sapiens, class: GPCR, accessions: P21452, gene: TACR2, swissprot: NK2R_HUMAN) Cannabinoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P21554, gene: CNR1, swissprot: CNR1_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) Somatostatin receptor type 4 (Organism: Homo sapiens, class: GPCR, accessions: P31391, gene: SSTR4, swissprot: SSR4_HUMAN) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Nischarin (Organism: Homo sapiens, class: Cytosolic other, accessions: Q9Y2I1, gene: NISCH, swissprot: NISCH_HUMAN) Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor Cephalosporin antibiotic, partly plasma-bound, that is effective against gram-negative and gram-positive organisms. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1974-03-12 FDA
Click to view bromoform Bromoform (Tribromomethane or Methyl tribromide) is classified as a member of the Trihalomethanes class, which are organic compounds in which exactly three of the four hydrogen atoms of methane (CH4) are replaced by halogen atoms. Bromoform is formally rated as an unfounded non-carcinogenic (IARC 3) potentially toxic compound. Exposure to bromoform may occur from the consumption of chlorinated drinking water. The acute (short-term) effects from inhalation or ingestion of high levels of bromoform in humans and animals consist of nervous system effects such as the slowing down of brain functions, and injury to the liver and kidney. Chronic (long-term) animal studies indicate effects on the liver, kidney, and central nervous system (CNS) from oral exposure to bromoform. In the past, it was used as a solvent, sedative and flame retardant, but now it is mainly used as a laboratory reagent. Carcinogens (Code: D002273) Noxae (Code: D009676) Teratogens (Code: D013723)
Click to view gallamine Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) negative allosteric modulator Muscarinic acetylcholine receptor M2 (Organism: Sus scrofa, class: GPCR, accessions: P06199, gene: CHRM2, swissprot: ACM2_PIG Acetylcholinesterase (Organism: Torpedo californica, class: Enzyme, accessions: P04058, gene: ache, swissprot: ACES_TORCA Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN Acetylcholine receptor subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P02708, gene: CHRNA1, swissprot: ACHA_HUMAN) blocker (Source: ) Muscarinic acetylcholine receptor M2 (Organism: Rattus norvegicus, class: GPCR, accessions: P10980, gene: Chrm2, swissprot: ACM2_RAT) allosteric modulator (Source: ) A synthetic nondepolarizing blocking drug. The actions of gallamine triethiodide are similar to those of TUBOCURARINE, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) FDA GMN
Click to view carfenazine D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist dopaminergic antagonist (Code: CHEBI:48561) antiemetic (Code: CHEBI:50919) phenothiazine antipsychotic drug (Code: CHEBI:37930) FDA
Click to view omoconazole Omoconazole is a topical imidazole derivative with antifungal activity against Candida albicans, Malassezia furfur and dematophytes. Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 1988-05-06 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view benzbromarone 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) Mitogen-activated protein kinase 14 (Organism: Homo sapiens, class: Kinase, accessions: Q16539, gene: MAPK14, swissprot: MK14_HUMAN) Mitogen-activated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P28482, gene: MAPK1, swissprot: MK01_HUMAN) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) Aldo-keto reductase family 1 member C1 (Organism: Homo sapiens, class: Enzyme, accessions: Q04828, gene: AKR1C1, swissprot: AK1C1_HUMAN) Solute carrier family 22 member 12 (Organism: Homo sapiens, class: Transporter, accessions: Q96S37, gene: SLC22A12, swissprot: S22AC_HUMAN) inhibitor (Source: ) Envelope glycoprotein gp160 (Organism: Human immunodeficiency virus 1, class: Unclassified, accessions: Q6QLK5, gene: env, swissprot: Q6QLK5_9HIV1) M1-family alanyl aminopeptidase (Organism: Plasmodium falciparum (isolate 3D7), class: Unclassified, accessions: Q8IEK1, gene: None, swissprot: Q8IEK1_PLAF7) Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout. Antirheumatic Agents (Code: D018501) Gout Suppressants (Code: D006074) Renal Agents (Code: D012076) Uricosuric Agents (Code: D014528) uricosuric drug (Code: CHEBI:35841)
Click to view cefuroxime Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Cefuroxime is a semisynthetic, broad-spectrum, beta-lactamase-resistant, second-generation cephalosporin. Cefuroxime acts by inhibition of bacterial cell wall synthesis. Cefuroxime has been shown to be active against Enterobacter spp., Escherichia coli, Klebsiella spp., Haemophilus influenzae, Neisseria meningitidis, Neisseria gonorrhoeae, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes. Cefuroxime is used for the treatment of Lower Respiratory Tract Infections (including pneumonia), Urinary Tract Infections, Skin and Skin-Structure Infections, Septicemia, Meningitis, Gonorrhea, Bone and Joint Infections and for prevention of certain postoperative infections in patients undergoing surgical procedures. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) drug allergen (Code: CHEBI:88188) Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) 1983-10-19 FDA KOV
DXF
Click to view epitizide Epitizide is a diuretic. Epitizide inhibits tubular sodium reabsorption resulting in enhanced urinary excretion of water and solutes. Epitizide is used in combination with triamterene for the treatment of mild to moderate hypertension, edema caused by congestive heart failure or nephrotic syndrome. 1966-01-21 Ministry of Health, Welfare and Sport (Netherlands)
Click to view benazepril Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor Angiotensin-converting enzyme (Organism: Oryctolagus cuniculus, class: Enzyme, accessions: P12822, gene: ACE, swissprot: ACE_RABIT Angiotensin-converting enzyme (Organism: Rattus norvegicus, class: Enzyme, accessions: P47820, gene: Ace, swissprot: ACE_RAT prodrug of benazeprilat inhibit angiotensin-converting enzyme (ACE) and results in decreased plasma angiotensin II, which leads to decreased vasopressor activity and to decreased aldosterone secretion Angiotensin Converting Enzyme Inhibitor (Code: N0000175562) Decreased Blood Pressure (Code: N0000178477) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor (Code: CHEBI:35457) prodrug (Code: CHEBI:50266) 1991-06-25 FDA
Click to view eprosartan Angiotensin II receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P25095|P29089|P35351, gene: Agtr1|Agtr1b|Agtr2, swissprot: AGTR2_RAT|AGTRA_RAT|AGTRB_RAT Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) antagonist Type-1B angiotensin II receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P29089, gene: Agtr1b, swissprot: AGTRB_RAT Type-2 angiotensin II receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P35351, gene: Agtr2, swissprot: AGTR2_RAT Angiotensin II receptor (AT-1) type-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25095|P29089, gene: Agtr1|Agtr1b, swissprot: AGTRA_RAT|AGTRB_RAT angiotensin II receptor antagonist; structure given in first source Angiotensin 2 Receptor Antagonists (Code: N0000000070) Angiotensin 2 Receptor Blocker (Code: N0000175561) Angiotensin II Type 2 Receptor Blockers (Code: D057912) Angiotensin Receptor Antagonists (Code: D057911) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) angiotensin receptor antagonist (Code: CHEBI:61016) antihypertensive agent (Code: CHEBI:35674) 1997-12-22 FDA
Click to view pravastatin 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Organism: Homo sapiens, class: Enzyme, accessions: P04035, gene: HMGCR, swissprot: HMDH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019898s066lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15616150) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10601278) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14978359) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14978359) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14978359) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14978359) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15901800) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Pravastatin is a HMG-CoA Reductase Inhibitor. Paravastatin is indicated as an adjunctive therapy to diet to reduce the risk of muocardial infraction, revascularization, and cardiovascular mortality in hypercholesterolemic patients, to reduce elevated Total-C, LDL-C, ApoB, and TG levels and to increase HDLC in patients with primary hypercholesterolemia and mixed dyslipidemia, to reduce elevated serum TG levels in patients with hypertriglyceridemia and to treat patients with primary dysbetalipoproteinemia who are not responding to diet. Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Hydroxymethylglutaryl-CoA Reductase Inhibitors (Code: D019161) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) HMG-CoA Reductase Inhibitor (Code: N0000175589) 1991-10-31 FDA
Click to view alvimopan Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) antagonist Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN mu opioid receptor antagonist; intended to treat constipation in patients taking opiates for pain Gastrointestinal Agents (Code: D005765) Opioid Antagonist (Code: N0000175691) Opioid Antagonists (Code: N0000000154) 2008-05-20 FDA
Click to view oleandomycin Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12065733) Oleandomycin is a macrolide antibiotic similar to erythromycin with antimicrobial activity produced by Streptomyces antibioticus. Oleandomycin targets and reversibly binds to the 50S subunit of bacterial ribosomes. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 2005-12-09 Ministry of Health of the Russian Federation
Click to view difenoxin Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist an orally administered antidiarrheal agent which is chemically related to the narcotic meperidine Antidiarrheal (Code: N0000178374) antidiarrhoeal drug (Code: CHEBI:55323) 1978-07-14 FDA
Click to view unoprostone isopropyl a safe and effective ocular hypotensive drug Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) antihypertensive agent (Code: CHEBI:35674) prodrug (Code: CHEBI:50266) antiglaucoma drug (Code: CHEBI:39456) 2000-08-03 FDA
Click to view pifarnine non-anticholinergic gastric antisecretory agent
Click to view clindamycin 23S rRNA (Organism: Enteric bacteria and other eubacteria, class: Ribosomal protein, accessions: None, gene: None, swissprot: None) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050162s100lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050162s100lbl.pdf) Clindamycin is a semisynthetic analog of lincomycin.Clindamycin is a broad spectrum antibiotic used orally, topically and parenterally for bacterial infections due to sensitive organisms. The physiologic effect of clindamycin is by means of Decreased Sebaceous Gland Activity. Clindamycin has been linked to rare instances of acute liver injury. Decreased Sebaceous Gland Activity (Code: N0000009982) Lincosamide Antibacterial (Code: N0000175443) Lincosamides (Code: N0000175442) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) 1970-02-22 FDA CLY
Click to view domperidone D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1683559) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15911273) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22996261) A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms. Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) antiemetic (Code: CHEBI:50919) dopaminergic antagonist (Code: CHEBI:48561) 1982-01-01 YEAR INTRODUCED
Click to view sozoiodolic acid Sozoiodolic acid (sozoiodole) is the diiodo-para-phenolsulphonic acid. It was used at the beginning of the XX century. Mercury sozoiodole was used in 10% ointment in parasitic and syphilitic skin diseases, and in 1% dusting-powder in intertrigo, leg ulcers, etc. Potassium sozoiodole was used externally in scabies, impetigo and other skin diseases, in gonorrhea, rhinitis, diphtheria, etc. It was also used as a diagnostic aid in retrograde pyelography. Now sozoiodolic acid in not available.
Click to view garenoxacin a des-fluoro(6) quinolone with antibacterial activity Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antibacterial drug (Code: CHEBI:36047) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) 2007-05-30 PMDA
Click to view iloperidone Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Serotonin 2 (5-HT2) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P30994, gene: Htr2a|Htr2b|Htr2c, swissprot: 5HT2A_RAT|5HT2B_RAT|5HT2C_RAT Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN Alpha-2A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P22909, gene: Adra2a, swissprot: ADA2A_RAT 5-hydroxytryptamine receptor 2A (Organism: Bos taurus, class: GPCR, accessions: Q75Z89, gene: HTR2A, swissprot: 5HT2A_BOVIN 5-hydroxytryptamine receptor 1A (Organism: Mus musculus, class: GPCR, accessions: Q64264, gene: Htr1a, swissprot: 5HT1A_MOUSE D(1A) dopamine receptor (Organism: Mus musculus, class: GPCR, accessions: Q61616, gene: Drd1, swissprot: DRD1_MOUSE D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT Gastrin/cholecystokinin type B receptor (Organism: Homo sapiens, class: GPCR, accessions: P32239, gene: CCKBR, swissprot: GASR_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT) antagonist (Source: ) 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT) antagonist (Source: ) an atypical, negative symptom antipsychotic agent Atypical Antipsychotic (Code: N0000175430) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) serotonergic antagonist (Code: CHEBI:48279) dopaminergic antagonist (Code: CHEBI:48561) second generation antipsychotic (Code: CHEBI:65191) 2009-05-06 FDA
Click to view etofamide Amebicides (Code: D000563) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981)
Click to view fenbenicillin
Click to view cetotiamine
Click to view darifenacin Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021513s010lbl.pdf) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021513s010lbl.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021513s010lbl.pdf) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021513s010lbl.pdf) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021513s010lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021513s010lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021513s010lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021513s010lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/021513s010lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily KQT member 1 (Organism: Homo sapiens, class: Ion channel, accessions: P51787, gene: KCNQ1, swissprot: KCNQ1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily D member 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UK17, gene: KCND3, swissprot: KCND3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Darifenacin is a competitive muscarinic receptor antagonist with greater affinity for the M3 receptor than for the other known muscarinic receptors (9- and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4). M3 receptors are involved in contraction of human bladder and gastrointestinal smooth muscle, saliva production, and iris sphincter function. Darifenacin is used for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency. Cholinergic Muscarinic Antagonist (Code: N0000175700) Cholinergic Muscarinic Antagonists (Code: N0000000125) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Urological Agents (Code: D064804) muscarinic antagonist (Code: CHEBI:48876) antispasmodic drug (Code: CHEBI:53784) 2004-10-22 EMA
Click to view oxatomide Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Histamine H1 receptor (Organism: Cavia porcellus, class: GPCR, accessions: P31389, gene: HRH1, swissprot: HRH1_CAVPO orally active H1-histamine receptor antagonist used to treat chronic urticaria and allergic rhinitis Anti-Allergic Agents (Code: D018926) Anti-Asthmatic Agents (Code: D018927) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) Respiratory System Agents (Code: D019141) 1981-01-01 YEAR INTRODUCED
Click to view perospirone D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: ) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: ) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2A (Organism: Rattus norvegicus, class: GPCR, accessions: P14842, gene: Htr2a, swissprot: 5HT2A_RAT) antagonist (Source: ) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 2000-12-22 PMDA
Click to view pemetrexed Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021677lbl.pdf) Thymidylate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P04818, gene: TYMS, swissprot: TYSY_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021677lbl.pdf) Trifunctional purine biosynthetic protein adenosine-3 (Organism: Homo sapiens, class: Enzyme, accessions: P22102, gene: GART, swissprot: PUR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/021677lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021462s053lbl.pdf) Deoxycytidine kinase (Organism: Homo sapiens, class: Kinase, accessions: P27707, gene: DCK, swissprot: DCK_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/21336182) Equilibrative nucleoside transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q99808, gene: SLC29A1, swissprot: S29A1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/21336182) Thymidylate synthase (Organism: Escherichia coli, class: Enzyme, accessions: C3SWJ7, gene: thyA, swissprot: C3SWJ7_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16279780) Dihydrofolate reductase (Organism: Escherichia coli, class: Unclassified, accessions: B0BL08, gene: dfrA17, swissprot: B0BL08_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16279780) Bifunctional dihydrofolate reductase-thymidylate synthase (Organism: Toxoplasma gondii, class: Enzyme, accessions: Q07422, gene: None, swissprot: DRTS_TOXGO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16279780) Proton-coupled folate transporter (Organism: Homo sapiens, class: Transporter, accessions: Q96NT5, gene: SLC46A1, swissprot: PCFT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20085328) Serine hydroxymethyltransferase, cytosolic (Organism: Homo sapiens, class: Enzyme, accessions: P34896, gene: SHMT1, swissprot: GLYC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21371789) Pemetrexed is a folate analog metabolic inhibitor that disrupts folate-dependent metabolic processes essential for cell replication. In vitro studies show that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase, and glycinamide ribonucleotide formyltransferase (GARFT), which are folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Pemetrexed is taken into cells by membrane carriers such as the reduced folate carrier and membrane folate binding protein transport systems. Once in the cell, pemetrexed is converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase. The polyglutamate forms are retained in cells and are inhibitors of TS and GARFT. Pemetrexed is used for the treatment of mesothelioma and non-small cell lung cancer. Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) Nucleic Acid Synthesis Inhibitors (Code: D019384) antineoplastic agent (Code: CHEBI:35610) Folate Analog Metabolic Inhibitor (Code: N0000175584) Folic Acid Metabolism Inhibitors (Code: N0000000111) 2004-02-04 FDA LYA
Click to view salazosulfadimidine
Click to view buclizine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Neurotransmitter Agents (Code: D018377) antiemetic (Code: CHEBI:50919) cholinergic antagonist (Code: CHEBI:48873) histamine antagonist (Code: CHEBI:37956) local anaesthetic (Code: CHEBI:36333) central nervous system depressant (Code: CHEBI:35488) FDA
Click to view cefoxitin Cefoxitin is a bactericidal agent that acts by inhibition of bacterial cell wall synthesis. Cefoxitin has activity in the presence of some beta-lactamases, both penicillinases and cephalosporinases, of Gram-negative and Gram-positive bacteria. Cefoxitin has been shown to be active against Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, Haemophilus influenzae, Klebsiella spp., Morganella morganii, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia spp., Clostridium spp., Peptococcus niger, Peptostreptococcus spp., Bacteroides distasonis, Bacteroides fragilis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides spp. Cefoxitin is indicated for the treatment of Lower Respiratory Tract Infections (due to S. pneumoniae, other streptococci (excluding enterococci, S. aureus, E. coli, Klebsiella spp., H. influenzae, and Bacteroides spp.), Urinary Tract Infections (due to E. coli, Klebsiella spp., P. mirabilis, M. morganii, P. vulgaris and Providencia spp.), Intra-abdominal Infections (due to E. coli, Klebsiella spp., Bacteroides spp., Clostridium spp.), Gynecological Infections (due to E. coli, N. gonorrhoeae, Bacteroides spp., Clostridium spp., P. niger, Peptostreptococcus spp., and S. agalactiae), Septicemia (due to S. pneumoniae, S. aureus, E. coli, Klebsiella spp., and Bacteroides spp.), Bone and Joint Infections (due to S. aureus), Skin and Skin Structure Infections (due to S. aureus, S. epidermidis, S. pyogenes and other streptococci (excluding enterococci), E. coli, P. mirabilis, Klebsiella spp., Bacteroides spp., Clostridium spp., P. niger, and Peptostreptococcus spp.) and for prophylaxis of infection in patients undergoing uncontaminated gastrointestinal surgery, vaginal hysterectomy, abdominal hysterectomy, or cesarean section. Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1978-10-18 FDA CFX
1QL
Click to view moracizine Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/12402511) Moracizine is an antiarrhythmia agent used primarily for ventricular rhythm disturbances. In 2007 it was withdrawn and discontinued for commercial reasons. Antiarrhythmic (Code: N0000175426) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) anti-arrhythmia drug (Code: CHEBI:38070) 1990-06-19 FDA
Click to view ranolazine Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s034lbl.pdf) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s034lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s034lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s034lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s034lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s034lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s034lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s034lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021526s034lbl.pdf) Beta-1 adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18090, gene: Adrb1, swissprot: ADRB1_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11330341) Beta-2 adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P10608, gene: Adrb2, swissprot: ADRB2_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11330341) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/24014644) Ranolazine is an orally available, piperazine derivative with anti-anginal activity. Ranolazine has anti-ischemic and antianginal effects that do not depend upon reductions in heart rate or blood pressure. It does not affect the rate-pressure product, a measure of myocardial work, at maximal exercise. Ranolazine at therapeutic levels can inhibit the cardiac late sodium current (INa). The QT prolongation effect of ranolazine on the surface electrocardiogram is the result of inhibition of IKr, which prolongs the ventricular action potential. Ranolazine is indicated for the treatment of chronic angina. Anti-anginal (Code: N0000175427) Cytochrome P450 3A Inhibitors (Code: N0000190114) P-Glycoprotein Inhibitors (Code: N0000185503) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Organic Cation Transporter 2 Inhibitors (Code: N0000187061) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) anti-arrhythmia drug (Code: CHEBI:38070) 2006-01-27 FDA
Click to view mozavaptan Vasopressin V1b receptor (Organism: Homo sapiens, class: GPCR, accessions: P47901, gene: AVPR1B, swissprot: V1BR_HUMAN) antagonist (Source: ) Vasopressin V2 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: Q00788, gene: Avpr2, swissprot: V2R_RAT Oxytocin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30559, gene: OXTR, swissprot: OXYR_HUMAN Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) antagonist Vasopressin V1a receptor (Organism: Homo sapiens, class: GPCR, accessions: P37288, gene: AVPR1A, swissprot: V1AR_HUMAN Vasopressin V1a receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30560, gene: Avpr1a, swissprot: V1AR_RAT Vasopressin V1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30560|P48974, gene: Avpr1a|Avpr1b, swissprot: V1AR_RAT|V1BR_RAT Mozavaptan is a benzazepine derivative that antagonizes the binding of arginine vasopressin (AVP) to vasopressin receptors. Mozavaptan can inhibit the antidiuretic action of AVP promoting aquaresis. Antidiuretic Hormone Receptor Antagonists (Code: D065092) Natriuretic Agents (Code: D045283) 2006-07-26 PMDA
Click to view dixyrazine Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Antiemetics (Code: D000932) Antipsychotic Agents (Code: D014150) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) Tranquilizing Agents (Code: D014149)
Click to view fosfestrol Fosfestrol is the diphosphate ester of a synthetic, nonsteroidal form of estrogen. It is inactive itself and acts as a prodrug of diethylstilbestrol. diethylstilbestrol is a very potent full agonist of the estrogen receptors. It is used in the treatment of menopausal and postmenopausal disorders, prostate cancer and in the prevention of miscarriage or premature delivery in pregnant women prone to miscarriage or premature delivery. Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) FDA
Click to view mebeverine Mebeverine is a musculotropic antispasmodic with a direct action on the smooth muscle of the gastrointestinal tract, without affecting normal gut motility. Anticonvulsants (Code: D000927) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) 1978-03-14 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view irbesartan Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020757s059s067lbl.pdf) Sodium/bile acid cotransporter (Organism: Homo sapiens, class: Transporter, accessions: Q14973, gene: SLC10A1, swissprot: NTCP_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23339484) Irbesartan is an angiotensin II receptor blocker used alone or in combination with other agents in the therapy of hypertension and diabetic nephropathy. Irbesartan is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury. Angiotensin 2 Receptor Antagonists (Code: N0000000070) Angiotensin 2 Receptor Blocker (Code: N0000175561) Angiotensin II Type 1 Receptor Blockers (Code: D047228) Angiotensin Receptor Antagonists (Code: D057911) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) antihypertensive agent (Code: CHEBI:35674) angiotensin receptor antagonist (Code: CHEBI:61016) 1997-09-30 FDA
Click to view nandrolone decanoate Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist Corticosteroid-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P08185, gene: SERPINA6, swissprot: CBG_HUMAN Sex hormone-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P04278, gene: SHBG, swissprot: SHBG_HUMAN Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT Anabolic Agents (Code: D045930) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1962-10-05 FDA
Click to view oxiconazole Oxiconazole is an imidazole derivative whose antifungal activity is derived primarily from the inhibition of ergosterol biosynthesis. It has in vitro activity against a wide range of pathogenic fungi. Oxiconazole has been shown to be active against most strains of the following organisms: Epidermophyton floccosum, Trichophyton mentagrophytes, Trichophyton rubrum, Malassezia furfur, Candida albicans, Microsporum audouini, Microsporum canis, Microsporum gypseum, Trichophyton tonsurans, Trichophyton violaceum. Oxiconazole is indicated for the topical treatment of tinea pedis, tinea cruris, tinea corporis and tinea (pityriasis) versicolor. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) antiinfective agent (Code: CHEBI:35441) 1988-12-30 FDA
Click to view altropane a SPECT imaging agent for viewing dopamine transporter sites
Click to view sarpogrelate 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: ) Serotonin 2 (5-HT2) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P30994, gene: Htr2a|Htr2b|Htr2c, swissprot: 5HT2A_RAT|5HT2B_RAT|5HT2C_RAT Cardiovascular Agents (Code: D002317) Fibrin Modulating Agents (Code: D050299) Fibrinolytic Agents (Code: D005343) Hematologic Agents (Code: D006401) Neurotransmitter Agents (Code: D018377) Platelet Aggregation Inhibitors (Code: D010975) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702)
Click to view zofenopril Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: https://farmaci.agenziafarmaco.gov.it/aifa/servlet/PdfDownloadServlet?pdfFileName=footer_000211_034934_RCP.pdf&retry=0&sys=m0b1l3) a sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, zofenopril is hydrolyzed in vivo into its active form zofenoprilat. It is used for the treatment of hypertension and acute myocardial infarction. Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) anticonvulsant (Code: CHEBI:35623) EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor (Code: CHEBI:35457) cardioprotective agent (Code: CHEBI:77307) prodrug (Code: CHEBI:50266) vasodilator agent (Code: CHEBI:35620) 1998-07-30 Italian Medicines Agency (AIFA)
Click to view piritramide A diphenylpropylamine with intense narcotic analgesic activity of long duration. It is a derivative of MEPERIDINE with similar activity and usage. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view mifepristone Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12238914) Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12238914) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12238914) Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15293993) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18722119) Mifepristone ia a progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. Abortifacient Agents (Code: D000019) Abortifacient Agents, Steroidal (Code: D000021) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Contraceptives, Postcoital (Code: D003281) Contraceptives, Postcoital, Synthetic (Code: D003283) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Luteolytic Agents (Code: D008186) Menstruation-Inducing Agents (Code: D008600) Reproductive Control Agents (Code: D012102) hormone antagonist (Code: CHEBI:49020) contraceptive drug (Code: CHEBI:49323) synthetic oral contraceptive (Code: CHEBI:49326) abortifacient (Code: CHEBI:50691) Progestational Hormone Receptor Antagonists (Code: N0000000115) Progestin Antagonist (Code: N0000175841) 2000-09-28 FDA 486
Click to view bicalutamide Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020498s028lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020498s028lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020498s028lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020498s028lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020498s028lbl.pdf) Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9484511) Bicalutamide is a non-steroidal androgen receptor inhibitor with no other known endocrine activity. Bicalutamide is a racemate with its antiandrogenic activity being almost exclusively exhibited by the R-enantiomer of bicalutamide; the S-enantiomer is essentially inactive. It competitively inhibits the action of androgens by binding to cytosol androgen receptors in the target tissue. Prostatic carcinoma is known to be androgen sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen. Bicalutamide is indicated for use in combination therapy with a luteinizing hormone-releasing hormone analog for the treatment of Stage D2 metastatic carcinoma of the prostate. Androgen Antagonists (Code: D000726) Antineoplastic Agents (Code: D000970) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) androgen antagonist (Code: CHEBI:35497) antineoplastic agent (Code: CHEBI:35610) Androgen Receptor Antagonists (Code: N0000000243) Androgen Receptor Inhibitor (Code: N0000175560) 1995-10-04 FDA 0U9
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Click to view budesonide Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/203634s004lbl.pdf) Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/203634s004lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/203634s004lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/28730856) Interleukin-5 (Organism: Homo sapiens, class: Cytokine, accessions: P05113, gene: IL5, swissprot: IL5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20627591) Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/28937774) Budesonide is a synthetic corticosteroid. Budesonide is provided as a mixture of two epimers (22R and 22S). Budesonide is an anti-inflammatory corticosteroid and has a high glucocorticoid effect and a weak mineralocorticoid effect, and the affinity of budesonide to glucocorticoid receptors, which reflects the intrinsic potency of the drug, is about 200-fold that of cortisol and 15-fold that of prednisolone. Budesonide is indicated for treatment of mild to moderate active Crohn’s disease involving the ileum and/or the ascending colon, for maintenance of clinical remission of mild to moderate Crohn’s disease involving the ileum and/or the ascending colon, for the induction of remission in patients with active, mild to moderate ulcerative colitis. Also budesonide is indicated for the management of nasal symptoms of seasonal or perennial allergic rhinitis. In combination with long-acting beta2-adrenergic agonist budesonide is used for the treatment of asthma. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Asthmatic Agents (Code: D018927) Anti-Inflammatory Agents (Code: D000893) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) bronchodilator agent (Code: CHEBI:35523) anti-inflammatory drug (Code: CHEBI:35472) 1994-02-14 FDA 8W5
Click to view benzthiazide Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16858005) Solute carrier family 12 member 3 (Organism: Homo sapiens, class: Transporter, accessions: P55017, gene: SLC12A3, swissprot: S12A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14766743) Benzthiazide is an intermediate acting agent belonging to the class of thiazide diuretics. Benzthiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Benzthiazide is used for the treatment of high blood pressure and management of edema. diuretic (Code: CHEBI:35498) antihypertensive agent (Code: CHEBI:35674) 1960-10-14 FDA
Click to view trandolapril Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020591s030lbl.pdf) Liver carboxylesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23141, gene: CES1, swissprot: EST1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19185566) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Trandolapril is the ethyl ester prodrug of a nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, trandolaprilat. Trandolapril is de-esterified to its diacid metabolite, trandolaprilat. Both inhibit angiotensinconverting enzyme (ACE) in human subjects and in animals. Trandolaprilat is about 8 times more potent than trandolapril. Trandolapril is used for the treatment of mild to moderate hypertension, as an adjunct in the treatment of congestive heart failure, to improve survival following myocardial infarction and to slow progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy. Angiotensin Converting Enzyme Inhibitor (Code: N0000175562) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 1996-04-26 FDA
Click to view carbifene
Click to view lafutidine histamine H(2)-receptor antagonist used as an antiulcer drug Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H2 Antagonists (Code: D006635) Neurotransmitter Agents (Code: D018377)
Click to view fluprednidene acetate has anti-inflammatory & anti-allergic properties; minor descriptor (75-83); on-line & Index Medicus search PREGNADIENETRIOLS (75-83); RN given refers to (11beta)-isomer; structure Adrenal Cortex Hormones (Code: D000305) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view mizolastine Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) a long-acting H1-antihistamine indicated for the symptomatic relief of seasonal allergic rhinoconjunctivitis (hay fever), perennial allergic rhinoconjunctivitis and urticaria Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Neurotransmitter Agents (Code: D018377) 2003-03-07 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view hydrocortisone butyrate Hydrocortisone Butyrate is the butyrate salt form of hydrocortisone, a synthetic glucocorticoid receptor agonist with antiinflammatory, antipruritic and vasoconstrictive effects. Hydrocortisone Butyrate is a prodrug of hydrocortisone. (See: hydrocortisone) dermatologic drug (Code: CHEBI:50177) 1982-03-31 FDA
Click to view latanoprost Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206185s000lbl.pdf) Latanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure. Prostaglandin Analog (Code: N0000175454) Prostaglandins (Code: N0000007706) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) antihypertensive agent (Code: CHEBI:35674) prodrug (Code: CHEBI:50266) antiglaucoma drug (Code: CHEBI:39456) 1996-06-05 FDA
Click to view clometocillin Clometocillin is benzylpenicillin in which the phenylacetyl group has been replaced by a (3,4-dichlorophenyl)(methoxy)acetyl group. It is an antibacterial drug. antibacterial drug (Code: CHEBI:36047)
Click to view brovincamine Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view mycophenolate mofetil Mycophenolate mofetil is absorbed following oral administration and hydrolyzed to mycophenolic acid (MPA), the active metabolite. MPA is a selective, uncompetitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation into DNA. 1995-05-03 FDA
Click to view belotecan DNA topoisomerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P11387, gene: TOP1, swissprot: TOP1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/9875499) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase I Inhibitors (Code: D059004) Topoisomerase Inhibitors (Code: D059003) 2003-12-10 Korean Food and Drug Administration (KFDA)
Click to view lubeluzole Sodium channel protein type 2 subunit alpha (Organism: Rattus norvegicus, class: Ion channel, accessions: P04775, gene: Scn2a, swissprot: SCN2A_RAT a benzothiazole compound; used for the treatment of acute ischemic stroke; R-91154 is the inactive isomer Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Neuroprotective Agents (Code: D018696) Protective Agents (Code: D020011)
Click to view sivelestat Myeloblastin (Organism: Homo sapiens, class: Unclassified, accessions: P24158, gene: PRTN3, swissprot: PRTN3_HUMAN Neutrophil elastase (Organism: Homo sapiens, class: Enzyme, accessions: P08246, gene: ELANE, swissprot: ELNE_HUMAN Neutrophil elastase (Organism: Mus musculus, class: Unclassified, accessions: Q3UP87, gene: Elane, swissprot: ELNE_MOUSE inhibitor of neutrophil elastase; structure given in first source Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) PMDA
Click to view fluperolone Adrenal Cortex Hormones (Code: D000305) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view triamcinolone acetonide Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) Annexin A1 (Organism: Homo sapiens, class: Cytosolic other, accessions: P04083, gene: ANXA1, swissprot: ANXA1_HUMAN) An esterified form of TRIAMCINOLONE. It is an anti-inflammatory glucocorticoid used topically in the treatment of various skin disorders. Intralesional, intramuscular, and intra-articular injections are also administered under certain conditions. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) 1960-01-04 FDA 1TA
Click to view rutoside Aldose reductase (Organism: Rattus norvegicus, class: Enzyme, accessions: P07943, gene: Akr1b1, swissprot: ALDR_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12193020) Sialidase (Organism: Clostridium perfringens, class: Enzyme, accessions: P10481, gene: nanH, swissprot: NANH_CLOPF) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19729316) Neuraminidase (Organism: Influenza A virus (A/WSN/1933(H1N1)), class: Enzyme, accessions: B4URF0, gene: NA, swissprot: B4URF0_9INFA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19729316) Bifunctional epoxide hydrolase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P34913, gene: EPHX2, swissprot: HYES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24679441) Neuromedin-U receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q9GZQ4, gene: NMUR2, swissprot: NMUR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25262941) Aldo-keto reductase family 1 member B10 (Organism: Homo sapiens, class: Enzyme, accessions: O60218, gene: AKR1B10, swissprot: AK1BA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26529431) Rutoside (rutin) is the glycoside flavonoid found in capers, olives, buckwheat (whole grain flour), asparagus, raspberry. As a component of dietary supplement, rutin is used for treatment of osteoarthritis. Rutoside is used to prevent mucositis due to cancer treatment, to treat blood vessel disease such as varicose veins, bleeding, hemorrhoids. 1963-12-31 Health Canada RUT
Click to view flunisolide Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) corticosteroid prescribed as treatment for allergic rhinitis Anti-Asthmatic Agents (Code: D018927) Anti-Inflammatory Agents (Code: D000893) Respiratory System Agents (Code: D019141) immunosuppressive agent (Code: CHEBI:35705) anti-inflammatory drug (Code: CHEBI:35472) anti-asthmatic drug (Code: CHEBI:49167) 1981-09-24 FDA
Click to view dexamethasone acetate Dexamethasone (betamethasone) acetate is an acetate ester, a derivative and a prodrug of dexamethasone (betamethasone). (See: dexamethasone) Anti-Inflammatory Agents (Code: D000893) dexamethasone acetate: 1973-09-06 FDA betamethasone acetate: 1965-03-03 FDA
Click to view niperotidine Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) antagonist (Source: CAROPPO, R, EFFECT OF NIPEROTIDINE ON HYDROGEN-ION SECRETION AND ELECTRICAL PARAMETERS OF ISOLATED ASTRIC-MUCOSA, Curr. Ther. Res.-Clin. Exp., 1990, 48, 1, 20-29)
Click to view pirarubicin Antineoplastic Agents (Code: D000970)
Click to view glisolamide
Click to view flupentixol D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1552626565904.pdf) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1552626565904.pdf) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1552626565904.pdf) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8301582) Potassium channel subfamily K member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O95069, gene: KCNK2, swissprot: KCNK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26588045) Ubiquitin carboxyl-terminal hydrolase 1 (Organism: Homo sapiens, class: Enzyme, accessions: O94782, gene: USP1, swissprot: UBP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27362876) Flupentixol is a D1 and D2 receptor antagonist and an antipsychotic neuroleptic drug. It is a thioxanthene, and therefore closely related to the phenothiazines. Its primary use is as a long acting injection given two or three weekly to people with schizophrenia who have a poor compliance with medication and suffer frequent relapses of illness. It is used for the treatment of schizophrenia and depression. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1964-01-01 YEAR INTRODUCED
Click to view chlorbenzoxamine
Click to view etravirine Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022187s025lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022187s025lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022187s025lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022187s025lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022187s025lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022187s025lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022187s025lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022187s025lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21189339) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/21189339) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/21189339) Canalicular multispecific organic anion transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: O15438, gene: ABCC3, swissprot: MRP3_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/21189339) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Etravirine is an antiretroviral agent more specifically classified as a Non-Nucleoside Reverse Transcriptase Inhibitor. Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1, and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma. Etraverine is used clinically for the treatment of human immunodeficiency virus type 1 (HIV-1) infection. Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175463) Non-Nucleoside Analog (Code: N0000175460) Non-Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009948) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 2008-01-18 FDA 65B
Click to view cloxotestosterone
Click to view sertaconazole Indoleamine 2,3-dioxygenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P14902, gene: IDO1, swissprot: I23O1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25036789) Sertaconazole, an azole antifungal agent, inhibits fungal cytochrome P-450-mediated 14 alpha-lanosterol demethylase enzyme. This enzyme functions to convert lanosterol to ergosterol. Ergosterol is a key component of fungal cell membranes and lack of this component leads to fungal cell injury by leakage of key constituents in the cytoplasm from the cell. Sertaconazole is indicated for the topical treatment of interdigital tinea pedis, caused by: Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) antibacterial drug (Code: CHEBI:36047) antipruritic drug (Code: CHEBI:59683) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) 2003-12-10 FDA
Click to view aztreonam Aztreonam is a monobactam. It was originally isolated from Chromobacterium violaceum. It is a synthetic bactericidal antibiotic. Aztreonam acts by inhibition of bacterial cell wall synthesis. Aztreonam has been shown to be active against Citrobacter spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae (including ampicillin-resistant and other penicillinaseproducing strains), Klebsiella oxytoca, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Serratia spp. Aztreonam is used for the treatment of urinary tract infections (including pyelonephritis and cystitis), lower respiratory tract infections (including pneumonia and bronchitis), skin and skin-structure infections, intra-abdominal infections ans gynecologic infections. Monobactam Antibacterial (Code: N0000175493) Monobactams (Code: N0000011311) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) drug allergen (Code: CHEBI:88188) antibacterial drug (Code: CHEBI:36047) 1986-12-31 FDA
Click to view exatecan DX-8951a is hydrochloride & DX-895If is methanesulfonate; exatecan mesylate is a synonym for DX-8951f; structure given in first and second source Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase I Inhibitors (Code: D059004) Topoisomerase Inhibitors (Code: D059003)
Click to view trimazosin Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665)
Click to view valsartan Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021283s053lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021283s053lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021283s053lbl.pdf) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021283s053lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/28281384) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28281384) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28281384) Valsartan is a nonpeptide, orally active, and specific angiotensin II receptor blocker acting on the AT1 receptor subtype. Valsartan has much greater affinity (about 20,000-fold) for the AT1 receptor than for the AT2 receptor. Valsartan is indicated for the treatment of hypertension to reduce the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. It is also indicated for the treatment of heart failure (NYHA class II-IV) and for left ventricular dysfunction or failure after myocardial infarction when the use of an angiotensin-converting enzyme inhibitor (ACEI) is not appropriate. Angiotensin II Type 1 Receptor Blockers (Code: D047228) Angiotensin Receptor Antagonists (Code: D057911) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) antihypertensive agent (Code: CHEBI:35674) angiotensin receptor antagonist (Code: CHEBI:61016) Angiotensin 2 Receptor Antagonists (Code: N0000000070) Angiotensin 2 Receptor Blocker (Code: N0000175561) 1996-12-23 FDA
Click to view decamethonium Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18249544) Histamine H3 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5N1, gene: HRH3, swissprot: HRH3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18249544) Decamethonium is a quaternary ammonium ion that is a depolarising muscle relaxant. It is similar to acetylcholine and acts as a partial agonist of the nicotinic acetylcholine receptor. Binds to the nicotinic acetycholine receptors in the motor endplate and blocks access to the receptors. Decamethonium is used in anesthesia. nicotinic acetylcholine receptor agonist (Code: CHEBI:47958) muscle relaxant (Code: CHEBI:51371) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Depolarizing Agents (Code: D009467) Peripheral Nervous System Agents (Code: D018373) 1975-05-21 FDA DME
Click to view cloxacillin Penicillin-binding protein 1A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918, gene: mrcA, swissprot: PBPA_ECOLI) inhibitor (Source: https://europepmc.org/backend/ptpmcrender.fcgi?accid=PMC1805370&blobtype=pdf) Peptidoglycan D,D-transpeptidase MrdA (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD65, gene: mrdA, swissprot: MRDA_ECOLI) inhibitor (Source: https://europepmc.org/backend/ptpmcrender.fcgi?accid=PMC1805370&blobtype=pdf) Peptidoglycan D,D-transpeptidase FtsI (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD68, gene: ftsI, swissprot: FTSI_ECOLI) inhibitor (Source: https://europepmc.org/backend/ptpmcrender.fcgi?accid=PMC1805370&blobtype=pdf) Penicillin-binding protein (Organism: Staphylococcus aureus, class: Enzyme, accessions: P72355|Q53707|Q53725|Q53729|Q9XDB3, gene: pbp4|mecA|pbpA|PBP2|pbpF, swissprot: P72355_STAAU|Q53707_STAAU|Q53725_STAAU|Q53729_STAAU|Q9XDB3_STAAU) inhibitor (Source: https://europepmc.org/backend/ptpmcrender.fcgi?accid=PMC1805370&blobtype=pdf) Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 15 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63424, gene: Slc15a2, swissprot: S15A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Cloxacillin is a semisynthetic beta-lactamase resistant penicillin antibiotic with antibacterial activity. Cloxacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall, thereby preventing the cross-linkage of peptidoglycans, which are critical components of the bacterial cell wall. This leads to an interruption of the bacterial cell wall and causes bacterial cell lysis. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1974-09-17 FDA
Click to view fluphenazine D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1826762) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1826762) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15821958) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15821958) Pleiotropic ABC efflux transporter of multiple drugs (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Transporter, accessions: P33302, gene: PDR5, swissprot: PDR5_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19188399) Potassium channel subfamily K member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O95069, gene: KCNK2, swissprot: KCNK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26588045) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10460810) Fluphenazine is a phenothiazine with antipsychotic activity. Fluphenazine exerts its actions by blocking postsynaptic dopamine D2 receptors in the limbic, cortical system and basal ganglia. This prevents the actions of dopamine, thereby reducing the hallucinations and delusions that are associated with schizophrenia. Fluphenazine isused for the management of manifestations of psychotic disorders. Phenothiazine (Code: N0000175746) Phenothiazines (Code: N0000007544) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) phenothiazine antipsychotic drug (Code: CHEBI:37930) dopaminergic antagonist (Code: CHEBI:48561) 1959-09-09 FDA
Click to view fludroxycortide Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) A corticosteroid used topically in the treatment of various skin disorders. It is usually employed as a cream or an ointment, and is also used as a polyethylene tape with an adhesive. (From Martindale, The Extra Pharmacopoeia, 30th ed, p733) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1963-03-19 FDA
Click to view docusate sodium All-purpose surfactant, wetting agent, and solubilizer used in the drug, cosmetics, and food industries. It has also been used in laxatives and as cerumenolytics. It is usually administered as either the calcium, potassium, or sodium salt. Surface-Active Agents (Code: D013501) FDA
Click to view bialamicol
Click to view tianeptine Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25026323) Tianeptine is used for treating major depressive episodes (mild, moderate, or severe). It has structural similarities to the tricyclic antidepressants, but it has different pharmacological properties. Tianeptine is a selective serotonin reuptake enhancer (SSRE), opposite to the action of SSRIs. One review points to the cancellative effects of tianeptine and fluoxetine coadministration on serotonin reuptake. Another suggests that long-term administration of tianeptine has no effect on serotonin pathways. Tianeptine enhances the extracellular concentration of dopamine in the nucleus accumbens and modulates the D2 and D3 dopamine receptors, but this effect is modest and almost certainly indirect. There is also action on the NMDA and AMPA receptors. Recent reviews point to this pathway as a hypothesized mechanism of action, based on tianeptine's effect of reversing impaired neuroplasticity associated with stress. In Russia tianeptine is a schedule III controlled substance in the same list as the majority of benzodiazepines and barbiturates. Antidepressive Agents (Code: D000928) Antidepressive Agents, Tricyclic (Code: D000929) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) 1987-02-06 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view tigemonam Tigemonam is a dialkylazetidinone derivative and a monobactam. It is a beta-lactam agent useful for the treatment of bacterial infections. Tigemonam has spectrum of activity similar to that of aztreonam and highly resistantce to hydrolysis by the beta-lactamase enzymes. Tigemonam is active against Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view pazopanib Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Fibroblast growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P22607, gene: FGFR3, swissprot: FGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Tyrosine-protein kinase ITK/TSK (Organism: Homo sapiens, class: Kinase, accessions: Q08881, gene: ITK, swissprot: ITK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Macrophage colony-stimulating factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P07333, gene: CSF1R, swissprot: CSF1R_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022465s024s025lbl.pdf) Discoidin domain-containing receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: Q16832, gene: DDR2, swissprot: DDR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24754677) Pazopanib is a multi-tyrosine kinase inhibitor. In vitro, pazopanib inhibited ligand-induced autophosphorylation of VEGFR-2, Kit, and PDGFR-beta receptors. In vivo, pazopanib inhibited VEGF-induced VEGFR-2 phosphorylation in mouse lungs, angiogenesis in a mouse model, and the growth of some human tumor xenografts in mice. Pazopanib is used in the therapy of advanced renal cell carcinoma and soft tissue sarcomas. Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Cytochrome P450 2C8 Inhibitors (Code: N0000187062) antineoplastic agent (Code: CHEBI:35610) angiogenesis modulating agent (Code: CHEBI:50926) 2009-10-19 FDA
Click to view triparanol Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN C-8 sterol isomerase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P32352, gene: ERG2, swissprot: ERG2_YEAST 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Organism: Homo sapiens, class: Enzyme, accessions: Q15125, gene: EBP, swissprot: EBP_HUMAN Antilipemic agent with high ophthalmic toxicity. According to Merck Index, 11th ed, the compound was withdrawn from the market in 1962 because of its association with the formation of irreversible cataracts. Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847)
Click to view suxibuzone Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) antirheumatic drug (Code: CHEBI:35842) non-narcotic analgesic (Code: CHEBI:35481) peripheral nervous system drug (Code: CHEBI:49110) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) prodrug (Code: CHEBI:50266)
Click to view quinapril Quinaprilat: Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019885s043lbl.pdf) Quinapril: Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Solute carrier family 15 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63424, gene: Slc15a2, swissprot: S15A2_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Quinapril is a prodrug and non-sulfhydryl angiotensin converting enzyme inhibitor with antihypertensive activity. Quinapril is hydrolized into its active form quinaprilat, which binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This abolishes the potent vasoconstrictive actions of angiotensin II and leads to vasodilatation. Quinapril also causes a decrease in angiotensin II-induced aldosterone secretion by the adrenal cortex, thereby promoting diuresis and natriuresis, and increases bradykinin levels. Quinapril is used in the therapy of hypertension and congestive heart failure. Angiotensin Converting Enzyme Inhibitor (Code: N0000175562) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor (Code: CHEBI:35457) 1991-11-19 FDA
Click to view flusalan Flusalan is an anti-bacterial agent. It was used in handwash solutions.
Click to view pivmecillinam Pivaloyloxymethyl ester of amdinocillin that is well absorbed orally, but broken down to amdinocillin in the intestinal mucosa. It is active against gram-negative organisms and used as for amdinocillin. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076) antibacterial drug (Code: CHEBI:36047) antiinfective agent (Code: CHEBI:35441) prodrug (Code: CHEBI:50266)
Click to view polythiazide Solute carrier family 12 member 3 (Organism: Homo sapiens, class: Transporter, accessions: P55017, gene: SLC12A3, swissprot: S12A3_HUMAN) inhibitor A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p826) Increased Diuresis (Code: N0000175359) Thiazide Diuretic (Code: N0000175419) Thiazides (Code: N0000166469) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283) Sodium Chloride Symporter Inhibitors (Code: D049993) 1961-09-26 FDA
Click to view estramustine Microtubule-associated protein 2 (Organism: Homo sapiens, class: Structural, accessions: P11137, gene: MAP2, swissprot: MTAP2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1647395) Microtubule-associated protein 1A (Organism: Homo sapiens, class: Structural, accessions: P78559, gene: MAP1A, swissprot: MAP1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1647395) Estramustine is an alkylating agent. The mechanism of action of estramustine is as an alkylating activity. The chemical classification of estramustine is estradiol, and nitrogen mustard compounds. Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Estradiol (Code: N0000007246) Nitrogen Mustard Compounds (Code: N0000007659) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Antineoplastic Agents, Hormonal (Code: D018931) Noxae (Code: D009676) antineoplastic agent (Code: CHEBI:35610)
Click to view aminopterin Dihydrofolate reductase (Organism: Lactobacillus casei, class: Enzyme, accessions: P00381, gene: folA, swissprot: DYR_LACCA Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN Dihydrofolate reductase (Organism: Escherichia coli, class: Unclassified, accessions: B0BL08, gene: dfrA17, swissprot: B0BL08_ECOLX Dihydrofolate reductase (Organism: Mus musculus, class: Enzyme, accessions: P00375, gene: Dhfr, swissprot: DYR_MOUSE Folylpoly-gamma-glutamate synthetase (Organism: Mus musculus, class: Unclassified, accessions: P48760, gene: Fpgs, swissprot: FOLC_MOUSE A folic acid derivative used as a rodenticide that has been shown to be teratogenic. Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) 04J
Click to view ceftezole Oligo-1,6-glucosidase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Unclassified, accessions: P53051, gene: IMA1, swissprot: MALX3_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17671744) Ceftezole is a semisynthetic first-generation cephalosporin with antibacterial activity. Ceftezole binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Ceftezole is active in vitro against many species of gram-positive and gram-negative bacteria except Pseudomonas aeruginosa, Serratia marcescens and Proteus vulgaris. Ceftezole is used for the treatment of susceptible bacterial infections including septicemia, respiratory, biliary or gastrointestinal tract, skin and skin structure, endocarditis and surgical prophylaxis. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1978 China Food and Drug Administration (CFDA)
Click to view flumedroxone acetate
Click to view lopinavir Pol polyprotein (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72874, gene: pol, swissprot: Q72874_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021906s051lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18473749) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12724045) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12724045) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12724045) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12724045) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20102298) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20102298) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17664327) Lopinavir is an antiretroviral protease inhibitor used in combination with ritonavir in the therapy and prevention of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS). Protease Inhibitor (Code: N0000175889) P-Glycoprotein Inhibitors (Code: N0000185503) Cytochrome P450 3A Inhibitors (Code: N0000190114) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Cytochrome P-450 CYP3A Inhibitors (Code: D065692) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) HIV Protease Inhibitors (Code: D017320) Metabolic Side Effects of Drugs and Substances (Code: D065606) Protease Inhibitors (Code: D011480) antiviral drug (Code: CHEBI:36044) 2000-09-15 FDA AB1
Click to view tirofiban Integrin alpha-IIb/beta-3 (Organism: Homo sapiens, class: Adhesion, accessions: P05106|P08514, gene: ITGA2B|ITGB3, swissprot: ITA2B_HUMAN|ITB3_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020912s021,020913s018lbl.pdf) a reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation, when administered intravenously inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner Decreased Platelet Aggregation (Code: N0000008832) Platelet Aggregation Inhibitor (Code: N0000175578) Cardiovascular Agents (Code: D002317) Fibrin Modulating Agents (Code: D050299) Fibrinolytic Agents (Code: D005343) Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) fibrin modulating drug (Code: CHEBI:48676) platelet glycoprotein-IIb/IIIa receptor antagonist (Code: CHEBI:50433) anticoagulant (Code: CHEBI:50249) 1998-05-14 FDA AGG
Click to view pentagestrone acetate
Click to view estradiol undecylate
Click to view sertindole Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1558671145067.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1558671145067.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1558671145067.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1558671145067.pdf) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1558671145067.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1558671145067.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1558671145067.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1558671145067.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9694935) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16135699) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16135699) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21341745) Sertindole is an antipsychotic drug with selective inhibitory effect on mesolimbic dopaminergic neurons and balanced inhibitory effects on central dopamine D2 and serotonin 5HT2 receptors as well as on alpha1-adrenergic receptors. Sertindole is indicated for the treatment of schizophrenia. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) second generation antipsychotic (Code: CHEBI:65191) serotonergic antagonist (Code: CHEBI:48279) alpha-adrenergic antagonist (Code: CHEBI:37890) H1-receptor antagonist (Code: CHEBI:37955) 1996-05-23 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view trimethidinium Trimethidinium is an asymmetric bisquaternary amine, possessing ganglionic blocking properties and antihypertensive activity. It was used for the treatment of hypertension.
Click to view folic acid ATP-binding cassette sub-family C member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q96J66, gene: ABCC11, swissprot: ABCCB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15537867) Canalicular multispecific organic anion transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: O15438, gene: ABCC3, swissprot: MRP3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11585759) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9827570) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) substrate (Source: lhttps://www.ncbi.nlm.nih.gov/pubmed/12036927) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12874005) Proton-coupled folate transporter (Organism: Homo sapiens, class: Transporter, accessions: Q96NT5, gene: SLC46A1, swissprot: PCFT_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17475902) Thymidylate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P04818, gene: TYMS, swissprot: TYSY_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3470522) Folate receptor alpha (Organism: Homo sapiens, class: Membrane receptor, accessions: P15328, gene: FOLR1, swissprot: FOLR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/25234128) Folate receptor beta (Organism: Homo sapiens, class: Membrane receptor, accessions: P14207, gene: FOLR2, swissprot: FOLR2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/25234128) Folic Acid (also known as folate or Vitamin B9) is a B complex vitamin. It is present in the liver and kidney and is found in mushrooms, spinach, yeast, green leaves, and grasses (POACEAE). Folic acid is required by the body for the synthesis of purines, pyrimidines, and methionine before incorporation into DNA or protein. Folic acid is the precursor of tetrahydrofolic acid, which is involved as a cofactor for transformylation reactions in the biosynthesis of purines and thymidylates of nucleic acids. Folic acid is required by the body for the synthesis of purines, pyrimidines, and methionine before incorporation into DNA or protein. Folic acid is the precursor of tetrahydrofolic acid, which is involved as a cofactor for transformylation reactions in the biosynthesis of purines and thymidylates of nucleic acids. Folic acid is used in the treatment and prevention of folate deficiencies, megaloblastic anemia and anemia of nutritional origin, pregnancy, infancy, or childhood. Growth Substances (Code: D006133) Hematinics (Code: D006397) Hematologic Agents (Code: D006401) Micronutrients (Code: D018977) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) B vitamin (Code: CHEBI:75769) 1946-08-13 FDA FOL
Click to view deflazacort Deflazacort: Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208684s003,208685s003lbl.pdf) 21-Desacetyldeflazacort: Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208684s003,208685s003lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208684s003,208685s003lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208684s003,208685s003lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208684s003,208685s003lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208684s003,208685s003lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208684s003,208685s003lbl.pdf) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208684s003,208685s003lbl.pdf) UDP-glucuronosyltransferase 2B15 (Organism: Homo sapiens, class: Enzyme, accessions: P54855, gene: UGT2B15, swissprot: UDB15_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208684s003,208685s003lbl.pdf) Deflazacort is a corticosteroid prodrug, whose active metabolite, 21-desDFZ, acts through the glucocorticoid receptor to exert anti-inflammatory and immunosuppressive effects. The precise mechanism by which deflazacort exerts its therapeutic effects in patients with Duchenne muscular dystrophy is unknown. Anti-Inflammatory Agents (Code: D000893) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) 1986-04-16 Italian Medicines Agency (AIFA)
Click to view troglitazone Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Thromboxane-A synthase (Organism: Homo sapiens, class: Enzyme, accessions: P24557, gene: TBXAS1, swissprot: THAS_HUMAN) Aldose reductase (Organism: Rattus norvegicus, class: Enzyme, accessions: P07943, gene: Akr1b1, swissprot: ALDR_RAT) Mitogen-activated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P28482, gene: MAPK1, swissprot: MK01_HUMAN) Glycogen [starch] synthase, liver (Organism: Homo sapiens, class: Enzyme, accessions: P54840, gene: GYS2, swissprot: GYS2_HUMAN) Aldose reductase (Organism: Homo sapiens, class: Enzyme, accessions: P15121, gene: AKR1B1, swissprot: ALDR_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Tyrosine-protein phosphatase non-receptor type 1 (Organism: Homo sapiens, class: Enzyme, accessions: P18031, gene: PTPN1, swissprot: PTN1_HUMAN Amine oxidase [flavin-containing] A (Organism: Homo sapiens, class: Enzyme, accessions: P21397, gene: MAOA, swissprot: AOFA_HUMAN Amine oxidase [flavin-containing] B (Organism: Homo sapiens, class: Enzyme, accessions: P27338, gene: MAOB, swissprot: AOFB_HUMAN UDP-glucuronosyltransferase 1-6 (Organism: Homo sapiens, class: Enzyme, accessions: P19224, gene: UGT1A6, swissprot: UD16_HUMAN Indoleamine 2,3-dioxygenase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q8R0V5, gene: Ido2, swissprot: I23O2_MOUSE Amine oxidase [flavin-containing] B (Organism: Rattus norvegicus, class: Enzyme, accessions: P19643, gene: Maob, swissprot: AOFB_RAT Indoleamine 2,3-dioxygenase 1 (Organism: Mus musculus, class: Enzyme, accessions: P28776, gene: Ido1, swissprot: I23O1_MOUSE Amine oxidase [flavin-containing] A (Organism: Rattus norvegicus, class: Enzyme, accessions: P21396, gene: Maoa, swissprot: AOFA_RAT Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT PPAR agonist formerly used for type II diabetes Cytochrome P-450 CYP3A Inducers (Code: D065701) Hypoglycemic Agents (Code: D007004) Metabolic Side Effects of Drugs and Substances (Code: D065606) platelet aggregation inhibitor (Code: CHEBI:50427) anticoagulant (Code: CHEBI:50249) antineoplastic agent (Code: CHEBI:35610) hypoglycemic agent (Code: CHEBI:35526) vasodilator agent (Code: CHEBI:35620) anticonvulsant (Code: CHEBI:35623) 1997-01-29 FDA GD4
TDZ
Click to view dofetilide Potassium voltage-gated channel subfamily H member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O95259, gene: KCNH1, swissprot: KCNH1_HUMAN) blocker (Source: ) Potassium channel subfamily K member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O95069, gene: KCNK2, swissprot: KCNK2_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) blocker Dofetilide show Vaughan Williams Class III antiarrhythmic activity. The mechanism of action is blockade of the cardiac ion channel carrying the rapid component of the delayed rectifier potassium current, IKr. At concentrations covering several orders of magnitude, dofetilide blocks only IKr with no relevant block of the other repolarizing potassium currents (e.g., IKs, IK1). At clinically relevant concentrations, dofetilide has no effect on sodium channels (associated with Class I effect), adrenergic alpha-receptors, or adrenergic beta-receptors. Antiarrhythmic (Code: N0000175426) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Potassium Channel Blockers (Code: D026902) anti-arrhythmia drug (Code: CHEBI:38070) 1999-10-01 FDA
Click to view diphemanil Diphemanil is a quarternary amine and a highly specific parasympathetic blocking agent. It binds muscarinic acetycholine receptors and thereby decreases secretory excretion of stomach acids as well as saliva and sweat. It was used in the treatment of peptic ulcer, gastric hyperacidity, and hypermotility in gastritis and pylorospasm, and in the treatment of hyperhidrosis (excessive perspiration). It was withdrawn from the market. muscarinic antagonist (Code: CHEBI:48876) parasympatholytic (Code: CHEBI:50370) bronchodilator agent (Code: CHEBI:35523) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) 1976-05-17 FDA
Click to view metacycline A broad-spectrum semisynthetic antibiotic related to TETRACYCLINE but excreted more slowly and maintaining effective blood levels for a more extended period. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) FDA
Click to view mazipredone Mazipredone is a water-soluble, long-acting prednisolone derivative used topically for skin conditions & parenterally as a glucocorticoid.
Click to view zuclopenthixol acetate Zuclopenthixol acetate is a lipophilic substance and a prodrug of zuclopenthixol which received by esterification of zuclopenthixol with acetic acid. When dissolved in oil and injected intramuscularly this substance diffuses slowly into the surrounding body water, where enzymatic breakdown occurs releasing the active component zuclopenthixol. Zuclopenthixol acetate is indicated for the initial treatment of acute psychoses including mania and exacerbation of chronic psychoses, particularly where a duration of effect of 2-3 days is desirable. (See: clopenthixol) 1987-10-15 Austrian Medicines and Medical Devices Agency
Click to view thiothixene Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: ) A thioxanthine used as an antipsychotic agent. Its effects are similar to the phenothiazine antipsychotics. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) Typical Antipsychotic (Code: N0000180182) 1967-07-24 FDA
Click to view prednival
Click to view raltegravir Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q76353, gene: None, swissprot: Q76353_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022145s038,205786s007,0203045s015lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022145s038,205786s007,0203045s015lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Raltegravir inhibits the catalytic activity of HIV-1 integrase, an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the covalent insertion, or integration, of unintegrated linear HIV-1 DNA into the host cell genome preventing the formation of the HIV-1 provirus. Raltegravir did not significantly inhibit human phosphoryltransferases including DNA polymerases alpha, beta and gamma. Raltegravir is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in patients 4 weeks of age and older. Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) HIV Integrase Inhibitors (Code: D019428) Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor (Code: N0000175887) 2007-10-12 FDA RLT
Click to view tetracycline Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11855680) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11855680) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11855680) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11855680) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11855680) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11855680) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11855680) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Tetracycline is a broad-spectrum naphthacene antibiotic produced semisynthetically from chlortetracycline, an antibiotic isolated from the bacterium Streptomyces aureofaciens. In bacteria, tetracycline binds to the 30S ribosomal subunit, interferes with the binding of aminoacyl-tRNA to the mRNA-ribosome complex, thereby inhibiting protein synthesis. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) antibacterial drug (Code: CHEBI:36047) antiprotozoal drug (Code: CHEBI:35820) Tetracycline-class Antimicrobial (Code: N0000175505) Tetracyclines (Code: N0000007948) 1953-11-19 FDA TAC
Click to view doxycycline 50S ribosomal protein L10 (Organism: Haloarcula marismortui (strain ATCC 43049 / DSM 3752 / JCM 8966 / VKM B-1809), class: Ribosomal protein, accessions: P15825, gene: rpl10, swissprot: RL10_HALMA) Tetracycline resistance protein, class B (Organism: Escherichia coli, class: Transporter, accessions: P02980, gene: tetA, swissprot: TCR2_ECOLX) Zinc finger protein mex-5 (Organism: Caenorhabditis elegans, class: Cytosolic other, accessions: Q9XUB2, gene: mex-5, swissprot: MEX5_CAEEL) Neutrophil collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P22894, gene: MMP8, swissprot: MMP8_HUMAN) inhibitor (Source: ) 72 kDa type IV collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P08253, gene: MMP2, swissprot: MMP2_HUMAN Stromelysin-1 (Organism: Homo sapiens, class: Enzyme, accessions: P08254, gene: MMP3, swissprot: MMP3_HUMAN Collagenase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P45452, gene: MMP13, swissprot: MMP13_HUMAN) inhibitor Matrilysin (Organism: Homo sapiens, class: Unclassified, accessions: P09237, gene: MMP7, swissprot: MMP7_HUMAN) inhibitor (Source: ) A synthetic tetracycline derivative with similar antimicrobial activity. Tetracycline-class Drug (Code: N0000175882) Tetracyclines (Code: N0000007948) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) antimalarial (Code: CHEBI:38068) antibacterial drug (Code: CHEBI:36047) 1967-12-05 FDA DXT
Click to view mitoxantrone DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2000/21120.pdf_Novantrone_Prntlbl.pdf) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Serine/threonine-protein kinase pim-1 (Organism: Homo sapiens, class: Kinase, accessions: P11309, gene: PIM1, swissprot: PIM1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23442188) Serine/threonine-protein kinase Chk2 (Organism: Homo sapiens, class: Kinase, accessions: O96017, gene: CHEK2, swissprot: CHK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23442188) Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23442188) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25618019) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25618019) Mitoxantrone is an antineoplastic antibiotic that is used in the treatment of acute leukemia, lymphoma, prostate and breast cancer. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Analgesics (Code: D000700) Antineoplastic Agents (Code: D000970) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) analgesic (Code: CHEBI:35480) antineoplastic agent (Code: CHEBI:35610) Topoisomerase Inhibitor (Code: N0000175609) 1987-12-23 FDA MIX
Click to view emepronium A muscarinic antagonist used mainly in the treatment of urinary syndromes. It is incompletely absorbed from the gastrointestinal tract and does not cross the blood-brain barrier. Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) Urological Agents (Code: D064804)
Click to view menatetrenone Cruzipain (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P25779, gene: None, swissprot: CYSP_TRYCR Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) bone density conservation agent (Code: CHEBI:50646)
Click to view halometasone Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Dermatologic Agents (Code: D003879) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view glisentide
Click to view glipizide Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16789425) Glipizide is an oral blood-glucose-lowering drug of the sulfonylurea class. Glipizide appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. Glipizide is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Sulfonylurea (Code: N0000175608) Sulfonylurea Compounds (Code: N0000008054) Hypoglycemic Agents (Code: D007004) hypoglycemic agent (Code: CHEBI:35526) 1984-05-08 FDA
Click to view metopimazine Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373)
Click to view thiopropazate minor descriptor (66-72); major descriptor (73-85); on-line search PHENOTHIAZINES (66-85); Index Medicus search PHENOTHIAZINES (66-72); THIOPROPAZATE (73-85); RN given refers to parent cpd phenothiazine antipsychotic drug (Code: CHEBI:37930) dopaminergic antagonist (Code: CHEBI:48561)
Click to view spiclomazine
Click to view baicalin GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN Prolyl endopeptidase (Organism: Homo sapiens, class: Enzyme, accessions: P48147, gene: PREP, swissprot: PPCE_HUMAN Cyclin-dependent kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P06493, gene: CDK1, swissprot: CDK1_HUMAN has iron chelating activity; chemical component of Chinese medicinal herb Huang-chin (Scutellaria baicalensis); do not confuse with baicalein Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Asthmatic Agents (Code: D018927) Anti-Infective Agents (Code: D000890) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) Sensory System Agents (Code: D018689) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) prodrug (Code: CHEBI:50266) 0XE
Click to view fluocortin butyl Adrenal Cortex Hormones (Code: D000305) Dermatologic Agents (Code: D003879) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view dalfopristin component of RP-59500 Streptogramin Antibacterial (Code: N0000175502) Streptogramins (Code: N0000011418) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1999-09-21 FDA
Click to view carpipramine D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view thioproperazine Thioproperazine is a phenothiazine derivative, a potent neuroleptic with antipsychotic properties. It is used for the treatment of all types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes. phenothiazine antipsychotic drug (Code: CHEBI:37930) 1962-12-31 Health Canada
Click to view gefitinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206995s003lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206995s003lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206995s003lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206995s003lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206995s003lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206995s003lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19932960) Beta-secretase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P56817, gene: BACE1, swissprot: BACE1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27046190) Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Tyrosine-protein kinase HCK (Organism: Homo sapiens, class: Kinase, accessions: P08631, gene: HCK, swissprot: HCK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Ephrin type-B receptor 4 (Organism: Homo sapiens, class: Kinase, accessions: P54760, gene: EPHB4, swissprot: EPHB4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Gefitinib reversibly inhibits the kinase activity of wild-type and certain activating mutations of EGFR, preventing autophosphorylation of tyrosine residues associated with the receptor, thereby inhibiting further downstream signalling and blocking EGFR-dependent proliferation. Gefitinib is indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations. Kinase Inhibitor (Code: N0000175605) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) antineoplastic agent (Code: CHEBI:35610) 2003-05-05 FDA
Click to view propyliodone Radiopaque medium usually in oil; used in bronchography. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) FDA
Click to view teclozan
Click to view tioclomarol
Click to view ampiroxicam prodrug of piroxicam; structure given in first source analgesic (Code: CHEBI:35480) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) antirheumatic drug (Code: CHEBI:35842) prodrug (Code: CHEBI:50266)
Click to view sisomicin 30S ribosomal protein S12 (Organism: Escherichia coli (strain K12), class: Cytosolic other, accessions: P0A7S3, gene: rpsL, swissprot: RS12_ECOLI) Antibiotic produced by Micromonospora inyoensis. It is closely related to gentamicin C1A, one of the components of the gentamicin complex (GENTAMICINS). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) 1977-01-01 YEAR INTRODUCED SIS
Click to view aripiprazole D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) partial agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021436s043,021713s034,021729s026,021866s028lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) partial agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021436s043,021713s034,021729s026,021866s028lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021436s043,021713s034,021729s026,021866s028lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207533s013lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207533s013lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021436s043,021713s034,021729s026,021866s028lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021436s043,021713s034,021729s026,021866s028lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27173799) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27173799) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24831693) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21341745) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12784105) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12784105) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12784105) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12784105) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12784105) Aripiprazole is an atypical antipsychotic drug. The mechanism of action of aripiprazole in schizophrenia or bipolar mania, is unclear. However, the efficacy of aripiprazole in the listed indications could be mediated through a combination of partial agonist activity at D2 and 5-HT1A receptors and antagonist activity at 5-HT2A receptors. Aripiprazole exhibits high affinity for dopamine D2 and D3, serotonin 5-HT1A and 5-HT2A receptors, moderate affinity for dopamine D4, serotonin 5-HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors, and moderate affinity for the serotonin reuptake site. Aripiprazole has no appreciable affinity for cholinergic muscarinic receptors. Aripiprazole is indicated for the treatment of schizophrenia, manic and mixed episodes associated with bipolar I disorder, major depressive disorder, irritability associated with autistic disorder and Tourette’s disorder. Atypical Antipsychotic (Code: N0000175430) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) second generation antipsychotic (Code: CHEBI:65191) H1-receptor antagonist (Code: CHEBI:37955) serotonergic agonist (Code: CHEBI:35941) 2002-11-15 FDA 9SC
Click to view algestone acetophenide A progesterone that has been used in ESTRUS SYNCHRONIZATION and has been evaluated as an injectable contraceptive in combination with estradiol enanthate. It is also used therapeutically as a topical anti-inflammatory and is applied topically in the treatment of ACNE. Anti-Inflammatory Agents (Code: D000893) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Oral (Code: D003276) Contraceptives, Oral, Synthetic (Code: D003280) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Progestins (Code: D011372) Reproductive Control Agents (Code: D012102) anti-inflammatory drug (Code: CHEBI:35472) synthetic oral contraceptive (Code: CHEBI:49326)
Click to view tolvaptan Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) antagonist Vasopressin V1a receptor (Organism: Homo sapiens, class: GPCR, accessions: P37288, gene: AVPR1A, swissprot: V1AR_HUMAN) antagonist (Source: ) Vasopressin V1a receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30560, gene: Avpr1a, swissprot: V1AR_RAT) antagonist (Source: ) Vasopressin V2 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: Q00788, gene: Avpr2, swissprot: V2R_RAT) antagonist (Source: ) Antidiuretic Hormone Receptor Antagonists (Code: D065092) Natriuretic Agents (Code: D045283) Vasopressin V2 Receptor Antagonist (Code: N0000193181) Vasopressin V2 Receptor Antagonists (Code: N0000193178) 2009-05-19 FDA
Click to view glisoxepide Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/2445740) oral sulfonylurea hypoglycemic agent which stimulates insulin secretion; minor descriptor (75-85); on-line & Index Medicus search SULFONYLUREA COMPOUNDS (75-85); RN given refers to parent cpd
Click to view sofalcone Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765)
Click to view tiomesterone
Click to view phytomenadione A lipid cofactor that is required for normal blood clotting. Several forms of vitamin K have been identified: VITAMIN K 1 (phytomenadione) derived from plants, VITAMIN K 2 (menaquinone) from bacteria, and synthetic naphthoquinone provitamins, VITAMIN K 3 (menadione). Vitamin K 3 provitamins, after being alkylated in vivo, exhibit the antifibrinolytic activity of vitamin K. Green leafy vegetables, liver, cheese, butter, and egg yolk are good sources of vitamin K. Antifibrinolytic Agents (Code: D000933) Coagulants (Code: D003029) Fibrin Modulating Agents (Code: D050299) Growth Substances (Code: D006133) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) Micronutrients (Code: D018977) Vitamins (Code: D014815) Increased Prothrombin Activity (Code: N0000175965) Reversed Anticoagulation Activity (Code: N0000175982) Vitamin K (Code: N0000006290) Warfarin Reversal Agent (Code: N0000175966) 2000-05-18 FDA PQN
Click to view doxazosin Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019668s028lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019668s028lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019668s028lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15098086) Potassium voltage-gated channel subfamily H member 6 (Organism: Homo sapiens, class: Ion channel, accessions: Q9H252, gene: KCNH6, swissprot: KCNH6_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15098086) Potassium voltage-gated channel subfamily H member 7 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NS40, gene: KCNH7, swissprot: KCNH7_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15098086) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11895100) A prazosin-related compound that is a selective alpha-1-adrenergic blocker. alpha-Adrenergic Blocker (Code: N0000175553) Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) antihypertensive agent (Code: CHEBI:35674) alpha-adrenergic antagonist (Code: CHEBI:37890) antineoplastic agent (Code: CHEBI:35610) vasodilator agent (Code: CHEBI:35620) antihyperplasia drug (Code: CHEBI:59844) 1990-11-02 FDA
Click to view dibekacin Macrolide 2'-phosphotransferase II; Macrolide 2'-phosphotransferase II protein MphB; Macrolide 2-phosphotransferase, mph(B) (Organism: Escherichia coli, class: Enzyme, accessions: O32553, gene: mphB, swissprot: O32553_ECOLX) Analog of KANAMYCIN with antitubercular as well as broad-spectrum antimicrobial properties. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1979-01-01 YEAR INTRODUCED 84D
Click to view homofenazine phenothiazine antipsychotic drug (Code: CHEBI:37930) anxiolytic drug (Code: CHEBI:35474)
Click to view cabergoline D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020664s013lbl.pdf) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020664s013lbl.pdf) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020664s013lbl.pdf) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12388666) Cabergoline is a long-acting dopamine receptor agonist with a high affinity for D2 receptors. Results of in vitro studies demonstrate that cabergoline exerts a direct inhibitory effect on the secretion of prolactin by rat pituitary lactotrophs. Cabergoline decreased serum prolactin levels in reserpinized rats Ergolines (Code: N0000007618) Ergot Derivative (Code: N0000175827) Anti-Dyskinesia Agents (Code: D018726) Antineoplastic Agents (Code: D000970) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) dopamine agonist (Code: CHEBI:51065) antiparkinson drug (Code: CHEBI:48407) antineoplastic agent (Code: CHEBI:35610) 1996-12-23 FDA
Click to view glucosaminylmuramyl dipeptide Glucosaminylmuramyl dipeptide (GMDP) is known as potent immunomodulator and an analogue of the peptidoglycan of the bacteria cell wall. GMDP affects marcophage function and cellular immunity. GMDP induces antigen expression on macrophage cell membranes and increases the production of superoxide radical. 2006-03-24 Ministry of Health of the Russian Federation
Click to view mannitol hexanitrate Mannitol hexanitrate is an explosive compound formed by the nitration of mannitol. Mannitol hexanitrate was used for the treatment of essential hypertension, for prevention of angina pectoris.
Click to view fluocinolone acetonide Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19744340) Fluocinolone Acetonide is a corticosteroid that binds to the cytosolic glucocorticoid receptor. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Fluocinolone Acetonide is used for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses, chronic non-infectious uveitis affecting the posterior segment of the eye. Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) antipruritic drug (Code: CHEBI:59683) anti-inflammatory drug (Code: CHEBI:35472) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) 1963-02-15 FDA
Click to view delapril Angiotensin-converting enzyme (Organism: Oryctolagus cuniculus, class: Enzyme, accessions: P12822, gene: ACE, swissprot: ACE_RABIT) Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/8891872) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480)
Click to view repaglinide ATP-binding cassette sub-family C member 8 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428, gene: ABCC8, swissprot: ABCC8_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020741s044lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020741s044lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020741s044lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020741s044lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24014644) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Repaglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus. Repaglinide closes ATP-dependent potassium channels in the beta-cell membrane by binding at characterizable sites. This potassium channel blockade depolarizes the ?-cell, which leads to an opening of calcium channels. The resulting increased calcium influx induces insulin secretion. Hypoglycemic Agents (Code: D007004) Glinide (Code: N0000175428) Potassium Channel Antagonists (Code: N0000175448) 1997-12-22 FDA BJX
Click to view diphenoxylate Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist Potassium voltage-gated channel subfamily A member 3 (Organism: Homo sapiens, class: Ion channel, accessions: P22001, gene: KCNA3, swissprot: KCNA3_HUMAN A MEPERIDINE congener used as an antidiarrheal, usually in combination with ATROPINE. At high doses, it acts like morphine. Its unesterified metabolite difenoxin has similar properties and is used similarly. It has little or no analgesic activity. Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Antidiarrheals (Code: D000930) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Gastrointestinal Agents (Code: D005765) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) antidiarrhoeal drug (Code: CHEBI:55323) Antidiarrheal (Code: N0000178374) 1960-09-15 FDA
Click to view butropium
Click to view cefixime Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Cefixime is a semisynthetic third-generation cephalosporin antibiotic. The bactericidal action of cefixime results from inhibition of cell wall synthesis. Cefixime is stable in the presence of certain beta-lactamase enzymes. As a result, certain organisms resistant to penicillins and some cephalosporins due to the presence of betalactamases may be susceptible to cefixime. Cefixime has been shown to be active against Streptococcus pneumoniae, Streptococcus pyogenes, Escherichia coli, Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, Proteus mirabilis. Cefixime is indicated for the treatment of Uncomplicated Urinary Tract Infections (due to E. coli and P. mirabilis),Otitis Media (due to H. influenzae, M. catarrhalis, and S. pyogenes), Pharyngitis and Tonsillitis (due to S. pyogenes), Acute Exacerbations of Chronic Bronchitis (due to S. pneumoniae and H. influenzae), Uncomplicated cervical/urethral Gonorrhea (due to N. gonorrhoeae). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) drug allergen (Code: CHEBI:88188) antibacterial drug (Code: CHEBI:36047) 1989-04-28 FDA C04
Click to view floxacillin Penicillin-binding protein 4 (Organism: Staphylococcus aureus, class: Enzyme, accessions: Q5D1E9, gene: None, swissprot: Q5D1E9_STAAU) inhibitor (Source: https://www.medsafe.govt.nz/profs/Datasheet/f/Flucloxacillinsodiuminj.pdf) Floxacillin is a narrow-spectrum, semisynthetic isoxazolyl penicillin with antibacterial activity. Floxacillin binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall, eventually causing cell lysis. Floxacillin is indicated for the treatment of infections due to sensitive Gram-positive organisms, including ?-lactamase-producing staphylococci and streptococci. Typical indications including, skin and soft tissue infections; respiratory tract infections; osteomyelitis, urinary tract infection, septicaemia, endocarditis. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1962-01-01 YEAR INTRODUCED
Click to view methotrexate Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208004s002lbl.pdf) 6-phosphogluconate dehydrogenase, decarboxylating (Organism: Homo sapiens, class: Enzyme, accessions: P52209, gene: PGD, swissprot: 6PGD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20235752) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20444863) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12849118) Canalicular multispecific organic anion transporter 2 (Organism: Rattus norvegicus, class: Transporter, accessions: O88563, gene: Abcc3, swissprot: MRP3_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12909565) Multidrug resistance-associated protein 7 (Organism: Homo sapiens, class: Transporter, accessions: Q5T3U5, gene: ABCC10, swissprot: MRP7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12527806) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20460822) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20460822) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8598312) Dihydrofolate reductase (Organism: Pneumocystis carinii, class: Enzyme, accessions: P16184, gene: None, swissprot: DYR_PNECA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7783147) Bifunctional dihydrofolate reductase-thymidylate synthase (Organism: Toxoplasma gondii, class: Enzyme, accessions: Q07422, gene: None, swissprot: DRTS_TOXGO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7783147) Thymidylate synthase (Organism: Escherichia coli, class: Enzyme, accessions: C3SWJ7, gene: thyA, swissprot: C3SWJ7_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11384244) Thymidylate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P04818, gene: TYMS, swissprot: TYSY_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11384244) Thymidylate synthase (Organism: Lactobacillus casei, class: Enzyme, accessions: P00469, gene: thyA, swissprot: TYSY_LACCA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11384244) Folate receptor beta (Organism: Homo sapiens, class: Membrane receptor, accessions: P14207, gene: FOLR2, swissprot: FOLR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25234128) Folate receptor alpha (Organism: Homo sapiens, class: Membrane receptor, accessions: P15328, gene: FOLR1, swissprot: FOLR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25234128) Folate transporter 1 (Organism: Homo sapiens, class: Unclassified, accessions: P41440, gene: SLC19A1, swissprot: S19A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25234128) Proton-coupled folate transporter (Organism: Homo sapiens, class: Transporter, accessions: Q96NT5, gene: SLC46A1, swissprot: PCFT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25234128) Serum paraoxonase/arylesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P27169, gene: PON1, swissprot: PON1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26458405) Methotrexate is an antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of tetrahydrofolate dehydrogenase and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA. Folate Analog Metabolic Inhibitor (Code: N0000175584) Folic Acid Metabolism Inhibitors (Code: N0000000111) Abortifacient Agents (Code: D000019) Abortifacient Agents, Nonsteroidal (Code: D000020) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Antirheumatic Agents (Code: D018501) Dermatologic Agents (Code: D003879) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Noxae (Code: D009676) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reproductive Control Agents (Code: D012102) 1953-12-07 FDA MT1
MTX
Click to view cetrimonium Dynamin-1 (Organism: Homo sapiens, class: Structural, accessions: Q05193, gene: DNM1, swissprot: DYN1_HUMAN Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Detergents (Code: D003902) Surface-Active Agents (Code: D013501) 16A
Click to view ribostamycin A broad-spectrum antimicrobial isolated from Streptomyces ribosifidicus. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) RIO
Click to view carfecillin The phenyl ester of CARBENICILLIN that, upon oral administration, is broken down in the intestinal mucosa to the active antibacterial. It is used for urinary tract infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Urinary (Code: D000892) Renal Agents (Code: D012076)
Click to view cefazolin Serum paraoxonase/arylesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P27169, gene: PON1, swissprot: PON1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16600468) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17344354) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Cefazolin is a semisynthetic cephalosporin analog, bactericidal agent that acts by inhibition of bacterial cell wall synthesis. Cefazolin has been shown to be active against most isolates of the following microorganisms: Staphylococcus aureus (methicillin-susceptible isolates only), Streptococcus agalactiae, Streptococcus pyogenes, Escherichia coli, Proteus mirabilis. Most isolates of indole positive Proteus (Proteus vulgaris), Enterobacter spp., Morganella morganii, Providencia rettgeri, Serratia spp., and Pseudomonas spp. are resistant to cefazolin. Cefazolin is indicated for preoperative prophylaxis and for the the treatment of Respiratory Tract Infections (Due to S. pneumoniae, Klebsiella spp., H. influenzae, S. aureus, and group A beta-hemolytic streptococci), Urinary Tract Infections (Due to E. coli, P. mirabilis, Klebsiella spp., and some strains of enterobacter and enterococci), Skin and Skin Structure Infections (Due to S. aureus, group A beta-hemolytic streptococci, and other strains of streptococci), Biliary Tract Infections (Due to E. coli, various strains of streptococci, P. mirabilis, Klebsiella spp., and S. aureus), Bone and Joint Infections (Due to S. aureus), Genital Infections (due to E. coli, P. mirabilis, Klebsiella spp., and some strains of enterococci), Septicemia (Due to S. pneumoniae, S. aureus, P. mirabilis, E. coli, and Klebsiella spp.) and Endocarditis (Due to S. aureus and group A beta-hemolytic streptococci). Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1973-10-04 FDA
Click to view verapamil Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11716514) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22587986) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Two pore calcium channel protein 1 (Organism: Homo sapiens, class: Unclassified, accessions: Q9ULQ1, gene: TPCN1, swissprot: TPC1_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/24776928) Two pore calcium channel protein 2 (Organism: Homo sapiens, class: Unclassified, accessions: Q8NHX9, gene: TPCN2, swissprot: TPC2_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/23063126) Potassium voltage-gated channel subfamily A member 10 (Organism: Homo sapiens, class: Ion channel, accessions: Q16322, gene: KCNA10, swissprot: KCA10_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/10836990) Potassium voltage-gated channel subfamily A member 7 (Organism: Homo sapiens, class: Ion channel, accessions: Q96RP8, gene: KCNA7, swissprot: KCNA7_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/11896454) Verapamil is a calcium ion influx inhibitor (slow-channel blocker or calcium ion antagonist) that exerts its pharmacologic effects by modulating the influx of ionic calcium across the cell membrane of the arterial smooth muscle as well as in conductile and contractile myocardial cells. Verapamil is indicated for the treatment of angina (in association with digitalis for the control of ventricular rate at rest and during stress in patients with chronic atrial flutter and/or atrial fibrillation), for prophylaxis of repetitive paroxysmal supraventricular tachycardia and fortheatment of essential hypertension. Calcium Channel Antagonists (Code: N0000000069) Calcium Channel Blocker (Code: N0000175566) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 3A Inhibitors (Code: N0000190114) P-Glycoprotein Inhibitors (Code: N0000185503) Anti-Arrhythmia Agents (Code: D000889) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) anti-arrhythmia drug (Code: CHEBI:38070) vasodilator agent (Code: CHEBI:35620) antihypertensive agent (Code: CHEBI:35674) 1981-08-12 FDA 4YH
Click to view lindane Lindane is the gamma isomer of 1,2,3,4,5,6-hexachlorocyclohexane. Lindane is an ectoparasiticide and ovicide effective against Pediculosis humanis capitis (head lice), Pthirus pubis (crab lice), and their ova. Lindane exerts its parasiticidal action by being directly absorbed into the parasites and their ova, where it interferes with GABA neurotransmitter function by interacting with the GABAA channel complex at the picrotoxin binding site. Due to toxicities, associated with lindane, it is used only in patients who cannot tolerate or have failed first-line treatment with safer medication. Lindane has been banned in many countries due to concerns about neurotoxicity and adverse effects on the environment. rodenticide (Code: CHEBI:33288) agrochemical (Code: CHEBI:33286) fungicide (Code: CHEBI:24127) pediculicide (Code: CHEBI:38706) Insecticides (Code: D007306) Pesticides (Code: D010575) 1974-12-19 FDA
Click to view sitaxentan Endothelin-1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P26684, gene: Ednra, swissprot: EDNRA_RAT) antagonist Endothelin-1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25101, gene: EDNRA, swissprot: EDNRA_HUMAN) antagonist Endothelin B receptor (Organism: Homo sapiens, class: GPCR, accessions: P24530, gene: EDNRB, swissprot: EDNRB_HUMAN) antagonist endothelin A receptor antagonist Endothelin Receptor Antagonists (Code: D065128) 2006-08-10 EMA
Click to view fenticonazole Fenticonazole is an imidazole derivative with a broad spectrum of antimycotic activity. Fenticonazole inhibits the synthesis of ergosterol, an important step in the formation of the wall of fungi and blocks the oxidizing enzymes with the corresponding accumulation of peroxides and necrosis of the fungal cell. In vitro studies have shown a broad fungistatic and fungicidal activity. Fenticonazole is used for the treatment of vaginal candidiasis. Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) antibacterial drug (Code: CHEBI:36047) 1986-03-10 Italian Medicines Agency (AIFA)
Click to view cefotaxime Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12650826) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Cefotaxime is a semisynthetic, broad spectrum cephalosporin antibiotic. The bactericidal activity of cefotaxime results from inhibition of cell wall synthesis. Cefotaxime has a high degree of stability in the presence of ?-lactamases, both penicillinases and cephalosporinases, of gram-negative and gram-positive bacteria. Cefotaxime has been shown to be active against Enterococcus spp., Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus spp. (Staphylococci which are resistant to methicillin/oxacillin must be considered resistant to cefotaxime), Acinetobacter spp., Citrobacter spp., Enterobacter spp., Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella spp., Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii, Serratia marcescens, some strains of Pseudomonas aeruginosa, Bacteroides spp., Clostridium spp. (Most strains of Clostridium difficile are resistant), Fusobacterium spp., Peptococcus spp., Peptostreptococcus spp. Cefotaxime is indicated for the treatment of Lower respiratory tract infections, Urinary tract infections, Gynecologic infections, Skin and skin structure infections, Intra-abdominal infections, Bone and joint infections, Central nervous system infections (meningitis and ventriculitis) and for the prevention of certain infections in patients undergoing surgical procedures. Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) drug allergen (Code: CHEBI:88188) antibacterial drug (Code: CHEBI:36047) 1981-03-11 FDA CE3
CEF
Click to view lacidipine Lacidipine is a calcium antagonist. Due to its long duration of action, lacidipine does not lead to reflex tachycardia. It displays specificity in the vascular smooth muscle, where it acts as an antihypertensive agent to dilate peripheral arterioles and reduce blood pressure. Compared to other dihydropyridine calcium antagonists, lacidipine exhibits a greater antioxidant activity which may confer potentially beneficial antiatherosclerotic effects. Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) 1998-05-18 Italian Medicines Agency (AIFA)
Click to view clevidipine Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Homo sapiens, class: Ion channel, accessions: Q01668, gene: CACNA1D, swissprot: CAC1D_HUMAN) blocker Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) blocker a calcium channel blocker and antihypertensive agent Calcium Channel Antagonists (Code: N0000000069) Dihydropyridine Calcium Channel Blocker (Code: N0000175421) Dihydropyridines (Code: N0000007556) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) 2008-08-01 FDA
Click to view riboflavin phosphate A coenzyme for a number of oxidative enzymes including NADH DEHYDROGENASE. It is the principal form in which RIBOFLAVIN is found in cells and tissues. Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) 1953-02-20 FDA
Click to view delavirdine Gag-Pol polyprotein (Organism: Human immunodeficiency virus type 1 group M subtype B (isolate ARV2/SF2), class: Polyprotein, accessions: P03369, gene: gag-pol, swissprot: POL_HV1A2) Histamine H4 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9H3N8, gene: HRH4, swissprot: HRH4_HUMAN) Malate dehydrogenase cytoplasmic (Organism: Homo sapiens, class: Enzyme, accessions: P40925, gene: MDH1, swissprot: MDHC_HUMAN Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1) inhibitor Beta-lactamase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P00811, gene: ampC, swissprot: AMPC_ECOLI Reverse transcriptase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q9WKE8, gene: reverse transcriptas, swissprot: Q9WKE8_9HIV1 A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175463) Non-Nucleoside Analog (Code: N0000175460) Non-Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009948) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) antiviral drug (Code: CHEBI:36044) 1997-04-04 FDA SPP
Click to view xenytropium
Click to view detajmium Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317)
Click to view testosterone undecanoate Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist Androgens (Code: D000728) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 2014-03-05 FDA
Click to view minocycline Multidrug transporter MdfA (Organism: Escherichia coli, class: Transporter, accessions: P0AEY8, gene: mdfA, swissprot: MDFA_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8426364) Minocycline is a tetracycline analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant staphylococcus infections. Minocycline is indicated for the treatment of infections caused by the following microorganisms: Gram-positive Bacteria (Bacillus anthracis, Listeria monocytogenes, Staphylococcus aureus, Streptococcus pneumoniae), Gram-negative Bacteria (Bartonella bacilliformis, Brucella species, Klebsiella granulomatis, Campylobacter fetus, Francisella tularensis, Haemophilus ducreyi, Vibrio cholerae, Yersinia pestis, Acinetobacter species, Enterobacter aerogenes, Escherichia coli, Haemophilus influenzae, Klebsiella species, Neisseria gonorrhoeae, Neisseria meningitidis, Shigella species) and Other Microorganisms (Actinomyces species, Borrelia recurrentis, Chlamydophila psittaci, Chlamydia trachomatis, Clostridium species, Entamoeba species, Fusobacterium nucleatum subspecies fusiforme, Mycobacterium marinum, Mycoplasma pneumoniae, Propionibacterium acnes, Rickettsiae, Treponema pallidum subspecies pallidum, Treponema pallidum subspecies pertenue, Ureaplasma urealyticum). Tetracycline-class Drug (Code: N0000175882) Tetracyclines (Code: N0000007948) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1971-06-30 FDA MIY
Click to view ormeloxifene A non-steroidal anti-fertility agent with anti-hormonal properties. Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Contraceptives, Postcoital (Code: D003281) Contraceptives, Postcoital, Synthetic (Code: D003283) Estrogen Antagonists (Code: D004965) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Reproductive Control Agents (Code: D012102)
Click to view azimilide Potassium voltage-gated channel subfamily KQT member 1 (Organism: Mus musculus, class: Unclassified, accessions: P97414, gene: Kcnq1, swissprot: KCNQ1_MOUSE) blocker (Source: ) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Cavia porcellus, class: Ion channel, accessions: O08703, gene: KCNH2, swissprot: KCNH2_CAVPO Potassium voltage-gated channel subfamily KQT member 1 (Organism: Cavia porcellus, class: Ion channel, accessions: O70344, gene: KCNQ1, swissprot: KCNQ1_CAVPO Anti-Arrhythmia Agents (Code: D000889) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990)
Click to view raltitrexed Thymidylate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P04818, gene: TYMS, swissprot: TYSY_HUMAN) inhibitor (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1553231488242.pdf) Reduced folate transporter (Organism: Homo sapiens, class: Transporter, accessions: P41440, gene: SLC19A1, swissprot: S19A1_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1553231488242.pdf) Folylpolyglutamate synthase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q05932, gene: FPGS, swissprot: FOLC_HUMAN) substrate (Source: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1553231488242.pdf) Thymidylate synthase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A884, gene: thyA, swissprot: TYSY_ECOLI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12570380) Thymidylate synthase (Organism: Escherichia coli, class: Enzyme, accessions: C3SWJ7, gene: thyA, swissprot: C3SWJ7_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12570380) Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16279780) Dihydrofolate reductase (Organism: Escherichia coli, class: Unclassified, accessions: B0BL08, gene: dfrA17, swissprot: B0BL08_ECOLX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16279780) Bifunctional dihydrofolate reductase-thymidylate synthase (Organism: Toxoplasma gondii, class: Enzyme, accessions: Q07422, gene: None, swissprot: DRTS_TOXGO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16279780) Raltitrexed is a folate analogue belonging to the family of anti-metabolites and has potent inhibitory activity against the enzyme thymidylate synthase (TS). Raltitrexed acts as a direct and specific TS inhibitor. Raltitrexed is transported into cells via a reduced folate carrier and is then extensively polyglutamated by the enzyme folyl polyglutamate synthetase to polyglutamate forms that are retained in cells and are even more potent inhibitors of TS. Raltitrexed is indicated for the palliative treatment of advanced colorectal cancer. Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) Noxae (Code: D009676) 1996-01-01 YEAR INTRODUCED D16
Click to view prifinium
Click to view fumagillin Methionine aminopeptidase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P50579, gene: METAP2, swissprot: MAP2_HUMAN empirical formula C25-27H34-37O7, a monoester of decatetraenedioic acid (HOOC-(C=CH)4-COOH and fumagillin (C16-17H25-26O3); FR 65814 lacks the fat Angiogenesis Inhibitors (Code: D020533) Angiogenesis Modulating Agents (Code: D043924) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Growth Inhibitors (Code: D006131) Growth Substances (Code: D006133) angiogenesis inhibitor (Code: CHEBI:48422) antiprotozoal drug (Code: CHEBI:35820) antibacterial drug (Code: CHEBI:36047)
Click to view astemizole Potassium voltage-gated channel subfamily H member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O95259, gene: KCNH1, swissprot: KCNH1_HUMAN) blocker (Source: ) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) Receptor tyrosine-protein kinase erbB-2 (Organism: Homo sapiens, class: Kinase, accessions: P04626, gene: ERBB2, swissprot: ERBB2_HUMAN) Substance-K receptor (Organism: Homo sapiens, class: GPCR, accessions: P21452, gene: TACR2, swissprot: NK2R_HUMAN) Sodium/nucleoside cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: O00337, gene: SLC28A1, swissprot: S28A1_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) Melanocortin receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: P32245, gene: MC4R, swissprot: MC4R_HUMAN) Melanocortin receptor 5 (Organism: Homo sapiens, class: GPCR, accessions: P33032, gene: MC5R, swissprot: MC5R_HUMAN) Melanocortin receptor 3 (Organism: Homo sapiens, class: GPCR, accessions: P41968, gene: MC3R, swissprot: MC3R_HUMAN) Membrane-associated progesterone receptor component 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: P70580, gene: Pgrmc1, swissprot: PGRC1_RAT) Calmodulin (Organism: Homo sapiens, class: Cytosolic other, accessions: P0DP23|P0DP24|P0DP25, gene: CALM1|CALM2|CALM3, swissprot: CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Histamine H4 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q9H3N8, gene: HRH4, swissprot: HRH4_HUMAN Somatostatin receptor type 5 (Organism: Homo sapiens, class: GPCR, accessions: P35346, gene: SSTR5, swissprot: SSR5_HUMAN Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN Protein farnesyltransferase (Organism: Bos taurus, class: Enzyme, accessions: P29702|P49355, gene: FNTA|FNTB, swissprot: FNTA_BOVIN|FNTB_BOVIN Polycomb protein EED (Organism: Homo sapiens, class: Unclassified, accessions: O75530, gene: EED, swissprot: EED_HUMAN Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects. Anti-Allergic Agents (Code: D018926) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Neurotransmitter Agents (Code: D018377) H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) 1988-12-31 FDA
Click to view prednisolone tebutate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN Glutamine synthetase (Organism: Homo sapiens, class: Enzyme, accessions: P15104, gene: GLUL, swissprot: GLNA_HUMAN Corticosteroid-binding globulin (Organism: Homo sapiens, class: Secreted, accessions: P08185, gene: SERPINA6, swissprot: CBG_HUMAN Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN Glucocorticoid receptor (Organism: Mus musculus, class: Transcription factor, accessions: P06537, gene: Nr3c1, swissprot: GCR_MOUSE Fatty acid-binding protein, liver (Organism: Rattus norvegicus, class: Unclassified, accessions: P02692, gene: Fabp1, swissprot: FABPL_RAT 1956-07-25 FDA
Click to view fluazacort
Click to view cerivastatin 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Organism: Homo sapiens, class: Enzyme, accessions: P04035, gene: HMGCR, swissprot: HMDH_HUMAN) inhibitor Nuclear receptor subfamily 1 group I member 3 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q14994, gene: NR1I3, swissprot: NR1I3_HUMAN) 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Organism: Rattus norvegicus, class: Enzyme, accessions: P51639, gene: Hmgcr, swissprot: HMDH_RAT cerivastatin is the ((E)-(+))-isomer; structure given in first source Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Hydroxymethylglutaryl-CoA Reductase Inhibitors (Code: D019161) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) 1997-06-26 FDA
Click to view fenoverine Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view oxytetracycline Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11855680) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11855680) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11855680) Oxytetracycline is a tetracycline used for treatment of infections caused by a variety of Gram positive and Gram negative microorganisms including Mycoplasma pneumoniae, Pasteurella pestis, Escherichia coli, Haemophilus influenzae (respiratory infections), and Diplococcus pneumoniae. Tetracycline-class Antimicrobial (Code: N0000175505) Tetracyclines (Code: N0000007948) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1964-09-08 FDA OTC
Click to view prednisolone succinate Adrenal Cortex Hormones (Code: D000305) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view cefotiam hexetil Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) prodrug (Code: CHEBI:50266)
Click to view hydrocortisone aceponate Hydrocortisone aceponate is a potent steroid with a low rate of percutaneous absorption and consequently a low potential for systemic toxicity. Hydrocortisone aceponate is used for the symptomatic treatment of various inflammatory or pruritic dermatoses. (See: hydrocortisone)
Click to view loxiglumide Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15108219) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15108219) Loxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide, the active enantiomer of loxiglumide, interacts competitively with CCK1 receptors. It is used for the treatment of Irritable Bowel Syndrome and Gastroesophageal Reflux Disease. In 2003, loxiglumide testing have been discontinued because the results of the studies showed that loxiglumide did not show statistically significant favorability over placebo. Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view prulifloxacin Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003)
Click to view bunamiodyl Bunamiodyl is structurally similar to iopanoic acid. Bunamiodyl is an cholecystographic agent which was used to aid the radiographic visualization of the gallbladder for detecting the presence of gallstones in cholelithiasis patients. It was withdrawn from the market due to nephropathy in 1983.
Click to view loprazolam GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P47869|P34903|P48169|P31644|Q16445|P18505|P47870|P28472|O14764|P78334|Q8N1C3|P18507|Q99928|O00591|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN) positive allosteric modulator (Source: www.mhra.gov.uk/home/groups/par/documents/websiteresources/con418469.pdf) Loprazolam is a hypnotic drug which stimulates GABA-A receptors. Loprazolam is indicated for the short-term treatment of insomnia including difficulty in falling asleep and/or frequent nocturnal awakenings. 1981-07-10 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view lenampicillin Lenampicillin is a prodrug of ampicillin. Lenampicillin is thought to enhance the absorption and decrease of side effects of ampicillin. (See: ampicillin) 2015-04-10 China Food and Drug Administration (CFDA)
Click to view cinnoxicam
Click to view azlocillin Penicillin-binding protein (Organism: Pseudomonas aeruginosa (strain ATCC 15692 / PAO1 / 1C / PRS 101 / LMG 12228), class: Enzyme, accessions: Q07806|Q51504|Q51505|Q9X6V3|Q9X6V7|Q9X6W0, gene: dacA|mrcA|pbpA|pbpB|pbpC|ponB, swissprot: PBPA_PSEAE|Q51504_PSEAI|Q51505_PSEAI|Q9X6V3_PSEAI|Q9X6V7_PSEAI|Q9X6W0_PSEAI) inhibitor A semisynthetic ampicillin-derived acylureido penicillin. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1982-09-03 FDA
Click to view cefalexin pivoxil
Click to view pimozide Ubiquitin carboxyl-terminal hydrolase 1 (Organism: Homo sapiens, class: Enzyme, accessions: O94782, gene: USP1, swissprot: UBP1_HUMAN D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Voltage-dependent T-type calcium channel subunit alpha-1I (Organism: Homo sapiens, class: Ion channel, accessions: Q9P0X4, gene: CACNA1I, swissprot: CAC1I_HUMAN) blocker (Source: ) Potassium voltage-gated channel subfamily A member 10 (Organism: Homo sapiens, class: Ion channel, accessions: Q16322, gene: KCNA10, swissprot: KCA10_HUMAN) blocker (Source: ) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) antagonist 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Calmodulin (Organism: Homo sapiens, class: Cytosolic other, accessions: P0DP23|P0DP24|P0DP25, gene: CALM1|CALM2|CALM3, swissprot: CALM1_HUMAN|CALM2_HUMAN|CALM3_HUMAN) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN D(2) dopamine receptor (Organism: Bos taurus, class: GPCR, accessions: P20288, gene: DRD2, swissprot: DRD2_BOVIN Dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901|P19020|P25115|P30729|P61169, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_RAT|DRD2_RAT|DRD3_RAT|DRD4_RAT|DRD5_RAT Voltage-dependent T-type calcium channel subunit alpha-1G (Organism: Homo sapiens, class: Ion channel, accessions: O43497, gene: CACNA1G, swissprot: CAC1G_HUMAN Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN Sodium channel protein type 2 subunit alpha (Organism: Rattus norvegicus, class: Ion channel, accessions: P04775, gene: Scn2a, swissprot: SCN2A_RAT Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN Voltage-dependent T-type calcium channel subunit alpha-1G (Organism: Rattus norvegicus, class: Ion channel, accessions: O54898, gene: Cacna1g, swissprot: CAC1G_RAT) blocker (Source: ) 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: ) G protein-activated inward rectifier potassium channel 2 (Organism: Mus musculus, class: Ion channel, accessions: P48542, gene: Kcnj6, swissprot: KCNJ6_MOUSE) gating inhibitor (Source: ) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Rattus norvegicus, class: Ion channel, accessions: Q9EQ60, gene: Cacna1h, swissprot: CAC1H_RAT) blocker (Source: ) A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403) Typical Antipsychotic (Code: N0000180182) Anti-Dyskinesia Agents (Code: D018726) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) H1-receptor antagonist (Code: CHEBI:37955) serotonergic antagonist (Code: CHEBI:48279) antidyskinesia agent (Code: CHEBI:66956) dopaminergic antagonist (Code: CHEBI:48561) first generation antipsychotic (Code: CHEBI:65190) 1984-07-31 FDA
Click to view tobuterol
Click to view bitolterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist a short-acting beta2 adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and COPD Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-2 Receptor Agonists (Code: D058666) Adrenergic beta-Agonists (Code: D000318) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) bronchodilator agent (Code: CHEBI:35523) anti-asthmatic drug (Code: CHEBI:49167) beta-adrenergic agonist (Code: CHEBI:35522) prodrug (Code: CHEBI:50266) 1984-12-28 FDA
Click to view cefatrizine Orally active semisynthetic cephalosporin antibiotic with broad-spectrum activity. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047)
Click to view cefamandole Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12650826) Cefamandole is a semisynthetic broad-spectrum cephalosporin antibiotic The bactericidal action of cefamandoleresults from inhibition of cell-wall synthesis. Cefamandole is usually active against: Staphylococcus aureus, Staphylococcus epidermidis, beta-hemolytic and other streptococci, Streptococcus pneumoniae, Escherichia coli, Klebsiella spp., Enterobacter spp., Haemophilus influenzae, Proteus mirabilis, Providencia rettgeri, Morganella morganii, Proteus vulgaris, Peptococcus and Peptostreptococcus spp., Clostridium spp., Bacteroides and Fusobacterium spp. Most strains of Bacteroides fragilis are resistant. Pseudomonas, Acinetobacter calcoaceticus (formerly Mima and Herellea spp.), and most Serratia strains are resistant to cefamandole. and certain other cephalosporins. Cefamandole is indicated for the treatment of Lower respiratory infections (due to S. pneumoniae, H. influenzae, Klebsiella spp., S. aureus, (beta)-hemolytic streptococci, and P. mirabilis), Urinary tract infections (due to E. coli, Proteus spp., Enterobacter spp., Klebsiella spp., group D streptococci and S. epidermidis), Peritonitis (due to E. coli and Enterobacter spp.), Septicemia (due to E. coli, S. aureus, S. pneumoniae, S. pyogenes, H. influenzae, and Klebsiella spp.), Skin and skin structure infections(due to S. aureus, S. pyogenes , H. influenzae, E. coli, Enterobacter spp., and P. mirabilis), Bone and joint infections (due to S. aureus). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1978-09-27 FDA SMX
Click to view tixocortol 21-thiol derivative of hydrocortisone Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) Anti-Allergic Agents (Code: D018926)
Click to view tafenoquine Tafenoquine, an 8-aminoquinoline antimalarial, is active against all the stages of Plasmodium species that include the hypnozoite (dormant stage) in the liver. Studies in vitro with the erythrocytic forms of Plasmodium falciparum suggest that tafenoquine may exert its effect by inhibiting hematin polymerization and inducing apoptotic like death of the parasite. In addition to its effect on the parasite, tafenoquine causes red blood cell shrinkage in vitro. The molecular target of tafenoquine is not known. Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) 2018-07-20 FDA
Click to view dibrompropamidine Urokinase-type plasminogen activator (Organism: Homo sapiens, class: Enzyme, accessions: P00749, gene: PLAU, swissprot: UROK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11311057) Suppressor of tumorigenicity 14 protein (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y5Y6, gene: ST14, swissprot: ST14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11311057) Prothrombin (Organism: Bos taurus, class: Enzyme, accessions: P00735, gene: F2, swissprot: THRB_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11311057) Dibrompropamidine is an antiseptic. Dibrompropamidine is used as dibrompropamidine isetionate for the treatment of wound infections due to Clostridia spp., E.coli, Pseudomonas pyocyanea and Proteus vulgaris. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 1959-01-16 Norwegian Medicines Agency
Click to view pivampicillin Pivampicillin is an ampicillin ester prodrug that is better absorbed from the gastrointestinal tract and after this completely hydrolyzed in the tissue and blood to ampicillin. (See: ampicillin) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) prodrug (Code: CHEBI:50266) 1975-02-07 Danish Medicines Agency
Click to view gentamicin DE 020 & DE 020 eyedrops both consist of KW 1062, benzalkonium chloride, sodium chloride, sodium hydroxide & distilled water pH 7.4; RN given refers to parent cpd; see also record for gentamicin C; structure Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view asulacrine DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) derivative of amsacrine; structure given in first source Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003)
Click to view sorafenib Serine/threonine-protein kinase B-raf (Organism: Homo sapiens, class: Kinase, accessions: P15056, gene: BRAF, swissprot: BRAF_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) RAF proto-oncogene serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P04049, gene: RAF1, swissprot: RAF1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021923s020lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19773380) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19773380) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19773380) Tyrosine-protein kinase ABL1 (Organism: Mus musculus, class: Kinase, accessions: P00520, gene: Abl1, swissprot: ABL1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621496) Mitogen-activated protein kinase 14 (Organism: Homo sapiens, class: Kinase, accessions: Q16539, gene: MAPK14, swissprot: MK14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20621496) Aurora kinase A (Organism: Homo sapiens, class: Kinase, accessions: O14965, gene: AURKA, swissprot: AURKA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23618709) Discoidin domain-containing receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: Q16832, gene: DDR2, swissprot: DDR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24754677) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26753815) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26753815) Mitogen-activated protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: P27361, gene: MAPK3, swissprot: MK03_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25778995) Mitogen-activated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P28482, gene: MAPK1, swissprot: MK01_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25778995) Receptor-interacting serine/threonine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: O43353, gene: RIPK2, swissprot: RIPK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17850214) Cytoplasmic tyrosine-protein kinase BMX (Organism: Homo sapiens, class: Kinase, accessions: P51813, gene: BMX, swissprot: BMX_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Sorafenib is a kinase inhibitor that decreases tumor cell proliferation in vitro. Sorafenib was shown to inhibit multiple intracellular (c-RAF, b-RAF and mutant BRAF) and cell surface kinases (KIT, FLT-3, RET, VEGFR-1, VEGFR-2, VEGFR-3, and PDGFR-beta). Several of these kinases are thought to be involved in tumor cell signaling, angiogenesis and apoptosis. Sorafenib is indicated for the treatment of unresectable hepatocellular carcinoma, advanced renal cell carcinoma, locally recurrent or metastatic, progressive, differentiated thyroid carcinoma refractory to radioactive iodine treatment. Kinase Inhibitor (Code: N0000175605) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) antineoplastic agent (Code: CHEBI:35610) angiogenesis inhibitor (Code: CHEBI:48422) 2005-12-20 FDA BAX
Click to view demeclocycline 30S ribosomal protein S4 (Organism: Escherichia coli (strain K12), class: Ribosomal protein, accessions: P0A7V8, gene: rpsD, swissprot: RS4_ECOLI) 30S ribosomal protein S9 (Organism: Escherichia coli (strain K12), class: Ribosomal protein, accessions: P0A7X3, gene: rpsI, swissprot: RS9_ECOLI) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN The tetracyclines are primarily bacteriostatic and are thought to exert their antimicrobial effect by the inhibition of protein synthesis. The tetracyclines, including demeclocycline have a similar antimicrobial spectrum of activity against a wide range of gram-negative and gram-positive organisms. Tetracycline-class Antimicrobial (Code: N0000175505) Tetracyclines (Code: N0000007948) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1960-01-14 FDA
Click to view bacampicillin Bacampicillin is a penicillin antibiotic. It is a prodrug of ampicillin with improved oral bioavailability. (See: ampicillin) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) prodrug (Code: CHEBI:50266) 1980-12-22 FDA
Click to view sulprostone Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN) agonist (Source: ) Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN) agonist (Source: ) Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN) agonist (Source: ) Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) Prostaglandin E2 receptor EP3 subtype (Organism: Mus musculus, class: GPCR, accessions: P30557, gene: Ptger3, swissprot: PE2R3_MOUSE) agonist (Source: ) Prostaglandin E2 receptor EP3 subtype (Organism: Rattus norvegicus, class: Unclassified, accessions: P34980, gene: Ptger3, swissprot: PE2R3_RAT) agonist (Source: ) Prostaglandin E2 receptor EP1 subtype (Organism: Mus musculus, class: GPCR, accessions: P35375, gene: Ptger1, swissprot: PE2R1_MOUSE) agonist (Source: ) Prostaglandin E2 receptor EP1 subtype (Organism: Rattus norvegicus, class: Unclassified, accessions: P70597, gene: Ptger1, swissprot: PE2R1_RAT) agonist (Source: ) Abortifacient Agents (Code: D000019) Abortifacient Agents, Nonsteroidal (Code: D000020) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Menstruation-Inducing Agents (Code: D008600) Reproductive Control Agents (Code: D012102)
Click to view cisapride 5-hydroxytryptamine receptor 4 (Organism: Rattus norvegicus, class: GPCR, accessions: Q62758, gene: Htr4, swissprot: 5HT4R_RAT) agonist (Source: ) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Organism: Homo sapiens, class: Enzyme, accessions: P04035, gene: HMGCR, swissprot: HMDH_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Membrane-associated progesterone receptor component 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: P70580, gene: Pgrmc1, swissprot: PGRC1_RAT) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) 5-hydroxytryptamine receptor 4 (Organism: Cavia porcellus, class: GPCR, accessions: O70528, gene: HTR4, swissprot: 5HT4R_CAVPO Serotonin 2 (5-HT2) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P08909|P14842|P30994, gene: Htr2a|Htr2b|Htr2c, swissprot: 5HT2A_RAT|5HT2B_RAT|5HT2C_RAT D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P19328|P22086|P22909, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT Serotonin 3 (5-HT3) receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35563|Q9JJ16, gene: Htr3a|Htr3b, swissprot: 5HT3A_RAT|5HT3B_RAT D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN D(1A) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901, gene: Drd1, swissprot: DRD1_RAT 5-hydroxytryptamine receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q13639, gene: HTR4, swissprot: 5HT4R_HUMAN) agonist Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Alpha-2A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P22909, gene: Adra2a, swissprot: ADA2A_RAT 5-hydroxytryptamine receptor 2A (Organism: Bos taurus, class: GPCR, accessions: Q75Z89, gene: HTR2A, swissprot: 5HT2A_BOVIN Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Serotonin 1 (5-HT1) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19327|P28564|P28565|P30940, gene: Htr1a|Htr1b|Htr1d|Htr1f, swissprot: 5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT Serotonin 3 (5-HT3) receptor (Organism: Homo sapiens, class: Ion channel, accessions: A5X5Y0|O95264|P46098|Q70Z44|Q8WXA8, gene: HTR3A|HTR3B|HTR3C|HTR3D|HTR3E, swissprot: 5HT3A_HUMAN|5HT3B_HUMAN|5HT3C_HUMAN|5HT3D_HUMAN|5HT3E_HUMAN D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN 5-hydroxytryptamine receptor 7 (Organism: Mus musculus, class: GPCR, accessions: P32304, gene: Htr7, swissprot: 5HT7R_MOUSE) agonist (Source: ) 5-hydroxytryptamine receptor 4 (Organism: Mus musculus, class: Unclassified, accessions: P97288, gene: Htr4, swissprot: 5HT4R_MOUSE) agonist (Source: ) A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed) Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) Neurotransmitter Agents (Code: D018377) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) serotonergic agonist (Code: CHEBI:35941) anti-ulcer drug (Code: CHEBI:49201) gastrointestinal drug (Code: CHEBI:55324) 1993-07-29 FDA
Click to view carumonam Carumonam is a N-sulfo-p-lactam antibiotic active against aerobic Gram-negative bacteria. It is resistant to hydrolysis by the common plasmid and beta-lactamases, but not by extended spectrum beta-lactamases. It is used for the treatment of urinary tract infections. antibacterial drug (Code: CHEBI:36047) 1988-01-01 YEAR INTRODUCED
Click to view benfotiamine Benfotiamine is a derivative of vitamin B1. It is prescribed there for treating sciatica and other painful nerve conditions. It is marketed as a medicine or dietary supplement. Benfotiamine reduces the extra biosynthesis and accumulation of a number of glucose metabolites, including glyceraldeyde-3-phosphate and dihydroxyacetone phosphate. Elevated levels of those glucose intermediates function as a trigger to most of the mechanisms accountable for hyperglycemia-caused cell damage. Benfotiamine increases tissue amounts of thiamine diphosphate, consequently growing transketolase activity and producing a significant decrease in glucose metabolites and precursors to AGEs. immunological adjuvant (Code: CHEBI:50847) nutraceutical (Code: CHEBI:50733) protective agent (Code: CHEBI:50267) BFT
Click to view spirapril Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Solute carrier family 15 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63424, gene: Slc15a2, swissprot: S15A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Spirapril is a prodrug and non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril is converted in the body to its active metabolite spiraprilat. Spiraprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Spiraprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 1994-12-29 FDA
Click to view loteprednol etabonate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist An androstadiene derivative corticosteroid that is used as an ANTI-ALLERGIC AGENT for the treatment of inflammatory and allergic eye conditions. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Anti-Allergic Agents (Code: D018926) 1998-03-09 FDA
Click to view edatrexate Folylpolyglutamate synthase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q05932, gene: FPGS, swissprot: FOLC_HUMAN) Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN) inhibitor Dihydrofolate reductase (Organism: Lactobacillus casei, class: Enzyme, accessions: P00381, gene: folA, swissprot: DYR_LACCA Dihydrofolate reductase (Organism: Mus musculus, class: Enzyme, accessions: P00375, gene: Dhfr, swissprot: DYR_MOUSE Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) 1978-01-01 YEAR INTRODUCED
Click to view tobramycin Tobramycin is an aminoglycoside antibacterial produced by Streptomyces tenebrarius. It acts primarily by disrupting protein synthesis, leading to altered cell membrane permeability, progressive disruption of the cell envelope, and eventual cell death. Tobramycin is indicated for the treatment of pseudomonas aeruginosa lung infections. Also being investigated for use in the treatment of sinus infections. Tobramycin is active against susceptible strains of the following microorganisms: Staphylococci, including S. aureus and S. epidermidis (coagulase-positive and coagulase-negative), including penicillin-resistant strains; Streptococci, including some of the Group A beta-hemolytic species, some nonhemolytic species, and some Streptococcus pneumoniae; Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Proteus mirabilis, Morganella morganii, most Proteus vulgaris strains, Haemophilus influenzae and H. aegyptius, Moraxella lacunata, and Acinetobacter calcoaceticus (Herellea aginacola) and some Neisseria species. Aminoglycoside Antibacterial (Code: N0000175477) Aminoglycosides (Code: N0000007853) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1975-06-11 FDA TOY
Click to view buprenorphine Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209819s009lbl.pdf) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) partial agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209819s009lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209819s009lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12033517) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12033517) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12033517) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12033517) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12033517) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12033517) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12033517) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12033517) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12033517) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19887017) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19887017) Buprenorphine is a morphinane alkaloid, a mu-opioid receptor partial agonist and a kappa-opioid receptor antagonist. Buprenorphine is used as an analgesic and for management of opioid dependence. Partial Opioid Agonist (Code: N0000175689) Partial Opioid Agonists (Code: N0000175685) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotic Antagonists (Code: D009292) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322) kappa-opioid receptor agonist (Code: CHEBI:59282) delta-opioid receptor antagonist (Code: CHEBI:59283) 1981-12-29 FDA
Click to view oxetacaine Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN isolated from bioactive leaf extracts of Rollinia mucosa Anesthetics (Code: D000777) Anesthetics, Local (Code: D000779) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view tiropramide Autonomic Agents (Code: D001337) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373)
Click to view adamexine mucolytic molecule in which cyclohexyl ring of bromhexine is replaced with adamantane
Click to view cromoglicic acid Protein S100-P (Organism: Homo sapiens, class: Unclassified, accessions: P25815, gene: S100P, swissprot: S100P_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17179482) A chromone complex that acts by inhibiting the release of chemical mediators from sensitized mast cells. It is used in the prophylactic treatment of both allergic and exercise-induced asthma, but does not affect an established asthmatic attack. Decreased Histamine Release (Code: N0000175628) Mast Cell Stabilizer (Code: N0000175630) Anti-Asthmatic Agents (Code: D018927) Respiratory System Agents (Code: D019141) anti-asthmatic drug (Code: CHEBI:49167) 1982-05-28 FDA
Click to view tartrazine An anionic, hydrophilic azo dye with an orange-yellow color used in fabrics, foods and cosmetics, and as a biological stain. Coloring Agents (Code: D004396) Food Additives (Code: D005503) Food Coloring Agents (Code: D005505) histological dye (Code: CHEBI:77178) food colouring (Code: CHEBI:77182)
Click to view lomerizine Voltage-dependent N-type calcium channel subunit alpha-1B (Organism: Homo sapiens, class: Ion channel, accessions: Q00975, gene: CACNA1B, swissprot: CAC1B_HUMAN used to treat migraines Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990)
Click to view ruboxistaurin Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN Protein kinase C theta type (Organism: Homo sapiens, class: Kinase, accessions: Q04759, gene: PRKCQ, swissprot: KPCT_HUMAN SRSF protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q96SB4, gene: SRPK1, swissprot: SRPK1_HUMAN Serine/threonine-protein kinase RIO3 (Organism: Homo sapiens, class: Kinase, accessions: O14730, gene: RIOK3, swissprot: RIOK3_HUMAN Ribosomal protein S6 kinase alpha-6 (Organism: Homo sapiens, class: Kinase, accessions: Q9UK32, gene: RPS6KA6, swissprot: KS6A6_HUMAN Ribosomal protein S6 kinase alpha-1 (Organism: Homo sapiens, class: Kinase, accessions: Q15418, gene: RPS6KA1, swissprot: KS6A1_HUMAN Cyclin-G-associated kinase (Organism: Homo sapiens, class: Kinase, accessions: O14976, gene: GAK, swissprot: GAK_HUMAN Dual specificity mitogen-activated protein kinase kinase 5 (Organism: Homo sapiens, class: Kinase, accessions: Q13163, gene: MAP2K5, swissprot: MP2K5_HUMAN Homeodomain-interacting protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q9H422, gene: HIPK3, swissprot: HIPK3_HUMAN Cyclin-dependent kinase-like 5 (Organism: Homo sapiens, class: Kinase, accessions: O76039, gene: CDKL5, swissprot: CDKL5_HUMAN Homeodomain-interacting protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9H2X6, gene: HIPK2, swissprot: HIPK2_HUMAN Serine/threonine-protein kinase pim-3 (Organism: Homo sapiens, class: Kinase, accessions: Q86V86, gene: PIM3, swissprot: PIM3_HUMAN NUAK family SNF1-like kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: O60285, gene: NUAK1, swissprot: NUAK1_HUMAN Protein kinase C iota type (Organism: Homo sapiens, class: Kinase, accessions: P41743, gene: PRKCI, swissprot: KPCI_HUMAN Serine/threonine-protein kinase TBK1 (Organism: Homo sapiens, class: Kinase, accessions: Q9UHD2, gene: TBK1, swissprot: TBK1_HUMAN Serine/threonine-protein kinase ICK (Organism: Homo sapiens, class: Kinase, accessions: Q9UPZ9, gene: ICK, swissprot: ICK_HUMAN Mitogen-activated protein kinase kinase kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q92918, gene: MAP4K1, swissprot: M4K1_HUMAN cAMP-dependent protein kinase catalytic subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: P17612, gene: PRKACA, swissprot: KAPCA_HUMAN Mitogen-activated protein kinase 15 (Organism: Homo sapiens, class: Kinase, accessions: Q8TD08, gene: MAPK15, swissprot: MK15_HUMAN MAP kinase-interacting serine/threonine-protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q9BUB5, gene: MKNK1, swissprot: MKNK1_HUMAN Serine/threonine-protein kinase Sgk3 (Organism: Homo sapiens, class: Kinase, accessions: Q96BR1, gene: SGK3, swissprot: SGK3_HUMAN Protein kinase C gamma type (Organism: Homo sapiens, class: Kinase, accessions: P05129, gene: PRKCG, swissprot: KPCG_HUMAN Dual specificity protein kinase CLK2 (Organism: Homo sapiens, class: Kinase, accessions: P49760, gene: CLK2, swissprot: CLK2_HUMAN G protein-coupled receptor kinase 7 (Organism: Homo sapiens, class: Kinase, accessions: Q8WTQ7, gene: GRK7, swissprot: GRK7_HUMAN Homeodomain-interacting protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q86Z02, gene: HIPK1, swissprot: HIPK1_HUMAN Dual specificity protein kinase CLK1 (Organism: Homo sapiens, class: Kinase, accessions: P49759, gene: CLK1, swissprot: CLK1_HUMAN Serine/threonine-protein kinase 10 (Organism: Homo sapiens, class: Kinase, accessions: O94804, gene: STK10, swissprot: STK10_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit gamma (Organism: Homo sapiens, class: Kinase, accessions: Q13555, gene: CAMK2G, swissprot: KCC2G_HUMAN Serine/threonine-protein kinase PLK4 (Organism: Homo sapiens, class: Kinase, accessions: O00444, gene: PLK4, swissprot: PLK4_HUMAN AP2-associated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q2M2I8, gene: AAK1, swissprot: AAK1_HUMAN Serine/threonine-protein kinase MARK2 (Organism: Homo sapiens, class: Kinase, accessions: Q7KZI7, gene: MARK2, swissprot: MARK2_HUMAN Protein kinase C epsilon type (Organism: Homo sapiens, class: Kinase, accessions: Q02156, gene: PRKCE, swissprot: KPCE_HUMAN Tyrosine-protein kinase JAK3 (Organism: Homo sapiens, class: Kinase, accessions: P52333, gene: JAK3, swissprot: JAK3_HUMAN Casein kinase II subunit alpha' (Organism: Homo sapiens, class: Kinase, accessions: P19784, gene: CSNK2A2, swissprot: CSK22_HUMAN Ribosomal protein S6 kinase alpha-5 (Organism: Homo sapiens, class: Kinase, accessions: O75582, gene: RPS6KA5, swissprot: KS6A5_HUMAN Serine/threonine-protein kinase pim-1 (Organism: Homo sapiens, class: Kinase, accessions: P11309, gene: PIM1, swissprot: PIM1_HUMAN Serine/threonine-protein kinase N2 (Organism: Homo sapiens, class: Kinase, accessions: Q16513, gene: PKN2, swissprot: PKN2_HUMAN Serine/threonine-protein kinase TAO1 (Organism: Homo sapiens, class: Kinase, accessions: Q7L7X3, gene: TAOK1, swissprot: TAOK1_HUMAN Tyrosine-protein kinase HCK (Organism: Homo sapiens, class: Kinase, accessions: P08631, gene: HCK, swissprot: HCK_HUMAN Aurora kinase C (Organism: Homo sapiens, class: Kinase, accessions: Q9UQB9, gene: AURKC, swissprot: AURKC_HUMAN Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN Citron Rho-interacting kinase (Organism: Homo sapiens, class: Kinase, accessions: O14578, gene: CIT, swissprot: CTRO_HUMAN Ribosomal protein S6 kinase alpha-3 (Organism: Homo sapiens, class: Kinase, accessions: P51812, gene: RPS6KA3, swissprot: KS6A3_HUMAN Myosin light chain kinase, smooth muscle (Organism: Homo sapiens, class: Kinase, accessions: Q15746, gene: MYLK, swissprot: MYLK_HUMAN Mitogen-activated protein kinase kinase kinase kinase 5 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y4K4, gene: MAP4K5, swissprot: M4K5_HUMAN Misshapen-like kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q8N4C8, gene: MINK1, swissprot: MINK1_HUMAN Leucine-rich repeat serine/threonine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q5S007, gene: LRRK2, swissprot: LRRK2_HUMAN Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN BMP-2-inducible protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9NSY1, gene: BMP2K, swissprot: BMP2K_HUMAN Serine/threonine-protein kinase pim-2 (Organism: Homo sapiens, class: Kinase, accessions: Q9P1W9, gene: PIM2, swissprot: PIM2_HUMAN TRAF2 and NCK-interacting protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9UKE5, gene: TNIK, swissprot: TNIK_HUMAN Calcium/calmodulin-dependent protein kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q96RR4, gene: CAMKK2, swissprot: KKCC2_HUMAN Ribosomal protein S6 kinase alpha-4 (Organism: Homo sapiens, class: Kinase, accessions: O75676, gene: RPS6KA4, swissprot: KS6A4_HUMAN STE20-like serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9H2G2, gene: SLK, swissprot: SLK_HUMAN Dual specificity protein kinase CLK4 (Organism: Homo sapiens, class: Kinase, accessions: Q9HAZ1, gene: CLK4, swissprot: CLK4_HUMAN Death-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9UIK4, gene: DAPK2, swissprot: DAPK2_HUMAN Serine/threonine-protein kinase 3 (Organism: Mus musculus, class: Kinase, accessions: Q9JI10, gene: Stk3, swissprot: STK3_MOUSE Serine/threonine-protein kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q13043, gene: STK4, swissprot: STK4_HUMAN Calcium/calmodulin-dependent protein kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q8N5S9, gene: CAMKK1, swissprot: KKCC1_HUMAN Serine/threonine-protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q13188, gene: STK3, swissprot: STK3_HUMAN Calcium/calmodulin-dependent protein kinase type 1D (Organism: Homo sapiens, class: Kinase, accessions: Q8IU85, gene: CAMK1D, swissprot: KCC1D_HUMAN Serine/threonine-protein kinase TAO2 (Organism: Homo sapiens, class: Kinase, accessions: Q9UL54, gene: TAOK2, swissprot: TAOK2_HUMAN Ribosomal protein S6 kinase alpha-2 (Organism: Homo sapiens, class: Kinase, accessions: Q15349, gene: RPS6KA2, swissprot: KS6A2_HUMAN Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform (Organism: Homo sapiens, class: Kinase, accessions: Q16816, gene: PHKG1, swissprot: PHKG1_HUMAN Mitogen-activated protein kinase kinase kinase kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q8IVH8, gene: MAP4K3, swissprot: M4K3_HUMAN Cyclin-dependent kinase 16 (Organism: Homo sapiens, class: Kinase, accessions: Q00536, gene: CDK16, swissprot: CDK16_HUMAN Casein kinase II subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: P68400, gene: CSNK2A1, swissprot: CSK21_HUMAN RAC-gamma serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q9Y243, gene: AKT3, swissprot: AKT3_HUMAN RAC-beta serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P31751, gene: AKT2, swissprot: AKT2_HUMAN Serine/threonine-protein kinase STK11 (Organism: Homo sapiens, class: Kinase, accessions: Q15831, gene: STK11, swissprot: STK11_HUMAN Rhodopsin kinase (Organism: Homo sapiens, class: Kinase, accessions: Q15835, gene: GRK1, swissprot: RK_HUMAN CaM kinase II (Organism: Homo sapiens, class: Kinase, accessions: Q13554|Q13555|Q13557|Q9UQM7, gene: CAMK2A|CAMK2B|CAMK2D|CAMK2G, swissprot: KCC2A_HUMAN|KCC2B_HUMAN|KCC2D_HUMAN|KCC2G_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit alpha (Organism: Homo sapiens, class: Kinase, accessions: Q9UQM7, gene: CAMK2A, swissprot: KCC2A_HUMAN G protein-coupled receptor kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P32298, gene: GRK4, swissprot: GRK4_HUMAN Mitogen-activated protein kinase kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y2U5, gene: MAP3K2, swissprot: M3K2_HUMAN Serine/threonine-protein kinase LATS2 (Organism: Homo sapiens, class: Kinase, accessions: Q9NRM7, gene: LATS2, swissprot: LATS2_HUMAN Dual specificity tyrosine-phosphorylation-regulated kinase 1B (Organism: Homo sapiens, class: Kinase, accessions: Q9Y463, gene: DYRK1B, swissprot: DYR1B_HUMAN Serine/threonine-protein kinase PRP4 homolog (Organism: Homo sapiens, class: Kinase, accessions: Q13523, gene: PRPF4B, swissprot: PRP4B_HUMAN Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma (Organism: Homo sapiens, class: Kinase, accessions: O60331, gene: PIP5K1C, swissprot: PI51C_HUMAN Proto-oncogene tyrosine-protein kinase ROS (Organism: Homo sapiens, class: Kinase, accessions: P08922, gene: ROS1, swissprot: ROS1_HUMAN Serine/threonine-protein kinase TAO3 (Organism: Homo sapiens, class: Kinase, accessions: Q9H2K8, gene: TAOK3, swissprot: TAOK3_HUMAN Cyclin-dependent kinase 7 (Organism: Homo sapiens, class: Kinase, accessions: P50613, gene: CDK7, swissprot: CDK7_HUMAN Death-associated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P53355, gene: DAPK1, swissprot: DAPK1_HUMAN Protein kinase C delta type (Organism: Homo sapiens, class: Kinase, accessions: Q05655, gene: PRKCD, swissprot: KPCD_HUMAN Death-associated protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: O43293, gene: DAPK3, swissprot: DAPK3_HUMAN Dual specificity tyrosine-phosphorylation-regulated kinase 1A (Organism: Homo sapiens, class: Kinase, accessions: Q13627, gene: DYRK1A, swissprot: DYR1A_HUMAN Myotonin-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: Q09013, gene: DMPK, swissprot: DMPK_HUMAN Serine/threonine-protein kinase LATS1 (Organism: Homo sapiens, class: Kinase, accessions: O95835, gene: LATS1, swissprot: LATS1_HUMAN Protein kinase C (PKC) (Organism: Rattus norvegicus, class: Kinase, accessions: P05696|P09215|P09216|P09217|P63319|P68403|Q64617|Q9WTQ0, gene: Prkca|Prkcb|Prkcd|Prkce|Prkcg|Prkch|Prkcq|Prkcz, swissprot: KPCA_RAT|KPCB_RAT|KPCD_RAT|KPCE_RAT|KPCG_RAT|KPCL_RAT|KPCT_RAT|KPCZ_RAT Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN Mitogen-activated protein kinase kinase kinase 9 (Organism: Homo sapiens, class: Kinase, accessions: P80192, gene: MAP3K9, swissprot: M3K9_HUMAN Mitogen-activated protein kinase kinase kinase 19 (Organism: Homo sapiens, class: Kinase, accessions: Q56UN5, gene: MAP3K19, swissprot: M3K19_HUMAN Phosphatidylinositol 5-phosphate 4-kinase type-2 beta (Organism: Homo sapiens, class: Kinase, accessions: P78356, gene: PIP4K2B, swissprot: PI42B_HUMAN 3-phosphoinositide-dependent protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: O15530, gene: PDPK1, swissprot: PDPK1_HUMAN Serine/threonine-protein kinase D2 (Organism: Homo sapiens, class: Kinase, accessions: Q9BZL6, gene: PRKD2, swissprot: KPCD2_HUMAN NUAK family SNF1-like kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q9H093, gene: NUAK2, swissprot: NUAK2_HUMAN SRSF protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P78362, gene: SRPK2, swissprot: SRPK2_HUMAN Dual specificity mitogen-activated protein kinase kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P45985, gene: MAP2K4, swissprot: MP2K4_HUMAN Serine/threonine-protein kinase tousled-like 1 (Organism: Homo sapiens, class: Kinase, accessions: Q9UKI8, gene: TLK1, swissprot: TLK1_HUMAN SRSF protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q9UPE1, gene: SRPK3, swissprot: SRPK3_HUMAN Dual specificity mitogen-activated protein kinase kinase 6 (Organism: Homo sapiens, class: Kinase, accessions: P52564, gene: MAP2K6, swissprot: MP2K6_HUMAN Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha (Organism: Homo sapiens, class: Kinase, accessions: Q99755, gene: PIP5K1A, swissprot: PI51A_HUMAN Mitogen-activated protein kinase kinase kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: Q99759, gene: MAP3K3, swissprot: M3K3_HUMAN Serine/threonine-protein kinase RIO1 (Organism: Homo sapiens, class: Kinase, accessions: Q9BRS2, gene: RIOK1, swissprot: RIOK1_HUMAN Cyclin-dependent kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P11802, gene: CDK4, swissprot: CDK4_HUMAN Ribosomal protein S6 kinase beta-1 (Organism: Homo sapiens, class: Kinase, accessions: P23443, gene: RPS6KB1, swissprot: KS6B1_HUMAN Serine/threonine-protein kinase Chk2 (Organism: Homo sapiens, class: Kinase, accessions: O96017, gene: CHEK2, swissprot: CHK2_HUMAN Serine/threonine-protein kinase 33 (Organism: Homo sapiens, class: Kinase, accessions: Q9BYT3, gene: STK33, swissprot: STK33_HUMAN Glycogen synthase kinase-3 beta (Organism: Homo sapiens, class: Kinase, accessions: P49841, gene: GSK3B, swissprot: GSK3B_HUMAN Calcium/calmodulin-dependent protein kinase type II subunit delta (Organism: Homo sapiens, class: Kinase, accessions: Q13557, gene: CAMK2D, swissprot: KCC2D_HUMAN Serine/threonine-protein kinase Chk1 (Organism: Homo sapiens, class: Kinase, accessions: O14757, gene: CHEK1, swissprot: CHK1_HUMAN cGMP-dependent protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q13237, gene: PRKG2, swissprot: KGP2_HUMAN cAMP-dependent protein kinase catalytic subunit beta (Organism: Homo sapiens, class: Kinase, accessions: P22694, gene: PRKACB, swissprot: KAPCB_HUMAN Protein kinase C eta type (Organism: Homo sapiens, class: Kinase, accessions: P24723, gene: PRKCH, swissprot: KPCL_HUMAN Serine/threonine-protein kinase N1 (Organism: Homo sapiens, class: Kinase, accessions: Q16512, gene: PKN1, swissprot: PKN1_HUMAN Mitogen-activated protein kinase kinase kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q12851, gene: MAP4K2, swissprot: M4K2_HUMAN Protein kinase C beta type (Organism: Homo sapiens, class: Kinase, accessions: P05771, gene: PRKCB, swissprot: KPCB_HUMAN Protein kinase C alpha type (Organism: Homo sapiens, class: Kinase, accessions: P17252, gene: PRKCA, swissprot: KPCA_HUMAN inhibits protein kinase C beta Enzyme Inhibitors (Code: D004791) LY4
Click to view clinofibrate
Click to view ivabradine Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 (Organism: Homo sapiens, class: Ion channel, accessions: O60741, gene: HCN1, swissprot: HCN1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16387796) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UL51, gene: HCN2, swissprot: HCN2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/206143Orig1s002lbl.pdf) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9P1Z3, gene: HCN3, swissprot: HCN3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16387796) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 (Organism: Mus musculus, class: Ion channel, accessions: O88703, gene: Hcn2, swissprot: HCN2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16387796) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y3Q4, gene: HCN4, swissprot: HCN4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16387796) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 (Organism: Mus musculus, class: Ion channel, accessions: O88704, gene: Hcn1, swissprot: HCN1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16387796) Ivabradine is a pure heart rate lowering agent, acting by selective and specific inhibition of the cardiac pacemaker If current that controls the spontaneous diastolic depolarisation in the sinus node and regulates heart rate. The cardiac effects are specific to the sinus node with no effect on intra-atrial, atrioventricular or intraventricular conduction times, nor on myocardial contractility or ventricular repolarisation.It is used in the treatment of chronic stable angina in patients unable to take beta-adrenergic blockers, and in the treatment of heart failure. Hyperpolarization-activated Cyclic Nucleotide-gated Channel Blocker (Code: N0000191544) Hyperpolarization-activated Cyclic Nucleotide-gated Channel Antagonists (Code: N0000191546) Cardiovascular Agents (Code: D002317) cardiotonic drug (Code: CHEBI:38147) 2005-10-25 EMA
Click to view diethylaminoethoxyhexestrol Diethylaminoethoxyhexestrol is a coronary vasodilator. Diethylaminoethoxyhexestrol was used for the treatment of angina pectoris. In 1970 it was withdrawn from production by the manufacturer due its effects on liver.
Click to view simfibrate
Click to view colforsin daropate Adenylate cyclase type 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q08828, gene: ADCY1, swissprot: ADCY1_HUMAN Solute carrier family 2, facilitated glucose transporter member 1 (Organism: Homo sapiens, class: Transporter, accessions: P11166, gene: SLC2A1, swissprot: GTR1_HUMAN Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Adenylate cyclase type 1 (Organism: Bos taurus, class: Unclassified, accessions: P19754, gene: ADCY1, swissprot: ADCY1_BOVIN Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland. Adjuvants, Immunologic (Code: D000276) Anti-Asthmatic Agents (Code: D018927) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Immunologic Factors (Code: D007155) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Respiratory System Agents (Code: D019141) Vasodilator Agents (Code: D014665)
Click to view bucladesine A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed) vasodilator agent (Code: CHEBI:35620) cardiotonic drug (Code: CHEBI:38147)
Click to view ebastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.geneesmiddeleninformatiebank.nl/smpc/h115466_smpc_en.pdf) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) substrate (Source: https://www.geneesmiddeleninformatiebank.nl/smpc/h115466_smpc_en.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.geneesmiddeleninformatiebank.nl/smpc/h115466_smpc_en.pdf) Cytochrome P450 4F12 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HCS2, gene: CYP4F12, swissprot: CP4FC_HUMAN) substrate (Source: https://www.geneesmiddeleninformatiebank.nl/smpc/h115466_smpc_en.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15911273) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21341745) Ebastine is a potent, highly selective antagonist of the histamine H1 receptor with prolonged effects and no anticholinergic effects. Ebastine is rapidly absorbed and undergoes extensive first-pass metabolism after oral administration. It is almost totally converted to the active metabolite carebastine. Ebastine is indicated for the treatment of allergic rhinitis and chronic idiopathic urticaria. Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) 1990-01-01 YEAR INTRODUCED
Click to view nefazodone 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q9WTR4, gene: Slc6a2, swissprot: Q9WTR4_RAT Sodium-dependent dopamine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P23977, gene: Slc6a3, swissprot: SC6A3_RAT Sodium-dependent serotonin transporter (Organism: Rattus norvegicus, class: Transporter, accessions: P31652, gene: Slc6a4, swissprot: SC6A4_RAT Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: ) an antidepressant for oral administration with a chemical structure unrelated to selective serotonin reuptake inhibitors, tricyclics, tetracyclics, or monoamine oxidase inhibitors (MAOI), inhibits neuronal uptake of serotonin and norepinephrine Serotonin Reuptake Inhibitor (Code: N0000175696) Antidepressive Agents (Code: D000928) Antidepressive Agents, Second-Generation (Code: D018687) Central Nervous System Agents (Code: D002491) Psychotropic Drugs (Code: D011619) antidepressant (Code: CHEBI:35469) serotonergic antagonist (Code: CHEBI:48279) serotonin uptake inhibitor (Code: CHEBI:50949) alpha-adrenergic antagonist (Code: CHEBI:37890) analgesic (Code: CHEBI:35480) 1994-12-22 FDA
Click to view troxerutin Troxerutin is a natural flavonoid drug, which has demonstrated an ability to: Inhibit the agglomeration of blood platelets and red blood cells; prevent thrombogenesis; protect endothelial cells; and enhance microcirculation. It has been reported that troxerutin can effectively cure venous diseases. Due to the ability of troxerutin to inhibit platelet aggregation and prevent thrombogenesis, it has also been reported that troxerutin can be used to treat sequelae of apoplexy (Yu Y., Zheng G.,Mol Med Rep. 2017;15(6):3473–3478). Anticoagulants (Code: D000925) Hematologic Agents (Code: D006401) 1986-04-21 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view dicloxacillin Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) cGMP-dependent 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O00408, gene: PDE2A, swissprot: PDE2A_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Streptokinase A (Organism: Streptococcus pyogenes serotype M1, class: Enzyme, accessions: P10520, gene: ska, swissprot: STRP_STRP1) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Penicillin-binding protein (Organism: Staphylococcus aureus, class: Enzyme, accessions: P72355|Q53707|Q53725|Q53729|Q9XDB3, gene: PBP2|mecA|pbp4|pbpA|pbpF, swissprot: P72355_STAAU|Q53707_STAAU|Q53725_STAAU|Q53729_STAAU|Q9XDB3_STAAU) inhibitor Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN One of the PENICILLINS which is resistant to PENICILLINASE. Penicillin-class Antibacterial (Code: N0000175497) Penicillins (Code: N0000011281) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1968-04-22 FDA
Click to view docarpamine a dopamine prodrug; RN given refers to (S)-isomer; structure given in first source Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377)
Click to view enoxolone Tyrosine-protein phosphatase non-receptor type 1 (Organism: Homo sapiens, class: Enzyme, accessions: P18031, gene: PTPN1, swissprot: PTN1_HUMAN Corticosteroid 11-beta-dehydrogenase isozyme 1 (Organism: Homo sapiens, class: Enzyme, accessions: P28845, gene: HSD11B1, swissprot: DHI1_HUMAN Corticosteroid 11-beta-dehydrogenase isozyme 2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P50233, gene: Hsd11b2, swissprot: DHI2_RAT Corticosteroid 11-beta-dehydrogenase isozyme 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P16232, gene: Hsd11b1, swissprot: DHI1_RAT Glycogen phosphorylase, muscle form (Organism: Oryctolagus cuniculus, class: Enzyme, accessions: P00489, gene: PYGM, swissprot: PYGM_RABIT Aldo-keto reductase family 1 member B10 (Organism: Homo sapiens, class: Enzyme, accessions: O60218, gene: AKR1B10, swissprot: AK1BA_HUMAN Corticosteroid 11-beta-dehydrogenase isozyme 1 (Organism: Mus musculus, class: Enzyme, accessions: P50172, gene: Hsd11b1, swissprot: DHI1_MOUSE Corticosteroid 11-beta-dehydrogenase isozyme 2 (Organism: Homo sapiens, class: Enzyme, accessions: P80365, gene: HSD11B2, swissprot: DHI2_HUMAN Protein-tyrosine phosphatase 1C (Organism: Homo sapiens, class: Enzyme, accessions: P29350, gene: PTPN6, swissprot: PTN6_HUMAN Tyrosine-protein phosphatase non-receptor type 11 (Organism: Homo sapiens, class: Enzyme, accessions: Q06124, gene: PTPN11, swissprot: PTN11_HUMAN Protein kinase C eta type (Organism: Homo sapiens, class: Kinase, accessions: P24723, gene: PRKCH, swissprot: KPCL_HUMAN An oleanolic acid from GLYCYRRHIZA that has some antiallergic, antibacterial, and antiviral properties. It is used topically for allergic or infectious skin inflammation and orally for its aldosterone effects in electrolyte regulation. Anti-Inflammatory Agents (Code: D000893) immunomodulator (Code: CHEBI:50846) CBW
Click to view cefmetazole Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Cefmetazole is a semisynthetic third-generation cephalosporin antibiotic. The bactericidal action of Cefmetazole results from inhibition of cell wall synthesis. Cefmetazole is used for the treatment of urinary tract infections (due to Escherichia coli), lower respiratory tract infections (due to Streptococcus pneumoniae, Staphylococcus aureus, E. coli, Haemophilus influenzae). In addition, it is effective against Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus agalactiae, Proteus vulgaris, and Bacteroides fragilis; preoperative prophylaxis of cesarean section, hysterectomy, cholecystectomy, and colorectal surgery. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1989-12-11 FDA 4KO
Click to view ebrotidine Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/8736619) an H2-receptor antagonist and gastric mucosa protector Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H2 Antagonists (Code: D006635) Neurotransmitter Agents (Code: D018377)
Click to view maraviroc C-C chemokine receptor type 5 (Organism: Homo sapiens, class: GPCR, accessions: P51681, gene: CCR5, swissprot: CCR5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022128s018,208984s001lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022128s018,208984s001lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Maraviroc is a member of a therapeutic class called CCR5 co-receptor antagonists. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the cell membrane, preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. CXCR4-tropic and dual-tropic HIV-1 entry is not inhibited by maraviroc. Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) CCR5 Receptor Antagonists (Code: D065100) antiviral drug (Code: CHEBI:36044) HIV fusion inhibitor (Code: CHEBI:59886) CCR5 Co-receptor Antagonist (Code: N0000175572) Chemokine Co-receptor 5 Antagonists (Code: N0000175445) 2007-08-06 FDA MRV
Click to view terfenadine Potassium voltage-gated channel subfamily H member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O95259, gene: KCNH1, swissprot: KCNH1_HUMAN) blocker (Source: ) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) C-C chemokine receptor type 5 (Organism: Homo sapiens, class: GPCR, accessions: P51681, gene: CCR5, swissprot: CCR5_HUMAN) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) Substance-K receptor (Organism: Homo sapiens, class: GPCR, accessions: P21452, gene: TACR2, swissprot: NK2R_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Heat shock protein HSP 90-alpha (Organism: Homo sapiens, class: Cytosolic other, accessions: P07900, gene: HSP90AA1, swissprot: HS90A_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Histamine H1 receptor (Organism: Cavia porcellus, class: GPCR, accessions: P31389, gene: HRH1, swissprot: HRH1_CAVPO Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN Transcriptional activator protein luxR (Organism: Aliivibrio fischeri, class: Unclassified, accessions: P12746, gene: luxR, swissprot: LUXR_ALIFS Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN Adrenergic receptor alpha-1 (Organism: Homo sapiens, class: GPCR, accessions: P25100|P35348|P35368, gene: ADRA1A|ADRA1B|ADRA1D, swissprot: ADA1A_HUMAN|ADA1B_HUMAN|ADA1D_HUMAN A selective histamine H1-receptor antagonist devoid of central nervous system depressant activity. The drug was used for ALLERGY but withdrawn due to causing LONG QT SYNDROME. Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Neurotransmitter Agents (Code: D018377) FDA
Click to view dexamethasone phosphate Dexamethasone (betamethasone) phosphate is a phosphate ester of dexamethasone (betamethasone). It is a soluble ester that provides prompt activity. (See: dextamethasone) dexamethasone phosphate: 1959-09-02 FDA betamethasone phosphate: 1965-03-03 FDA 3T5
Click to view methylprednisolone aceponate Methylprednisolone aceponate is a prodrug of methylprednisolone for topical use. It is used for the treatment of contact, allergic or atopic dermatitis. (See: methylprednisolone) Anti-Inflammatory Agents (Code: D000893) 1992-03-26 New Zealand Medicines and Medical Devices Safety Authority
Click to view clofazimine Uncharacterized oxidoreductase CzcO-like (Organism: Geobacillus kaustophilus (strain HTA426), class: Enzyme, accessions: Q5L2G3, gene: None, swissprot: CZCO_GEOKA) Cruzipain (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P25779, gene: None, swissprot: CYSP_TRYCR A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619) Antimycobacterial (Code: N0000175483) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Inflammatory Agents (Code: D000893) Leprostatic Agents (Code: D007917) leprostatic drug (Code: CHEBI:35816) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) dye (Code: CHEBI:37958) 1986-12-15 FDA
Click to view carbetocin Oxytocin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30559, gene: OXTR, swissprot: OXYR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9760035) A synthetic carba-analogue of oxytocin, it is used to control bleeding after giving birth. Like oxytocin, it causes contraction of the uterus. It has a role as an oxytocic. Delayed-Action Preparations (Code: D003692) Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102) oxytocic (Code: CHEBI:36063) 2007-11-05 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view ximelagatran Prothrombin (Organism: Homo sapiens, class: Enzyme, accessions: P00734, gene: F2, swissprot: THRB_HUMAN) inhibitor Vitamin K-dependent protein C (Organism: Homo sapiens, class: Enzyme, accessions: P04070, gene: PROC, swissprot: PROC_HUMAN Tissue-type plasminogen activator (Organism: Homo sapiens, class: Enzyme, accessions: P00750, gene: PLAT, swissprot: TPA_HUMAN Plasminogen (Organism: Homo sapiens, class: Enzyme, accessions: P00747, gene: PLG, swissprot: PLMN_HUMAN Coagulation factor VII (Organism: Homo sapiens, class: Enzyme, accessions: P08709, gene: F7, swissprot: FA7_HUMAN Coagulation factor X (Organism: Homo sapiens, class: Enzyme, accessions: P00742, gene: F10, swissprot: FA10_HUMAN Coagulation factor XI (Organism: Homo sapiens, class: Enzyme, accessions: P03951, gene: F11, swissprot: FA11_HUMAN Cationic trypsin (Organism: Bos taurus, class: Enzyme, accessions: P00760, gene: None, swissprot: TRY1_BOVIN Ximelagatran is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy. In 2006, its manufacturer announced that it would not attempt to market ximelagatran after reports of hepatotoxicity during trials, and to discontinue its distribution in countries where the drug had been approved. Anticoagulants (Code: D000925) Antithrombins (Code: D000991) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) anticoagulant (Code: CHEBI:50249) prodrug (Code: CHEBI:50266) 2004-01-01 YEAR INTRODUCED
Click to view raloxifene Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022042lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17101742) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15601807) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14709625) Xanthine dehydrogenase/oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P47989, gene: XDH, swissprot: XDH_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14709625) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12019197) UDP-glucuronosyltransferase 1-8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW9, gene: UGT1A8, swissprot: UD18_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12019197) UDP-glucuronosyltransferase 1-10 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HAW8, gene: UGT1A10, swissprot: UD110_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12019197) C-8 sterol isomerase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P32352, gene: ERG2, swissprot: ERG2_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16033255) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16033255) 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (Organism: Homo sapiens, class: Enzyme, accessions: Q15125, gene: EBP, swissprot: EBP_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16033255) Cruzipain (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P25779, gene: None, swissprot: CYSP_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20426472) Phospholipase D2 (Organism: Homo sapiens, class: Enzyme, accessions: O14939, gene: PLD2, swissprot: PLD2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19136975) Phospholipase D1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13393, gene: PLD1, swissprot: PLD1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19136975) Aldehyde oxidase (Organism: Homo sapiens, class: Enzyme, accessions: Q06278, gene: AOX1, swissprot: AOXA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20853847) Raloxifene is an estrogen agonist/antagonist, commonly referred to as a selective estrogen receptor modulator (SERM). The agonistic or antagonistic action of raloxifene depends on the extent of recruitment of coactivators and corepressors to estrogen receptor (ER) target gene promotors. Raloxifene appears to act as an estrogen agonist in bone. It decreases bone resorption and bone turnover, increases bone mineral density (BMD) and decreases fracture incidence. Preclinical data demonstrate that raloxifene is an estrogen antagonist in uterine and breast tissues. Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women, reduction in risk of invasive breast cancer in postmenopausal women and at high risk for invasive breast cancer. Estrogen Agonist/Antagonist (Code: N0000175826) Bone Density Conservation Agents (Code: D050071) Estrogen Antagonists (Code: D004965) Estrogen Receptor Modulators (Code: D020847) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Selective Estrogen Receptor Modulators (Code: D020845) bone density conservation agent (Code: CHEBI:50646) estrogen receptor modulator (Code: CHEBI:50739) estrogen antagonist (Code: CHEBI:50837) 1997-12-09 FDA RAL
Click to view prednisolamate
Click to view mitopodozide an ethylhydrazide derivative of podophyllic acid; RN given refers to cpd without isomeric designation Antineoplastic Agents (Code: D000970)
Click to view methylprednisolone succinate Methylprednisolone succinate is a water-soluble ester of methylprednisolone and its prodrug used for cardiac, allergic, and hypoxic emergencies. Methylprednisolone succinate has the same metabolic and anti-inflammatory actions as methylprednisolone. It is used in the endocrine disorders, rheumatic disorders, collagen diseases, dermatologic diseases, allergic states, ophthalmic diseases, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, gastrointestinal diseases, acute exacerbations of multiple sclerosis, tuberculous meningitis with subarachnoid block or impending block, trichinosis with neurologic or myocardial involvement. (See: methylprednisolone) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Central Nervous System Agents (Code: D002491) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Neuroprotective Agents (Code: D018696) Protective Agents (Code: D020011) 1959-05-18 FDA
Click to view sildenafil cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha (Organism: Homo sapiens, class: Enzyme, accessions: P16499, gene: PDE6A, swissprot: PDE6A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha' (Organism: Homo sapiens, class: Enzyme, accessions: P51160, gene: PDE6C, swissprot: PDE6C_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022473s012,203109s012lbl.pdf) Multidrug resistance-associated protein 5 (Organism: Homo sapiens, class: Transporter, accessions: O15440, gene: ABCC5, swissprot: MRP5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12695538) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12695538) Multidrug resistance-associated protein 7 (Organism: Homo sapiens, class: Transporter, accessions: Q5T3U5, gene: ABCC10, swissprot: MRP7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12527806) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17496208) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17496208) Phosphodiesterase 1 (Organism: Bos taurus, class: Enzyme, accessions: P14100|Q01061, gene: PDE1A|PDE1B, swissprot: PDE1A_BOVIN|PDE1B_BOVIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14521415) Phosphodiesterase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27815|Q07343|Q08493|Q08499, gene: PDE4A|PDE4B|PDE4C|PDE4D, swissprot: PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15125967) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12873512) Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HCR9, gene: PDE11A, swissprot: PDE11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18976905) High affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A (Organism: Homo sapiens, class: Enzyme, accessions: Q13946, gene: PDE7A, swissprot: PDE7A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23137303) Indoleamine 2,3-dioxygenase 2 (Organism: Mus musculus, class: Enzyme, accessions: Q8R0V5, gene: Ido2, swissprot: I23O2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23122865) High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A (Organism: Homo sapiens, class: Enzyme, accessions: O76083, gene: PDE9A, swissprot: PDE9A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25801159) Sildenafil is an inhibitor of cGMP specific phosphodiesterase type-5 (PDE-5) in the smooth muscle of the pulmonary vasculature, where PDE-5 is responsible for degradation of cGMP. Sildenafil, therefore, increases cGMP within pulmonary vascular smooth muscle cells resulting in relaxation. Studies in vitro have shown that sildenafil is selective for PDE-5. Its effect is more potent on PDE-5 than on other known phosphodiesterases (10-fold for PDE6, greater than 80-fold for PDE1, greater than 700-fold for PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11). The approximately 4,000-fold selectivity for PDE-5 versus PDE3 is important because PDE3 is involved in control of cardiac contractility. Sildenafil is only about 10-fold as potent for PDE-5 compared to PDE6, an enzyme found in the retina and involved in the phototransduction pathway of the retina. This lower selectivity is thought to be the basis for abnormalities related to color vision observed with higher doses or plasma levels. Phosphodiesterase 5 Inhibitor (Code: N0000175599) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Phosphodiesterase 5 Inhibitors (Code: D058986) Phosphodiesterase Inhibitors (Code: D010726) Urological Agents (Code: D064804) Vasodilator Agents (Code: D014665) vasodilator agent (Code: CHEBI:35620) 1998-03-27 FDA VIA
Click to view tibezonium
Click to view rilmazafone Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Hypnotics and Sedatives (Code: D006993)
Click to view picloxydine Acetylcholinesterase (Organism: Electrophorus electricus, class: Enzyme, accessions: O42275, gene: ache, swissprot: ACES_ELEEL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27689726) Butyrylcholinesterase (Organism: Equus caballus, class: Enzyme, accessions: Q9N1N9, gene: BCHE, swissprot: Q9N1N9_HORSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27689726) Picloxydine is a heterocyclic biguanide with antibacterial and antiplaque activity. It is used for the treatment of superficial ophthalmic infections. 1993-10-28 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view ertapenem Penicillin-binding protein 1B (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02919, gene: mrcB, swissprot: PBPB_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021337s048lbl.pdf) Penicillin-binding protein 1A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918, gene: mrcA, swissprot: PBPA_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021337s048lbl.pdf) Penicillin-binding protein 2 (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD65, gene: mrdA, swissprot: PBP2_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021337s048lbl.pdf) Ertapenem is a 1-beta methyl-carbapenem. The bactericidal activity of ertapenem results from the inhibition of cell wall synthesis and is mediated through ertapenem binding to penicillin binding proteins (PBPs). In Escherichia coli, it has strong affinity toward PBPs 1a, 1b, 2, 3, 4 and 5 with preference for PBPs 2 and 3. Ertapenem has been shown to be active against Staphylococcus aureus (methicillin susceptible isolates only), Streptococcus agalactiae, Streptococcus pneumoniae (penicillin susceptible isolates only), Streptococcus pyogenes, Escherichia coli, Haemophilus influenzae (beta-lactamase negative isolates only), Klebsiella pneumoniae, Moraxella catarrhalis, Proteus mirabilis, Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, Bacteroides uniformis, Clostridium clostridioforme, Eubacterium lentum, Peptostreptococcus species, Porphyromonas asaccharolytica, Prevotella bivia. Ertapenem is indicated for the treatment of complicated intra-abdominal infections, complicated skin and skin structure infections (including diabetic foot infections without osteomyelitis), community-acquired pneumonia, complicated urinary tract infections (including pyelonephritis), acute pelvic infections (including postpartum endomyometritis, septic abortion and post surgical gynecologic infections). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) Carbapenems (Code: N0000011294) Penem Antibacterial (Code: N0000175496) 2001-11-21 FDA 1RG
2RG
Click to view fluspirilene Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: ) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) antagonist (Source: ) Nociceptin receptor (Organism: Homo sapiens, class: GPCR, accessions: P41146, gene: OPRL1, swissprot: OPRX_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN A long-acting injectable antipsychotic agent used for chronic schizophrenia. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view gallopamil Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Coronary vasodilator that is an analog of iproveratril (VERAPAMIL) with one more methoxy group on the benzene ring. Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990)
Click to view netilmicin Acyl-protein thioesterase 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: P70470, gene: Lypla1, swissprot: LYPA1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7473599) Netilmicin is a semisynthetic, water soluble aminoglycoside derived from sisomicin, a naturally occurring antibiotic produced by the fermentation of Micromonospora inyoensis. Netilmicin irreversibly binds to the 16S rRNA and S12 protein of the bacterial 30S ribosomal subunit. As a result, this agent interferes with the assembly of initiation complex between mRNA and the bacterial ribosome, thereby inhibiting the initiation of protein synthesis. In addition, netilmicin induces misreading of the mRNA template and causes translational frameshift, thereby results in premature termination. This eventually leads to bacterial cell death. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) Aminoglycoside Antibacterial (Code: N0000175477) Aminoglycosides (Code: N0000007853) 1983-02-28 FDA
Click to view hydrocortamate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist immunosuppressive agent (Code: CHEBI:35705) anti-inflammatory drug (Code: CHEBI:35472) 1956-10-15 FDA
Click to view pipotiazine palmitate Pipotiazine palmitate is the palmitic ester of pipotiazine, a piperidine phenothiazine with antipsychotic properties and weak sedative activity. The esterification of pipotiazine is responsible for its prolonged duration of action. Pipotiazine palmitate is indicated for the treatment of behavioral disorders. (See: pipotiazine) 1988-08-18 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view dexamethasone valerate Dexamethasone (betamethasone) valerate belongs to a class of potent topical corticosteroids. The mechanism of anti-inflammatory activity of topical corticosteroids is unclear.Dexamethasone (betamethasone) valerate is a steroid ester that is dexamethasone (betamethasone) in which the hydroxy group at the 17alpha position has been converted to the corresponding pentanoate ester. (See: dexamethasone) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) betamethasone valerate: 1967-09-02 FDA
Click to view loperamide Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10087042) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10087042) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10087042) Voltage-dependent P/Q-type calcium channel subunit alpha-1A (Organism: Rattus norvegicus, class: Ion channel, accessions: P54282, gene: Cacna1a, swissprot: CAC1A_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8183255) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16415122) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18788725) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11964599) Loperamide is synthetic opioid that primarily affects opiate receptors in the intestine and is used to treat diarrhea. Opioid Agonist (Code: N0000175690) Opioid Agonists (Code: N0000000174) Antidiarrheals (Code: D000930) Gastrointestinal Agents (Code: D005765) mu-opioid receptor agonist (Code: CHEBI:55322) antidiarrhoeal drug (Code: CHEBI:55323) 1976-12-28 FDA
Click to view temocapril Angiotensin-converting enzyme (Organism: Oryctolagus cuniculus, class: Enzyme, accessions: P12822, gene: ACE, swissprot: ACE_RABIT) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/2851680) Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/8427943) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 1994-01-01 YEAR INTRODUCED
Click to view meclocycline Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) FDA
Click to view feclobuzone
Click to view Streptomycin B
Click to view pralatrexate Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN) inhibitor (Source: ) Pralatrexate is a folate analog metabolic inhibitor that competitively inhibits dihydrofolate reductase. It is also a competitive inhibitor for polyglutamylation by the enzyme folylpolyglutamyl synthetase. This inhibition results in the depletion of thymidine and other biological molecules the synthesis of which depends on single carbon transfer. Folate Analog Metabolic Inhibitor (Code: N0000175584) antineoplastic agent (Code: CHEBI:35610) 2009-09-24 FDA
Click to view almitrine Almitrine is a respiratory stimulant that enhances respiration by acting as an agonist of peripheral chemoreceptors located on the carotid bodies. The drug increases arterial oxygen tension while decreasing arterial carbon dioxide tension in patients with chronic obstructive pulmonary disease. It may also prove useful in the treatment of nocturnal oxygen desaturation without impairing the quality of sleep. Respiratory System Agents (Code: D019141) central nervous system stimulant (Code: CHEBI:35337) 1977-07-25 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view thyroxine Solute carrier organic anion transporter family member 1C1 (Organism: Homo sapiens, class: Transporter, accessions: Q9NYB5, gene: SLCO1C1, swissprot: SO1C1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12351693) Monocarboxylate transporter 8 (Organism: Rattus norvegicus, class: Transporter, accessions: Q8K1P8, gene: SLC16A2, swissprot: MOT8_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12871948) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159893) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159893) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159893) Thyroxine, one of the two major hormones secreted by the thyroid gland. Levothyroxine (T4) is a synthetically prepared levo isomer of thyroxine. Dextrothyroxine is the dextrorotary isomer of thyroxine. Dextrothyroxine stimulates the formation of low-density lipoprotein (LDL) and increases the catabolism of LDL thereby leading to increased excretion of cholesterol and bile acids via the biliary route. Levothyroxine acts like the endogenous thyroid hormone thyroxine (T4, a tetra-iodinated tyrosine derivative). In the liver and kidney, T4 is converted to T3, the active metabolite. Thus by acting as a replacement for natural thyroxine, symptoms of thyroxine deficiency are relieved. Levothyroxine is used for use alone or in combination with antithyroid agents to treat hypothyroidism, goiter, chronic lymphocytic thyroiditis, myxedema coma, and stupor. Dextrothyroxine is used to lower high cholesterol levels in the blood. l-Thyroxine (Code: N0000175945) Thyroxine (Code: N0000007632) dextrothyroxine: 1967-04-14 FDA levotrothyroxine: 2000-08-21 FDA T44
Click to view triamcinolone diacetate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist lysyl oxidase antagonist; Polcortolon may also refers to triamcinolone Enzyme Inhibitors (Code: D004791) 1959-03-12 FDA
Click to view tribenoside Tribenoside is a glucofuranoside derivative. Tribenoside has been shown to have potent anti-allergic and anti-inflammatory properties. It is used for treatment of venous circulation diseases. In combination with lidocaine tribenoside is used for the local treatment of hemorrhoids. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 1978-10 PMDA
Click to view dihydroemetine was MH 1991-94 (see under EMETINE 1976-90); use EMETINE to search DEHYDROEMETINE 1976-94; amebicide, derivative of emetine
Click to view lymecycline A semisynthetic antibiotic related to TETRACYCLINE. It is more readily absorbed than TETRACYCLINE and can be used in lower doses. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antiprotozoal drug (Code: CHEBI:35820) antibacterial drug (Code: CHEBI:36047)
Click to view chlortetracycline Major prion protein (Organism: Homo sapiens, class: Surface antigen, accessions: P04156, gene: PRNP, swissprot: PRIO_HUMAN) cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN Protein-arginine deiminase type-4 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UM07, gene: PADI4, swissprot: PADI4_HUMAN A TETRACYCLINE with a 7-chloro substitution. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) antiprotozoal drug (Code: CHEBI:35820) fluorescent probe (Code: CHEBI:39442) antibacterial drug (Code: CHEBI:36047) 1950-01-23 FDA CTC
Click to view clobetasone butyrate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: http://www.kegg.jp/entry/D01273) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) PMDA
Click to view mosapramine PMDA
Click to view cefteram Cefteram is a semisynthetic cephalosporin formulated for oral administration as the prodrug ester, cefteram pivoxil. The mechanism of action of cefteram is inhibition of bacterial cell wall synthesis. Cefteram exerts its bactericidal activity by strongly binding to penicillin-binding protein (PBP) 3, 1A, and 1Bs. Cefteram is active against Streptococcus pneumoniae, Neisseria gonorrhoeae, Escherichia coli, Klebsiella spp., Enterobacter spp., Proteus spp., Morganella morganii, Haemophilus influenzae, Peptostreptococcus spp.. It is used for the treatment of respiratory tractiInfections, urinary tract infections, otitis media, sinusitis and intra-abdominal infections. 1987-08-01 PMDA
Click to view stallimycin DNA topoisomerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P11387, gene: TOP1, swissprot: TOP1_HUMAN Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372|Q92731, gene: ESR1|ESR2, swissprot: ESR1_HUMAN|ESR2_HUMAN GTPase HRas (Organism: Homo sapiens, class: Cytosolic other, accessions: P01112, gene: HRAS, swissprot: RASH_HUMAN Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) DMY
Click to view nicardipine Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P19328|P22086|P22909, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT Malate dehydrogenase cytoplasmic (Organism: Homo sapiens, class: Enzyme, accessions: P40925, gene: MDH1, swissprot: MDHC_HUMAN Equilibrative nucleoside transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: O54698, gene: Slc29a1, swissprot: S29A1_RAT Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN Beta-lactamase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P00811, gene: ampC, swissprot: AMPC_ECOLI Adenosine receptor A3 (Organism: Rattus norvegicus, class: GPCR, accessions: P28647, gene: Adora3, swissprot: AA3R_RAT Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT Adenosine receptor A2a (Organism: Rattus norvegicus, class: GPCR, accessions: P30543, gene: Adora2a, swissprot: AA2AR_RAT Voltage-gated L-type calcium channel (Organism: Rattus norvegicus, class: Ion channel, accessions: P22002|P27732|Q02485, gene: Cacna1c|Cacna1d|Cacna1s, swissprot: CAC1C_RAT|CAC1D_RAT|CAC1S_RAT Adenosine receptor A1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25099, gene: Adora1, swissprot: AA1R_RAT ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker Potassium voltage-gated channel subfamily A member 4 (Organism: Rattus norvegicus, class: Unclassified, accessions: P15385, gene: Kcna4, swissprot: KCNA4_RAT) blocker (Source: ) Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022276s003lbl.pdf) A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. S-enantiomer of nicardipine is a calcium entry blocker (slow channel blocker or calcium ion antagonist) which inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle without changing serum calcium concentrations Calcium Channel Antagonists (Code: N0000000069) Dihydropyridine Calcium Channel Blocker (Code: N0000175421) Dihydropyridines (Code: N0000007556) Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Cytochrome P450 2C8 Inhibitors (Code: N0000187062) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) 1988-12-21 FDA
Click to view emetine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) Putative hydrolase RBBP9 (Organism: Homo sapiens, class: Enzyme, accessions: O75884, gene: RBBP9, swissprot: RBBP9_HUMAN Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT The principal alkaloid of ipecac, from the ground roots of Uragoga (or Cephaelis) ipecacuanha or U. acuminata, of the Rubiaceae. It is used as an amebicide in many different preparations and may cause serious cardiac, hepatic, or renal damage and violent diarrhea and vomiting. Emetine inhibits protein synthesis in EUKARYOTIC CELLS but not PROKARYOTIC CELLS. Amebicides (Code: D000563) Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Autonomic Agents (Code: D001337) Cathartics (Code: D002400) Central Nervous System Agents (Code: D002491) Emetics (Code: D004639) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Peripheral Nervous System Agents (Code: D018373) Protein Synthesis Inhibitors (Code: D011500) antiprotozoal drug (Code: CHEBI:35820)
Click to view clocapramine
Click to view pranlukast Cysteinyl leukotriene receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y271, gene: CYSLTR1, swissprot: CLTR1_HUMAN) antagonist (Source: ) Cysteinyl leukotriene receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q9NS75, gene: CYSLTR2, swissprot: CLTR2_HUMAN) antagonist (Source: ) Cruzipain (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P25779, gene: None, swissprot: CYSP_TRYCR Cysteinyl leukotriene receptor 1 (Organism: Cavia porcellus, class: GPCR, accessions: Q2NNR5, gene: CYSLTR1, swissprot: CLTR1_CAVPO Uracil nucleotide/cysteinyl leukotriene receptor (Organism: Homo sapiens, class: GPCR, accessions: Q13304, gene: GPR17, swissprot: GPR17_HUMAN SRS-A antagonist; leukotriene D4 receptor antagonist Anti-Asthmatic Agents (Code: D018927) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Leukotriene Antagonists (Code: D020024) Respiratory System Agents (Code: D019141) 2007-03-15 PMDA
Click to view iodoalphionic acid Iodoalphionic acid is the contrast medium, which was used for gallbladder examination. It is rarely appeared in the colon and, therefore, rarely masked the gallbladder. 1943 YEAR INTRODUCED
Click to view talampicillin Talampicillin is a prodrug that is a thiazolidine carboxylic ester of ampicillin. It is well absorbed from the gastrointestinal tract resulting in a greater bioavailability of ampicillin than can be achieved with equivalent doses of ampicillin. It has no antibacterial activity until it is hydrolyzed by tissue esterases in the intestial wall to ampicillin. (See: ampicillin) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) prodrug (Code: CHEBI:50266) 2015-09-21 China Food and Drug Administration (CFDA)
Click to view rosuvastatin 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Organism: Homo sapiens, class: Enzyme, accessions: P04035, gene: HMGCR, swissprot: HMDH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021366s038lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021366s038lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021366s038lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021366s038lbl.pdf) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19940267) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19940267) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19940267) Multidrug resistance-associated protein 5 (Organism: Homo sapiens, class: Transporter, accessions: O15440, gene: ABCC5, swissprot: MRP5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19940267) Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19853032) Rosuvastatin is a statin with antilipidemic and potential antineoplastic activities. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This leads to a decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol. Rosuvastatin is used for treatment of dyslipidaemia and has also been approved to slow the progression of atherosclerosis. HMG-CoA Reductase Inhibitor (Code: N0000175589) Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Hydroxymethylglutaryl-CoA Reductase Inhibitors (Code: D019161) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) antilipemic drug (Code: CHEBI:35679) anti-inflammatory agent (Code: CHEBI:67079) cardioprotective agent (Code: CHEBI:77307) 2003-08-12 FDA
Click to view cefepime Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10636865) Solute carrier family 15 member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q16348, gene: SLC15A2, swissprot: S15A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15567297) Cefepime is a semi-synthetic, cephalosporin antibacterial agent. Cefepime is a bactericidal drug that acts by inhibition of bacterial cell wall synthesis. Within bacterial cells, the molecular targets of cefepime are the penicillin binding proteins. Cefepime has been shown to be active against Enterobacter spp., Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Staphylococcus aureus (methicillin-susceptible isolates only), Streptococcus pneumoniae, Streptococcus pyogenes, Viridans group streptococci. Cefepime is indicated for the treatment of pneumonia (due to S. pneumoniae, P. aeruginosa, K. pneumoniae, or Enterobacter spp.), Febrile Neutropenic, Uncomplicated and Complicated Urinary Tract Infections (due to E. coli or K. pneumoniae), Uncomplicated Skin and Skin Structure Infections (due to S. aureus (methicillin-susceptible isolates only) or S. pyogenes), Complicated Intra-abdominal Infections (due to E. coli, viridans group streptococci, P. aeruginosa, K. pneumoniae, E. species, or B. fragilis). Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1996-01-18 FDA 9WT
Click to view amrubicin ; a 9-amino-anthracycline antibiotic Antineoplastic Agents (Code: D000970)
Click to view bekanamycin 3-oxoacyl-[acyl-carrier-protein] synthase 3 (Organism: Escherichia coli, class: Enzyme, accessions: C3TDZ2, gene: fabH, swissprot: C3TDZ2_ECOLX kanendomycin is the sulfate of bekanamycin; RN given refers to parent cpd; structure Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 9CS
Click to view otilonium bromide Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9721598) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9721598) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9721598) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9721598) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9721598) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Rattus norvegicus, class: Ion channel, accessions: P22002, gene: Cacna1c, swissprot: CAC1C_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/9721598) Voltage-dependent L-type calcium channel subunit alpha-1D (Organism: Rattus norvegicus, class: Ion channel, accessions: P27732, gene: Cacna1d, swissprot: CAC1D_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/9721598) Voltage-dependent L-type calcium channel subunit alpha-1S (Organism: Rattus norvegicus, class: Ion channel, accessions: Q02485, gene: Cacna1s, swissprot: CAC1S_RAT) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/9721598) Otilonium bromide is a spasmolytic agent acting as an L-type calcium channel antagonist in intestinal and colonic smooth muscle cells used for the treatment of Irritable bowel syndrome. 1983-03-16 Italian Medicines Agency (AIFA)
Click to view uridine triphosphate P2Y purinoceptor 2 (Organism: Homo sapiens, class: GPCR, accessions: P41231, gene: P2RY2, swissprot: P2RY2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11206448) P2Y purinoceptor 4 (Organism: Homo sapiens, class: GPCR, accessions: P51582, gene: P2RY4, swissprot: P2RY4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11206448) P2Y purinoceptor 11 (Organism: Homo sapiens, class: GPCR, accessions: Q96G91, gene: P2RY11, swissprot: P2Y11_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12761346) P2Y purinoceptor 6 (Organism: Homo sapiens, class: GPCR, accessions: Q15077, gene: P2RY6, swissprot: P2RY6_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8670200) Uridine triphosphate (UTP) is a pyrimidine ribonucleoside 5'-triphosphate having uracil as the nucleobase. UTP is used as a short-acting, aerosolized solution used for a diagnostic aid for lung cancer. IUTP appears to improve sputum expectoration mediated through the P2Y2 receptor, a nucleotide receptor expressed in human airway epithelial cells and some other tissues. UTP binding to the P2Y2 receptor triggers signal transduction that leads to chloride ion secretion, thereby resulting in mucociliary clearance of airway. UTP
Click to view nicergoline Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10027088) Nicergoline is a semisynthetic ergoline derivative. It is used for symptomatic treatment of chronic pathological cognitive and neurosensorial impairment in elderly (excluding Alzheimer’s disease and other dementia): Ancillary treatment of intermittent claudication in symptomatic peripheral arterial occlusive disease (PAOD Stage II), Ancillary treatment of Raynaud’s syndrome, Ancillary treatment of visual acuity decrease and visual field disturbances presumably of vascular origin, Acute retinopathies of vascular origin, Prophylaxis of migraine headache, Orthostatic hypotension, Symptomatic treatment of veno-lymphatic insufficiency. Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Neurotransmitter Agents (Code: D018377) Nootropic Agents (Code: D018697) Vasodilator Agents (Code: D014665) 1987-07-01 Italian Medicines Agency (AIFA)
Click to view kanamycin Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components. Aminoglycoside Antibacterial (Code: N0000175477) Aminoglycosides (Code: N0000007853) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) 1973-02-13 FDA KAN
Click to view fentonium less effect on eye, heart & gland functions than atropine; proposed for therapy of gastrointestinal ulcers; minor descriptor (78-84); on-line & Index Medicus search ATROPINE DERIVATIVES (78-84); RN given refers to bromide(3(S)-endo)-isomer
Click to view ulobetasol propionate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist used in ointment to treat psoriasis; Ulobetasol cream contains 0.05% 6-fluoroclobetasol 17-propionate 1990-12-17 FDA
Click to view etiprednol dicloacetate a soft corticosteroid
Click to view imiclopazine
Click to view prednisolone valerate acetate topical steroid used for skin disease therapy
Click to view hydrocortisone cypionate Hydrocortisone cypionate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester. (See: hydrocortisone) 1955-05-10 FDA
Click to view fenoxedil
Click to view fluclorolone acetonide synthetic glucocorticoid with anti-inflammatory properties; minor descriptor (75-83); on-line & Index Medicus search PREGNADIENETROLS (75-83); RN given refers to (6alpha,11beta,16alpha)-isomer; structure
Click to view riodoxol Riodoxol is a member of resorcinols with high antiviral and antifungal activity. Riodoxol did not inhibit synthesis of viral RNA and proteins of the influenza virus. The exact mode of action of riodoxol is unknown. It is used for the treatment of skin infections (dermal herpes, lesions due to molluscum contagiosum, planar and common warts, acne), fungal skin infections (microsporia, trichophytosis, mycoses, epidermophytosis) and of stomatological diseases (acute and chronic relapsing aphthous stomatitis, ulcerative-necrotic gingivostomatitis). 1981-12-28 Ministry of Health of the Russian Federation
Click to view dasatinib Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Bcr/Abl fusion protein (Organism: Homo sapiens, class: Kinase, accessions: P00519|P11274, gene: ABL1|BCR, swissprot: ABL1_HUMAN|BCR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Tyrosine-protein kinase Yes (Organism: Homo sapiens, class: Kinase, accessions: P07947, gene: YES1, swissprot: YES_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Ephrin type-A receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P29317, gene: EPHA2, swissprot: EPHA2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Dimethylaniline monooxygenase [N-oxide-forming] 3 (Organism: Homo sapiens, class: Enzyme, accessions: P31513, gene: FMO3, swissprot: FMO3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021986s021lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19785662) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19785662) Mitogen-activated protein kinase 14 (Organism: Homo sapiens, class: Kinase, accessions: Q16539, gene: MAPK14, swissprot: MK14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15615512) Receptor tyrosine-protein kinase erbB-2 (Organism: Homo sapiens, class: Kinase, accessions: P04626, gene: ERBB2, swissprot: ERBB2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15615512) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15615512) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15615512) Dual specificity mitogen-activated protein kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q02750, gene: MAP2K1, swissprot: MP2K1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15615512) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Organism: Homo sapiens, class: Kinase, accessions: P42336, gene: PIK3CA, swissprot: PK3CA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Organism: Homo sapiens, class: Kinase, accessions: O00329, gene: PIK3CD, swissprot: PK3CD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Serine/threonine-protein kinase mTOR (Organism: Homo sapiens, class: Kinase, accessions: P42345, gene: MTOR, swissprot: MTOR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Tyrosine-protein kinase HCK (Organism: Homo sapiens, class: Kinase, accessions: P08631, gene: HCK, swissprot: HCK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Ephrin type-B receptor 4 (Organism: Homo sapiens, class: Kinase, accessions: P54760, gene: EPHB4, swissprot: EPHB4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18849971) Tyrosine-protein kinase receptor UFO (Organism: Homo sapiens, class: Kinase, accessions: P30530, gene: AXL, swissprot: UFO_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase Fes/Fps (Organism: Homo sapiens, class: Kinase, accessions: P07332, gene: FES, swissprot: FES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Interleukin-1 receptor-associated kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q9NWZ3, gene: IRAK4, swissprot: IRAK4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) LIM domain kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P53667, gene: LIMK1, swissprot: LIMK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Receptor-interacting serine/threonine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: O43353, gene: RIPK2, swissprot: RIPK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Angiopoietin-1 receptor (Organism: Homo sapiens, class: Kinase, accessions: Q02763, gene: TEK, swissprot: TIE2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) High affinity nerve growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P04629, gene: NTRK1, swissprot: NTRK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) BDNF/NT-3 growth factors receptor (Organism: Homo sapiens, class: Kinase, accessions: Q16620, gene: NTRK2, swissprot: NTRK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase TXK (Organism: Homo sapiens, class: Kinase, accessions: P42681, gene: TXK, swissprot: TXK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase Lyn (Organism: Homo sapiens, class: Kinase, accessions: P07948, gene: LYN, swissprot: LYN_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17154512) Cyclin-dependent kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P24941, gene: CDK2, swissprot: CDK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17154512) Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17684099) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily KQT member 1 (Organism: Homo sapiens, class: Ion channel, accessions: P51787, gene: KCNQ1, swissprot: KCNQ1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Dasatinib is a selective tyrosine kinase receptor inhibitor. Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFR-beta. Dasatinib is indicated for the treatment of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia, Philadelphia chromosome-positive acute lymphoblastic leukemia. Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) antineoplastic agent (Code: CHEBI:35610) 2006-06-28 FDA 1N1
Click to view neltenexine elastase inhibitor; may be useful for preventing pulmonary emphysema 2001-10-16 Korean Food and Drug Administration (KFDA)
Click to view estriol succinate
Click to view prednicarbate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12677094) Prednicarbate is a synthetic non-halogenated double-ester derivative of the corticosteroid prednisolone with anti-inflammatory, antipruritic and vasoconstrictive properties. Following skin permeation, prednicarbate enters cells and binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of pro-inflammatory cytokine production by increasing the expression of lipocortins. These block phospholipase A-dependent release of arachidonic acid thereby inhibiting prostaglandin synthesis. This agent also decreases the number of circulating lymphocytes by suppression of the production of vasodilators such as prostacyclin and nitric oxide. Prednicarbate is used for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1991-09-23 FDA
Click to view vardenafil cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha (Organism: Homo sapiens, class: Enzyme, accessions: P16499, gene: PDE6A, swissprot: PDE6A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HCR9, gene: PDE11A, swissprot: PDE11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A (Organism: Homo sapiens, class: Enzyme, accessions: P54750, gene: PDE1A, swissprot: PDE1A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021400s020lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21552528) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22775210) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22775210) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22775210) Phosphodiesterase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27815|Q07343|Q08493|Q08499, gene: PDE4A|PDE4B|PDE4C|PDE4D, swissprot: PDE4A_HUMAN|PDE4B_HUMAN|PDE4C_HUMAN|PDE4D_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15837326) Phosphodiesterase 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q13370|Q14432, gene: PDE3A|PDE3B, swissprot: PDE3A_HUMAN|PDE3B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15837326) High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A (Organism: Homo sapiens, class: Enzyme, accessions: O76083, gene: PDE9A, swissprot: PDE9A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15837326) cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y233, gene: PDE10A, swissprot: PDE10_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15837326) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily KQT member 1 (Organism: Homo sapiens, class: Ion channel, accessions: P51787, gene: KCNQ1, swissprot: KCNQ1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily D member 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UK17, gene: KCND3, swissprot: KCND3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Vardenafil is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). In vitro studies have shown that vardenafil is a selective inhibitor of PDE5. The inhibitory effect of vardenafil is more selective on PDE5 than for other known phosphodiesterases (>15-fold relative to PDE6, >130-fold relative to PDE1, >300-fold relative to PDE11, and >1,000-fold relative to PDE2, 3, 4, 7, 8, 9, and 10). Vardenafil is indicated for the treatment of erectile dysfunction. Phosphodiesterase 5 Inhibitor (Code: N0000175599) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Phosphodiesterase 5 Inhibitors (Code: D058986) Phosphodiesterase Inhibitors (Code: D010726) Urological Agents (Code: D064804) Vasodilator Agents (Code: D014665) vasodilator agent (Code: CHEBI:35620) 2003-08-19 FDA VDN
Click to view citicoline Donor of choline in biosynthesis of choline-containing phosphoglycerides. Central Nervous System Agents (Code: D002491) Nootropic Agents (Code: D018697) psychotropic drug (Code: CHEBI:35471) neuroprotective agent (Code: CHEBI:63726) 1983-06-01 Italian Medicines Agency (AIFA) CDC
Click to view cefamandole nafate Cefamandole Nafate is the sodium salt form of cefamandole formyl ester. Cefamandole nafate is a prodrug that is hydrolyzed by plasma esterases to produce cefamandole, a semi-synthetic beta-lactam, second-generation cephalosporin antibiotic with bactericidal activity. Cefamandole Nafate is indicated for the treatment of Lower respiratory infections (due to S. pneumoniae, H. influenzae, Klebsiella spp., S. aureus, (beta)-hemolytic streptococci, and P. mirabilis), Urinary tract infections (due to E. coli, Proteus spp., Enterobacter spp., Klebsiella spp., group D streptococci and S. epidermidis), Peritonitis (due to E. coli and Enterobacter spp.), Septicemia (due to E. coli, S. aureus, S. pneumoniae, S. pyogenes, H. influenzae, and Klebsiella spp.), Skin and skin structure infections(due to S. aureus, S. pyogenes , H. influenzae, E. coli, Enterobacter spp., and P. mirabilis), Bone and joint infections (due to S. aureus). (See: cefamandole) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) prodrug (Code: CHEBI:50266) antibacterial drug (Code: CHEBI:36047) 1978-09-27 FDA
Click to view glimepiride Sulfonylurea receptor 2, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: O60706|Q14654, gene: ABCC9|KCNJ11, swissprot: ABCC9_HUMAN|KCJ11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12086984) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020496s029lbl.pdf) Glimepiride is a long-acting, third-generation sulfonylurea with hypoglycemic activity. Glimepiride is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Hypoglycemic Agents (Code: D007004) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) hypoglycemic agent (Code: CHEBI:35526) Sulfonylurea (Code: N0000175608) Sulfonylurea Compounds (Code: N0000008054) 1995-11-30 FDA GMR
Click to view sulisatin
Click to view barnidipine Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: ) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990)
Click to view lidoflazine Equilibrative nucleoside transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q99808, gene: SLC29A1, swissprot: S29A1_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Rattus norvegicus, class: Ion channel, accessions: P04774|P04775|P08104, gene: Scn1a|Scn2a|Scn3a, swissprot: SCN1A_RAT|SCN2A_RAT|SCN3A_RAT Coronary vasodilator with some antiarrhythmic action. Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665)
Click to view teicoplanin aglycone Teicoplanin aglycone is the only chiral selector without saccharide groups attached. Teicoplanin aglycone is an inhibitor of bacterial cell wall biosynthesis. Teicoplanin aglycone is more active in vitro than teicoplanin, particularly against Staphylococcus epidermidis strains, Escherichia coli and Proteus vulgaris and is less active than teicoplanin. http:
Click to view cilnidipine Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/9298526) Voltage-dependent N-type calcium channel subunit alpha-1B (Organism: Rattus norvegicus, class: Unclassified, accessions: Q02294, gene: Cacna1b, swissprot: CAC1B_RAT) blocker (Source: ) has excitatory & inhibitory action on the Ca+ channels in the rabbit basilar artery; structure given in first source; RN given is for (+-) isomer Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) antihypertensive agent (Code: CHEBI:35674) cardiovascular drug (Code: CHEBI:35554)
Click to view bezitramide Analgesics (Code: D000700) Central Nervous System Agents (Code: D002491) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view loperamide oxide Antidiarrheals (Code: D000930) Gastrointestinal Agents (Code: D005765)
Click to view aspoxicillin
Click to view imatinib Platelet-derived growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P09619|P16234, gene: PDGFRA|PDGFRB, swissprot: PGFRA_HUMAN|PGFRB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021588s053lbl.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021588s053lbl.pdf) Bcr/Abl fusion protein (Organism: Homo sapiens, class: Kinase, accessions: P00519|P11274, gene: ABL1|BCR, swissprot: ABL1_HUMAN|BCR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15206509) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16782438) Macrophage colony-stimulating factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P07333, gene: CSF1R, swissprot: CSF1R_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15917650) Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16205964) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20423956) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19540211) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19708828) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18078752) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Tyrosine-protein kinase Blk (Organism: Homo sapiens, class: Kinase, accessions: P51451, gene: BLK, swissprot: BLK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22037378) Epithelial discoidin domain-containing receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: Q08345, gene: DDR1, swissprot: DDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22037378) Epithelial discoidin domain-containing receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: Q16832, gene: DDR2, swissprot: DDR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22037378) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) A tyrosine kinase inhibitor and antineoplastic agent that inhibits the BCR-ABL kinase created by chromosome rearrangements in chronic myeloid leukemia and acute lymphoblastic leukemia, as well as PDG-derived tyrosine kinases that are overexpressed in gastrointestinal stromal tumors. Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) 2001-05-10 FDA STI
Click to view glibenclamide Cystic fibrosis transmembrane conductance regulator (Organism: Homo sapiens, class: Ion channel, accessions: P13569, gene: CFTR, swissprot: CFTR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1281220) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00038563.PDF) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00038563.PDF) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22587986) Solute carrier family 22 member 6 (Organism: Rattus norvegicus, class: Transporter, accessions: O35956, gene: Slc22a6, swissprot: S22A6_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10854830) Sulfonylurea receptor 1, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: Q09428|Q14654, gene: ABCC8|KCNJ11, swissprot: ABCC8_HUMAN|KCJ11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11356099) Sulfonylurea receptor 2, Kir6.2 (Organism: Homo sapiens, class: Ion channel, accessions: O60706|Q14654, gene: ABCC9|KCNJ11, swissprot: ABCC9_HUMAN|KCJ11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11356099) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12404239) Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12404239) Solute carrier family 15 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P51574, gene: Slc15a1, swissprot: S15A1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10578127) Solute carrier family 15 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63424, gene: Slc15a2, swissprot: S15A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10578127) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12920163) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12920163) Cytochrome P450 3A7 (Organism: Homo sapiens, class: Enzyme, accessions: P24462, gene: CYP3A7, swissprot: CP3A7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/25450675) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16460798) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16460798) Canalicular multispecific organic anion transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: O15438, gene: ABCC3, swissprot: MRP3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16460798) Canalicular multispecific organic anion transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: O15438, gene: ABCC3, swissprot: MRP3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16460798) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16460798) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10087141) Glibenclamide is an oral blood-glucose-lowering drug of the sulfonylurea class. Glibenclamide appears to lower the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. The mechanism by which glyburide lowers blood glucose during long-term administration has not been clearly established. Glibenclamide is indicated as an adjunct to proper dietary management, exercise and weight reduction to lower blood glucose in adult patients with type 2 diabetes whose hyperglycemia cannot be controlled by diet and exercise alone or when insulin therapy is not required. Sulfonylurea (Code: N0000175608) Sulfonylurea Compounds (Code: N0000008054) Hypoglycemic Agents (Code: D007004) anti-arrhythmia drug (Code: CHEBI:38070) hypoglycemic agent (Code: CHEBI:35526) 1984-05-01 FDA GBM
Click to view fluocinonide Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) A topical glucocorticoid used in the treatment of ECZEMA. Adrenal Cortex Hormones (Code: D000305) Anti-Allergic Agents (Code: D018926) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) 1971-06-30 FDA
Click to view carindacillin Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor acid stable indanyl ester of carbenicillin for oral use; same side-effects as carbenicillin; minor descriptor (75-86); on line & INDEX MEDICUS search CARBENICILLIN/AA (75-86); RN given refers to (mono-Na salt(2S-(2alpha,5alpha,6beta))-isomer) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1972-10-26 FDA
Click to view tiquizium Muscarinic acetylcholine receptor (Organism: Canis familiaris, class: GPCR, accessions: F1PT23, gene: CHRM1, swissprot: F1PT23_CANFA) Muscarinic acetylcholine receptor (Organism: Canis familiaris, class: GPCR, accessions: F1PWR7, gene: CHRM2, swissprot: F1PWR7_CANFA) Muscarinic acetylcholine receptor (Organism: Canis familiaris, class: GPCR, accessions: F1PGZ2, gene: CHRM3, swissprot: F1PGZ2_CANFA) antispasmodic; RN refers to bromide (trans)-isomer
Click to view flumetasone pivalate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Adrenal Cortex Hormones (Code: D000305) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) anti-inflammatory drug (Code: CHEBI:35472) antipruritic drug (Code: CHEBI:59683) FDA
Click to view nicomorphine Analgesics (Code: D000700) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689)
Click to view mibefradil Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) blocker Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) blocker (Source: ) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Cation channel sperm-associated protein 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q8NEC5, gene: CATSPER1, swissprot: CTSR1_HUMAN) blocker (Source: ) Cation channel sperm-associated protein 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q96P56, gene: CATSPER2, swissprot: CTSR2_HUMAN) blocker (Source: ) Cation channel sperm-associated protein 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q86XQ3, gene: CATSPER3, swissprot: CTSR3_HUMAN) blocker (Source: ) Cation channel sperm-associated protein 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q7RTX7, gene: CATSPER4, swissprot: CTSR4_HUMAN) blocker (Source: ) Voltage-dependent T-type calcium channel subunit alpha-1I (Organism: Homo sapiens, class: Ion channel, accessions: Q9P0X4, gene: CACNA1I, swissprot: CAC1I_HUMAN Voltage-dependent T-type calcium channel subunit alpha-1G (Organism: Homo sapiens, class: Ion channel, accessions: O43497, gene: CACNA1G, swissprot: CAC1G_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Voltage-dependent N-type calcium channel subunit alpha-1B (Organism: Homo sapiens, class: Ion channel, accessions: Q00975, gene: CACNA1B, swissprot: CAC1B_HUMAN Voltage-dependent P/Q-type calcium channel subunit alpha-1A (Organism: Rattus norvegicus, class: Unclassified, accessions: P54282, gene: Cacna1a, swissprot: CAC1A_RAT) gating inhibitor (Source: ) Voltage-dependent R-type calcium channel subunit alpha-1E (Organism: Rattus norvegicus, class: Unclassified, accessions: Q07652, gene: Cacna1e, swissprot: CAC1E_RAT) gating inhibitor (Source: ) A benzimidazoyl-substituted tetraline that selectively binds and inhibits CALCIUM CHANNELS, T-TYPE. Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Cytochrome P-450 CYP1A2 Inhibitors (Code: D065609) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Membrane Transport Modulators (Code: D049990) Metabolic Side Effects of Drugs and Substances (Code: D065606) Vasodilator Agents (Code: D014665) 1997-08-01 FDA
Click to view orlistat hatidylserine lipase ABHD16A (Organism: Homo sapiens, class: Enzyme, accessions: O95870, gene: ABHD16A, swissprot: ABHGA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18657971) Monoacylglycerol lipase ABHD12 (Organism: Homo sapiens, class: Enzyme, accessions: Q8N2K0, gene: ABHD12, swissprot: ABD12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18657971) Platelet-activating factor acetylhydrolase (Organism: Homo sapiens, class: Enzyme, accessions: Q13093, gene: PLA2G7, swissprot: PAFA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18657971) Pancreatic triacylglycerol lipase (Organism: Sus scrofa, class: Enzyme, accessions: P00591, gene: PNLIP, swissprot: LIPP_PIG) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22450131) Fatty acid synthase (Organism: Homo sapiens, class: Enzyme, accessions: P49327, gene: FASN, swissprot: FAS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21726077) Monoacylglycerol lipase ABHD6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BV23, gene: ABHD6, swissprot: ABHD6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21726077) Sn1-specific diacylglycerol lipase alpha (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y4D2, gene: DAGLA, swissprot: DGLA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22738638) Orlistat is a reversible active-site inhibitor of gastrointestinal lipases.Orlistat is used weight loss agent. Anti-Obesity Agents (Code: D019440) Central Nervous System Agents (Code: D002491) Enzyme Inhibitors (Code: D004791) Intestinal Lipase Inhibitor (Code: N0000175591) Lipase Inhibitors (Code: N0000009916) 1999-04-23 FDA
Click to view perflexane Perflexane is chemically characterized as n-perfluorohexane. Perflexane is a fluorinated hydrocarbon and gaseous substance used as an imaging contrast agent in echocardiogram. After administration in microsphere form, perflexane increases ultrasound reflectivity of blood. This leads to an improvement of ultrasound signaling. Perflexane is indicated for use in subjects with suboptimal echocardiograms to opacify the left ventricular chamber and to improve the delineation of the left ventricular endocardial border. Contrast Agent for Ultrasound Imaging (Code: N0000175864) Ultrasound Contrast Activity (Code: N0000010259) radioopaque medium (Code: CHEBI:37338) 2002-05-31 FDA
Click to view betamethasone benzoate Betamethasone benzoate is a 17-substituted ester. It is a derivative of betamethasone. (See: dexamethasone) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1973-12-31 Health Canada
Click to view idarubicin DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050734s022lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9188796) An orally administered anthracycline antineoplastic. It has shown activity against breast neoplasms, lymphoma and leukemia. Anthracycline Topoisomerase Inhibitor (Code: N0000175414) Anthracyclines (Code: N0000007530) Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1990-09-27 FDA DM5
Click to view tebipenem pivoxil an oral carbapenem antibiotic, against penicillin-nonsusceptible Streptococcus pneumoniae
Click to view moexipril Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor Moexipril is a non-sulfhydryl angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity which is used in the therapy of hypertension. As a prodrug, moexipril is hydrolyzed into its active form moexiprilat, which competitively inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. Angiotensin Converting Enzyme Inhibitor (Code: N0000175562) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) 1995-04-19 FDA
Click to view binifibrate two nicotinic & one clofibiric radical esterified by glycerol moiety Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847)
Click to view clobenoside
Click to view halofantrine Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN used in treatment of mild to moderate acute malaria Antimalarial (Code: N0000175482) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) 1992-07-24 FDA
Click to view tritoqualine Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377)
Click to view travoprost Travoprost is a synthetic lipophilic isopropyl ester prodrug of the active compound travoprost free acid, a prostaglandin F2alpha analog with anti-glaucoma property. Upon administration, travoprost is hydrolysed to a free acid by corneal esterases, and then selectively stimulating the prostaglandin F (FP prostanoid) receptor, thereby increasing the uveoscleral outflow which leads to a reduction in intra-ocular pressure. Travoprost is indicated for the treatment of open-angle glaucoma or ocular hypertension. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) ophthalmology drug (Code: CHEBI:66981) antiglaucoma drug (Code: CHEBI:39456) antihypertensive agent (Code: CHEBI:35674) prodrug (Code: CHEBI:50266) Prostaglandin Analog (Code: N0000175454) Prostaglandins (Code: N0000007706) 2001-03-16 FDA
Click to view fluticasone propionate Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist (Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209022s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209022s000lbl.pdf) Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Cytosolic phospholipase A2 (Organism: Homo sapiens, class: Enzyme, accessions: P47712, gene: PLA2G4A, swissprot: PA24A_HUMAN) Glucocorticoid receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P06536, gene: Nr3c1, swissprot: GCR_RAT Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) agonist (Source: ) Fluticasone propionate is a synthetic trifluorinated corticosteroid with anti-inflammatory activity. Fluticasone propionate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor. Fluticasone propionate is indicated for the treatment of nasal polyps, asthma, inflammatory and pruritic dermatoses, allergic and nonallergic rhinitis. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Anti-Allergic Agents (Code: D018926) Anti-Asthmatic Agents (Code: D018927) Anti-Inflammatory Agents (Code: D000893) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Dermatologic Agents (Code: D003879) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) anti-allergic agent (Code: CHEBI:50857) anti-asthmatic drug (Code: CHEBI:49167) anti-inflammatory drug (Code: CHEBI:35472) adrenergic agent (Code: CHEBI:37962) dermatologic drug (Code: CHEBI:50177) bronchodilator agent (Code: CHEBI:35523) 1990-12-14 FDA
Click to view mupirocin Isoleucine--tRNA ligase (Organism: Staphylococcus aureus, class: Enzyme, accessions: P41972, gene: ileS, swissprot: SYI1_STAAU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/50788_Mupirocin_lbl.pdf) Isoleucine--tRNA ligase (Organism: Streptococcus pyogenes serotype M1, class: Enzyme, accessions: Q99YW3, gene: ileS, swissprot: SYI_STRP1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/50788_Mupirocin_lbl.pdf) Isoleucine--tRNA ligase (Organism: Thermus thermophilus (strain HB8 / ATCC 27634 / DSM 579), class: Enzyme, accessions: P56690, gene: ileS, swissprot: SYI_THET8) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11584022) Mupirocin is a topically used antibiotic from a strain of Pseudomonas fluorescens. It has shown excellent activity against gram-positive staphylococci and streptococci. The antibiotic is used primarily for the treatment of primary and secondary skin disorders, nasal infections, and wound healing. RNA Synthetase Inhibitor Antibacterial (Code: N0000175515) RNA Synthetase Inhibitors (Code: N0000175516) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) antibacterial drug (Code: CHEBI:36047) 1987-12-31 FDA MRC
Click to view adefovir dipivoxil DNA polymerase subunit gamma-1 (Organism: Homo sapiens, class: Enzyme, accessions: P54098, gene: POLG, swissprot: DPOG1_HUMAN) Protein P (Organism: Hepatitis B virus, class: Polyprotein, accessions: Q9IF40, gene: P, swissprot: Q9IF40_HBV) inhibitor inhibitor of African swine fever virus Hepatitis B Virus Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175656) Nucleoside Analog (Code: N0000175459) Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009947) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) prodrug (Code: CHEBI:50266) antiviral drug (Code: CHEBI:36044) 2002-09-20 FDA
Click to view fexofenadine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021963s007lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10421612) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14610227) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Unclassified, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10421612) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16931010) Fexofenadine, the major active metabolite of terfenadine, is an antihistamine with selective H1receptor antagonist activity. Both enantiomers of fexofenadine displayed approximately equipotent antihistaminic effects. Fexofenadine is a highly selective and reversible competitor at peripheral H1 histamine receptors in the gastrointestinal (GI) tract, blood vessels, and bronchial smooth muscle. Fexofenadine is used for the treatment of allergic rhinitis, angioedema and chronic urticaria. Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Antagonist (Code: N0000175587) Anti-Allergic Agents (Code: D018926) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Histamine H1 Antagonists, Non-Sedating (Code: D039563) Neurotransmitter Agents (Code: D018377) H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) 1996-07-25 FDA
Click to view amcinonide Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) anti-inflammatory drug (Code: CHEBI:35472) 1979-10-18 FDA
Click to view dexamethasone dipropionate Dexamethasone (betamethasone) dipropionate is a synthetic adrenocorticosteroid. Dexamethasone (betamethasone) dipropionate is the 17,21-dipropionate ester of dexamethasone (betamethasone). It is used in combination with calcipotriene hydrate, a synthetic vitamin D analogue, for the topical treatment of plaque psoriasis in adult patients. (See: dexamethasone) betamethasone dipropionate: 1975-01-29 FDA
Click to view betamethasone acibutate Betamethasone acibutate, derives from Betamethasone, is an acetate ester. Betamethasone acibutate is a glucocorticoid. (See: dexamethasone)
Click to view dipyridamole cAMP-specific 3',5'-cyclic phosphodiesterase 4A (Organism: Homo sapiens, class: Enzyme, accessions: P27815, gene: PDE4A, swissprot: PDE4A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B (Organism: Homo sapiens, class: Enzyme, accessions: O95263, gene: PDE8B, swissprot: PDE8B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) Equilibrative nucleoside transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q99808, gene: SLC29A1, swissprot: S29A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14634039) Phosphodiesterase 6 (Organism: Homo sapiens, class: Enzyme, accessions: O43924|P16499|P18545|P35913|P51160|Q13956, gene: PDE6A|PDE6B|PDE6C|PDE6D|PDE6G|PDE6H, swissprot: CNCG_HUMAN|CNRG_HUMAN|PDE6A_HUMAN|PDE6B_HUMAN|PDE6C_HUMAN|PDE6D_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) cAMP-specific 3',5'-cyclic phosphodiesterase 7B (Organism: Homo sapiens, class: Enzyme, accessions: Q9NP56, gene: PDE7B, swissprot: PDE7B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) Phosphodiesterase 7 (Organism: Homo sapiens, class: Enzyme, accessions: Q13946|Q9NP56, gene: PDE7A|PDE7B, swissprot: PDE7A_HUMAN|PDE7B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) Phosphodiesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P54750|Q01064|Q14123, gene: PDE1A|PDE1B|PDE1C, swissprot: PDE1A_HUMAN|PDE1B_HUMAN|PDE1C_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) cGMP-dependent 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O00408, gene: PDE2A, swissprot: PDE2A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) Phosphodiesterase 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q13370|Q14432, gene: PDE3A|PDE3B, swissprot: PDE3A_HUMAN|PDE3B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y233, gene: PDE10A, swissprot: PDE10_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A (Organism: Homo sapiens, class: Enzyme, accessions: O60658, gene: PDE8A, swissprot: PDE8A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/012836s057lbl.pdf) A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Phosphodiesterase Inhibitors (Code: D010726) Platelet Aggregation Inhibitors (Code: D010975) Vasodilator Agents (Code: D014665) platelet aggregation inhibitor (Code: CHEBI:50427) vasodilator agent (Code: CHEBI:35620) Decreased Platelet Aggregation (Code: N0000008832) 1961-12-06 FDA
Click to view clindamycin phosphate Clindamycin phosphate is the prodrug of clindamycin with no antimicrobial activity. Biologically inactive clindamycin phosphate is converted to active clindamycin. It is indicated in the treatment of serious infections caused by susceptible anaerobic bacteria: Lower respiratory tract infections including pneumonia, empyema, and lung abscess caused by anaerobes; Skin and skin structure infections; Gynecological infections including endometritis, nongonococcal tubo-ovarian abscess, pelvic cellulitis, and postsurgical vaginal cuff infection caused by susceptible anaerobes; Intra-abdominal infections; Septicemia; Bone and joint infections. (See: clindamycin) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1972-10-02 FDA
Click to view chlorhexidine Histamine N-methyltransferase (Organism: Rattus norvegicus, class: Enzyme, accessions: Q01984, gene: Hnmt, swissprot: HNMT_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3337739) Trypanothione reductase (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P28593, gene: TPR, swissprot: TYTR_TRYCR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16033259) Matrix metalloproteinase-9 (Organism: Homo sapiens, class: Enzyme, accessions: P14780, gene: MMP9, swissprot: MMP9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20053563) 72 kDa type IV collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P08253, gene: MMP2, swissprot: MMP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20053563) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Chlorhexidine is a biguanide compound used as an antiseptic agent with topical antibacterial activity. The chlorhexidine molecule, due to its positive charge, reacts with the microbial cell surface, destroys the integrity of the cell membrane, penetrates into the cell, precipitates the cytoplasm, and the cell dies. Since gram positive bacteria are more negatively charged, they are more sensitive to this agent. Decreased Cell Wall Integrity (Code: N0000008478) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Cosmetics (Code: D003358) Dermatologic Agents (Code: D003879) Disinfectants (Code: D004202) Mouthwashes (Code: D009067) antiinfective agent (Code: CHEBI:35441) 1976-09-17 FDA
Click to view benidipine Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/21466810) Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/17276408) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Vasodilator Agents (Code: D014665) 1991-01-01 YEAR INTRODUCED
Click to view hepronicate
Click to view amprenavir Pol polyprotein (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72874, gene: pol, swissprot: Q72874_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/021039s017lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/021039s017lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/021039s017lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) weak inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159797) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12584153) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11602674) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12218384) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21861202) Amprenavir is an inhibitor of the human immunodeficiency virus (HIV) protease. Amprenavir binds to the active site of HIV-1 protease and thereby prevents the processing of viral gag and gag-pol polyprotein precursors, resulting in the formation of immature non-infectious viral particles. Amprenavir is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. Protease Inhibitor (Code: N0000175889) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 3A4 Inducers (Code: N0000185506) P-Glycoprotein Inducers (Code: N0000191264) Anti-Bacterial Agents (Code: D000900) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antibiotics, Antitubercular (Code: D000904) Antitubercular Agents (Code: D000995) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) HIV Protease Inhibitors (Code: D017320) Protease Inhibitors (Code: D011480) antiviral drug (Code: CHEBI:36044) 1999-04-15 FDA 478
Click to view tropesin
Click to view indocyanine green A tricarbocyanine dye that is used diagnostically in liver function tests and to determine blood volume and cardiac output. Diagnostic Dye (Code: N0000175536) Dyes (Code: N0000175533) Coloring Agents (Code: D004396) 1959-02-09 FDA
Click to view ixabepilone Tubulin beta (Organism: Homo sapiens, class: Structural, accessions: Q9H4B7|Q13885|Q9BVA1|Q13509|P04350|P68371|P07437|Q9BUF5|Q3ZCM7, gene: TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB|TUBB6|TUBB8, swissprot: TBB1_HUMAN|TBB2A_HUMAN|TBB2B_HUMAN|TBB3_HUMAN|TBB4A_HUMAN|TBB4B_HUMAN|TBB5_HUMAN|TBB6_HUMAN|TBB8_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/19010832) Ixabepilone is a semi-synthetic analog of epothilone B. Ixabepilone binds directly to beta-tubulin subunits on microtubules, leading to suppression of microtubule dynamics. Ixabepilone is approved for use in refractory cases of advanced breast cancer. antineoplastic agent (Code: CHEBI:35610) Microtubule Inhibition (Code: N0000175085) Microtubule Inhibitor (Code: N0000175592) 2007-10-16 FDA
Click to view adenosine triphosphate P2X purinoceptor 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P49653, gene: P2rx2, swissprot: P2RX2_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) P2X purinoceptor 1 (Organism: Homo sapiens, class: Ion channel, accessions: P51575, gene: P2RX1, swissprot: P2RX1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) P2X purinoceptor 5 (Organism: Rattus norvegicus, class: Unclassified, accessions: P51578, gene: P2rx5, swissprot: P2RX5_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) P2X purinoceptor 6 (Organism: Rattus norvegicus, class: Unclassified, accessions: P51579, gene: P2rx6, swissprot: P2RX6_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) P2X purinoceptor 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q99571, gene: P2RX4, swissprot: P2RX4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) P2X purinoceptor 3 (Organism: Homo sapiens, class: Ion channel, accessions: P56373, gene: P2RX3, swissprot: P2RX3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) P2Y purinoceptor 2 (Organism: Homo sapiens, class: GPCR, accessions: P41231, gene: P2RY2, swissprot: P2RY2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) P2Y purinoceptor 4 (Organism: Homo sapiens, class: GPCR, accessions: P51582, gene: P2RY4, swissprot: P2RY4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) P2Y purinoceptor 11 (Organism: Homo sapiens, class: GPCR, accessions: Q96G91, gene: P2RY11, swissprot: P2Y11_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) P2Y purinoceptor 1 (Organism: Meleagris gallopavo, class: GPCR, accessions: P49652, gene: P2RY1, swissprot: P2RY1_MELGA) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12213051) Adenosine Triphosphate is an adenine nucleotide comprised of three phosphate groups esterified to the sugar moiety, found in all living cells. Adenosine triphosphate is involved in energy production for metabolic processes and RNA synthesis. In addition, this substance acts as a neurotransmitter. In cancer studies, adenosine triphosphate is synthesized to examine its use to decrease weight loss and improve muscle strength. nutraceutical (Code: CHEBI:50733) 1961-07 PMDA ATP
Click to view oxaflumazine psychosedative
Click to view difluprednate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Adrenal Cortex Hormones (Code: D000305) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 2008-06-23 FDA
Click to view argatroban Prothrombin (Organism: Homo sapiens, class: Enzyme, accessions: P00734, gene: F2, swissprot: THRB_HUMAN) inhibitor Tissue-type plasminogen activator (Organism: Homo sapiens, class: Enzyme, accessions: P00750, gene: PLAT, swissprot: TPA_HUMAN Cationic trypsin (Organism: Bos taurus, class: Enzyme, accessions: P00760, gene: None, swissprot: TRY1_BOVIN Prothrombin (Organism: Bos taurus, class: Enzyme, accessions: P00735, gene: F2, swissprot: THRB_BOVIN Coagulation factor X (Organism: Homo sapiens, class: Enzyme, accessions: P00742, gene: F10, swissprot: FA10_HUMAN Anti-coagulant (Code: N0000175980) Direct Thrombin Inhibitor (Code: N0000175518) Thrombin Inhibitors (Code: N0000009963) Anticoagulants (Code: D000925) Antithrombins (Code: D000991) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) 2000-06-30 FDA 15U
MIT
Click to view alexidine Toll-like receptor 9 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q9NR96, gene: TLR9, swissprot: TLR9_HUMAN Beta-lactamase (Organism: Pseudomonas aeruginosa, class: Unclassified, accessions: Q932Y6, gene: bla(tem-2), swissprot: Q932Y6_PSEAI until June 1975 was mistakenly treated as synonym for chlorhexidine; RN given refers to parent cpd
Click to view clomocycline antibacterial drug (Code: CHEBI:36047) antiprotozoal drug (Code: CHEBI:35820)
Click to view landiolol Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) antagonist (Source: http://www.kegg.jp/entry/D01847) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377)
Click to view chlorisondamine A nicotinic antagonist used primarily as a ganglionic blocker in animal research. It has been used as an antihypertensive agent but has been supplanted by more specific drugs in most clinical applications. Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Ganglionic Blockers (Code: D005730) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373)
Click to view cefuroxime axetil Cefuroxime axetil is an acetoxyethyl ester prodrug of cefuroxime cefuroxime axetil is absorbed from the gastrointestinal tract and rapidly hydrolyzed by nonspecific esterases in the intestinal mucosa and blood to cefuroxime. It is used for the treatment of pharyngitis/tonsillitis, acute bacterial otitis media, acute bacterial maxillary sinusitis, acute bacterial exacerbations of chronic bronchitis, skin and skin-structure infections, urinary tract infections, gonorrhea, early Lyme disease and impetigo. (See: cefuroxime) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1987-12-28 FDA
Click to view pinaverium Voltage-dependent L-type calcium channel subunit alpha-1S (Organism: Homo sapiens, class: Ion channel, accessions: Q13698, gene: CACNA1S, swissprot: CAC1S_HUMAN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00028699.PDF) Pinaverium is a calcium antagonist which inhibits the calcium influx by blocking the voltage-dependent calcium channel at the smooth muscle cell level. It possesses a high degree of selectivity for the intestinal smooth muscle. pinaverium is indicated for the treatment and relief of symptoms associated with irritable bowel syndrome and for the treatment of symptoms related to functional disorders of the biliary tract. Autonomic Agents (Code: D001337) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Parasympatholytics (Code: D010276) Peripheral Nervous System Agents (Code: D018373) 1981-02-11 Italian Medicines Agency (AIFA)
Click to view cefmenoxime Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor (Source: ) A cephalosporin antibiotic that is administered intravenously or intramuscularly. It is active against most common gram-positive and gram-negative microorganisms, is a potent inhibitor of Enterobacteriaceae, and is highly resistant to hydrolysis by beta-lactamases. The drug has a high rate of efficacy in many types of infection and to date no severe side effects have been noted. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1987-12-30 FDA
Click to view cefetamet pivoxil Cefetamet pivoxil is the pivalate ester prodrug form of cefetamet, a semi-synthetic, beta-lactamase-stable, third-generation cephalosporin with antibacterial activity. After oral administration of cefetamet pivoxil, the ester bond is cleaved, releasing active cefetamet. Cefetamet pivoxil is used for the treatment of both upper and lower community-acquired respiratory tract infections, urinary tract infections. (See: cefetamet) 2002-11-14 CDSCO (INDIA)
Click to view sobuzoxane used in treatment of leukemia L1210 Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003)
Click to view flomoxef Flomoxef is a cephamycin antibiotic with a difluoromethylthio-acetamido group at the 7-beta position of the cephem nucleus, commonly used for postoperative prophylaxis. Flomoxef has activity against staphylococci, streptococci, and pneumococci, Neisseria gonorrhoeae, Moraxella (Branhamella) catarrhalis, Escherichia coli, Klebsiella spp., Proteus spp., Morganella morgani, Providencia spp., and Haemophilus influenzae, Peptostreptococci, Bacteroides, and Prevotella. It is used for the treatment of sepsis, endocarditis, respiratory tract infections, urinary tract infections, intra-abdominal infections, gynecological infections, otitis media, sinusitis. antibacterial drug (Code: CHEBI:36047) 1988-05-01 PMDA
Click to view acetoxolone Estradiol 17-beta-dehydrogenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P14061, gene: HSD17B1, swissprot: DHB1_HUMAN Corticosteroid 11-beta-dehydrogenase isozyme 1 (Organism: Homo sapiens, class: Enzyme, accessions: P28845, gene: HSD11B1, swissprot: DHI1_HUMAN Corticosteroid 11-beta-dehydrogenase isozyme 2 (Organism: Homo sapiens, class: Enzyme, accessions: P80365, gene: HSD11B2, swissprot: DHI2_HUMAN Estradiol 17-beta-dehydrogenase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P37059, gene: HSD17B2, swissprot: DHB2_HUMAN
Click to view carubicin DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) A very toxic anthracycline-type antineoplastic related to DAUNORUBICIN, obtained from Actinomadura carminata. Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antineoplastic agent (Code: CHEBI:35610)
Click to view cefuzonam article gives L-105 as synonym, however L 105 is a rifamycin derivative according to Chemline antibacterial drug (Code: CHEBI:36047)
Click to view telmisartan Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020850s040lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020850s040lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20222053) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20222053) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20222053) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20079636) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) potentiator (Source: https://www.ncbi.nlm.nih.gov/pubmed/25790278) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) Telmisartan is a benzimidazole derivative and a non-peptide angiotensin II receptor antagonist with antihypertensive property. Telmisartan selectively antagonizes angiotensin II binding to the AT1 subtype receptor, located in vascular smooth muscle and adrenal gland. The antagonism results in vasodilation and inhibits the angiotensin II-mediated aldosterone production, which in turn leading to a decrease in sodium and water as well as an increase in potassium excretion leading to a subsequent reduction in blood pressure. Angiotensin II Type 1 Receptor Blockers (Code: D047228) Angiotensin Receptor Antagonists (Code: D057911) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) antihypertensive agent (Code: CHEBI:35674) EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor (Code: CHEBI:35457) angiotensin receptor antagonist (Code: CHEBI:61016) Angiotensin 2 Receptor Antagonists (Code: N0000000070) Angiotensin 2 Receptor Blocker (Code: N0000175561) 1998-11-10 FDA TLS
Click to view cefpirome Cefpirome is a semisynthetic, broad-spectrum, fourth-generation cephalosporin with antibacterial activity. Cefpirome binds to and inactivates penicillin-binding proteins (PBPs). Cefpirome is stable against most plasmid- and chromosome-mediated beta-lactamases. Cefpirome has activity against Enterobacteriaceae, methicillin-susceptible Staphylococcus aureus, coagulase-negative staphylococci, viridans group streptococci, Streptococcus pneumoniae. Cefpirome is indicated for the treatment of Lower respiratory tract infections, Septicemia, Skin infections, Soft tissue infections, Urinary tract infections, Febrile Neutropenic, Meningitis. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1993-12-02 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view cynarine Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q7ZJM1, gene: pol, swissprot: Q7ZJM1_9HIV1 active principle of the artichoke; functions primarily as a cholagogue and choleretic and also as antilipemic agent Cholagogues and Choleretics (Code: D002756) Gastrointestinal Agents (Code: D005765)
Click to view cefozopran
Click to view probucol Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Arachidonate 15-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P16050, gene: ALOX15, swissprot: LOX15_HUMAN ATP-binding cassette sub-family A member 1 (Organism: Homo sapiens, class: Transporter, accessions: O95477, gene: ABCA1, swissprot: ABCA1_HUMAN) inhibitor A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993). Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Antioxidants (Code: D000975) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Protective Agents (Code: D020011) anti-inflammatory drug (Code: CHEBI:35472) cardiovascular drug (Code: CHEBI:35554) antilipemic drug (Code: CHEBI:35679) anticholesteremic drug (Code: CHEBI:35821) 1977-02-01 FDA
Click to view piperacillin Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) Streptokinase A (Organism: Streptococcus pyogenes serotype M1, class: Enzyme, accessions: P10520, gene: ska, swissprot: STRP_STRP1) Beta-lactamase (Organism: Citrobacter freundii, class: Enzyme, accessions: A2RP81, gene: blaPER-2, swissprot: A2RP81_CITFR Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor Semisynthetic, broad-spectrum, AMPICILLIN derived ureidopenicillin antibiotic proposed for PSEUDOMONAS infections. It is also used in combination with other antibiotics. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1981-12-29 FDA WPP
Click to view retapamulin 50S ribosomal protein L3 (Organism: Staphylococcus aureus (strain N315), class: Cytosolic other, accessions: P60449, gene: rplC, swissprot: RL3_STAAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022055s002lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022055s002lbl.pdf) Retapamulin is bacteriostatic against Staphylococcus aureus and Streptococcus pyogenes. Retapamulin selectively inhibits bacterial protein synthesis by interacting at a site on the 50S subunit of the bacterial ribosome through an interaction that is different from that of other antibiotics. This binding site involves ribosomal protein L3 and is in the region of the ribosomal P site and peptidyl transferase center. Retapamulin is indicated for the topical treatment of impetigo due to Staphylococcus aureus (methicillin-susceptible isolates only) or Streptococcus pyogenes. pleuromutilin (Code: N0000175433) Pleuromutilin Antibacterial (Code: N0000175434) 2007-04-12 FDA G34
Click to view benziodarone Baculoviral IAP repeat-containing protein 5 (Organism: Homo sapiens, class: Unclassified, accessions: O15392, gene: BIRC5, swissprot: BIRC5_HUMAN) minor descriptor (75-89); on-line & INDEX MEDICUS search BENZOFURANS (68-89) & IODOBENZOATES (74) Antirheumatic Agents (Code: D018501) Gout Suppressants (Code: D006074) Renal Agents (Code: D012076) Uricosuric Agents (Code: D014528)
Click to view gossypol Bcl-2-like protein 1 (Organism: Homo sapiens, class: Cytosolic other, accessions: Q07817, gene: BCL2L1, swissprot: B2CL1_HUMAN Kinesin-like protein 1 (Organism: Homo sapiens, class: Unclassified, accessions: P52732, gene: KIF11, swissprot: KIF11_HUMAN Malate dehydrogenase, mitochondrial (Organism: Sus scrofa, class: Enzyme, accessions: P00346, gene: MDH2, swissprot: MDHM_PIG Apoptosis regulator Bcl-2 (Organism: Homo sapiens, class: Cytosolic other, accessions: P10415, gene: BCL2, swissprot: BCL2_HUMAN Aldose reductase (Organism: Homo sapiens, class: Enzyme, accessions: P15121, gene: AKR1B1, swissprot: ALDR_HUMAN Beta-lactamase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P00811, gene: ampC, swissprot: AMPC_ECOLI Malate dehydrogenase, cytoplasmic (Organism: Sus scrofa, class: Enzyme, accessions: P11708, gene: MDH1, swissprot: MDHC_PIG Malate dehydrogenase (Organism: Plasmodium falciparum, class: Enzyme, accessions: Q6VVP7, gene: None, swissprot: Q6VVP7_PLAFA Lactate dehydrogenase (Organism: Plasmodium falciparum, class: Enzyme, accessions: Q0PJ46, gene: LDH, swissprot: Q0PJ46_PLAFA Apoptosis regulator Bcl-W (Organism: Homo sapiens, class: Cytosolic other, accessions: Q92843, gene: BCL2L2, swissprot: B2CL2_HUMAN Induced myeloid leukemia cell differentiation protein Mcl-1 (Organism: Homo sapiens, class: Cytosolic other, accessions: Q07820, gene: MCL1, swissprot: MCL1_HUMAN Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN DNA-3-methyladenine glycosylase (Organism: Homo sapiens, class: Enzyme, accessions: P29372, gene: MPG, swissprot: 3MG_HUMAN A dimeric sesquiterpene found in cottonseed (GOSSYPIUM). The (-) isomer is active as a male contraceptive (CONTRACEPTIVE AGENTS, MALE) whereas toxic symptoms are associated with the (+) isomer. Contraceptive Agents (Code: D003270) Contraceptive Agents, Male (Code: D003272) Reproductive Control Agents (Code: D012102)
Click to view betamethasone butyrate propionate Betamethasone butyrate propionate is a topical corticosteroid. (See: dexamethasone) 2019-06-01 PMDA
Click to view glucametacin Glucametacin is a prodrug, composed of indomethacin and glucosamine, linked by amide bond. Administered glucametacin has both anti-inflammatory and gastric mucosa protective effect. (See: indomethacin) (See: glucosamine) It is used for the treatment of rheumatoid arthritis, gout, inflammation of various localization and pain. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Italian Medicines Agency (AIFA)
Click to view tenofovir disoproxil Gag-Pol polyprotein (Organism: Human immunodeficiency virus type 1 group M subtype B (isolate ARV2/SF2), class: Polyprotein, accessions: P03369, gene: gag-pol, swissprot: POL_HV1A2) Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1) inhibitor Tenofovir disoproxil fumarate is the fumarate salt of the prodrug tenofovir disoproxil. Tenofovir disoproxil is absorbed and converted to the active substance tenofovir, which is a nucleoside monophosphate (nucleotide) analogue. Tenofovir is then converted to the active metabolite, tenofovir diphosphate, an obligate chain terminator, by constitutively expressed cellular enzymes. Tenofovir diphosphate has an intracellular half-life of 10 hours in activated and 50 hours in resting peripheral blood mononuclear cells (PBMCs). Tenofovir diphosphate inhibits HIV-1 reverse transcriptase and the HBV polymerase by direct binding competition with the natural deoxyribonucleotide substrate and, after incorporation into DNA, by DNA chain termination. Tenofovir diphosphate is a weak inhibitor of cellular polymerases alpha, beta, and gamma. At concentrations of up to 300 umol/l, tenofovir has also shown no effect on the synthesis of mitochondrial DNA or the production of lactic acid in in vitro assays. prodrug (Code: CHEBI:50266) antiviral drug (Code: CHEBI:36044) 2001-10-26 FDA
Click to view ceforanide Ceforanide is a semi-synthetic, broad-spectrum, beta-lactam, second-generation cephalosporin antibiotic with bactericidal activity. Ceforanide causes inhibition of bacterial cell wall synthesis by inactivating penicillin binding proteins (PBPs) thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of the cell wall. This results in a reduction of cell wall stability and causes cell lysis. Ceforanide is primarily indicated in conditions like bone and joint infection, endocarditis, respiratory tract infections, skin infections, surgical infections, urinary tract infection. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1984-05-24 FDA
Click to view cefminox Cefminox is a broad-spectrum, bactericidal cephalosporin antibiotic. Cefminox binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Cefminox is active against Streptococcus pneumoniae, Escherichia coli, Klebsiella pneumoniae, Proteus spp., Morganella morganii, Providencia, spp., Haemophilus influenzae, Bacteroides spp., Prevotella spp. (excluding Prevotella vivia). It is used for the treatment of urinary tract infections (cystitis, pyelonephritis), respiratory tract infections (tonsillitis, acute bronchitis, pneumonia), intra-abdominal infections. Also it is used for the post-surgical infections prevention. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1994-10-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view atosiban Oxytocin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30559, gene: OXTR, swissprot: OXYR_HUMAN) antagonist (Source: https://www.ema.europa.eu/documents/product-information/tractocile-epar-product-information_en.pdf) Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) antagonist (Source: https://www.ema.europa.eu/documents/product-information/tractocile-epar-product-information_en.pdf) Vasopressin V1a receptor (Organism: Homo sapiens, class: GPCR, accessions: P37288, gene: AVPR1A, swissprot: V1AR_HUMAN) antagonist (Source: https://www.ema.europa.eu/documents/product-information/tractocile-epar-product-information_en.pdf) Vasopressin V1b receptor (Organism: Homo sapiens, class: GPCR, accessions: P47901, gene: AVPR1B, swissprot: V1BR_HUMAN) antagonist (Source: https://www.ema.europa.eu/documents/product-information/tractocile-epar-product-information_en.pdf) Atosiban is a synthetic peptide which is a competitive antagonist of human oxytocin at receptor level. Atosiban was also shown to bind to the vasopressin receptor, thus inhibiting the effect of vasopressin. Atosiban is indicated to delay imminent pre-term birth in pregnant adult women with regular uterine contractions of at least 30 seconds duration at a rate of 4 per 30 minutes, with a cervical dilation of 1 to 3 cm (0-3 for nulliparas) and effacement of 50%, with a gestational age from 24 until 33 completed weeks. Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Reproductive Control Agents (Code: D012102) Tocolytic Agents (Code: D015149) 2000-01-20 EMA
Click to view estramustine phosphate Tyrosine-protein phosphatase non-receptor type 1 (Organism: Homo sapiens, class: Enzyme, accessions: P18031, gene: PTPN1, swissprot: PTN1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21193311) Protein-tyrosine phosphatase 1C (Organism: Homo sapiens, class: Enzyme, accessions: P29350, gene: PTPN6, swissprot: PTN6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21193311) Tyrosine-protein phosphatase non-receptor type 11 (Organism: Homo sapiens, class: Enzyme, accessions: Q06124, gene: PTPN11, swissprot: PTN11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21193311) Estramustine phosphate is a synthetic molecule that combines estradiol and nornitrogen mustard through a carbamate link. Estramustine and its major metabolite estramustine bind to microtubule-associated proteins (MAPs) and tubulin, thereby inhibiting microtubule dynamics and leading to anaphase arrest in a dose-dependent fashion. (See: estramustine) 1981-12-24 FDA
Click to view latamoxef Penicillin-binding protein 1B (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02919, gene: mrcB, swissprot: PBPB_ECOLI) inhibitor Penicillin-binding protein 1A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918, gene: mrcA, swissprot: PBPA_ECOLI) inhibitor Peptidoglycan synthase FtsI (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD68, gene: ftsI, swissprot: FTSI_ECOLI) inhibitor Broad- spectrum beta-lactam antibiotic similar in structure to the CEPHALOSPORINS except for the substitution of an oxaazabicyclo moiety for the thiaazabicyclo moiety of certain CEPHALOSPORINS. It has been proposed especially for the meningitides because it passes the blood-brain barrier and for anaerobic infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) FDA
Click to view perfluamine Perfluamine is an organofluorine compound. It derives from a tripropylamine. It was used in coronary angioplasty in combination with perflunafene as "artificial blood". This combination was withdrawn for multiple reasons: efficacy was marginal, the product was technically difficult to use, and new developments in coronary angioplasty (the indication for which it was approved) made its use obsolete. blood substitute (Code: CHEBI:38849) 1990 FDA
Click to view apalcillin
Click to view cefoselis Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view penfluridol 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901|P19020|P25115|P30729|P61169, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_RAT|DRD2_RAT|DRD3_RAT|DRD4_RAT|DRD5_RAT One of the long-acting ANTIPSYCHOTIC AGENTS used for maintenance or long-term therapy of SCHIZOPHRENIA and other PSYCHOTIC DISORDERS. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149)
Click to view falecalcitriol 2001-04-04 PMDA
Click to view cefotiam Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) Matrix metalloproteinase-9 (Organism: Homo sapiens, class: Enzyme, accessions: P14780, gene: MMP9, swissprot: MMP9_HUMAN) Vasoactive intestinal polypeptide receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P32241, gene: VIPR1, swissprot: VIPR1_HUMAN) Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor One of the CEPHALOSPORINS that has a broad spectrum of activity against both gram-positive and gram-negative microorganisms. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) FDA
Click to view protoverine
Click to view pirozadil
Click to view daunorubicin DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209401s000lbl.pdf) DNA topoisomerase 2-beta (Organism: Homo sapiens, class: Enzyme, accessions: Q02880, gene: TOP2B, swissprot: TOP2B_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209401s000lbl.pdf) Carbonyl reductase [NADPH] 1 (Organism: Homo sapiens, class: Enzyme, accessions: P16152, gene: CBR1, swissprot: CBR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209401s000lbl.pdf) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9647783) Collagenase ColG (Organism: Hathewaya histolytica, class: Enzyme, accessions: Q9X721, gene: colG, swissprot: COLG_HATHI) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1322986) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11405287) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12134946) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11770832) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11160641) NADPH--cytochrome P450 reductase (Organism: Homo sapiens, class: Enzyme, accessions: P16435, gene: POR, swissprot: NCPR_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/34156) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10342576) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10188979) Multidrug resistance-associated protein 7 (Organism: Homo sapiens, class: Transporter, accessions: Q5T3U5, gene: ABCC10, swissprot: MRP7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19118001) Multidrug resistance-associated protein 6 (Organism: Homo sapiens, class: Transporter, accessions: O95255, gene: ABCC6, swissprot: MRP6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12414644) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11437380) Daunorubicin is an anthracycline topoisomerase inhibitor. Daunorubicin has antimitotic and cytotoxic activity, which is achieved by forming complexes with DNA, inhibiting topoisomerase II activity, inhibiting DNA polymerase activity, affecting regulation of gene expression, and producing DNA-damaging free radicals. Daunorubicin should only be administered in a rapid intravenous infusion. It should not be administered intramuscularly, subcutaneously or intrathecally, since it may cause extensive tissue necrosis and may lead to death. Daunorubicin is used for acute myeloid leukemia (AML), acute lymphocytic leukemia (ALL), chronic myelogenous leukemia (CML), and Kaposi's sarcoma. Anthracycline Topoisomerase Inhibitor (Code: N0000175414) Anthracyclines (Code: N0000007530) Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antineoplastic agent (Code: CHEBI:35610) 1979-12-19 FDA DM1
Click to view pibrentasvir Pibrentasvir is an inhibitor of HCV NS5A, which is essential for viral RNA replication and virion assembly. The mechanism of action of pibrentasvir has been characterized based on cell culture antiviral activity and drug resistance mapping studies. Hepatitis C Virus NS5A Inhibitor (Code: N0000191256) P-Glycoprotein Inhibitors (Code: N0000185503) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Cytochrome P450 3A Inhibitors (Code: N0000190114) Cytochrome P450 1A2 Inhibitors (Code: N0000182138) UGT1A1 Inhibitors (Code: N0000191272) 2017-07-26 EMA
Click to view rolitetracycline Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q76353, gene: None, swissprot: Q76353_9HIV1 A pyrrolidinylmethyl TETRACYCLINE. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) antiprotozoal drug (Code: CHEBI:35820) prodrug (Code: CHEBI:50266)
Click to view gliquidone Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23987740) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23987740) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23987740) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23987740) Gliquidone is an anti-diabetic drug in the sulfonylurea class. It is an ATP-dependent K+ channel blocker. Gliquidone is used in the treatment of diabetes mellitus type 2. Hypoglycemic Agents (Code: D007004) 1977-08-11 Austrian Medicines and Medical Devices Agency
Click to view dutasteride 3-oxo-5-alpha-steroid 4-dehydrogenase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P18405, gene: SRD5A1, swissprot: S5A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021319s028s029lbl.pdf) 3-oxo-5-alpha-steroid 4-dehydrogenase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P31213, gene: SRD5A2, swissprot: S5A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021319s028s029lbl.pdf) a synthetic 4-azasteroid compound. Dutasteride competitively and specifically binds to isoenzymes 1 and 2 of 5 alpha-reductase, forming stable enzyme complexes and inhibiting the conversion of testosterone to 5 alpha-dihydrotestosterone (DHT); the reduction in DHT activity may mitigate or prevent enlargement of the prostate gland. Dutasteride is used to treat benign prostatic hyperplasia. 5-alpha Reductase Inhibitor (Code: N0000175836) 5-alpha Reductase Inhibitors (Code: D058891) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Steroid Synthesis Inhibitors (Code: D065088) 2001-11-20 FDA
Click to view dexamethasone acefurate
Click to view lumefantrine Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Lumefantrine is an antimalarial agent. Available data suggest lumefantrine inhibits the formation of beta-hematin by forming a complex with hemin. Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) antimalarial (Code: CHEBI:38068) 2009-04-07 FDA
Click to view niceritrol An ester of nicotinic acid that lowers cholesterol and triglycerides in total plasma and in the VLD- and LD-lipoprotein fractions. Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847)
Click to view davercin
Click to view nilotinib Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Macrophage colony-stimulating factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P07333, gene: CSF1R, swissprot: CSF1R_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Epithelial discoidin domain-containing receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: Q08345, gene: DDR1, swissprot: DDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022068s029lbl.pdf) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19527930) Discoidin domain-containing receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: Q16832, gene: DDR2, swissprot: DDR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23273517) Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23273517) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23273517) Tyrosine-protein kinase Lyn (Organism: Homo sapiens, class: Kinase, accessions: P07948, gene: LYN, swissprot: LYN_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23273517) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Ribosyldihydronicotinamide dehydrogenase [quinone] (Organism: Homo sapiens, class: Enzyme, accessions: P16083, gene: NQO2, swissprot: NQO2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28280261) Nilotinib is an inhibitor of the BCR-ABL kinase indicated for the treatment of Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase and accelerated phase. Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of ABL protein. Nilotinib inhibited the autophosphorylation of the following kinases at IC50 values as indicated: BCR-ABL, PDGFR, c-KIT, CSF-1R and DDR1. Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) antineoplastic agent (Code: CHEBI:35610) 2007-10-29 FDA NIL
Click to view rocuronium Acetylcholine receptor; alpha1/beta1/delta/gamma (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P07510|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND|CHRNG, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN|ACHG_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18633030) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11408531) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11408531) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10648343) Rocuronium bromide is a nondepolarizing neuromuscular blocking agent with a rapid to intermediate onset depending on dose and intermediate duration. It acts by competing for cholinergic receptors at the motor end-plate. Rocuronium bromide competitively binds to the nicotinic receptor at the motor end plate, and antagonizes acetylcholine binding, which results in skeletal muscle relaxation and paralysis. Rocuronium bromide is indicated as an adjunct to general anesthesia to facilitate both rapid sequence and routine tracheal intubation, and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Neuromuscular Nondepolarizing Blockade (Code: N0000175732) Nondepolarizing Neuromuscular Blocker (Code: N0000175720) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Peripheral Nervous System Agents (Code: D018373) neuromuscular agent (Code: CHEBI:51372) muscle relaxant (Code: CHEBI:51371) 1994-03-17 FDA
Click to view proscillaridin Sodium/potassium-transporting ATPase subunit alpha-2 (Organism: Sus scrofa, class: Ion channel, accessions: D2WKD8, gene: ATP1A2, swissprot: AT1A2_PIG) Sodium/potassium-transporting ATPase subunit alpha-1 (Organism: Homo sapiens, class: Transporter, accessions: P05023, gene: ATP1A1, swissprot: AT1A1_HUMAN) A cardiotonic glycoside isolated from Scilla maritima var. alba (Squill). Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protective Agents (Code: D020011) 1967-01-01 YEAR INTRODUCED
Click to view deslanoside Sodium/potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P05023|P05026|P13637|P14415|P50993|P54709|P54710|Q13733, gene: ATP1A1|ATP1A2|ATP1A3|ATP1A4|ATP1B1|ATP1B2|ATP1B3|FXYD2, swissprot: AT1A1_HUMAN|AT1A2_HUMAN|AT1A3_HUMAN|AT1A4_HUMAN|AT1B1_HUMAN|AT1B2_HUMAN|AT1B3_HUMAN|ATNG_HUMAN) inhibitor Deacetyllanatoside C. A cardiotonic glycoside from the leaves of Digitalis lanata. Anti-Arrhythmia Agents (Code: D000889) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protective Agents (Code: D020011) anti-arrhythmia drug (Code: CHEBI:38070) cardiotonic drug (Code: CHEBI:38147) FDA
Click to view cortivazol Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: http://www.kegg.jp/entry/D03594) Anti-Inflammatory Agents (Code: D000893)
Click to view tocopherol succinate Tocopherol succinate is a watersoluble derivative of the natural active isomer of vitamin E. The active constituent of the medicinal product is essentially vitamin E (alpha tocopherol). It is used in children up to the age of 18 years who have congenital or hereditary chronic cholestasis and who cannot absorb vitamin E from the gut. Tocopherol succinate can be absorbed from the gut in children who have difficulty absorbing fats and vitamin E from the diet. This can increase vitamin E levels in the blood and help to prevent neurological deterioration (problems in the nervous system) due to vitamin E deficiency. FDA
Click to view ketoconazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20625155) Cytochrome P450 11B1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P15538, gene: CYP11B1, swissprot: C11B1_HUMAN) inhibitor (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/003906/WC500181492.pdf) Cytochrome P450 11B2, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P19099, gene: CYP11B2, swissprot: C11B2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/18672868) Potassium voltage-gated channel subfamily A member 10 (Organism: Homo sapiens, class: Ion channel, accessions: Q16322, gene: KCNA10, swissprot: KCA10_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/10836990) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/10836990) Potassium voltage-gated channel subfamily A member 5 (Organism: Homo sapiens, class: Ion channel, accessions: P22460, gene: KCNA5, swissprot: KCNA5_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/10836990) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11751127) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24014644) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14709627) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14709627) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14709627) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14709627) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14709627) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14709627) Phylloquinone omega-hydroxylase CYP4F2 (Organism: Homo sapiens, class: Enzyme, accessions: P78329, gene: CYP4F2, swissprot: CP4F2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14709627) Cytochrome P450 4F12 (Organism: Homo sapiens, class: Enzyme, accessions: Q9HCS2, gene: CYP4F12, swissprot: CP4FC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14709627) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16166450) Ketoconazole is an imidazole fungicidal agent with a very broad spectrum of activity against many fungal species that is used for treatment of superficial and systemic fungal infections. Ketoconazole is a well documented cause of clinically apparent acute drug induced liver injury and is no longer recommended as a first line antifungal agent. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 3A5 Inhibitors (Code: N0000190115) P-Glycoprotein Inhibitors (Code: N0000185503) 14-alpha Demethylase Inhibitors (Code: D058888) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Cytochrome P-450 CYP3A Inhibitors (Code: D065692) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) 1981-06-12 FDA KKK
KLN
KTN
Click to view terconazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) Sodium/nucleoside cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: O00337, gene: SLC28A1, swissprot: S28A1_HUMAN) 5-hydroxytryptamine receptor 4 (Organism: Cavia porcellus, class: GPCR, accessions: O70528, gene: HTR4, swissprot: 5HT4R_CAVPO) Arachidonate 15-lipoxygenase (Organism: Oryctolagus cuniculus, class: Enzyme, accessions: P12530, gene: ALOX15, swissprot: LOX15_RABIT) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) Membrane-associated progesterone receptor component 1 (Organism: Rattus norvegicus, class: Membrane receptor, accessions: P70580, gene: Pgrmc1, swissprot: PGRC1_RAT) Lanosterol 14-alpha demethylase (Organism: Homo sapiens, class: Enzyme, accessions: Q16850, gene: CYP51A1, swissprot: CP51A_HUMAN Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) 1987-12-31 FDA
Click to view cefsulodin Penicillin-binding protein 1B (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02919, gene: mrcB, swissprot: PBPB_ECOLI) Penicillin-binding protein 1A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918, gene: mrcA, swissprot: PBPA_ECOLI) Beta-adrenergic receptor kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P25098, gene: GRK2, swissprot: ARBK1_HUMAN Protein-tyrosine phosphatase 1C (Organism: Homo sapiens, class: Enzyme, accessions: P29350, gene: PTPN6, swissprot: PTN6_HUMAN Tyrosine-protein phosphatase non-receptor type 11 (Organism: Homo sapiens, class: Enzyme, accessions: Q06124, gene: PTPN11, swissprot: PTN11_HUMAN tRNA 2'-phosphotransferase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Unclassified, accessions: Q5A7N4, gene: TPT1, swissprot: Q5A7N4_CANAL A pyridinium-substituted semisynthetic, broad-spectrum antibacterial used especially for Pseudomonas infections in debilitated patients. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1981-01-01 YEAR INTRODUCED
Click to view ciclesonide Des-ciclesonide: Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022004s018lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022004s018lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022004s018lbl.pdf) Ciclesonide: Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022004s018lbl.pdf) Liver carboxylesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23141, gene: CES1, swissprot: EST1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17331475) Ciclesonide is a prodrug that is enzymatically hydrolyzed to a pharmacologically active metabolite, a corticosteroid C21-desisobutyryl-ciclesonide (des-ciclesonide or RM1) following intranasal application. Des-ciclesonide has anti-inflammatory activity with affinity for the glucocorticoid receptor that is 120-times higher than the parent compound. Ciclesonide is indicated for treatment of nasal symptoms associated with allergic rhinitis. Adrenal Cortex Hormones (Code: D000305) Anti-Allergic Agents (Code: D018926) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 2006-10-20 FDA Des-c
Click to view aprepitant Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021549s031,207865s004lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021549s031,207865s004lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021549s031,207865s004lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021549s031,207865s004lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021549s031,207865s004lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021549s031,207865s004lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021549s031,207865s004lbl.pdf) Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV). Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Aprepitant is indicated in patients 6 months of age and older for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin and for the treatment of nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC). Neurokinin 1 Antagonists (Code: N0000010262) Substance P/Neurokinin-1 Receptor Antagonist (Code: N0000175786) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 2C9 Inducers (Code: N0000185507) Cytochrome P450 3A4 Inducers (Code: N0000185506) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Neurokinin-1 Receptor Antagonists (Code: D064729) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) antidepressant (Code: CHEBI:35469) antiemetic (Code: CHEBI:50919) peripheral nervous system drug (Code: CHEBI:49110) 2003-03-27 FDA GBQ
Click to view cetalkonium chloride Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Surface-Active Agents (Code: D013501)
Click to view tocopheryl nicotinate
Click to view ambenonium Acetylcholinesterase (Organism: Bos taurus, class: Enzyme, accessions: P23795, gene: ACHE, swissprot: ACES_BOVIN Acetylcholinesterase (Organism: Mus musculus, class: Enzyme, accessions: P21836, gene: Ache, swissprot: ACES_MOUSE Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor A quaternary ammonium compound that is an inhibitor of cholinesterase activity with actions similar to those of NEOSTIGMINE, but of longer duration. Ambenonium is given by mouth in the treatment of myasthenia gravis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1112) Cholinesterase Inhibitor (Code: N0000175723) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) 1956-05-01 FDA
Click to view nafiverine
Click to view mezlocillin Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) Serum albumin (Organism: Homo sapiens, class: Secreted, accessions: P02768, gene: ALB, swissprot: ALBU_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Arachidonate 5-lipoxygenase (Organism: Homo sapiens, class: Enzyme, accessions: P09917, gene: ALOX5, swissprot: LOX5_HUMAN) Interleukin-8 (Organism: Homo sapiens, class: Cytokine, accessions: P10145, gene: CXCL8, swissprot: IL8_HUMAN) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Interleukin-1 receptor type 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: P14778, gene: IL1R1, swissprot: IL1R1_HUMAN) Aldose reductase (Organism: Homo sapiens, class: Enzyme, accessions: P15121, gene: AKR1B1, swissprot: ALDR_HUMAN) Cannabinoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P21554, gene: CNR1, swissprot: CNR1_HUMAN) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) Thromboxane-A synthase (Organism: Homo sapiens, class: Enzyme, accessions: P24557, gene: TBXAS1, swissprot: THAS_HUMAN) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) Cannabinoid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: P34972, gene: CNR2, swissprot: CNR2_HUMAN) Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) Prostaglandin E2 receptor EP4 subtype (Organism: Homo sapiens, class: GPCR, accessions: P35408, gene: PTGER4, swissprot: PE2R4_HUMAN) Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) Prostaglandin-H2 D-isomerase (Organism: Homo sapiens, class: Enzyme, accessions: P41222, gene: PTGDS, swissprot: PTGDS_HUMAN) Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN) Prostaglandin E2 receptor EP2 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43116, gene: PTGER2, swissprot: PE2R2_HUMAN) Prostaglandin D2 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q13258, gene: PTGDR, swissprot: PD2R_HUMAN) Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HCR9, gene: PDE11A, swissprot: PDE11_HUMAN) Prostaglandin D2 receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5Y4, gene: PTGDR2, swissprot: PD2R2_HUMAN) Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor Semisynthetic ampicillin-derived acylureido penicillin. It has been proposed for infections with certain anaerobes and may be useful in inner ear, bile, and CNS infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1981-09-21 FDA
Click to view amenamevir Amenamevir is an anti-herpes virus agent for the treatment of herpes zoster (shingles) with a novel mechanism of action. Amenamevir has been observed to inhibit the proliferation of the varicella-zoster virus by inhibiting the activity of the helicase-primase complex, which is essential for viral DNA replication. 2016-07-03 PMDA
Click to view netarsudil Rho-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: O75116, gene: ROCK2, swissprot: ROCK2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208254lbl.pdf) Netarsudil is a rho kinase inhibitor, which is believed to reduce IOP by increasing the outflow of aqueous humor through the trabecular meshwork route. Rho Kinase Inhibitor (Code: N0000193788) Rho Kinase Inhibitors (Code: N0000193789) 2017-12-18 FDA
Click to view benzalkonium Benzalkonium is a type of cationic surfactant. It is an organic salt called a quaternary ammonium compound. It is used topically in medicaments, deodorants, mouthwashes, as a surgical antiseptic, and as a as preservative and emulsifier in drugs and cosmetics. FDA
Click to view romidepsin Histone deacetylase (Organism: Homo sapiens, class: Enzyme, accessions: O15379|P56524|Q13547|Q8WUI4|Q92769|Q969S8|Q96DB2|Q9BY41|Q9UBN7|Q9UKV0|Q9UQL6, gene: HDAC1|HDAC10|HDAC11|HDAC2|HDAC3|HDAC4|HDAC5|HDAC6|HDAC7|HDAC8|HDAC9, swissprot: HDA10_HUMAN|HDA11_HUMAN|HDAC1_HUMAN|HDAC2_HUMAN|HDAC3_HUMAN|HDAC4_HUMAN|HDAC5_HUMAN|HDAC6_HUMAN|HDAC7_HUMAN|HDAC8_HUMAN|HDAC9_HUMAN) inhibitor (Source: ) Histone deacetylase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P56524, gene: HDAC4, swissprot: HDAC4_HUMAN) Histone deacetylase 7 (Organism: Homo sapiens, class: Enzyme, accessions: Q8WUI4, gene: HDAC7, swissprot: HDAC7_HUMAN) inhibitor (Source: ) Histone deacetylase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBN7, gene: HDAC6, swissprot: HDAC6_HUMAN) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) Histone deacetylase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UKV0, gene: HDAC9, swissprot: HDAC9_HUMAN) inhibitor (Source: ) Histone deacetylase 5 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UQL6, gene: HDAC5, swissprot: HDAC5_HUMAN) inhibitor (Source: ) Histone deacetylase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BY41, gene: HDAC8, swissprot: HDAC8_HUMAN) inhibitor (Source: ) Histone deacetylase 6 (Organism: Mus musculus, class: Unclassified, accessions: Q9Z2V5, gene: Hdac6, swissprot: HDAC6_MOUSE Histone deacetylase 3/NCoR1 (Organism: Homo sapiens, class: Transcription factor, accessions: O15379|O75376, gene: HDAC3|NCOR1, swissprot: HDAC3_HUMAN|NCOR1_HUMAN Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) (Organism: Homo sapiens, class: Transcription factor, accessions: O15379|Q9Y618, gene: HDAC3|NCOR2, swissprot: HDAC3_HUMAN|NCOR2_HUMAN a bicyclic depsipeptide and a potent histone deacetylase inhibitor from Chromobacterium violaceum Histone Deacetylase Inhibitor (Code: N0000175588) Histone Deacetylase Inhibitors (Code: N0000175071) Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) antineoplastic agent (Code: CHEBI:35610) 2009-11-05 FDA
Click to view cefonicid Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) Matrix metalloproteinase-9 (Organism: Homo sapiens, class: Enzyme, accessions: P14780, gene: MMP9, swissprot: MMP9_HUMAN) Somatostatin receptor type 4 (Organism: Homo sapiens, class: GPCR, accessions: P31391, gene: SSTR4, swissprot: SSR4_HUMAN) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor A second-generation cephalosporin administered intravenously or intramuscularly. Its bactericidal action results from inhibition of cell wall synthesis. It is used for urinary tract infections, lower respiratory tract infections, and soft tissue and bone infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) FDA
Click to view pantethine nutraceutical (Code: CHEBI:50733) FDA
Click to view doxorubicin DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) intercalation (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050778s024s025lbl.pdf) DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050778s024s025lbl.pdf) Carbonyl reductase [NADPH] 1 (Organism: Homo sapiens, class: Enzyme, accessions: P16152, gene: CBR1, swissprot: CBR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18635746) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8258200) Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18635746) Aldo-keto reductase family 1 member C4 (Organism: Homo sapiens, class: Enzyme, accessions: P17516, gene: AKR1C4, swissprot: AK1C4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18635746) Aldo-keto reductase family 1 member B10 (Organism: Homo sapiens, class: Enzyme, accessions: O60218, gene: AKR1B10, swissprot: AK1BA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18635746) Aldo-keto reductase family 1 member A1 (Organism: Homo sapiens, class: Enzyme, accessions: P14550, gene: AKR1A1, swissprot: AK1A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18635746) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19631272) Multidrug resistance-associated protein 6 (Organism: Homo sapiens, class: Transporter, accessions: O95255, gene: ABCC6, swissprot: MRP6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12414644) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/11437380) RalA-binding protein 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q15311, gene: RALBP1, swissprot: RBP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17273774) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11302935) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) DNA topoisomerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P11387, gene: TOP1, swissprot: TOP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10.1021/jm1005447) Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q7ZJM1, gene: pol, swissprot: Q7ZJM1_9HIV1) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10841789) CDGSH iron-sulfur domain-containing protein 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q9NZ45, gene: CISD1, swissprot: CISD1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27687671) Aurora kinase A (Organism: Homo sapiens, class: Kinase, accessions: O14965, gene: AURKA, swissprot: AURKA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21664013) DNA polymerase I, thermostable (Organism: Thermus aquaticus, class: Enzyme, accessions: P19821, gene: polA, swissprot: DPO1_THEAQ) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9703471) Doxorubicin is a cytotoxic anthracycline antibiotic isolated from cultures of Streptomyces peucetius var. caesius. Doxorubicin has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Doxorubicin forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes. Epirubicin is the 4'-epi-isomer of doxorubicin. Epirubicin has been reported to be less cardiotoxic than doxorubicin and to have comparable antitumor activity. Doxorubicin is used for the treatment of ovarian cancer (after failure of platinum-based chemotherapy), AIDS-related Kaposi’s Sarcoma (after failure of prior systemic chemotherapy or intolerance to such therapy) and multiple myeloma (in combination with bortezomib). Epirubicin is used as a component of adjuvant therapy in patients with evidence of axillary node tumor involvement following resection of primary breast cancer. Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) Anthracycline Topoisomerase Inhibitor (Code: N0000175414) Anthracyclines (Code: N0000007530) doxorubicin: 1974-08-07 FDA epirubicin: 1999-09-15 FDA DM2
DM6
Click to view prednisolone sulfobenzoate
Click to view meproscillarin Sodium/potassium-transporting ATPase subunit alpha-1 (Organism: Homo sapiens, class: Transporter, accessions: P05023, gene: ATP1A1, swissprot: AT1A1_HUMAN) semi-synthetic derivative of proscillaridin of Scilla (Liliaceae); structure in Negwer, 5th ed, #6625; RN given refers to (3beta)-isomer
Click to view octotiamine
Click to view everolimus Peptidyl-prolyl cis-trans isomerase FKBP1A (Organism: Homo sapiens, class: Enzyme, accessions: P62942, gene: FKBP1A, swissprot: FKB1A_HUMAN) inhibitor Serine/threonine-protein kinase mTOR (Organism: Homo sapiens, class: Kinase, accessions: P42345, gene: MTOR, swissprot: MTOR_HUMAN) inhibitor (Source: ) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) A derivative of sirolimus and an inhibitor of TOR SERINE-THREONINE KINASES. It is used to prevent GRAFT REJECTION in heart and kidney transplant patients by blocking cell proliferation signals. It is also an ANTINEOPLASTIC AGENT. Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) P-Glycoprotein Inhibitors (Code: N0000185503) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) mTOR Inhibitor Immunosuppressant (Code: N0000175625) mTOR Inhibitors (Code: N0000175624) Decreased Immunologic Activity (Code: N0000175550) Antineoplastic Agents (Code: D000970) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) immunosuppressive agent (Code: CHEBI:35705) antineoplastic agent (Code: CHEBI:35610) 2009-03-30 FDA
Click to view ceftazidime Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10636865) Ceftazidime is a semisynthetic, broad-spectrum, beta-lactam antibiotic derived from cephaloridine. Ceftazidime acts by inhibition of bacterial cell wall synthesis. Ceftazidime has activity in the presence of some beta-lactamases, both penicillinases and cephalosporinases. Resistance to ceftazidime is primarily through hydrolysis by beta-lactamase, alteration of penicillin-binding proteins (PBPs), and decreased permeability. Ceftazidime has been shown to be active against Citrobacter species, Enterobacter species, Escherichia coli, Klebsiella species, Haemophilus influenzae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Serratia species, Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus agalactiae, Bacteroides species (many isolates of Bacteroides species are resistant). Ceftazidime is used for the treatment od Lower Respiratory Tract Infections (including pneumonia), Skin and Skin-Structure Infections, Urinary Tract Infections, Septicemia, Bone and Joint Infections, Gynecologic Infections, Intra-abdominal Infections (including peritonitis) and Central Nervous System Infections (including meningitis). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) drug allergen (Code: CHEBI:88188) 1985-07-19 FDA
Click to view cefazedone Cefazedone is a semisynthetic first-generation cephalosporin with activity against Gram-positive and Gram-negative bacteria. Cefazedone binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Cefazedone was used for the treatment of urinary tract infections and gynecological infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047)
Click to view peruvoside
Click to view fluphenazine enanthate Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1967-03-15 FDA
Click to view octenidine Octenidine is a member of cation-active compounds, and as a result of its two cationic centres possesses marked surface-active properties. It reacts with cell wall and membrane components of themicrobial cell and thus leads to disruption of cell function. Octenidine is used as antiseptic prior to medical procedures. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 1988-03-01 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view bufeniode
Click to view alpha-Ergocryptine Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT a component of the ergotoxine complex; it is the main ergot alkaloid of Japanese & South American wid grasses; minor descriptor (76-86); on-line & INDEX MEDICUS search ERGOLINES (76-86); RN given refers to ((5'alpha)-isomer) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377)
Click to view bosentan Endothelin-1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25101, gene: EDNRA, swissprot: EDNRA_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021290s039,209279s005lbl.pdf) Endothelin B receptor (Organism: Homo sapiens, class: GPCR, accessions: P24530, gene: EDNRB, swissprot: EDNRB_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021290s039,209279s005lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021290s039,209279s005lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021290s039,209279s005lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021290s039,209279s005lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021290s039,209279s005lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) Bosentan is an endothelin receptor antagonist that belongs to a class of highly substituted pyrimidine derivatives, with no chiral centers. Bosentan is a specific and competitive antagonist at endothelin receptor types ETA and ETB. Bosentan has a slightly higher affinity for ETA receptors than for ETB receptors. The clinical impact of dual endothelin blockage is unknown. Bosentan is indicated for the treatment of pulmonary arterial hypertension. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Endothelin Receptor Antagonists (Code: D065128) antihypertensive agent (Code: CHEBI:35674) endothelin receptor antagonist (Code: CHEBI:51451) Cytochrome P450 3A Inducers (Code: N0000190118) Cytochrome P450 2C9 Inducers (Code: N0000185507) 2001-11-20 FDA K86
Click to view aliskiren Renin (Organism: Homo sapiens, class: Enzyme, accessions: P00797, gene: REN, swissprot: RENI_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021985s034lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021985s034lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021985s034lbl.pdf) Protease (Organism: Human immunodeficiency virus 1 , class: Polyprotein, accessions: Q7SSI0, gene: pol, swissprot: Q7SSI0_9HIV1) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22621689) Aliskiren is a direct renin inhibitor, decreasing plasma renin activity (PRA) and inhibiting the conversion of angiotensinogen to Ang I. Aliskiren is indicated for the treatment of hypertension in adults and children 6 years of age and older, to lower blood pressure. Renin Inhibitor (Code: N0000175900) Renin Inhibitors (Code: N0000175899) antihypertensive agent (Code: CHEBI:35674) 2007-03-05 FDA C41
Click to view arbekacin Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 84G
Click to view ceftriaxone Penicillin-binding protein 1A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918, gene: mrcA, swissprot: PBPA_ECOLI) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00048733.PDF) Peptidoglycan D,D-transpeptidase FtsI (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD68, gene: ftsI, swissprot: FTSI_ECOLI) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00048733.PDF) D-alanyl-D-alanine carboxypeptidase DacB (Organism: Haemophilus influenzae, class: Enzyme, accessions: P45161, gene: dacB, swissprot: DACB_HAEIN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00048733.PDF) D-alanyl-D-alanine carboxypeptidase DacA (Organism: Haemophilus influenzae, class: Enzyme, accessions: P44466, gene: dacA, swissprot: DACA_HAEIN) inhibitor (Source: https://pdf.hres.ca/dpd_pm/00048733.PDF) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23033255) D-amino-acid oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P14920, gene: DAO, swissprot: OXDA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26309148) Ceftriaxone is a beta-lactam, third-generation cephalosporin antibiotic with bactericidal activity. Ceftriaxone acts by inhibition of bacterial cell wall synthesis. Ceftriaxone has activity in the presence of some beta-lactamases, both penicillinases and cephalosporinases. Ceftriaxone has been shown to be active against Acinetobacter calcoaceticus, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis, Morganella morganii, Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Pseudomonas aeruginosa, Serratia marcescens, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, Viridans group streptococci, Bacteroides fragilis, Clostridium species, Peptostreptococcus species. Ceftriaxone is used for the treatment of Lower Respiratory Tract Infections, Skin and Skin Structure Infections, Urinary Tract Infections, Gynecological Infections, Septicemia, Bone and Joint Infections, Intra-abdominal Infections, Meningitis and for Prophylaxis of postoperative infections. Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) drug allergen (Code: CHEBI:88188) 1984-12-21 FDA 9F2
NZV
Click to view dronedarone Potassium channel subfamily K member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O95069, gene: KCNK2, swissprot: KCNK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22790794) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17896959) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 (Organism: Homo sapiens, class: Ion channel, accessions: O60741, gene: HCN1, swissprot: HCN1_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/23647933) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UL51, gene: HCN2, swissprot: HCN2_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/23647933) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9P1Z3, gene: HCN3, swissprot: HCN3_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/23647933) Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q9Y3Q4, gene: HCN4, swissprot: HCN4_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/23647933) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022425s025lbl.pdf) Dronedarone has antiarrhythmic properties belonging to all four Vaughan-Williams classes, but the contribution of each of these activities to the clinical effect is unknown. Antiarrhythmic (Code: N0000175426) anti-arrhythmia drug (Code: CHEBI:38070) 2009-07-01 FDA
Click to view demecarium Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor major descriptor (65-85); on-line search AMMONIUM COMPOUNDS (66-85); Index Medicus search DEMECARIUM BROMIDE (65-85) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) 1959-08-05 FDA
Click to view perflunafene Perflunafene (perfluorodecalin) is a fluorocarbon that is decalin in which every hydrogen is replaced by fluorine. Capable of dissolving large quantities of oxygen, it was used in coronary angioplasty in combination with perfluamine as "artificial blood". This combination was withdrawn for multiple reasons: efficacy was marginal, the product was technically difficult to use, and new developments in coronary angioplasty (the indication for which it was approved) made its use obsolete. Intra-ocular injection of perflunafene is used to provide temporary tamponade in ophthalmic procedures such as retinal re-attachment. solvent (Code: CHEBI:46787) blood substitute (Code: CHEBI:38849) 1990 FDA
Click to view acetrizoic acid Acetrizoic acid is an iodinated radiographic contrast medium used as acetrizoate sodium in hysterosalpingography. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) FDA
Click to view voacamine
Click to view ertugliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209803s000lbl.pdf) Sodium/glucose cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P13866, gene: SLC5A1, swissprot: SC5A1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21449606) Low affinity sodium-glucose cotransporter (Organism: Homo sapiens, class: Transporter, accessions: Q9NY91, gene: SLC5A4, swissprot: SC5A4_HUMAN Sodium/glucose cotransporter 2 (Organism: Rattus norvegicus, class: Transporter, accessions: P53792, gene: Slc5a2, swissprot: SC5A2_RAT SGLT2 is the predominant transporter responsible for reabsorption of glucose from the glomerular filtrate back into the circulation. Ertugliflozin is an inhibitor of SGLT2. By inhibiting SGLT2, ertugliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion. 2017-12-19 FDA
Click to view cefpodoxime proxetil Cefpodoxime proxetil is an orally administered, extended spectrum, semisynthetic antibiotic of the cephalosporin class. Cefpodoxime proxetil is a prodrug that is absorbed from the gastrointestinal tract and de-esterified to its active metabolite, cefpodoxime. (See: cefpodoxime) Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1992-08-07 FDA
Click to view vecuronium Acetylcholine receptor (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN) antagonist (Source: https://pdf.hres.ca/dpd_pm/00020615.PDF) Vecuronium is a neuromuscular blocking agent. Vecuronium operates by competing for the cholinoceptors at the motor end plate thereby exerting its muscle-relaxing properties which are used adjunctively to general anesthesia. Vecuronium is indicated as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Neuromuscular Nondepolarizing Blockade (Code: N0000175732) Nondepolarizing Neuromuscular Blocker (Code: N0000175720) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) nicotinic antagonist (Code: CHEBI:48878) neuromuscular agent (Code: CHEBI:51372) muscle relaxant (Code: CHEBI:51371) 1984-04-30 FDA
Click to view phenobutiodil Phenobutiodil is a contrast medium with properties and uses similar to those of iopanoic acid. Phenobutiodil was used in cholecystography and cholangiography for the visualization of the gall bladder. It is no longer available.
Click to view alatrofloxacin Alatrofloxacin is a fluoroquinolone antibiotic. Alatrofloxacin is a prodrug, which is rapidly hydrolysed in serum to trovafloxacin. It was withdrawn from market due to the occurence of severe, serious and unpredictable hepatic injuries. (See: trovafloxacin) Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1997-12-18 FDA
Click to view deferoxamine iron (Organism: None, class: Inorganic material, accessions: None, gene: None, swissprot: None) chelating agent (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/016267s050lbl.pdf) Deferoxamine is a natural product isolated from Streptomyces pilosus. It forms iron complexes and is used as a chelating agent, particularly in the mesylate form. It readily chelates iron from ferritin and hemosiderin but not readily from transferrin; it does not combine with the iron from cytochromes and hemoglobin. Deferoxamine is indicated for the treatment of acute iron intoxication and of chronic iron overload due to transfusion-dependent anemias. Iron Chelating Activity (Code: N0000000144) Iron Chelator (Code: N0000175522) Chelating Agents (Code: D002614) Iron Chelating Agents (Code: D007502) Sequestering Agents (Code: D064449) Siderophores (Code: D017262) antidote (Code: CHEBI:50247) 1968-04-01 FDA DEFER
Click to view olmesartan medoxomil Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23571415) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23571415) Olmesartan medoxomil, a prodrug, is hydrolyzed to olmesartan. Olmesartan blocks the vasoconstrictor effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in vascular smooth muscle. Angiotensin 2 Receptor Antagonists (Code: N0000000070) Angiotensin 2 Receptor Blocker (Code: N0000175561) Angiotensin II Type 1 Receptor Blockers (Code: D047228) Angiotensin Receptor Antagonists (Code: D057911) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) 2002-04-25 FDA
Click to view lividomycin LIV
Click to view atorvastatin 3-hydroxy-3-methylglutaryl-coenzyme A reductase (Organism: Homo sapiens, class: Enzyme, accessions: P04035, gene: HMGCR, swissprot: HMDH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020702s073lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020702s073lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020702s073lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020702s073lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020702s073lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15998357) Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18068977) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11523064) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11523064) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11523064) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12433810) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/12433810) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11474784) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14531725) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20797388) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19940267) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19940267) Multidrug resistance-associated protein 4 (Organism: Homo sapiens, class: Transporter, accessions: O15439, gene: ABCC4, swissprot: MRP4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19940267) Multidrug resistance-associated protein 5 (Organism: Homo sapiens, class: Transporter, accessions: O15440, gene: ABCC5, swissprot: MRP5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19940267) Histone deacetylase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBN7, gene: HDAC6, swissprot: HDAC6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23570542) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23570542) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23570542) Sterol regulatory element-binding protein 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q12772, gene: SREBF2, swissprot: SRBP2_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/26784936) Atorvastatin is a synthetic lipid-lowering agent. Atorvastatin is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis. v indicatedas an adjunct therapy to diet to reduce the risk of miocardial infarction, stroke, revascularization procedures, and angina in adult patients with/without CHD or with type 2 diabetes without CHD, but with multiple risk factor, to reduce elevated total-C, LDL-C, apo B, and TG levels and increase HDLC in adult patients with primary hyperlipidemia (heterozygous familial and nonfamilial), mixed dyslipidemia, primary dysbetalipoproteinemia or homozygous familial hypercholesterolemia (HoFH) and to reduce elevated total-C, LDL-C, and apo B levels in pediatric patients, 10 years to 17 years of age, with heterozygous familial hypercholesterolemia (HeFH) after failing an adequate trial of diet therapy. HMG-CoA Reductase Inhibitor (Code: N0000175589) Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Enzyme Inhibitors (Code: D004791) Hydroxymethylglutaryl-CoA Reductase Inhibitors (Code: D019161) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) 1996-12-17 FDA 117
Click to view halopredone acetate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: http://www.kegg.jp/entry/D01743)
Click to view sulfamazone antibacterial drug (Code: CHEBI:36047) antipyretic (Code: CHEBI:35493)
Click to view protoporphyrin Cytoplasmic zinc-finger protein (Organism: Caenorhabditis elegans, class: Unclassified, accessions: G5EF15, gene: pos-1, swissprot: G5EF15_CAEEL Zinc finger protein mex-5 (Organism: Caenorhabditis elegans, class: Cytosolic other, accessions: Q9XUB2, gene: mex-5, swissprot: MEX5_CAEEL Dermatologic Agents (Code: D003879) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) photosensitizing agent (Code: CHEBI:47868) PP9
Click to view ecamsule an organic chemical agent capable of absorbing light throughout the entire UVA spectrum 2006-07-21 FDA
Click to view fosinopril Fosinoprilat: Angiotensin-converting enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P12821, gene: ACE, swissprot: ACE_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2003/19915se5-037_monopril_lbl.pdf) Fosinopril: Solute carrier family 15 member 1 (Organism: Homo sapiens, class: Transporter, accessions: P46059, gene: SLC15A1, swissprot: S15A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951) Solute carrier family 15 member 2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63424, gene: Slc15a2, swissprot: S15A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18713951 Fosinopril is a phosphinic acid-containing ester prodrug. It is hydrolyzed by esterases to the pharmacologically active form, fosinoprilat, a specific competitive inhibitor of angiotensin converting enzyme (ACE). Fosinoprilat specifically and competitively inhibits angiotensin-converting enzyme thereby decreasing the formation of the potent vasoconstrictor angiotensin II, resulting in diminished vasopressor activity. In addition, angiotensin II-mediated aldosterone secretion by adrenal cortex is decreased, which results in a decrease of sodium retention and an increase in water outflow. Fosinopril may be used to treat mild to moderate hypertension, as an adjunct in the treatment of congestive heart failure, and to slow the rate of progression of renal disease in hypertensive individuals with diabetes mellitus and microalbuminuria or overt nephropathy. Angiotensin Converting Enzyme Inhibitor (Code: N0000175562) Angiotensin-Converting Enzyme Inhibitors (Code: D000806) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor (Code: CHEBI:35457) prodrug (Code: CHEBI:50266) antihypertensive agent (Code: CHEBI:35674) 1991-05-16 FDA Fosin
Click to view dihydroergocornine A 9,10alpha-dihydro derivative of ERGOTAMINE that contains isopropyl sidechains at the 2' and 5' positions of the molecule. Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) FDA
Click to view deserpidine Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) inhibitor minor descriptor (66-84); on-line search RESERPINE/AA (75-84), RESERPINE (66-74); Index Medicus search RESERPINE/AA (75-84), YOHIMBANS (69-74), RESERPINE (66-68); RN given refers to (3beta,16beta,17alpha,18beta,20alpha)-isomer Catecholamine-depleting Sympatholytic (Code: N0000175640) Decreased Sympathetic Activity (Code: N0000175650) 1957-04-19 FDA
Click to view enocitabine Anti-Infective Agents (Code: D000890) Antineoplastic Agents (Code: D000970) Antiviral Agents (Code: D000998)
Click to view desoxymycin
Click to view cefcapene pivoxil Cefcapene pivoxil is the pivalate ester prodrug form of cefcapene, a semi-synthetic third-generation cephalosporin with antibacterial activity. After oral administration of cefcapene pivoxil, the ester bond is cleaved, releasing active cefcapene. It is used for the treatment of skin and skin structure infections, respiratory tract infections, urinary tract infections, cholecystitis, cholangitis, otitis externa and media. 1997-06-01 PMDA
Click to view nelfinavir Protease (Organism: Human immunodeficiency virus 1 , class: Polyprotein, accessions: Q7SSI0, gene: pol, swissprot: Q7SSI0_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020778s041,020779s062,021503s024lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020778s041,020779s062,021503s024lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020778s041,020779s062,021503s024lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020778s041,020779s062,021503s024lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17101742) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9660842) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9660842) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12699389) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10681378) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15007102) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12699389) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16118329) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16118329) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16118329) Nelfinavir is an inhibitor of the human immunodeficiency virus type 1 (HIV-1) protease. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children. Nelfinavir was found to be active against several laboratory strains and clinical isolates of HIV-1, and the HIV-2 strain ROD. In HBV or HCV coinfected patients, hepatic injury during antiretroviral therapy that includes nelfinavir may be a result of exacerbation of the underlying chronic hepatitis B or C, rather than a direct effect of the medication. Protease Inhibitor (Code: N0000175889) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) HIV Protease Inhibitors (Code: D017320) Protease Inhibitors (Code: D011480) antineoplastic agent (Code: CHEBI:35610) Cytochrome P450 3A Inhibitors (Code: N0000190114) 1997-03-14 FDA 1UN
Click to view brovanexine
Click to view zotarolimus Peptidyl-prolyl cis-trans isomerase FKBP1A (Organism: Homo sapiens, class: Enzyme, accessions: P62942, gene: FKBP1A, swissprot: FKB1A_HUMAN) inhibitor (Source: ) synthetic analog of rapamycin
Click to view cefuroxime pivoxetil Cefuroxime pivoxetil is an ester prodrug of cefuroxime, a semisynthetic, broad-spectrum, beta-lactamase-resistant, second-generation cephalosporin with antibacterial activity. (See: cefuroxime)
Click to view formocortal
Click to view isepamicin Macrolide 2'-phosphotransferase II; Macrolide 2'-phosphotransferase II protein MphB; Macrolide 2-phosphotransferase, mph(B) (Organism: Escherichia coli, class: Enzyme, accessions: O32553, gene: mphB, swissprot: O32553_ECOLX) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1988-01-01 YEAR INTRODUCED
Click to view iodol Iodol (tetra-iodo-pyrrol) obtained by the iodination of alkaline solution of pyrrole. Its antiseptic action is similar to iodoform.
Click to view diathymosulfone
Click to view doxacurium Acetylcholine receptor (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN) antagonist Neuronal acetylcholine receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: Q15822, gene: CHRNA2, swissprot: ACHA2_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) according to Unlisted Drugs, BW-A938U is a bis-benzylisoquinolinium diester and a highly potent neuromuscular blocker Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Peripheral Nervous System Agents (Code: D018373) muscle relaxant (Code: CHEBI:51371) 1991-03-07 FDA
Click to view carbenoxolone Corticosteroid 11-beta-dehydrogenase isozyme 1 (Organism: Homo sapiens, class: Enzyme, accessions: P28845, gene: HSD11B1, swissprot: DHI1_HUMAN) inhibitor Corticosteroid 11-beta-dehydrogenase isozyme 2 (Organism: Mus musculus, class: Enzyme, accessions: P51661, gene: Hsd11b2, swissprot: DHI2_MOUSE Corticosteroid 11-beta-dehydrogenase isozyme 1 (Organism: Mus musculus, class: Enzyme, accessions: P50172, gene: Hsd11b1, swissprot: DHI1_MOUSE An agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise the drug is low in toxicity. Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) CBO
Click to view iopanoic acid Radiopaque medium used as diagnostic aid. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 1951-07-16 FDA
Click to view iophenoic acid Iophenoic acid is an iodinated marker. It was used as a radiocontrast agent. It was withdrawn from the clinical use because of its high-affinity binding to human serum albumin. IO3
Click to view myrophine prodrug (Code: CHEBI:50266) opioid analgesic (Code: CHEBI:35482)
Click to view clodantoin Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18171730) Clodantoin (chlordantoin) is a topical imidazole antifugal agent with activity against Candida albicans.
Click to view cytarabine ocfosfate 1997-05-06 PMDA
Click to view cefotetan Penicillin-binding protein 1A (Organism: Clostridium perfringens (strain 13 / Type A), class: Enzyme, accessions: Q8XJ01, gene: pbpA, swissprot: PBPA_CLOPE) Interstitial collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P03956, gene: MMP1, swissprot: MMP1_HUMAN) 72 kDa type IV collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P08253, gene: MMP2, swissprot: MMP2_HUMAN) Matrix metalloproteinase-9 (Organism: Homo sapiens, class: Enzyme, accessions: P14780, gene: MMP9, swissprot: MMP9_HUMAN) Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative microorganisms. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) 1985-12-27 FDA
Click to view zafirlukast Cysteinyl leukotriene receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y271, gene: CYSLTR1, swissprot: CLTR1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020547s033lbl.pdf) Cysteinyl leukotriene receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q9NS75, gene: CYSLTR2, swissprot: CLTR2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10851239) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22614107) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) a leukotriene receptor antagonist (LTRA), with anti-asthmatic and potential capsular contracture-preventing activities. Upon administration, zafirlukast selectively and competitively binds to and blocks the cysteinyl leukotriene 1 receptor (CYSLTR1), thereby preventing the potent pro-inflammatory mediators leukotriene C4, D4 and E4 from binding. This prevents leukotriene-mediated actions, including enhanced migration of eosinophils and neutrophils, increased adhesion of leukocytes, increased monocyte and neutrophil aggregation, increased airway edema, inflammation, capillary permeability and bronchoconstriction Leukotriene Receptor Antagonist (Code: N0000175777) Leukotriene Receptor Antagonists (Code: N0000000083) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) Anti-Asthmatic Agents (Code: D018927) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Leukotriene Antagonists (Code: D020024) Respiratory System Agents (Code: D019141) leukotriene antagonist (Code: CHEBI:49159) anti-asthmatic agent (Code: CHEBI:65023) 1996-09-26 FDA
Click to view oleandrin
Click to view difebarbamate
Click to view clofenotane Clofenotane (chlorophenothane, dichlorodiphenyltrichloroethane, DDT) is a chlorinated hydrocarbon that is soluble in most organic solvents, fat and oils and tends to accumulate in ecosystems. It was used in the second half of World War II to control malaria and typhus among civilians and troops. DDT was once widely used as a pesticide to control insects in agriculture, but its use is now limited. Exposure to DDT mainly affects the nervous system resulting in tremors, dizziness, nausea, incoordination, convulsions and seizures. This substance is reasonably anticipated to be a human carcinogen based on evidence of carcinogenicity in experimental animals. endocrine disruptor (Code: CHEBI:138015) bridged diphenyl acaricide (Code: CHEBI:39412) 6WT
Click to view prednisolone farnesylate
Click to view lapatinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022059s024lbl.pdf) Receptor tyrosine-protein kinase erbB-2 (Organism: Homo sapiens, class: Kinase, accessions: P04626, gene: ERBB2, swissprot: ERBB2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022059s024lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022059s024lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22511346) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022059s024lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022059s024lbl.pdf) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21080629) Insulin receptor (Organism: Homo sapiens, class: Kinase, accessions: P06213, gene: INSR, swissprot: INSR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21080629) Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21080629) Cyclin-dependent kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P24941, gene: CDK2, swissprot: CDK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21080629) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Lapatinib is a 4-anilinoquinazoline kinase inhibitor of the intracellular tyrosine kinase domains of both Epidermal Growth Factor Receptor and of Human Epidermal Receptor Type 2 receptors. Lapatinib inhibits ErbB-driven tumor cell growth in vitro and in various animal models. The growth inhibitory effects of lapatinib were evaluated in trastuzumab-conditioned cell lines. Lapatinib retained significant activity against breast cancer cell lines selected for long-term growth in trastuzumab-containing medium in vitro. Kinase Inhibitor (Code: N0000175605) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2007-03-13 FDA FMM
Click to view streptomycin Streptomycin is an aminoglycoside antibiotic derived from Streptomyces griseus with antibacterial activity. Streptomycin irreversibly binds to the 16S rRNA and S12 protein within the bacterial 30S ribosomal subunit. As a result, this agent interferes with the assembly of initiation complex between mRNA and the bacterial ribosome, thereby inhibiting the initiation of protein synthesis. In addition, streptomycin induces misreading of the mRNA template and causes translational frameshift, thereby results in premature termination. Streptomycin is indicated for the treatment of infections caused by Mycobacterium tuberculosis and non-tuberculosis infections due to Pasteurella pestis, Francisella tularensis, Brucella, Calymmatobacterium granulomatis, H. ducreyi, H. influenzae, K. pneumoniae, E.coli, Proteus, A. aerogenes, and Enterococcus faecalis in urinary tract infections, Streptococcus viridans, Enterococcus faecalis. Aminoglycoside Antibacterial (Code: N0000175477) Aminoglycosides (Code: N0000007853) Antimycobacterial (Code: N0000175483) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) 1946-02-18 FDA SRY
Click to view ergotamine Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) agonist/antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/9000s22s23lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) agonist/antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/9000s22s23lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) agonist/antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/9000s22s23lbl.pdf) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) agonist/antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/9000s22s23lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) agonist/antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/9000s22s23lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) agonist/antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/9000s22s23lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2002/9000s22s23lbl.pdf) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) agonist/antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8380639) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) agonist/antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8380639) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) agonist/antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9284367) Ergotamine is a naturally occurring ergot alkaloid with vasoconstrictor and analgesic property. Ergotamine is a partial agonist at various tryptaminergic receptors (including the serotonin receptor [5-HT2]) and at various ?-adrenergic receptors in blood vessels and various smooth muscles. Ergotamine selectively binds and activates serotonin (5-HT) 1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, thereby resulting in vasoconstriction and reducing the blood flow in cerebral arteries that may lead to relieve of vascular headaches. This agent also selectively binds to alpha-adrenergic receptors, thereby stimulating vascular smooth muscle and causing vasoconstriction in both arteries and veins, which also contributes to the relief of headaches. Furthermore, the activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release. Ergotamine is used in the abortion or prevention of vascular headaches, such as migraine, migraine variant, cluster headache, and histaminic cephalalgia. Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic alpha-1 Receptor Agonists (Code: D058646) Adrenergic alpha-Agonists (Code: D000316) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Neurotransmitter Agents (Code: D018377) Oxytocics (Code: D010120) Peripheral Nervous System Agents (Code: D018373) Reproductive Control Agents (Code: D012102) Sensory System Agents (Code: D018689) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Vasoconstrictor Agents (Code: D014662) non-narcotic analgesic (Code: CHEBI:35481) vasoconstrictor agent (Code: CHEBI:50514) serotonergic agonist (Code: CHEBI:35941) alpha-adrenergic agonist (Code: CHEBI:35569) Ergotamine Derivative (Code: N0000175766) Ergotamines (Code: N0000007621) 1948-11-26 FDA ERM
Click to view azelnidipine Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: )
Click to view dihydrostreptomycin A semi-synthetic aminoglycoside antibiotic that is used in the treatment of TUBERCULOSIS. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view dihydroergotamine 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: ) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 1F (Organism: Homo sapiens, class: GPCR, accessions: P30939, gene: HTR1F, swissprot: 5HT1F_HUMAN) agonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: ) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) agonist (Source: ) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) 5-hydroxytryptamine receptor 4 (Organism: Cavia porcellus, class: GPCR, accessions: O70528, gene: HTR4, swissprot: 5HT4R_CAVPO) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P19328|P22086|P22909, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN Gastrin/cholecystokinin type B receptor (Organism: Mus musculus, class: GPCR, accessions: P56481, gene: Cckbr, swissprot: GASR_MOUSE 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT) antagonist (Source: ) Dihydroergotamine is ergotamine in which a single bond replaces the double bond between positions 9 and 10. A semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine. Dihydroergotamine binds with high affinity to 5-HT1D? and 5-HT1D?, 5-HT1A, 5-HT2A, and 5-HT2C receptors, noradrenaline ?2A, ?2B and ?, receptors, and dopamine D2L and D3 receptors. The therapeutic activity of dihydroergotamine in migraine is generally attributed to the agonist effect at 5-HT1D receptors. Two current theories have been proposed to explain the efficacy of 5-HT1D receptor agonists in migraine. Dihydroergotamine is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. Ergotamine Derivative (Code: N0000175766) Ergotamines (Code: N0000007621) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Vasoconstrictor Agents (Code: D014662) serotonergic agonist (Code: CHEBI:35941) non-narcotic analgesic (Code: CHEBI:35481) vasoconstrictor agent (Code: CHEBI:50514) dopamine agonist (Code: CHEBI:51065) sympatholytic agent (Code: CHEBI:66991) 1946-04-12 FDA 2GM
Click to view ouabain Sodium/potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P05023|P50993|P13637|Q13733|P05026|P14415|P54709|P54710, gene: ATP1A1|ATP1A2|ATP1A3|ATP1A4|ATP1B1|ATP1B2|ATP1B3|FXYD2, swissprot: AT1A1_HUMAN|AT1A2_HUMAN|AT1A3_HUMAN|AT1A4_HUMAN|AT1B1_HUMAN|AT1B2_HUMAN|AT1B3_HUMAN|ATNG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10564763) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8938553) Solute carrier organic anion transporter family member 4C1 (Organism: Homo sapiens, class: Transporter, accessions: Q6ZQN7, gene: SLCO4C1, swissprot: SO4C1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14993604) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11159893) Ouabain (uabain) is a cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae. Ouabain inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations. Ouabain is used for the treatment of atrial fibrillation and flutter and heart failure. Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protective Agents (Code: D020011) cardiotonic drug (Code: CHEBI:38147) anti-arrhythmia drug (Code: CHEBI:38070) 1865-01-01 YEAR INTRODUCED OBN
Click to view cefodizime Cefodizime is a third-generation cephalosporin with a broad spectrum of antibacterial activity. Cefodizime targets penicillin-binding proteins (PBPs) 1A/B, 2, and 3 resulting in the eventual death of the bacterial cell. Cefodizime is active against Staphylococcus aureus, Streptococcus pneumoniae, Neisseria gonorrhoeae, Neisseria meningitidis, Branhamella catarrhalis, Escherichia coli, Shigella spp., Salmonella spp., Citrobacter spp., Klebsiella spp., Proteus vulgaris, Proteus mirabilis, Providencia spp., Morganella morganii, Haemophilus influenzae, Corynebacterium spp. Cefodizime is used for the treatment of urinary tract infections, including infections due to Neisseria gonorrhoeae, and respiratory tract infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) Italian Medicines Agency (AIFA)
Click to view dilazep Equilibrative nucleoside transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q99808, gene: SLC29A1, swissprot: S29A1_HUMAN Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Equilibrative nucleoside transporter 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: O54699, gene: Slc29a2, swissprot: S29A2_RAT Coronary vasodilator with some antiarrhythmic activity. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view amikacin Amikacin is a semi-synthetic aminoglycoside antibiotic derived from kanamycin. Amikacin inhibits protein synthesis by binding to the 30S ribosomal subunit to prevent the formation of an initiation complex with messenger RNA. Amikacin is used for short-term treatment of serious infections due to susceptible strains of Gram-negative bacteria, including Pseudomonas species, Escherichia coli, species of indole-positive and indole-negative Proteus, Providencia species, Klebsiella-Enterobacter-Serratia species, and Acinetobacter (Mima-Herellea) species. Amikacin may also be used to treat Mycobacterium avium and Mycobacterium tuberculosis infections. Amikacin was used for the treatment of gram-negative pneumonia. Aminoglycoside Antibacterial (Code: N0000175477) Aminoglycosides (Code: N0000007853) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1981-01-22 FDA AKN
Click to view fosamprenavir Fosamprenavir is a prodrug that is rapidly hydrolyzed to amprenavir by cellular phosphatases in the gut epithelium as it is absorbed. Amprenavir is an inhibitor of HIV-1 protease. (See: amprenavir) Fosamprenavir is indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus (HIV-1) infection, as well as postexposure prophylaxis of HIV infection in individuals who have had occupational or nonoccupational exposure to potentially infectious body fluids of a person known to be infected with HIV when that exposure represents a substantial risk for HIV transmission. Protease Inhibitor (Code: N0000175889) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) HIV Protease Inhibitors (Code: D017320) Protease Inhibitors (Code: D011480) prodrug (Code: CHEBI:50266) 2003-10-20 FDA
Click to view tigecycline Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021821s045lbl.pdf) Tigecycline inhibits protein translation in bacteria by binding to the 30S ribosomal subunit and blocking entry of amino-acyl tRNA molecules into the A site of the ribosome. This prevents incorporation of amino acid residues into elongating peptide chains. Tigecycline has been shown to be active against most of the following microorganisms: Enterococcus faecalis (vancomycin-susceptible isolates), Staphylococcus aureus (methicillin-susceptible and -resistant isolates), Streptococcus agalactiae, Streptococcus anginosus group (includes S. anginosus, S. intermedius, and S. constellatus), Streptococcus pneumoniae (penicillin-susceptible isolates), Streptococcus pyogenes, Citrobacter freundii Enterobacter cloacae Escherichia coli Haemophilus influenzae Klebsiella oxytoca Klebsiella pneumoniae Legionella pneumophila, Anaerobic bacteria, Bacteroides fragilis, Bacteroides thetaiotaomicron, Bacteroides uniformis, Bacteroides vulgatus, Clostridium perfringens and Peptostreptococcus micros. Tetracycline-class Antibacterial (Code: N0000175938) Tetracyclines (Code: N0000007948) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 2005-06-15 FDA T1C
Click to view montelukast Cysteinyl leukotriene receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y271, gene: CYSLTR1, swissprot: CLTR1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020829s070s071,020830s072s073,021409s048s049lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020829s070s071,020830s072s073,021409s048s049lbl.pdf) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19151602) Uracil nucleotide/cysteinyl leukotriene receptor (Organism: Mus musculus, class: Unclassified, accessions: Q6NS65, gene: Gpr17, swissprot: GPR17_MOUSE) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18974869) Montelukast is an orally active compound that binds with high affinity and selectivity to the CysLT1 receptor (in preference to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or beta-adrenergic receptor). Montelukast inhibits physiologic actions of cysteinyl leukotriene LTD4 at the CysLT1 receptor without any agonist activity. Montelukast has a role as an anti-asthmatic drug and an anti-arrhythmia drug. Leukotriene Receptor Antagonist (Code: N0000175777) Leukotriene Receptor Antagonists (Code: N0000000083) Anti-Asthmatic Agents (Code: D018927) Cytochrome P-450 CYP1A2 Inducers (Code: D065694) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Leukotriene Antagonists (Code: D020024) Metabolic Side Effects of Drugs and Substances (Code: D065606) Respiratory System Agents (Code: D019141) anti-arrhythmia drug (Code: CHEBI:38070) anti-asthmatic drug (Code: CHEBI:49167) leukotriene antagonist (Code: CHEBI:49159) 1998-02-20 FDA MTK
Click to view hidrosmin a benzopyrone derivative; water-soluble flavonoid
Click to view irinotecan DNA topoisomerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P11387, gene: TOP1, swissprot: TOP1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020571s050lbl.pdf) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19190342) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15608127) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18479118) Irinotecan is a derivative of camptothecin. Camptothecins act as specific inhibitors of the enzyme DNA topoisomerase I. Irinotecan and its active metabolite SN-38 bind reversibly to the topoisomerase I-DNA complex and induce single-strand DNA lesions which block the DNA replication fork and are responsible for the cytotoxicity. Irinotecan is metabolized by carboxylesterase to SN-38. SN-38 is approximately 1000 times as potent as irinotecan as an inhibitor of topoisomerase I purified from human and rodent tumour cell lines. Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Phytogenic (Code: D000972) Enzyme Inhibitors (Code: D004791) Radiation-Sensitizing Agents (Code: D011838) Topoisomerase I Inhibitors (Code: D059004) Topoisomerase Inhibitors (Code: D059003) antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) Topoisomerase Inhibitor (Code: N0000175609) 1996-06-14 FDA CP0
Click to view antrafenine
Click to view etoposide DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020457s019lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020457s019lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020457s019lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9732391) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9732391) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17151191) Canalicular multispecific organic anion transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: O15438, gene: ABCC3, swissprot: MRP3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11581266) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11901101) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9281595) Multidrug resistance-associated protein 7 (Organism: Homo sapiens, class: Transporter, accessions: Q5T3U5, gene: ABCC10, swissprot: MRP7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12527806) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25618019) Etoposide (also known as VP-16) is a semisynthetic derivative of podophyllotoxin used in the treatment of certain neoplastic diseases. Etoposide causes the induction of DNA strand breaks by an interaction with DNA-topoisomerase II or the formation of free radicals, leading to cell cycle arrest, primarily at the G2 stage of the cell cycle, and cell death.Etoposide is indicated in the management of the refractory testicular tumors (in patients with refractory testicular tumors who have already received appropriate surgical, chemotherapeutic, and radiotherapeutic therapy) and of the small cell lung cancer (as first line treatment). Topoisomerase Inhibitor (Code: N0000175609) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Phytogenic (Code: D000972) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antineoplastic agent (Code: CHEBI:35610) 1983-11-10 FDA EVP
Click to view rescimetol
Click to view fluphenazine decanoate D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist 1972-06-20 FDA
Click to view hexobendine Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN A potent vasoactive agent that dilates cerebral and coronary arteries, but slightly constricts femoral arteries, without any effects on heart rate, blood pressure or cardiac output. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view rapacuronium Muscle-type nicotinic acetylcholine receptor (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P07510|P11230|Q04844|Q07001, gene: CHRNA1|CHRNB1|CHRND|CHRNE|CHRNG, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN|ACHE_HUMAN|ACHG_HUMAN) antagonist a nondepolarizing neuromuscular blocking agent with a rapid onset of action acts by competing for cholinergic receptors at the motor end plate Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Peripheral Nervous System Agents (Code: D018373) 1999-08-18 FDA
Click to view cefteram pivoxil Cefteram Pivoxil is the pivalate ester prodrug of cefteram, a semi-synthetic, broad-spectrum, third-generation cephalosporin with antibacterial activity. After oral administration of cefteram pivoxil, the ester bond is cleaved, releasing active cefteram. (See: cefteram) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1987-08-01 PMDA
Click to view sultamicillin Sultamicillin is the mutual prodrug of sulbactam and ampicillin. Sultamicillin inhibits ?-lactamases in penicillin-resistant microorganisms and it acts against sensitive organisms during the stage of active multiplication by inhibiting biosynthesis of cell wall mucopeptide. It is indicated for the treatmrnt of bacterial infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1987-12-01 Italian Medicines Agency (AIFA)
Click to view selenium (75Se) tauroselcholic acid
Click to view keracyanin an anthocyanin compound
Click to view perflubron Perflubron is a synthetic radiopaque liquid form of perfluorooctyl bromide. Used as a contrast agent for magnetic resonance imaging (MRI) or ultrasound imaging procedures, perflubron is also used as a liquid ventilation agent to improve pulmonary gas exchange and lung compliance and may be used in surgery to reduce or eliminate the need for donor blood. Anti-Obesity Agents (Code: D019440) Central Nervous System Agents (Code: D002491) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) Radiation-Sensitizing Agents (Code: D011838) radioopaque medium (Code: CHEBI:37338) blood substitute (Code: CHEBI:38849) 1993-08-13 FDA
Click to view iopodic acid Ionic monomeric contrast media. Usually the sodium or calcium salts are used for examination of the gall bladder and biliary tract. (From Martindale, The Extra Pharmacopoeia, 30th ed, p704) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 1962-03-15 FDA
Click to view metofenazate
Click to view hematoporphyrin Iron-free derivatives of heme with 4 methyl groups, 2 hydroxyethyl groups and 2 propionic acid groups attached to the pyrrole rings. Some of these PHOTOSENSITIZING AGENTS are used in the PHOTOTHERAPY of malignant NEOPLASMS. photosensitizing agent (Code: CHEBI:47868)
Click to view nicofuranose derivative of nicotinic acid that produces fewer side effects than pure nicotinic acid; used in peripheral vascular disease; also proposed as anticholesteremic; minor descriptor (75-84); on-line search NIACIN/AA (75-84); Index Medicus search NIACIN/AA (83-84), NICOTINIC ACIDS (75-82) Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665)
Click to view fulvestrant Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021344Orig1s039lbl.pdf) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021344Orig1s039lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021344Orig1s039lbl.pdf) Bifunctional epoxide hydrolase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P34913, gene: EPHX2, swissprot: HYES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23684894) Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/26407012) Fulvestrant is a synthetic estrogen receptor antagonist. Unlike tamoxifen (which has partial agonist effects) and the aromatase inhibitors (which reduce the estrogen available to tumor cells), fulvestrant binds competitively to estrogen receptors in breast cancer cells, resulting in estrogen receptor deformation and decreased estrogen binding. In vitro studies indicate that fulvestrant reversibly inhibits the growth of tamoxifen-resistant, estrogen-sensitive, human breast cancer cell lines. Fulvestrant is used in the treatment of hormone-receptor positive metastatic breast cancer. Selective Estrogen Receptor Modulators (Code: N0000000168) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Estrogen Antagonists (Code: D004965) Estrogen Receptor Antagonists (Code: D065171) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) estrogen receptor antagonist (Code: CHEBI:50792) antineoplastic agent (Code: CHEBI:35610) estrogen antagonist (Code: CHEBI:50837) 2002-04-25 FDA FVS
Click to view anazolene
Click to view diosmin Aryl hydrocarbon receptor (Organism: Homo sapiens, class: Transcription factor, accessions: P35869, gene: AHR, swissprot: AHR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/14644660) a semisynthetic drug indicated for the treatment of venous disease anti-inflammatory agent (Code: CHEBI:67079) 1971 Italian Medicines Agency (AIFA)
Click to view reserpine Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) inhibitor (Source: ) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Chromaffin granule amine transporter (Organism: Homo sapiens, class: Transporter, accessions: P54219, gene: SLC18A1, swissprot: VMAT1_HUMAN) inhibitor (Source: ) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN Sodium channel alpha subunits; brain (Types I, II, III) (Organism: Homo sapiens, class: Ion channel, accessions: P35498|Q99250|Q9NY46, gene: SCN1A|SCN2A|SCN3A, swissprot: SCN1A_HUMAN|SCN2A_HUMAN|SCN3A_HUMAN Quinolone resistance protein NorA (Organism: Staphylococcus aureus, class: Transporter, accessions: P0A0J7, gene: norA, swissprot: NORA_STAAU ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN Synaptic vesicular amine transporter (Organism: Bos taurus, class: Transporter, accessions: Q27963, gene: SLC18A2, swissprot: VMAT2_BOVIN An alkaloid found in the roots of Rauwolfia serpentina and R. vomitoria. Reserpine inhibits the uptake of norepinephrine into storage vesicles resulting in depletion of catecholamines and serotonin from central and peripheral axon terminals. It has been used as an antihypertensive and an antipsychotic as well as a research tool, but its adverse effects limit its clinical use. Catecholamine-depleting Sympatholytic (Code: N0000175640) Decreased Sympathetic Activity (Code: N0000175650) Adrenergic Agents (Code: D018663) Adrenergic Uptake Inhibitors (Code: D018759) Antihypertensive Agents (Code: D000959) Antipsychotic Agents (Code: D014150) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) first generation antipsychotic (Code: CHEBI:65190) adrenergic uptake inhibitor (Code: CHEBI:35640) antihypertensive agent (Code: CHEBI:35674) 1955-10-12 FDA
Click to view methoserpidine
Click to view dexniguldipine Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/2547493) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN Voltage-gated L-type calcium channel (Organism: Rattus norvegicus, class: Ion channel, accessions: P22002|P27732|Q02485, gene: Cacna1c|Cacna1d|Cacna1s, swissprot: CAC1C_RAT|CAC1D_RAT|CAC1S_RAT Adenosine receptor A1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25099, gene: Adora1, swissprot: AA1R_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT Alpha-1A adrenergic receptor (Organism: Bos taurus, class: GPCR, accessions: P18130, gene: ADRA1A, swissprot: ADA1A_BOVIN Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT
Click to view tubocurarine 5-hydroxytryptamine receptor 3A (Organism: Mus musculus, class: Ion channel, accessions: P23979, gene: Htr3a, swissprot: 5HT3A_MOUSE) antagonist (Source: ) Neuronal acetylcholine receptor; alpha2/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P17787|Q15822, gene: CHRNA2|CHRNB2, swissprot: ACHA2_HUMAN|ACHB2_HUMAN) Neuronal acetylcholine receptor; alpha4/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P30926|P43681, gene: CHRNA4|CHRNB4, swissprot: ACHA4_HUMAN|ACHB4_HUMAN) Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P17787|P43681, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) Acetylcholine receptor (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN) antagonist 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Small conductance calcium-activated potassium channel protein 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UGI6, gene: KCNN3, swissprot: KCNN3_HUMAN) blocker (Source: ) Small conductance calcium-activated potassium channel protein 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q92952, gene: KCNN1, swissprot: KCNN1_HUMAN) blocker (Source: ) Serotonin 3 receptor (5HT3) (Organism: Homo sapiens, class: Ion channel, accessions: O95264|P46098, gene: HTR3A|HTR3B, swissprot: 5HT3A_HUMAN|5HT3B_HUMAN) antagonist (Source: ) Small conductance calcium-activated potassium channel protein 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q9H2S1, gene: KCNN2, swissprot: KCNN2_HUMAN) blocker (Source: ) Small conductance calcium-activated potassium channel protein 3 (Organism: Rattus norvegicus, class: Ion channel, accessions: P70605, gene: Kcnn3, swissprot: KCNN3_RAT Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN GABA-A receptor; anion channel (Organism: Homo sapiens, class: Ion channel, accessions: O00591|O14764|P14867|P18505|P18507|P28472|P31644|P34903|P47869|P47870|P48169|P78334|Q16445|Q8N1C3|Q99928|Q9UN88, gene: GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ, swissprot: GBRA1_HUMAN|GBRA2_HUMAN|GBRA3_HUMAN|GBRA4_HUMAN|GBRA5_HUMAN|GBRA6_HUMAN|GBRB1_HUMAN|GBRB2_HUMAN|GBRB3_HUMAN|GBRD_HUMAN|GBRE_HUMAN|GBRG1_HUMAN|GBRG2_HUMAN|GBRG3_HUMAN|GBRP_HUMAN|GBRT_HUMAN Acetylcholine receptor subunit alpha (Organism: Torpedo californica, class: Ion channel, accessions: P02710, gene: CHRNA1, swissprot: ACHA_TORCA Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN Zinc-activated ligand-gated ion channel (Organism: Homo sapiens, class: Ion channel, accessions: Q401N2, gene: ZACN, swissprot: ZACN_HUMAN Neuronal acetylcholine receptor subunit alpha-7 (Organism: Rattus norvegicus, class: Ion channel, accessions: Q05941, gene: Chrna7, swissprot: ACHA7_RAT Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Rattus norvegicus, class: Ion channel, accessions: P09483|P12390, gene: Chrna4|Chrnb2, swissprot: ACHA4_RAT|ACHB2_RAT Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN Nicotinic acetylcholine receptor alpha 5 subunit (Organism: Musca domestica, class: Ion channel, accessions: A9XFY4, gene: nAChRalpha5, swissprot: A9XFY4_MUSDO Acetylcholine receptor; alpha1/beta1/delta/gamma (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P07510|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND|CHRNG, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN|ACHG_HUMAN Neuronal acetylcholine receptor; alpha3/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P30926|P32297, gene: CHRNA3|CHRNB4, swissprot: ACHA3_HUMAN|ACHB4_HUMAN Small conductance calcium-activated potassium channel protein 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P70604, gene: Kcnn2, swissprot: KCNN2_RAT) blocker (Source: ) A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae. Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) nicotinic antagonist (Code: CHEBI:48878) muscle relaxant (Code: CHEBI:51371) 1945-02-20 FDA TC9
Click to view candesartan cilexetil Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020838s039lbl.pdf) Type-2 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P50052, gene: AGTR2, swissprot: AGTR2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020838s039lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21861202) Candesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is, therefore, independent of the pathways for angiotensin II synthesis. Angiotensin 2 Receptor Antagonists (Code: N0000000070) Angiotensin 2 Receptor Blocker (Code: N0000175561) Angiotensin II Type 1 Receptor Blockers (Code: D047228) Angiotensin Receptor Antagonists (Code: D057911) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) 1998-06-04 FDA
Click to view manidipine Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/8287905) Cruzipain (Organism: Trypanosoma cruzi, class: Enzyme, accessions: P25779, gene: None, swissprot: CYSP_TRYCR Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990)
Click to view dihydroergocristine D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) 5-hydroxytryptamine receptor 4 (Organism: Cavia porcellus, class: GPCR, accessions: O70528, gene: HTR4, swissprot: 5HT4R_CAVPO) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) antagonist (Source: ) A 9,10alpha-dihydro derivative of ERGOTAMINE that contains an isopropyl sidechain at the 2' position of the molecule. Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) alpha-adrenergic antagonist (Code: CHEBI:37890) vasodilator agent (Code: CHEBI:35620) 1975-01-01 YEAR INTRODUCED
Click to view novobiocin ParE (Organism: Streptococcus pneumoniae, class: Enzyme, accessions: Q7X1P7, gene: parE, swissprot: Q7X1P7_STREE DNA gyrase subunit B (Organism: Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4), class: Enzyme, accessions: P0A4L9, gene: gyrB, swissprot: GYRB_STRPN DNA gyrase subunit B (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES6, gene: gyrB, swissprot: GYRB_ECOLI DNA gyrase subunit B (Organism: Mycobacterium smegmatis, class: Unclassified, accessions: P0C559, gene: gyrB, swissprot: GYRB_MYCSM DNA gyrase subunit B (Organism: Escherichia coli, class: Enzyme, accessions: C3SLN2, gene: gyrB, swissprot: C3SLN2_ECOLX DNA gyrase (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AES4|P0AES6, gene: gyrA|gyrB, swissprot: GYRA_ECOLI|GYRB_ECOLI ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN DNA gyrase (Organism: Staphylococcus epidermidis (strain ATCC 35984 / RP62A), class: Enzyme, accessions: Q5HK03|Q5HK04, gene: gyrA|gyrB, swissprot: GYRA_STAEQ|GYRB_STAEQ) inhibitor DNA gyrase subunit B (Organism: Staphylococcus aureus, class: Unclassified, accessions: P0A0K8, gene: gyrB, swissprot: GYRB_STAAU An antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin. Novobiocin binds to DNA gyrase, and blocks adenosine triphosphatase (ATPase) activity. (From Reynolds, Martindale The Extra Pharmacopoeia, 30th ed, p189) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) 1964-09-04 FDA NOV
Click to view dexamethasone palmitate Fatty acid-binding protein, liver (Organism: Rattus norvegicus, class: Unclassified, accessions: P02692, gene: Fabp1, swissprot: FABPL_RAT Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN Glucocorticoid receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P06536, gene: Nr3c1, swissprot: GCR_RAT Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN a liposteroid for treatment of hemophagocytic lymphohistiocytosis
Click to view cefpiramide Bacterial penicillin-binding protein (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918|P02919|P08506|P0AD65|P0AD68|P0AEB2|P24228, gene: dacA|dacB|dacC|ftsI|mrcA|mrcB|mrdA, swissprot: DACA_ECOLI|DACB_ECOLI|DACC_ECOLI|FTSI_ECOLI|PBP2_ECOLI|PBPA_ECOLI|PBPB_ECOLI) inhibitor antipseudomonal cephalosporin derivative Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1989-01-31 FDA
Click to view indinavir Pol polyprotein (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72874, gene: pol, swissprot: Q72874_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020685s078lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10820137) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10681378) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12218384) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20102298) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20102298) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20102298) A potent and specific HIV protease inhibitor that appears to have good oral bioavailability. Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) HIV Protease Inhibitors (Code: D017320) Protease Inhibitors (Code: D011480) 1996-03-13 FDA MK1
Click to view iotalamic acid A contrast medium in diagnostic radiology with properties similar to those of diatrizoic acid. It is used primarily as its sodium and meglumine (IOTHALAMATE MEGLUMINE) salts. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) 1963-09-30 FDA
Click to view diatrizoate A commonly used x-ray contrast medium. As DIATRIZOATE MEGLUMINE and as Diatrizoate sodium, it is used for gastrointestinal studies, angiography, and urography. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338) Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) 1954-11-26 FDA
Click to view framycetin Lethal factor (Organism: Bacillus anthracis, class: Enzyme, accessions: P15917, gene: lef, swissprot: LEF_BACAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16870442) Transient receptor potential cation channel subfamily V member 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q8NER1, gene: TRPV1, swissprot: TRPV1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15621372) Framycetin is an aminoglycoside antibiotic and a component of neomycin that is produced by Streptomyces fradiae. The spectrum of activity of framycetin includes Staph. aureus and most clinically significant gram negative organisms. Framycetin is not active against fungi, viruses and most kinds of anaerobic bacteria. Framycetin works by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Framycetin is used mostly as a topical preparation and is poorly absorbed. Upon parenteral administration, this agent can cause nephrotoxicity and ototoxicity. Framycetin is used for the treatment of bacterial eye infections (such as conjunctivitis) and bacterial ear infections (such as otitis externa). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1972-01-01 UK Medicines and Healthcare Products Regulatory Agency (MHRA) NMY
Click to view paromomycin An oligosaccharide antibiotic produced by various STREPTOMYCES. Antiprotozoal (Code: N0000175485) Amebicides (Code: D000563) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) antibacterial drug (Code: CHEBI:36047) antiprotozoal drug (Code: CHEBI:35820) anthelminthic drug (Code: CHEBI:35443) antiparasitic agent (Code: CHEBI:35442) 1969-03-24 FDA PAR
Click to view cefditoren pivoxil Cefditoren Pivoxil is a semi-synthetic, broad-spectrum, beta-lactamase resistant, third-generation cephalosporin antibiotic with bactericidal activity. Cefditoren pivoxil is a prodrug that is rapidly hydrolyzed by intestinal esterases during absorption to the microbiologically active cefditoren. Cefditoren pivoxil is indicated for the treatment of Acute Bacterial Exacerbation of Chronic Bronchitis (due to H. influenzae, H. parainfluenzae, S. pneumoniae (penicillin susceptible strains only), or M. catarrhalis), Community-Acquired Pneumonia (due to H. influenzae, H. parainfluenzae, S. (penicillin-susceptible strains only), or M. catarrhalis), Pharyngitis/Tonsillitis (due to S. pyogenes), Uncomplicated Skin and Skin-Structure Infections (due to S. aureus or S. pyogenes). (See: cefditoren) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) prodrug (Code: CHEBI:50266) Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) 2001-08-29 FDA
Click to view butobendine Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317)
Click to view tiratricol Thyroid hormone receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10828, gene: THRB, swissprot: THB_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12699376) Tiratricol (triiodothyroacetic acid) is a thyroid hormone analogue, which is a naturally occurring chemical in the body. Tiratricol is used as a dietary supplement for thyroid problems including thyroid cancer. Tiratricol is used to slow the secretion of TSH (a hormone that stimulates the functioning of the thyroid gland). 1997-12-05 ANSM (French National Agency for Medicines and Health Products Safety) 4HY
Click to view sulfobromophthalein Hematopoietic prostaglandin D synthase (Organism: Homo sapiens, class: Enzyme, accessions: O60760, gene: HPGDS, swissprot: HPGDS_HUMAN A phenolphthalein that is used as a diagnostic aid in hepatic function determination. Coloring Agents (Code: D004396) Indicators and Reagents (Code: D007202) dye (Code: CHEBI:37958) BSP
Click to view triamcinolone benetonide Adrenal Cortex Hormones (Code: D000305) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view tirilazad Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) Mitogen-activated protein kinase 3 (Organism: Homo sapiens, class: Kinase, accessions: P27361, gene: MAPK3, swissprot: MK03_HUMAN) Mitogen-activated protein kinase 14 (Organism: Homo sapiens, class: Kinase, accessions: Q16539, gene: MAPK14, swissprot: MK14_HUMAN) a lazaroid; potent inhibitor of iron-dependent lipid peroxidation; has shown excellent activity in in vivo models of experimental central nervous system trauma & ischemia; structure given in first source; tradename Freedox Antioxidants (Code: D000975) Central Nervous System Agents (Code: D002491) Neuroprotective Agents (Code: D018696) Protective Agents (Code: D020011)
Click to view guamecycline
Click to view tocofibrate
Click to view cefbuperazone
Click to view dabigatran etexilate Dabigatran: Prothrombin (Organism: Homo sapiens, class: Enzyme, accessions: P00734, gene: F2, swissprot: THRB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022512s038lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20551237) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20551237) UDP-glucuronosyltransferase 2B15 (Organism: Homo sapiens, class: Enzyme, accessions: P54855, gene: UGT2B15, swissprot: UDB15_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20551237) Ribosyldihydronicotinamide dehydrogenase [quinone] (Organism: Homo sapiens, class: Enzyme, accessions: P16083, gene: NQO2, swissprot: NQO2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22494098) Dabigatran Etexilate: Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022512s038lbl.pdf) Liver carboxylesterase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23141, gene: CES1, swissprot: EST1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23239178) Cocaine esterase (Organism: Homo sapiens, class: Enzyme, accessions: O00748, gene: CES2, swissprot: EST2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23239178) Dabigatran etexilate is a prodrug of direct thrombin inhibitor dabigatran. Dabigatran and its acyl glucuronides are competitive, direct thrombin inhibitors. Because thrombin (serine protease) enables the conversion of fibrinogen into fibrin during the coagulation cascade, its inhibition prevents the development of a thrombus. Both free and clot-bound thrombin, and thrombin-induced platelet aggregation are inhibited by the active moieties. Dabigatran etexilate is indicated to reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation, for the treatment of deep venous thrombosis and pulmonary embolism, to reduce the risk of recurrence of deep venous thrombosis and pulmonary embolism and for the prophylaxis of deep venous thrombosis and pulmonary embolism. Anticoagulants (Code: D000925) Antithrombins (Code: D000991) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) anticoagulant (Code: CHEBI:50249) prodrug (Code: CHEBI:50266) 2010-10-19 FDA Dabig
Click to view bemotrizinol FDA
Click to view metrizoic acid A diagnostic radiopaque that usually occurs as the sodium salt. Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338) 1973-11-17 FDA
Click to view iodamide An ionic monomeric contrast medium. (From Martindale, The Extra Pharmacopoeia, 30th ed, p706) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338) 1978-07-25 FDA
Click to view efonidipine Voltage-dependent T-type calcium channel subunit alpha-1G (Organism: Rattus norvegicus, class: Ion channel, accessions: O54898, gene: Cacna1g, swissprot: CAC1G_RAT) blocker (Source: ) Voltage-dependent T-type calcium channel subunit alpha-1H (Organism: Homo sapiens, class: Ion channel, accessions: O95180, gene: CACNA1H, swissprot: CAC1H_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/21466810) Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q01668|Q13936, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/17276408) Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Diuretics (Code: D004232) Membrane Transport Modulators (Code: D049990) Natriuretic Agents (Code: D045283)
Click to view rescinnamine Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) inhibitor antihypertensive agent (Code: CHEBI:35674) 1956-10-31 FDA
Click to view cefoperazone Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11909604) Solute carrier family 22 member 7 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y694, gene: SLC22A7, swissprot: S22A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9650585) Cefoperazone, a third-generation cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase, interferes with cell wall synthesis by binding to the penicillin-binding proteins (PBPs), thus preventing cross-linking of nascent peptidoglycan. Cefoperazone has been shown to be active against Staphylococcus aureus (methicillin-susceptible isolates only), Staphylococcus epidermidis (methicillin-susceptible isolates only), Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, Citrobacter species, Enterobacter species, Escherichia coli, Haemophilus influenzae, Klebsiella species, Morganella morganii, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris, Providencia rettgeri, Providencia stuartii ,Pseudomonas species, Serratia marcescens, Peptococcus and Peptostreptococcus spp., Clostridium species (with the exception of C. difficile) and Bacteroides species. Cefoperazone is indicated for the treatment of Respiratory Tract Infections (due to S. pneumoniae, H. influenzae, S. aureus, S. pyogenes, P. aeruginosa, K. pneumoniae, E. coli, P. mirabilis, and Enterobacter spp.), Intra-abdominal Infections (due to E. coli, P. aeruginosa, Bacteroides fragilis), Septicemia (due to S. pneumoniae, S. agalactiae, S. aureus, P. aeruginosa, E. coli, Klebsiella spp., Proteus spp., Clostridium spp.), Infections of the Skin and Skin Structures (due to S. aureus, S. pyogenes, and P. aeruginosa), Infections of the Female Genital Tract (due to N. gonorrhoeae, S. epidermidis, S. agalactiae, E. coli, Clostridium spp., Bacteroides species). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) 1982-11-18 FDA
Click to view nicomol
Click to view tyropanoate A diagnostic aid as a radiopaque medium in cholecystography. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 1969-10-24 FDA
Click to view amiodarone Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/12873512) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022325s013lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022325s013lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022325s013lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022325s013lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022325s013lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022325s013lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022325s013lbl.pdf) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26972388) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/23812503) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/23812503) Potassium voltage-gated channel subfamily A member 7 (Organism: Homo sapiens, class: Ion channel, accessions: Q96RP8, gene: KCNA7, swissprot: KCNA7_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/11896454) Amiodarone is a class III antiarrhythmic drug, but it possesses electrophysiologic characteristics of all four Vaughan Williams classes. Like class I drugs, amiodarone blocks sodium channels at rapid pacing frequencies, and like class II drugs, amiodarone exerts a noncompetitive antisympathetic action. One of its main effects, with prolonged administration, is to lengthen the cardiac action potential, a class III effect. The negative chronotropic effect of amiodarone in nodal tissues is similar to the effect of class IV drugs. In addition to blocking sodium channels, amiodarone blocks myocardial potassium channels, which contributes to slowing of conduction and prolongation of refractoriness. Amiodarone is indicated for initiation of treatment and prophylaxis of frequently recurring ventricular fibrillation and hemodynamically unstable ventricular tachycardia in patients refractory to other therapy. Antiarrhythmic (Code: N0000175426) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) P-Glycoprotein Inhibitors (Code: N0000185503) Cytochrome P450 1A2 Inhibitors (Code: N0000182138) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) Cytochrome P-450 CYP1A2 Inhibitors (Code: D065609) Cytochrome P-450 CYP2C9 Inhibitors (Code: D065688) Cytochrome P-450 CYP2D6 Inhibitors (Code: D065690) Cytochrome P-450 CYP3A Inhibitors (Code: D065692) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Membrane Transport Modulators (Code: D049990) Metabolic Side Effects of Drugs and Substances (Code: D065606) Potassium Channel Blockers (Code: D026902) Sodium Channel Blockers (Code: D026941) Vasodilator Agents (Code: D014665) cardiovascular drug (Code: CHEBI:35554) 1985-12-24 FDA BBI
Click to view acarbose Pancreatic alpha-amylase (Organism: Homo sapiens, class: Enzyme, accessions: P04746, gene: AMY2A, swissprot: AMYP_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020482s027lbl.pdf) Maltase-glucoamylase, intestinal (Organism: Homo sapiens, class: Enzyme, accessions: O43451, gene: MGAM, swissprot: MGA_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/020482s027lbl.pdf) Acarbose is an oligosaccharide which is obtained from fermentation processes of a microorganism, Actinoplanes utahensis. The antihyperglycemic action of acarbose results from a competitive, reversible inhibition of pancreatic alpha-amylase and membrane-bound intestinal alpha-glucoside hydrolase enzymes. Acarbose is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. alpha Glucosidase Inhibitors (Code: N0000000166) alpha-Glucosidase Inhibitor (Code: N0000175559) Enzyme Inhibitors (Code: D004791) Glycoside Hydrolase Inhibitors (Code: D065089) Hypoglycemic Agents (Code: D007004) hypoglycemic agent (Code: CHEBI:35526) 1995-09-06 FDA ACR
Click to view metildigoxin Sodium/potassium-transporting ATPase subunit alpha-1 (Organism: Homo sapiens, class: Transporter, accessions: P05023, gene: ATP1A1, swissprot: AT1A1_HUMAN) A semisynthetic digitalis glycoside with the general properties of DIGOXIN but more rapid onset of action. Its cardiotonic action is prolonged by its demethylation to DIGOXIN in the liver. It has been used in the treatment of congestive heart failure (HEART FAILURE). Anti-Arrhythmia Agents (Code: D000889) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protective Agents (Code: D020011)
Click to view zorubicin Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970)
Click to view prednimustine Ester of CHLORAMBUCIL and PREDNISOLONE used as a combination alkylating agent and synthetic steroid to treat various leukemias and other neoplasms. It causes gastrointestinal and bone marrow toxicity. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676)
Click to view liothyronine Thyroid hormone receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10827, gene: THRA, swissprot: THA_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/010379s054lbl.pdf) Thyroid hormone receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10828, gene: THRB, swissprot: THB_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/010379s054lbl.pdf) Solute carrier organic anion transporter family member 1C1 (Organism: Mus musculus, class: Transporter, accessions: Q9ERB5, gene: Slco1c1, swissprot: SO1C1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15166123) Liothyronine is a therapeutic formulation of the primary physiologically active form of endogenous thyroid hormone. In vivo, triiodothyronine enters the nucleus and binds to nuclear thyroid hormone receptors that subsequently bind to thyroid response elements located in target genes. l-Triiodothyronine (Code: N0000175946) Triiodothyronine (Code: N0000006165) 1956-05-08 FDA T3
Click to view methylprednisolone suleptanate Methylprednisolone suleptanate is a prodrug of methylprednisolone. It is a bioequivalent to other prodrug, methylprednisolone succinate. It is used for the treatment of asthma. (See: methylprednisolone)
Click to view dimethyltubocurarinium Neuronal acetylcholine receptor; alpha2/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P17787|Q15822, gene: CHRNA2|CHRNB2, swissprot: ACHA2_HUMAN|ACHB2_HUMAN) Acetylcholine receptor (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN) antagonist from Chinese herb Cyclea hainanensis Mrr Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Peripheral Nervous System Agents (Code: D018373) FDA CU9
Click to view bromocriptine 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT) agonist (Source: ) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) agonist (Source: ) D(4) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21917, gene: DRD4, swissprot: DRD4_HUMAN) antagonist (Source: ) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) agonist (Source: ) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: ) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) 5-hydroxytryptamine receptor 1B (Organism: Rattus norvegicus, class: GPCR, accessions: P28564, gene: Htr1b, swissprot: 5HT1B_RAT) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) agonist Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) Dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P18901|P19020|P25115|P30729|P61169, gene: Drd1|Drd2|Drd3|Drd4|Drd5, swissprot: DRD1_RAT|DRD2_RAT|DRD3_RAT|DRD4_RAT|DRD5_RAT Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P19328|P22086|P22909, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT Cerebral cortex alpha adrenergic receptor (Organism: Bos taurus, class: GPCR, accessions: P18130|Q28838, gene: ADRA1A|ADRA2A, swissprot: ADA1A_BOVIN|ADA2A_BOVIN D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Alpha-1A adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P43140, gene: Adra1a, swissprot: ADA1A_RAT Vesicular glutamate transporter 3 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q7TSF2, gene: Slc17a8, swissprot: VGLU3_RAT 5-hydroxytryptamine receptor 6 (Organism: Rattus norvegicus, class: GPCR, accessions: P31388, gene: Htr6, swissprot: 5HT6R_RAT) agonist (Source: ) A semisynthetic ergotamine alkaloid that is a dopamine D2 agonist. It suppresses prolactin secretion. Ergolines (Code: N0000007618) Ergot Derivative (Code: N0000175827) Anti-Dyskinesia Agents (Code: D018726) Antiparkinson Agents (Code: D000978) Central Nervous System Agents (Code: D002491) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Neurotransmitter Agents (Code: D018377) hormone antagonist (Code: CHEBI:49020) antiparkinson drug (Code: CHEBI:48407) antidyskinesia agent (Code: CHEBI:66956) dopamine agonist (Code: CHEBI:51065) 1978-06-28 FDA 08Y
Click to view nicofetamide
Click to view teniposide DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020119s010s011lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8114683) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11770832) Multidrug resistance-associated protein 6 (Organism: Homo sapiens, class: Transporter, accessions: O95255, gene: ABCC6, swissprot: MRP6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12414644) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q7TMS5, gene: Abcg2, swissprot: ABCG2_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12649196) Teniposide is a semisynthetic derivative of podophyllotoxin with antineoplastic activity. Teniposide forms a ternary complex with the enzyme topoisomerase II and DNA, resulting in dose-dependent single- and double-stranded breaks in DNA, DNA: protein cross-links, inhibition of DNA strand religation, and cytotoxicity. This agent acts in the late S or early G phase of the cell cycle. Teniposide is indicated for induction therapy in patients with refractory childhood acute lymphoblastic leukemia. Topoisomerase Inhibitor (Code: N0000175609) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) antineoplastic agent (Code: CHEBI:35610) 1992-07-14 FDA 9TP
Click to view bisoctrizole FDA
Click to view fytic acid Fytic acid is a natural antioxidant that is found in cereals, vegetables, nuts, and natural oils. Fytic acid has ability to chelate with such minerals as iron, copper, zinc, and calcium. Fytic acid may be considered a phytonutrient, providing an antioxidant effect. It was used for the treatment of hypercalciuria. Now it is used as technetium phytate (99mTc) for the diagnosis of liver and reticuloendothelial system. 2013-12-26 Spanish Agency of Medicines and Medical Products (AEMPS) I6P
IHP
Click to view syrosingopine
Click to view zinostatin DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) other (Source: http://www.ncbi.nlm.nih.gov/pubmed/7527033) An enediyne that alkylates DNA and RNA like MITOMYCIN does, so it is cytotoxic. Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Cytotoxins (Code: D003603) Enzyme Inhibitors (Code: D004791) Noxae (Code: D009676) Nucleic Acid Synthesis Inhibitors (Code: D019384) CHR
Click to view iobenzamic acid Iobenzamic acid is a contrast medium. It was was used for cholecystography. It is no longer marketed. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907)
Click to view clindamycin palmitate Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) 1986-04-07 FDA
Click to view natamycin Natamycin is a tetraene polyene antibiotic derived from Streptomyces natalensis. It possesses in vitro activity against a variety of yeast and filamentous fungi, including Candida, Aspergillus, Cephalosporium, Fusarium and Penicillium. Polyene Antimicrobial (Code: N0000175936) Polyenes (Code: N0000007672) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Antifungal Agents (Code: D000935) 1978-10-30 FDA
Click to view alcuronium Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) allosteric modulator (Source: ) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) allosteric modulator (Source: ) Neuronal acetylcholine receptor; alpha4/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P30926|P43681, gene: CHRNA4|CHRNB4, swissprot: ACHA4_HUMAN|ACHB4_HUMAN) Acetylcholine receptor (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN) Neuronal acetylcholine receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: Q15822, gene: CHRNA2, swissprot: ACHA2_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Sus scrofa, class: GPCR, accessions: P06199, gene: CHRM2, swissprot: ACM2_PIG A non-depolarizing skeletal muscle relaxant similar to TUBOCURARINE. It is used as an anesthesia adjuvant. Adjuvants, Anesthesia (Code: D000759) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) 1963-01-01 YEAR INTRODUCED
Click to view etoposide phosphate DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) inhibitor Etoposide phosphate is a prodrug that is converted to its active moiety, etoposide, by dephosphorylation. Etoposide causes the induction of DNA strand breaks by an interaction with DNA-topoisomerase II or the formation of free radicals, leading to cell cycle arrest, primarily at the G2 stage of the cell cycle, and cell death. Antineoplastic Agents (Code: D000970) antineoplastic agent (Code: CHEBI:35610) 1996-05-17 FDA
Click to view pentamycin
Click to view saquinavir Pol polyprotein (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72874, gene: pol, swissprot: Q72874_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020628s047,021785s023lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020628s047,021785s023lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16433896) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16433896) Cytochrome P450 3A7 (Organism: Homo sapiens, class: Enzyme, accessions: P24462, gene: CYP3A7, swissprot: CP3A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16433896) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26721703) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9758674) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10820137) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9732409) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20102298) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20102298) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20102298) Chloroquine resistance transporter (Organism: Plasmodium falciparum, class: Unclassified, accessions: Q9N623, gene: CRT, swissprot: CRT_PLAFA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22354298) Saquinavir is an inhibitor of HIV-1 protease. Saquinavir is a peptide-like substrate analogue that binds to the protease active site and inhibits the activity of the enzyme. Saquinavir inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature noninfectious viral particles. Saquinavir is used in the therapy and prevention of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS). Protease Inhibitor (Code: N0000175889) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Cytochrome P-450 CYP3A Inhibitors (Code: D065692) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) HIV Protease Inhibitors (Code: D017320) Metabolic Side Effects of Drugs and Substances (Code: D065606) Protease Inhibitors (Code: D011480) antiviral drug (Code: CHEBI:36044) Cytochrome P450 3A Inhibitors (Code: N0000190114) 1995-12-06 FDA ROC
Click to view thymopentin Synthetic pentapeptide corresponding to the amino acids 32-36 of thymopoietin and exhibiting the full biological activity of the natural hormone. It is an immunomodulator which has been studied for possible use in the treatment of rheumatoid arthritis, AIDS, and other primary immunodeficiencies. Adjuvants, Immunologic (Code: D000276) Immunologic Factors (Code: D007155)
Click to view temoporfin used as PHOTOCHEMOTHERAPY Antineoplastic Agents (Code: D000970) Dermatologic Agents (Code: D003879) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) photosensitizing agent (Code: CHEBI:47868) 2001-10-24 EMA
Click to view prednisolone steaglate
Click to view enviomycin Cyclic basic peptide related to VIOMYCIN. It is isolated from an induced mutant of Streptomyces griseoverticillatus var. tuberacticus and acts as an antitubercular agent with less ototoxicity than tuberactinomycin. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antibiotics, Antitubercular (Code: D000904) Antitubercular Agents (Code: D000995)
Click to view viomycin A strongly basic peptide, antibiotic complex from several strains of Streptomyces. It is allergenic and toxic to kidneys and the labyrinth. Viomycin is used in tuberculosis as several different salts and in combination with other agents. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antibiotics, Antitubercular (Code: D000904) Antitubercular Agents (Code: D000995) Enzyme Inhibitors (Code: D004791) Protein Synthesis Inhibitors (Code: D011500) antitubercular agent (Code: CHEBI:33231) FDA
Click to view posaconazole Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022003s024,205053s008,205596s007lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022003s024,205053s008,205596s007lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022003s024,205053s008,205596s007lbl.pdf) Posaconazole is a broad-spectrum, second generation, triazole compound with antifungal activity. Posaconazole strongly inhibits 14-alpha demethylase, a cytochrome P450-dependent enzyme. It is used for prophylaxis or treatment invasive infections by Candida species and Aspergillus species in severely immunocompromised patients. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) 14-alpha Demethylase Inhibitors (Code: D058888) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) Trypanocidal Agents (Code: D014344) trypanocidal drug (Code: CHEBI:36335) 2006-09-15 FDA X2N
Click to view sulbutiamine Sulbutiamine is a synthetic derivative of thiamine (vitamin B1) that is composed of two modified thiamine molecules to form a dimer. It is highly lipophilic, allowing it to cross the blood-brain barrier more easily than other thiamine derivatives. Although its clinical efficacy is not yet defined, sulbutiamine is used to treat asthenia. While its other uses include improvement of erectile dysfunction and reduction of psycho-behavioural inhibition, sulbutiamine showed evidence of modulatory effect on dopaminergic and glutamatergic cortical transmissions. The chronic administration of the drug has demonstrated to improve long term memory formation in mice. Sulbutiamine remedies the symptoms of weakness by increasing focus, strength (both physical and mental) and whilst also helping to stabilize sleeping patterns. This product is also popular with athletes as a nutritional supplement as it is a vitamin compound. 1996-08-28 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view atazanavir Pol polyprotein (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72874, gene: pol, swissprot: Q72874_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021567s042,206352s007lbl.pdf) Gag-Pol polyprotein (Organism: Human immunodeficiency virus type 2 subtype A (isolate ROD) (HIV-2), class: Enzyme, accessions: P04584, gene: gag-pol, swissprot: POL_HV2RO) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021567s042,206352s007lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021567s042,206352s007lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021567s042,206352s007lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021567s042,206352s007lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021567s042,206352s007lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19918100) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19918100) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19918100) Solute carrier family 23 member 1 (Organism: Homo sapiens, class: Unclassified, accessions: Q9UHI7, gene: SLC23A1, swissprot: S23A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19918100) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Atazanavir is an HIV-1 protease inhibitor. Atazanavir has activity against HIV-1 Group M subtype viruses A, B, C, D, AE, AG, F, G, and J isolates in cell culture. Atazanavir has variable activity against HIV-2 isolates. The I50L and I50V substitutions yielded selective resistance to atazanavir and amprenavir, respectively, and did not appear to be cross-resistant. Atazanavir is indicated for use in combination with other antiretroviral agents for the treatment of HIV-1 infection. Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) HIV Protease Inhibitors (Code: D017320) Protease Inhibitors (Code: D011480) antiviral drug (Code: CHEBI:36044) Protease Inhibitor (Code: N0000175889) UGT1A1 Inhibitors (Code: N0000191272) UDP Glucuronosyltransferases Inhibitors (Code: N0000191269) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 3A Inhibitors (Code: N0000190114) Cytochrome P450 2C8 Inhibitors (Code: N0000187062) 2003-06-20 FDA DR7
Click to view itraconazole Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16141567) Lanosterol 14-alpha demethylase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P10614, gene: ERG11, swissprot: CP51_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12606318) Lanosterol 14-alpha demethylase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: P10613, gene: ERG11, swissprot: CP51_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991846) Lanosterol 14-alpha demethylase (Organism: Candida tropicalis (Yeast), class: Enzyme, accessions: P14263, gene: ERG11, swissprot: CP51_CANTR) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10991846) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/2699389) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23437772) C-C chemokine receptor type 4 (Organism: Homo sapiens, class: GPCR, accessions: P51679, gene: CCR4, swissprot: CCR4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23437772) C-X-C chemokine receptor type 1 (Organism: Homo sapiens, class: GPCR, accessions: P25024, gene: CXCR1, swissprot: CXCR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23437772) Itraconazole is a orally administered, triazole antifungal agent used in the treatment of systemic and superficial fungal infections. Itraconazole therapy is associated with transient, mild-to-moderate serum elevations and can lead to clinically apparent acute drug induced liver injury. Itraconazole inhibits the cytochrome P450-dependent synthesis of ergosterol, which is a vital component of fungal cell membranes. Azole Antifungal (Code: N0000175487) Azoles (Code: N0000008217) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) P-Glycoprotein Inhibitors (Code: N0000185503) 14-alpha Demethylase Inhibitors (Code: D058888) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Cytochrome P-450 CYP3A Inhibitors (Code: D065692) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) 1992-09-11 FDA 1YN
Click to view benproperine antitussive (Code: CHEBI:51177)
Click to view lucimycin A macrolide antibiotic isolated from cultures of Streptomyces lucensis. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935)
Click to view bietaserpine hypotensive agent; structure Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317)
Click to view talaporfin effective tumor localizer that brings about the selective degradation of tumor tissue following light exposure; structure given in first source Antineoplastic Agents (Code: D000970) Dermatologic Agents (Code: D003879) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) 2003-10-26 PMDA
Click to view digitalin
Click to view erythromycin Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050536s026lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050536s026lbl.pdf) Motilin receptor (Organism: Homo sapiens, class: GPCR, accessions: O43193, gene: MLNR, swissprot: MTLR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2782416) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17296622) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17296622) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18509328) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18509328) Solute carrier organic anion transporter family member 1B2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9QZX8, gene: Slco1b2, swissprot: SO1B2_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18509328) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24154606) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9822896) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9822896) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21451505) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19821563) A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins. Decreased Sebaceous Gland Activity (Code: N0000009982) Macrolide (Code: N0000175877) Macrolide Antimicrobial (Code: N0000175935) Macrolides (Code: N0000007529) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Protein Synthesis Inhibitors (Code: D011500) 1964-06-24 FDA ERY
Click to view tretinoin tocoferil a hybrid compound composed of alpha-tocopherol esterified with retinoic acid; RN refers to (2R*(4R*,8R*)-(+-))-isomer
Click to view ritonavir Pol polyprotein (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72874, gene: pol, swissprot: Q72874_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022417s021lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022417s021lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022417s021lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022417s021lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022417s021lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022417s021lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022417s021lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022417s021lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15601807) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9278209) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24411125) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12218384) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12441801) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12699389) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18285471) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21030469) Ritonavir is a peptidomimetic inhibitor of the HIV-1 protease. Inhibition of HIV protease renders the enzyme incapable of processing the Gag-Pol polyprotein precursor which leads to production of non-infectious immature HIV particles. It is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Cytochrome P450 3A Inhibitor (Code: N0000191001) Protease Inhibitor (Code: N0000175889) Cytochrome P450 3A Inhibitors (Code: N0000190114) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Cytochrome P450 2C19 Inducers (Code: N0000185607) Cytochrome P450 3A Inducers (Code: N0000190118) P-Glycoprotein Inhibitors (Code: N0000185503) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 1A2 Inducers (Code: N0000191266) Cytochrome P450 2C9 Inducers (Code: N0000185507) Cytochrome P450 2B6 Inducers (Code: N0000187064) UDP Glucuronosyltransferases Inducers (Code: N0000190117) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Cytochrome P-450 CYP3A Inhibitors (Code: D065692) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) HIV Protease Inhibitors (Code: D017320) Metabolic Side Effects of Drugs and Substances (Code: D065606) Protease Inhibitors (Code: D011480) antiviral drug (Code: CHEBI:36044) 1996-03-01 FDA RIT
Click to view valrubicin DNA topoisomerase 2-alpha (Organism: Homo sapiens, class: Enzyme, accessions: P11388, gene: TOP2A, swissprot: TOP2A_HUMAN) inhibitor Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 1998-09-25 FDA
Click to view petrichloral Petrichloral is the tetrahemiacetal pentaerythritol derivative of chloral. Petrichloral exhibits a hypnotic and sedative action similar to chloral hydrate. It was used as a sedative and a hypnotic agent. 1955 FDA
Click to view colfosceril palmitate used in the treatment of unilateral pulmonary interstitial emphysema; component of Exosurf 1990-08-02 FDA PCF
Click to view glucosulfone
Click to view clarithromycin 50S ribosomal protein L10 (Organism: Shigella flexneri, class: Cytosolic other, accessions: P0A7J6, gene: rplJ, swissprot: RL10_SHIFL) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/050824s006lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/050824s006lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/050824s006lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/050824s006lbl.pdf) A semisynthetic macrolide antibiotic derived from erythromycin that is active against a variety of microorganisms. It can inhibit protein synthesis in bacteria by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Cytochrome P-450 CYP3A Inhibitors (Code: D065692) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Metabolic Side Effects of Drugs and Substances (Code: D065606) Protein Synthesis Inhibitors (Code: D011500) antibacterial drug (Code: CHEBI:36047) Macrolide Antimicrobial (Code: N0000175935) Macrolides (Code: N0000007529) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 3A Inhibitors (Code: N0000190114) P-Glycoprotein Inhibitors (Code: N0000185503) 1991-10-31 FDA CTY
Click to view azithromycin Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14982769) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14982769) Motilin receptor (Organism: Homo sapiens, class: GPCR, accessions: O43193, gene: MLNR, swissprot: MTLR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23190027) Azithromycin is a semi-synthetic macrolide antibiotic structurally related to erythromycin. Azithromycin acts by binding to the 50S ribosomal subunit of susceptible microorganisms and interfering with microbial protein synthesis. Azithromycin has been shown to be active against Haemophilus influenzae, Staphylococcus aureus, Streptococcus mitis group, Streptococcus pneumoniae. Azithromycin is indicated for the treatment of bacterial conjunctivitis caused by susceptible isolates of microorganisms. Macrolide Antimicrobial (Code: N0000175935) Macrolides (Code: N0000007529) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1991-11-01 FDA ZIT
Click to view ciclosporin Peptidyl-prolyl cis-trans isomerase A (Organism: Homo sapiens, class: Enzyme, accessions: P62937, gene: PPIA, swissprot: PPIA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27687672) Peptidyl-prolyl cis-trans isomerase D (Organism: Homo sapiens, class: Enzyme, accessions: Q08752, gene: PPID, swissprot: PPID_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26985318) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050715s035,050716s038lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050715s035,050716s038lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050715s035,050716s038lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050715s035,050716s038lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17202802) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17202802) Canalicular multispecific organic anion transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: O15438, gene: ABCC3, swissprot: MRP3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11585759) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12404239) Solute carrier organic anion transporter family member 1A4 (Organism: Rattus norvegicus, class: Transporter, accessions: O35913, gene: Slco1a4, swissprot: SO1A4_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11883641) Solute carrier organic anion transporter family member 1A1 (Organism: Rattus norvegicus, class: Transporter, accessions: P46720, gene: Slco1a1, swissprot: SO1A1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11883641) Ileal sodium/bile acid cotransporter (Organism: Homo sapiens, class: Transporter, accessions: Q12908, gene: SLC10A2, swissprot: NTCP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9458785) Sodium/bile acid cotransporter (Organism: Rattus norvegicus, class: Transporter, accessions: P26435, gene: Slc10a1, swissprot: NTCP_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9486191) Multidrug resistance-associated protein 7 (Organism: Homo sapiens, class: Transporter, accessions: Q5T3U5, gene: ABCC10, swissprot: MRP7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12527806) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10570049) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11437380) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12538813) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24184213) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19933795) Cyclosporine is a calcineurin inhibitor immunosuppressant agent when administered systemically. In patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca, topical administration of cyclosporine is thought to act as a partial immunomodulator. Cyclosporine’s primary immunosuppressive mechanism of action is inhibition of T-lymphocyte function. Upon administration cyclosporine binds to cyclophilin A and thus inhibits calcineurin, leading to immune system suppression. Cyclosporine is indicated to increase tear production in patients with keratoconjunctivitis sicca (dry eye). Also cyclosporine is used for the treatment of rheumatoid arthritis, psoriasis and for prevention of transplant rejections. Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antirheumatic Agents (Code: D018501) Calcineurin Inhibitors (Code: D065095) Dermatologic Agents (Code: D003879) Enzyme Inhibitors (Code: D004791) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) antirheumatic drug (Code: CHEBI:35842) dermatologic drug (Code: CHEBI:50177) immunosuppressive agent (Code: CHEBI:35705) anti-asthmatic drug (Code: CHEBI:49167) Calcineurin Inhibitor Immunosuppressant (Code: N0000175457) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) P-Glycoprotein Inhibitors (Code: N0000185503) 1983-11-14 FDA PRD_0
Click to view flurithromycin fluorine derivative of erythromycin Enzyme Inhibitors (Code: D004791) antibacterial drug (Code: CHEBI:36047)
Click to view benzquercin
Click to view vindesine Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) Vinblastine derivative with antineoplastic activity against CANCER. Major side effects are myelosuppression and neurotoxicity. Vindesine is used extensively in chemotherapy protocols (ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS). Antimitotic Agents (Code: D050256) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Phytogenic (Code: D000972) Mitosis Modulators (Code: D050258) Tubulin Modulators (Code: D050257) antineoplastic agent (Code: CHEBI:35610) 1979-01-01 YEAR INTRODUCED
Click to view digitoxin Sodium/potassium-transporting ATPase subunit alpha-2 (Organism: Sus scrofa, class: Ion channel, accessions: D2WKD8, gene: ATP1A2, swissprot: AT1A2_PIG) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) Sodium/potassium-transporting ATPase subunit alpha-1 (Organism: Homo sapiens, class: Transporter, accessions: P05023, gene: ATP1A1, swissprot: AT1A1_HUMAN) inhibitor Sodium/potassium-transporting ATPase subunit alpha-1 (Organism: Canis familiaris, class: Transporter, accessions: P50997, gene: ATP1A1, swissprot: AT1A1_CANFA Sodium/potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P05023|P05026|P13637|P14415|P50993|P54709|P54710|Q13733, gene: ATP1A1|ATP1A2|ATP1A3|ATP1A4|ATP1B1|ATP1B2|ATP1B3|FXYD2, swissprot: AT1A1_HUMAN|AT1A2_HUMAN|AT1A3_HUMAN|AT1A4_HUMAN|AT1B1_HUMAN|AT1B2_HUMAN|AT1B3_HUMAN|ATNG_HUMAN Signal transducer and activator of transcription 3 (Organism: Homo sapiens, class: Transcription factor, accessions: P40763, gene: STAT3, swissprot: STAT3_HUMAN A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665) Anti-Arrhythmia Agents (Code: D000889) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protective Agents (Code: D020011) FDA
Click to view iopamidol A non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiological procedures. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338) Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) 1985-12-31 FDA
Click to view pentagastrin Gastrin/cholecystokinin type B receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30553, gene: Cckbr, swissprot: GASR_RAT Cholecystokinin receptor type A (Organism: Rattus norvegicus, class: GPCR, accessions: P30551, gene: Cckar, swissprot: CCKAR_RAT Gastrin/cholecystokinin type B receptor (Organism: Homo sapiens, class: GPCR, accessions: P32239, gene: CCKBR, swissprot: GASR_HUMAN Gastrin/cholecystokinin type B receptor (Organism: Mus musculus, class: GPCR, accessions: P56481, gene: Cckbr, swissprot: GASR_MOUSE A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid. 1974-07-26 FDA
Click to view bisbentiamine
Click to view erythromycin acistrate Erythromycin acistrate is a erythromycin prodrug. Like other esters of erythromycin, it is partly hydrolyzed in blood and tissues to free erythromycin, which is responsible for the antibacterial activity. (See: erythromycin) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Protein Synthesis Inhibitors (Code: D011500)
Click to view levothyroxine Thyroid hormone receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10828, gene: THRB, swissprot: THB_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16053391) Thyroid hormone receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10827, gene: THRA, swissprot: THA_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20615127) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15601807) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21030469) The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines and the coupling of iodotyrosines in the thyroglobulin. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form triiodothyronine which exerts a broad spectrum of stimulatory effects on cell metabolism. l-Thyroxine (Code: N0000175945) Thyroxine (Code: N0000007632) 2000-08-21 FDA T44
Click to view iomeprol Iomeprol is benzenedicarboxamide and an organoiodine compound. It has a role as a radioopaque medium, an environmental contaminant and a xenobiotic. Iomeprol has been investigated for the diagnostic of Coronary Artery Disease. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338) 2012-12-18 Ministry of Health of the Russian Federation
Click to view vinorelbine Tubulin beta (Organism: Homo sapiens, class: Structural, accessions: Q9H4B7, gene: TUBB1, swissprot: TBB1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020388s036lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020388s036lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/8258200) Vinorelbine is a semi-synthetic vinca alkaloid. The antitumor activity of vinorelbine is thought to be due primarily to inhibition of mitosis at metaphase through its interaction with tubulin. Vinorelbine may also interfere with: 1) amino acid, cyclic AMP and glutathione metabolism, 2) calmodulin-dependent Ca++-transport ATPase activity, 3) cellular respiration, and 4) nucleic acid and lipid biosynthesis. Vinorelbine inhibited mitotic microtubule formation. Vinorelbine is indicated alone or in combination with cisplatin for first-line treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC). Vinca Alkaloid (Code: N0000175612) Vinca Alkaloids (Code: N0000007780) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Phytogenic (Code: D000972) photosensitizing agent (Code: CHEBI:47868) antineoplastic agent (Code: CHEBI:35610) 1994-12-23 FDA
Click to view gitoxin an isomer of digoxin; the OH group which is in the C16 position while it is in the C12 position for Digoxin
Click to view digoxin Sodium/potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P05023|P05026|P13637|P14415|P50993|P54709|P54710|Q13733, gene: ATP1A1|ATP1A2|ATP1A3|ATP1A4|ATP1B1|ATP1B2|ATP1B3|FXYD2, swissprot: AT1A1_HUMAN|AT1A2_HUMAN|AT1A3_HUMAN|AT1A4_HUMAN|AT1B1_HUMAN|AT1B2_HUMAN|AT1B3_HUMAN|ATNG_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/009330s033lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/009330s033lbl.pdf) A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone DIGOXIGENIN. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in ATRIAL FIBRILLATION and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666) Cardiac Glycoside (Code: N0000175568) Cardiac Glycosides (Code: N0000008157) Anti-Arrhythmia Agents (Code: D000889) Cardiotonic Agents (Code: D002316) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protective Agents (Code: D020011) anti-arrhythmia drug (Code: CHEBI:38070) cardiotonic drug (Code: CHEBI:38147) 1975-10-24 FDA DGX
Click to view rifaximin DNA-directed RNA polymerase subunit beta (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A8V2, gene: rpoB, swissprot: RPOB_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022554lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022554lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022554lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021361s023lbl.pdf) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021361s023lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021361s023lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021361s023lbl.pdf) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021361s023lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021361s023lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021361s023lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021361s011lbl.pdf) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24388834) Rifaximin is a semi-synthetic derivative of rifampin and acts by binding to the beta-subunit of bacterial DNA-dependent RNA polymerase blocking one of the steps in transcription. This results in inhibition of bacterial protein synthesis and consequently inhibits the growth of bacteria. Rifaximin is used as treatment and prevention of travelers’ diarrhea and, in higher doses, for prevention of hepatic encephalopathy in patients with advanced liver disease and to treat diarrhea in patients with irritable bowel syndrome. Rifamycin Antibacterial (Code: N0000175500) Rifamycins (Code: N0000007911) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Nucleic Acid Synthesis Inhibitors (Code: D019384) orphan drug (Code: CHEBI:71031) gastrointestinal drug (Code: CHEBI:55324) 2004-05-25 FDA RXM
Click to view canfosfamide a glutathione-based glutathione S-transferase-activated cytotoxin; TLK-286 is the ((R)-(-))-isomer
Click to view meradimate Meradimate (menthyl anthranilate) is an active ingredient used in sunscreen as a UV filter. Meradimate acts by absorbing both the UVA and UVB radiation, this provides this ingredient with a broad spectrum. Its function is related to the intrinsic structure of meradimate which is an ortho-disubstituted aminobenzoate. This structure allows easy electron delocalization and shifts in the maximum absorption. 1980-12-31 Health Canada
Click to view estradiol mustard Estrogen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P06211, gene: Esr1, swissprot: ESR1_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/992905) Estradiol mustard is a synthetic, steroidal estrogen and alkylating antineoplastic agent and a nitrogen mustard-coupled estrogen ester. Estradiol mustard is used in the treatment of prostate cancer.
Click to view metrizamide A solute for density gradient centrifugation offering higher maximum solution density without the problems of increased viscosity. It is also used as a resorbable, non-ionic contrast medium. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 1978-08-23 FDA
Click to view erythromycin propionate Erythromycin propionate is the lauryl sulfate salt of the propionic ester of erythromycin. Erythromycin propionate is a prodrug of erythromycin. (See: erythromycin) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Protein Synthesis Inhibitors (Code: D011500) 2014-01-06 NAMMDR (National Agency for Medicines and Medical Devices of Romania)
Click to view ioxilan Ioxilan is a nonionic, water soluble, triiodinated x-ray contrast agent for intravascular injection. is indicated for cerebral arteriography. Ioxilan is indicated for coronary arteriography and left ventriculography, visceral angiography, aortography, and peripheral arteriography. Also it is indicated for excretory urography and contrast enhanced computed tomographic (CECT) imaging of the head and body. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) 1995-12-21 FDA
Click to view iopromide Iopromide is a molecule used as a contrast medium. It is used in radiographic studies such as intravenous urograms, brain computer tomography and CT pulmonary angiograms. Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338) 1995-05-10 FDA
Click to view anhydrovinblastine Tubulin beta-4B chain (Organism: Homo sapiens, class: Structural, accessions: P68371, gene: TUBB4B, swissprot: TBB4B_HUMAN) Multidrug resistance-associated protein 7 (Organism: Homo sapiens, class: Transporter, accessions: Q5T3U5, gene: ABCC10, swissprot: MRP7_HUMAN) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) 1965-01-01 YEAR INTRODUCED
Click to view bisdequalinium chloride Bisdequalinium chloride is a aminoquinoline. It is used as antiseptic.
Click to view tacrolimus Peptidyl-prolyl cis-trans isomerase FKBP1A (Organism: Homo sapiens, class: Enzyme, accessions: P62942, gene: FKBP1A, swissprot: FKB1A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050708s050,050709s042,210115s002lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050708s050,050709s042,210115s002lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18827354) ATP-binding cassette sub-family A member 5 (Organism: Homo sapiens, class: Transporter, accessions: Q8WWZ7, gene: ABCA5, swissprot: ABCA5_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/18827354) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16595711) Peptidyl-prolyl cis-trans isomerase FKBP5 (Organism: Homo sapiens, class: Enzyme, accessions: Q13451, gene: FKBP5, swissprot: FKBP5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23647266) Tacrolimus is a macrolide isolated from the culture broth of a strain of Streptomyces tsukubaensis that has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro. Tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin (a ubiquitous mammalian intracellular enzyme) is then formed, after which the phosphatase activity of calcineurin is inhibited. Such inhibition prevents the dephosphorylation and translocation of various factors such as the nuclear factor of activated T-cells (NF-AT), and nuclear factor kappa-light-chain enhancer of activated B-cells (NF-?B). Tacrolimus is indicated for the prophylaxis of organ rejection in adult and pediatric patients receiving allogeneic liver, kidney or heart transplants, in combination with other immunosuppressants. Calcineurin Inhibitor Immunosuppressant (Code: N0000175457) Calcineurin Inhibitors (Code: D065095) Enzyme Inhibitors (Code: D004791) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) immunosuppressive agent (Code: CHEBI:35705) 1994-04-08 FDA FK5
Click to view solasulfone used in drug therapy of leprosy; structure
Click to view acetyldigitoxin Sodium/potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P05023|P05026|P13637|P14415|P50993|P54709|P54710|Q13733, gene: ATP1A1|ATP1A2|ATP1A3|ATP1A4|ATP1B1|ATP1B2|ATP1B3|FXYD2, swissprot: AT1A1_HUMAN|AT1A2_HUMAN|AT1A3_HUMAN|AT1A4_HUMAN|AT1B1_HUMAN|AT1B2_HUMAN|AT1B3_HUMAN|ATNG_HUMAN) inhibitor Cardioactive derivatives of lanatoside A or of DIGITOXIN. They are used for fast digitalization in congestive heart failure. anti-arrhythmia drug (Code: CHEBI:38070) cardiotonic drug (Code: CHEBI:38147) 1975-04-24 FDA
Click to view ioversol Ioversol is a sterile, nonpyrogenic, aqueous solution intended for intravascular administration as a diagnostic radiocontrast agent. Intravascular injection of ioversol opacifies vessels in the path of the flow of the contrast medium, permitting visualization of the internal structures until significant hemodilution occurs. In imaging of the body, iodinated contrast agents diffuse from the vascular into the extravascular space. In normal brain with an intact blood-brain barrier, contrast does not diffuse into the extravascular space. In patients with a disrupted blood-brain barrier, contrast agent accumulates in the interstitial space in the region of disruption. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) 1988-12-30 FDA
Click to view apatinib Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21443688) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21443688) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21443688) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21443688) Tyrosine-protein kinase CSK (Organism: Homo sapiens, class: Kinase, accessions: P41240, gene: CSK, swissprot: CSK_HUMAN) inhibitor (Source: ) Apatinib is an oral tyrosine kinase inhibitor approved in China for the treatment of patients with advanced metastatic gastric cancer. Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) China Food and Drug Administration (CFDA)
Click to view docetaxel Tubulin beta (Organism: Homo sapiens, class: Structural, accessions: Q9H4B7, gene: TUBB1, swissprot: TBB1_HUMAN) binder (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022534s007lbl.pdf) Apoptosis regulator Bcl-2 (Organism: Homo sapiens, class: Cytosolic other, accessions: P10415, gene: BCL2, swissprot: BCL2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17674353) Microtubule-associated protein 2 (Organism: Homo sapiens, class: Structural, accessions: P11137, gene: MAP2, swissprot: MTAP2_HUMAN) binder (Source: https://www.ncbi.nlm.nih.gov/pubmed/18068131) Microtubule-associated protein 4 (Organism: Homo sapiens, class: Structural, accessions: P27816, gene: MAP4, swissprot: MTAP4_HUMAN) binder (Source: https://www.ncbi.nlm.nih.gov/pubmed/18068131) Microtubule-associated protein tau (Organism: Homo sapiens, class: Structural, accessions: P10636, gene: MAPT, swissprot: TAU_HUMAN) binder (Source: https://www.ncbi.nlm.nih.gov/pubmed/18068131) Docetaxel is a semisynthetic side-chain analogue of paclitaxel with antineoplastic property. Docetaxel binds specifically to the beta-tubulin subunit of microtubules and thereby antagonizes the disassembly of the microtubule proteins. This results in the persistence of aberrant microtubule structures and results in cell-cycle arrest and subsequent cell death. Microtubule Inhibition (Code: N0000175085) Microtubule Inhibitor (Code: N0000175592) Antimitotic Agents (Code: D050256) Antineoplastic Agents (Code: D000970) Mitosis Modulators (Code: D050258) Tubulin Modulators (Code: D050257) antineoplastic agent (Code: CHEBI:35610) photosensitizing agent (Code: CHEBI:47868) antimalarial (Code: CHEBI:38068) 1996-05-14 FDA
Click to view pimecrolimus Serine/threonine-protein phosphatase 2B catalytic subunit gamma isoform (Organism: Homo sapiens, class: Enzyme, accessions: P48454, gene: PPP3CC, swissprot: PP2BC_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021302s018lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021302s018lbl.pdf) Peptidyl-prolyl cis-trans isomerase FKBP1A (Organism: Homo sapiens, class: Enzyme, accessions: P62942, gene: FKBP1A, swissprot: FKB1A_HUMAN) potentiator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021302s018lbl.pdf) Pimecrolimus is a derivative of the ascomycin macrolactam with immunosuppressant property. Pimecrolimus binds with high affinity to macrophilin-12 (FKBP-12). The pimecrolimus-FKBP complex further binds to calcineurin, an enzyme vital for the early activation of T cells. Therefore, it inhibits T cell activation by blocking the transcription of early cytokines. In particular, pimecrolimus inhibits at nanomolar concentrations Interleukin-2 and interferon gamma (Th1-type) and Interleukin-4 and Interleukin-10 (Th2-type) cytokine synthesis in human T-cells. Pimecrolimus is used for the treatment of psoriasis and allergic, irritant and atopic dermatitis. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Calcineurin Inhibitors (Code: D065095) Dermatologic Agents (Code: D003879) Enzyme Inhibitors (Code: D004791) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) Calcineurin Inhibitor Immunosuppressant (Code: N0000175457) 2001-12-13 FDA
Click to view inositol nicotinate Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) FDA
Click to view vinblastine Tubulin beta (Organism: Homo sapiens, class: Structural, accessions: Q9H4B7, gene: TUBB1, swissprot: TBB1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/1260766) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11770832) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11716514) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12739759) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21861202) Vinblastine is a Vinca alkaloid obtained from the Madagascar periwinkle plant. The mechanism of action of vinblastine has been related to the inhibition of microtubule formation in the mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. Vinblastine is used to treat Hodgkin's disease, non-Hodgkin's lymphomas, mycosis fungoides, cancer of the testis, Kaposi's sarcoma, Letterer-Siwe disease, as well as other cancers. Vinca Alkaloid (Code: N0000175612) Vinca Alkaloids (Code: N0000007780) Antimitotic Agents (Code: D050256) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Phytogenic (Code: D000972) Mitosis Modulators (Code: D050258) Tubulin Modulators (Code: D050257) 1965-11-05 FDA
Click to view aclarubicin 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) 72 kDa type IV collagenase (Organism: Homo sapiens, class: Enzyme, accessions: P08253, gene: MMP2, swissprot: MMP2_HUMAN An anthracycline produced by Streptomyces galilaeus. It has potent antineoplastic activity. Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003)
Click to view telithromycin Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021144s018lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021144s018lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17296622) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17296622) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19775168) Telithromycin belongs to the ketolide class of antibacterials and is structurally related to the macrolides. Telithromycin blocks protein synthesis by binding to domains II and V of 23S rRNA of the 50S ribosomal subunit. Telithromycin may also inhibit the assembly of nascent ribosomal units. Telithromycin has been shown to be active against most strains of the following microorganisms: Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Chlamydophila pneumoniae, Mycoplasma pneumoniae. Ketolide Antibacterial (Code: N0000175492) Ketolides (Code: N0000011414) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 2004-04-01 FDA TEL
Click to view sorbinicate
Click to view troleandomycin Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12235267) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12235267) Troleandomycin is a semi-synthetic macrolide antibiotic which used to for the treat of infections of the upper and lower respiratory tract: such as tonsillitis, bronchitis, sinusitis, and pneumonia. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1969-05-27 FDA
Click to view delafloxacin Delafloxacin belongs to the fluoroquinolone class of antibacterial drugs and is anionic in nature. The antibacterial activity of delafloxacin is due to the inhibition of both bacterial topoisomerase IV and DNA gyrase (topoisomerase II) enzymes which are required for bacterial DNA replication, transcription, repair, and recombination. Delafloxacin exhibits a concentration-dependent bactericidal activity against gram-positive and gram-negative bacteria in vitro. Fluoroquinolone Antibacterial (Code: N0000193223) Fluoroquinolones (Code: N0000011190) Anti-Infective Agents (Code: D000890) 2017-06-19 FDA
Click to view mydecamycin Midecamycin is a macrolide antibiotic. It is synthesized from Streptomyces mycarofaciens. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 2009-01-29 Ministry of Health of the Russian Federation
Click to view vinflunine Tubulin beta (Organism: Homo sapiens, class: Structural, accessions: Q9H4B7, gene: TUBB1, swissprot: TBB1_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/javlor-epar-product-information_en.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/javlor-epar-product-information_en.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/javlor-epar-product-information_en.pdf) Vinflunine is a bi-fluorinated derivative of the semi-synthetic vinca alkaloid vinorelbine with antitubulin, antineoplastic, and antiangiogenic activities. Vinflunine binds to tubulin at or near to the vinca binding sites inhibiting its polymerisation into microtubules, which results in treadmilling suppression, disruption of microtubule dynamic, mitotic arrest and apoptosis. In vivo, vinflunine displays significant antitumor activity against a broad spectrum of human xenografts in mice both in terms of survival prolongation and tumour growth inhibition. Vinflunine is indicated in monotherapy for the treatment of adult patients with advanced or metastatic transitional cell carcinoma of the urothelial tract after failure of a prior platinum-containing regimen antineoplastic agent (Code: CHEBI:35610) 2009-09-21 EMA
Click to view cystine Cystine/glutamate transporter (Organism: Homo sapiens, class: Transporter, accessions: Q9UPY5, gene: SLC7A11, swissprot: XCT_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15151999) Cystine is a sulfur-containing derivative obtained from oxidation of cysteine amino acid thiol side chains. It functions as an antioxidant and protects tissues against radiation and pollution, slowing the aging process. It also aids protein synthesis. Cystine is abundant in many proteins of skeletal tissues and skin, and found in insulin and digestive enzymes chromotrypsinogen A, papain, and trypsinogen. It is common in many foods such as eggs, meat, dairy products, and whole grains as well as skin, horns and hair. Human hair and skin contain approximately 10–14% cystine by mass. 1987-10-16 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view pralmorelin Growth hormone secretagogue receptor type 1 (Organism: Homo sapiens, class: GPCR, accessions: Q92847, gene: GHSR, swissprot: GHSR_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/15646370) Growth hormone secretagogue receptor type 1 (Organism: Rattus norvegicus, class: Unclassified, accessions: O08725, gene: Ghsr, swissprot: GHSR_RAT) agonist (Source: ) 2004-10-22 PMDA
Click to view evogliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21093089) Evogliptin is an orally bioavailable, selective dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes mellitus. DPP-4 inhibitors control glucose levels by preventing the breakdown of the incretin hormones glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1), which stimulate insulin secretion in response to the increased levels of glucose in the period following meals. 2015-10-02 Korean Food and Drug Administration (KFDA)
Click to view etiroxate Etiroxate is a synthetic thyroxine derivative. Etiroxate caused a significant reduction in serum cholesterol, LDL-cholesterol, and serum apolipoprotein B. There was a significant decrease in HDL-cholesterol. It was used for the treatment of patients with hyperlipoproteinaemia. Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847)
Click to view iohexol An effective non-ionic, water-soluble contrast agent which is used in myelography, arthrography, nephroangiography, arteriography, and other radiographic procedures. Its low systemic toxicity is the combined result of low chemotoxicity and low osmolality. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338) Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) 1985-12-26 FDA
Click to view glycyrrhizic acid Corticosteroid 11-beta-dehydrogenase isozyme 1 (Organism: Homo sapiens, class: Enzyme, accessions: P28845, gene: HSD11B1, swissprot: DHI1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19564108) Corticosteroid 11-beta-dehydrogenase isozyme 2 (Organism: Homo sapiens, class: Enzyme, accessions: P80365, gene: HSD11B2, swissprot: DHI2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19564108) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15618649) Solute carrier organic anion transporter family member 1B2 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9QZX8, gene: Slco1b2, swissprot: SO1B2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12963436) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12963436) Glycyrrhizic acid (glycyrrhizinic acid) is a triterpene glycoside found in the roots of Liquorice plants. Glycyrrhizic acid has anti-inflammatory, antiviral, and anti-allergic properties. It is metabolized to glycyrrhetinic acid, which inhibits 11-beta-hydroxysteroid dehydrogenases and other enzymes involved in the metabolism of corticosteroids. Therefore, glycyrrhizic acid, which is the main and sweet component of licorice, has been investigated for its ability to cause hypermineralocorticoidism with sodium retention and potassium loss, edema, increased blood pressure, as well as depression of the renin-angiotensin-aldosterone system. Glycyrrhizic acid is used for the treatment of of premenstrual syndrome, treatment of viral infections, anti-lipidemic and antihyperglycemic. It is also known to be used as a remedy for peptic ulcer and other stomach diseases. Anti-Inflammatory Agents (Code: D000893)
Click to view rifampicin DNA-directed RNA polymerase subunit beta (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WGY9, gene: rpoB, swissprot: RPOB_MYCTU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050420s080,050627s023lbl.pdf) DNA-directed RNA polymerase subunit beta (Organism: Neisseria meningitidis serogroup B (strain MC58), class: Enzyme, accessions: Q59622, gene: rpoB, RPOB_NEIMB) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050420s080,050627s023lbl.pdf) DNA-directed RNA polymerase subunit beta (Organism: Neisseria meningitidis serogroup C / serotype 2a (strain ATCC 700532 / DSM 15464 / FAM18), class: Enzyme, accessions: A1KRG6, gene: rpoB, RPOB_NEIMF) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050420s080,050627s023lbl.pdf) DNA-directed RNA polymerase subunit beta (Organism: Neisseria meningitidis serogroup A / serotype 4A (strain Z2491), class: Enzyme, accessions: P57009, gene: rpoB, RPOB_NEIMA) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/050420s080,050627s023lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Solute carrier organic anion transporter family member 1A4 (Organism: Rattus norvegicus, class: Transporter, accessions: O35913, gene: Slco1a4, swissprot: SO1A4_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12085361) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inducer (Source: https://www.medsafe.govt.nz/profs/Datasheet/r/Rifadin.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.medsafe.govt.nz/profs/Datasheet/r/Rifadin.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inducer (Source: https://www.medsafe.govt.nz/profs/Datasheet/r/Rifadin.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inducer (Source: https://www.medsafe.govt.nz/profs/Datasheet/r/Rifadin.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inducer (Source: https://www.medsafe.govt.nz/profs/Datasheet/r/Rifadin.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.medsafe.govt.nz/profs/Datasheet/r/Rifadin.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inducer (Source: https://www.medsafe.govt.nz/profs/Datasheet/r/Rifadin.pdf) Canalicular multispecific organic anion transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q92887, gene: ABCC2, swissprot: MRP2_HUMAN) inducer (Source: https://www.medsafe.govt.nz/profs/Datasheet/r/Rifadin.pdf) Lanosterol 14-alpha demethylase (Organism: Homo sapiens, class: Enzyme, accessions: Q16850, gene: CYP51A1, swissprot: CP51A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17194716) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) Bile salt export pump (Organism: Rattus norvegicus, class: Unclassified, accessions: O70127, gene: Abcb11, swissprot: ABCBB_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21965623) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/26905831) Rifampin is a semisynthetic derivative of rifamycin with broad antibacterial activity. Rifampin inhibits DNA-dependent RNA polymerase in susceptible bacteria and is often used in combination with other antibiotics for various infections including tuberculosis. Rifamycin Antibacterial (Code: N0000175500) Rifamycins (Code: N0000007911) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antibiotics, Antitubercular (Code: D000904) Antitubercular Agents (Code: D000995) Cytochrome P-450 CYP2B6 Inducers (Code: D065695) Cytochrome P-450 CYP2C19 Inducers (Code: D065697) Cytochrome P-450 CYP2C8 Inducers (Code: D065696) Cytochrome P-450 CYP2C9 Inducers (Code: D065698) Cytochrome P-450 CYP3A Inducers (Code: D065701) Enzyme Inhibitors (Code: D004791) Leprostatic Agents (Code: D007917) Metabolic Side Effects of Drugs and Substances (Code: D065606) Nucleic Acid Synthesis Inhibitors (Code: D019384) 1971-05-21 FDA RFP
Click to view polmacoxib Prostaglandin G/H synthase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P35354, gene: PTGS2, swissprot: PGH2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22278334) Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/14761182) Polmacoxib is a nonsteroidal anti-inflammatory drug (NSAID) used to treat osteoarthritis. It is a selective COX-2 inhibitor. 2015-02-05 Korean Food and Drug Administration (KFDA) 949
Click to view betrixaban Coagulation factor X (Organism: Homo sapiens, class: Enzyme, accessions: P00742, gene: F10, swissprot: FA10_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208383s000lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Betrixaban is an oral FXa inhibitor that selectively blocks the active site of FXa and does not require a cofactor (such as Anti-thrombin III) for activity. Betrixaban inhibits free FXa and prothrombinase activity. By directly inhibiting FXa, betrixaban decreases thrombin generation. Betrixaban has no direct effect on platelet aggregation. Factor Xa Inhibitor (Code: N0000175637) Anticoagulants (Code: D000925) Antithrombins (Code: D000991) Enzyme Inhibitors (Code: D004791) Factor Xa Inhibitors (Code: D065427) Hematologic Agents (Code: D006401) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) anticoagulant (Code: CHEBI:50249) 2017-06-23 FDA
Click to view acetyldigoxin Alpha- or beta-acetyl derivatives of DIGOXIN or lanatoside C from Digitalis lanata. They are better absorbed and longer acting than digoxin and are used in congestive heart failure.
Click to view vincristine Tubulin beta (Organism: Homo sapiens, class: Structural, accessions: Q9H4B7, gene: TUBB1, swissprot: TBB1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202497s000lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202497s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202497s000lbl.pdf) Multidrug resistance-associated protein 7 (Organism: Homo sapiens, class: Transporter, accessions: Q5T3U5, gene: ABCC10, swissprot: MRP7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12527806) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10617675) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Vincristine is a vinca alkaloid isolated as a 1:1 sulfate salt from the periwinkle plant (Catharanthus roseus). Vincristine binds to tubulin, altering the tubulin polymerization equilibrium, resulting in altered microtubule structure and function. Vincristine is indicated for the treatment of adult patients with Philadelphia chromosome-negative (Ph-) acute lymphoblastic leukemia (ALL) in second or greater relapse or whose disease has progressed following two or more anti-leukemia therapies. Antimitotic Agents (Code: D050256) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Phytogenic (Code: D000972) Mitosis Modulators (Code: D050258) Tubulin Modulators (Code: D050257) Vinca Alkaloid (Code: N0000175612) Vinca Alkaloids (Code: N0000007780) 1963-07-10 FDA
Click to view rokitamycin
Click to view josamycin Josamycin is a macrolide antibiotic produced by Streptomyces narbonensis var. josamyceticus. It is similar to erythromycin, but does not induce macrolide resistance in staphylococci and appears to have a lower incidence of gastrointestinal side effects. The mechanism of action of macrolides such as Josamycin is via inhibition of bacterial protein biosynthesis by binding reversibly to the subunit 50S of the bacterial ribosome, thereby inhibiting translocation of peptidyl tRNA. This action is mainly bacteriostatic, but can also be bactericidal in high concentrations. Macrolides tend to accumulate within leukocytes, and are therefore actually transported into the site of infection. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 1981-05-18 Italian Medicines Agency (AIFA) JOS
Click to view eptifibatide Integrin alpha-IIb/beta-3 (Organism: Homo sapiens, class: Adhesion, accessions: P05106|P08514, gene: ITGA2B|ITGB3, swissprot: ITA2B_HUMAN|ITB3_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/020718s037lbl.pdf) used in clinical studies as a platelet glycoprotein IIB/IIIA antagonist Decreased Platelet Aggregation (Code: N0000008832) Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) platelet aggregation inhibitor (Code: CHEBI:50427) anticoagulant (Code: CHEBI:50249) 1998-05-18 FDA
Click to view dirithromycin Dirithromycin is a semi-synthetic macrolide antibiotic pro-drug. Dirithromycin is converted by hydrolysis during intestinal absorption into the microbiologically active erythromycylamine. Erythromycylamine binds to the 50 S subunit of the 70 S ribosome of susceptible organisms, thereby inhibiting bacterial RNA-dependent protein synthesis. This antibiotic is used in the treatment of infections of the respiratory tract, skin and soft tissue caused by gram-positive microorganisms, including S. aureus, S. pneumonia and pyogenes, gram-negative microorganisms, including H. influenzae, L. pneumophila, M. catarrhalis, and M. pneumoniae. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) prodrug (Code: CHEBI:50266) 1995-06-19 FDA eryth
Click to view iopentol Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907)
Click to view iobitridol a nonionic monomeric low-osmolality contrast medium; structure given in second source Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907)
Click to view roxithromycin Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) weak inhibitor (Source: https://www.medsafe.govt.nz/profs/Datasheet/a/ArrowRoxithromycintab.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17164692) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17164692) Motilin receptor (Organism: Homo sapiens, class: GPCR, accessions: O43193, gene: MLNR, swissprot: MTLR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10381885) Roxithromycin is a semi-synthetic derivative of the macrolide antibiotic erythromycin that includes an N-oxime side chain on the lactone ring, with antibacterial and anti-malarial activities. Roxithromycin binds to the subunit 50S of the bacterial ribosome, which inhibits bacterial protein synthesis and leads to inhibition of bacterial cell growth and replication. Roxithromycin has been demonstrated to have in vitro and clinical activity against the following micro-organisms: Streptococcus pneumoniae, Strep. pyogenes, Mycoplasma pneumoniae, Moraxella catarrhalis, Ureaplasma urealyticum and Chlamydia sp. Roxithromycin is used for the treatment of respiratory and genital tract infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1987-01-01 YEAR INTRODUCED ROX
Click to view Spiramycin I Spiramycin I is a macrolide antibiotic produced by Streptomyces ambofaciens. It is active against the following Gram-positive organisms: Staphylococcus aureus (including penicillin-resistant strains), ?-haemolytic streptococci, Streptococcus viridans, Streptococcus faecalis and Streptococcus pneumoniae, Corynebacterium diphteriae, clostridia. Except for Bordetella pertussis, Hemophilus influenzae (approximately 50% of strains) and neisseria, gram-negative organisms are generally considered as resistant to spiramycin. antibacterial drug (Code: CHEBI:36047) 1957-12-31 Health Canada SPR
Click to view dodeclonium bromide
Click to view proglumetacin Proglumetacin is a pdrodrug of indometacin and proglumide. Following oral administration, it is metabolised to indometacin and proglumide, a drug with antisecretory effects that helps prevent injury to the stomach lining. Proglumetacin is used as its dimaleate salt to control pain and inflammation associated with musculoskeletal and joint disorders. (See: indometacin) (See: proglumide) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) antipyretic (Code: CHEBI:35493) prodrug (Code: CHEBI:50266) 1994-06-01 PMDA
Click to view rifabutin DNA-directed RNA polymerase subunit alpha (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A7Z4, gene: rpoA, swissprot: RPOA_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050689Orig1s018lbl.pdf) DNA-directed RNA polymerase subunit beta (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A8V2, gene: rpoB, swissprot: RPOB_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050689Orig1s018lbl.pdf) DNA-directed RNA polymerase subunit beta' (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0A8T7, gene: rpoC, swissprot: RPOC_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050689Orig1s018lbl.pdf) DNA-directed RNA polymerase subunit alpha (Organism: Bacillus subtilis (strain 168), class: Enzyme, accessions: P20429, gene: rpoA, swissprot: RPOA_BACSU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050689Orig1s018lbl.pdf) DNA-directed RNA polymerase subunit beta (Organism: Bacillus subtilis (strain 168), class: Enzyme, accessions: P37870, gene: rpoB, swissprot: RPOB_BACSU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050689Orig1s018lbl.pdf) DNA-directed RNA polymerase subunit beta' (Organism: Bacillus subtilis (strain 168), class: Enzyme, accessions: P37871, gene: rpoC, swissprot: RPOC_BACSU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050689Orig1s018lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/050689Orig1s018lbl.pdf) Rifabutin is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties. Rifabutin inhibits bacterial DNA-dependent RNA polymerase. Rifabutin is indicated for the prevention of disseminated Mycobacterium avium complex disease in patients with advanced HIV infection. Rifamycin Antimycobacterial (Code: N0000175501) Rifamycins (Code: N0000007911) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antibiotics, Antitubercular (Code: D000904) Antitubercular Agents (Code: D000995) antitubercular agent (Code: CHEBI:33231) 1992-12-23 FDA RBT
Click to view paclitaxel Tubulin beta chain (Organism: Homo sapiens, class: Structural, accessions: P07437, gene: TUBB, swissprot: TBB5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021660s045lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021660s045lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021660s045lbl.pdf) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18839173) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12739759) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhbitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11716514) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11504826) Multidrug resistance-associated protein 7 (Organism: Homo sapiens, class: Transporter, accessions: Q5T3U5, gene: ABCC10, swissprot: MRP7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12527806) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16210916) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25618019) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25618019) Tubulin beta (Organism: Homo sapiens, class: Structural, accessions: P04350|P07437|P68371|Q13509|Q13885|Q3ZCM7|Q9BUF5|Q9BVA1|Q9H4B7, gene: TUBB|TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB6|TUBB8, swissprot: TBB1_HUMAN|TBB2A_HUMAN|TBB2B_HUMAN|TBB3_HUMAN|TBB4A_HUMAN|TBB4B_HUMAN|TBB5_HUMAN|TBB6_HUMAN|TBB8_HUMAN) inhibitor (Source: ) Botulinum neurotoxin type A (Organism: Clostridium botulinum, class: Enzyme, accessions: P10845, gene: botA, swissprot: BXA1_CLOBO) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23484537) Tyrosine-protein kinase Mer (Organism: Homo sapiens, class: Kinase, accessions: Q12866, gene: MERTK, swissprot: MERTK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27238842) Paclitaxel is a compound extracted from the Pacific yew tree Taxus brevifolia with antineoplastic activity. Paclitaxel binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Paclitaxel induces abnormal arrays or “bundles” of microtubules throughout the cell cycle and multiple asters of microtubules during mitosis. Paclitaxel is used in the treatment of Kaposi's sarcoma and cancer of the lung, ovarian, and breast. Antimitotic Agents (Code: D050256) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Phytogenic (Code: D000972) Mitosis Modulators (Code: D050258) Tubulin Modulators (Code: D050257) antineoplastic agent (Code: CHEBI:35610) Microtubule Inhibition (Code: N0000175085) Microtubule Inhibitor (Code: N0000175592) 1992-12-29 FDA
Click to view erythromycin ethyl succinate Erythromycin ethylsuccinate is an ester of erythromycin suitable for oral administration. Erythromycin ethylsuccinate is a prodrug of erythromycin. (See: erythromycin) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Enzyme Inhibitors (Code: D004791) Gastrointestinal Agents (Code: D005765) Protein Synthesis Inhibitors (Code: D011500) 1965-04-02 FDA
Click to view evans blue Tyrosine-protein phosphatase non-receptor type 1 (Organism: Homo sapiens, class: Enzyme, accessions: P18031, gene: PTPN1, swissprot: PTN1_HUMAN Tyrosine-protein phosphatase 1 (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P25044, gene: PTP1, swissprot: PTP1_YEAST Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q13822, gene: ENPP2, swissprot: ENPP2_HUMAN Vesicular glutamate transporter 3 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q7TSF2, gene: Slc17a8, swissprot: VGLU3_RAT An azo dye used in blood volume and cardiac output measurement by the dye dilution method. It is very soluble, strongly bound to plasma albumin, and disappears very slowly. Coloring Agents (Code: D004396) histological dye (Code: CHEBI:77178) fluorochrome (Code: CHEBI:51217) FDA
Click to view rifapentine DNA-directed RNA polymerase subunit beta (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WGY9, gene: rpoB, swissprot: RPOB_MYCTU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021024s011lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021024s011lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021024s011lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021024s011lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/9402947) Rifapentine, a cyclopentyl rifamycin, inhibits DNA-dependent RNA polymerase in susceptible strains of Mycobacterium tuberculosis but does not affect mammalian cells at concentrations that are active against these bacteria. At therapeutic levels, rifapentine inhibits RNA transcription by preventing the initiation of RNA chain formation. It forms a stable complex with bacterial DNA-dependent RNA polymerase, leading to repression of RNA synthesis and cell death. Rifapentine and its 25-desacetyl metabolite accumulate in human monocyte-derived macrophages and are bactericidal to both intracellular and extracellular M. tuberculosis bacilli. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antibiotics, Antitubercular (Code: D000904) Antitubercular Agents (Code: D000995) Leprostatic Agents (Code: D007917) antitubercular agent (Code: CHEBI:33231) leprostatic drug (Code: CHEBI:35816) Rifamycin Antimycobacterial (Code: N0000175501) Rifamycins (Code: N0000007911) 1998-06-22 FDA RPT
Click to view Spiramycin II antibacterial drug (Code: CHEBI:36047)
Click to view romurtide a synthetic muramyl dipeptide analog; stimulates chemotactic mobility, phagocytic activity & superoxide production by neutrophils in mice; used for the prophylaxis of leukocytopenia during radiation therapy; structure given in first source Adjuvants, Immunologic (Code: D000276) Immunologic Factors (Code: D007155)
Click to view miocamycin A macrolide antibiotic that has a wide antimicrobial spectrum and is particularly effective in respiratory and genital infections. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890)
Click to view ioglycamic acid A radiopaque medium. It is a mixture of its meglumine and sodium salts and is used to visualize the biliary tract. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907)
Click to view Spiramycin III
Click to view saralasin Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) antagonist Type-1B angiotensin II receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P29089, gene: Agtr1b, swissprot: AGTRB_RAT Type-2 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P50052, gene: AGTR2, swissprot: AGTR2_HUMAN Angiotensin II receptor (AT-1) type-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P25095|P29089, gene: Agtr1|Agtr1b, swissprot: AGTRA_RAT|AGTRB_RAT Type-2 angiotensin II receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P35351, gene: Agtr2, swissprot: AGTR2_RAT) antagonist (Source: ) An octapeptide analog of angiotensin II (bovine) with amino acids 1 and 8 replaced with sarcosine and alanine, respectively. It is a highly specific competitive inhibitor of angiotensin II that is used in the diagnosis of HYPERTENSION. Angiotensin II Type 1 Receptor Blockers (Code: D047228) Angiotensin Receptor Antagonists (Code: D057911) FDA
Click to view sirolimus Peptidyl-prolyl cis-trans isomerase FKBP1A (Organism: Homo sapiens, class: Enzyme, accessions: P62942, gene: FKBP1A, swissprot: FKB1A_HUMAN) binder (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021083s064,021110s083lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021083s064,021110s083lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021083s064,021110s083lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14530907) Sirolimus is a natural macrocyclic lactone produced by the bacterium Streptomyces hygroscopicus, with immunosuppressant properties. In cells, sirolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. This results in inhibition of T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (IL-2, IL-4, and IL-15) stimulation and inhibition of antibody production. Sirolimus is used alone or in combination with calcineurin inhibitors to prevent cellular rejection after organ transplantation. Decreased Immunologic Activity (Code: N0000175550) mTOR Inhibitor Immunosuppressant (Code: N0000175625) mTOR Inhibitors (Code: N0000175624) Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antibiotics, Antineoplastic (Code: D000903) Antifungal Agents (Code: D000935) Antineoplastic Agents (Code: D000970) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) immunosuppressive agent (Code: CHEBI:35705) antineoplastic agent (Code: CHEBI:35610) antibacterial drug (Code: CHEBI:36047) 1999-09-15 FDA RAP
Click to view cargutocin
Click to view ceruletide Cholecystokinin receptor type A (Organism: Homo sapiens, class: GPCR, accessions: P32238, gene: CCKAR, swissprot: CCKAR_HUMAN) agonist A specific decapeptide obtained from the skin of Hila caerulea, an Australian amphibian. Caerulein is similar in action and composition to CHOLECYSTOKININ. It stimulates gastric, biliary, and pancreatic secretion; and certain smooth muscle. It is used in paralytic ileus and as diagnostic aid in pancreatic malfunction. diagnostic agent (Code: CHEBI:33295) gastrointestinal drug (Code: CHEBI:55324) FDA
Click to view gitoformate
Click to view amphotericin B Ergosterol (Organism: None, class: Metabolite, accessions: None, gene: None, swissprot: None) binder (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/050740s021lbl.pdf) Amphotericin B is a macrocyclic, polyene, antifungal antibiotic produced from a strain of Streptomyces nodosus. Amphotericin B acts by binding to the sterol component, ergosterol, of the cell membrane of susceptible fungi. It forms transmembrane channels leading to alterations in cell permeability through which monovalent ions (NA+, K+, H+, and Cl-) leak out of the cell resulting in cell death. While amphotericin B has a higher affinity for the ergosterol component of the fungal cell membrane, it can also bind to the cholesterol component of the mammalian cell leading to cytotoxicity. Amphotericin B is indicated for the empirical therapy for presumed fungal infection in febrile, neutropenic patients, for the treatment of Cryptococcal Meningitis in HIV infected patients, for the treatment of visceral leishmaniasis and Aspergillus spp., Candida spp., Cryptococcus spp. infections. Lipid-based Polyene Antifungal (Code: N0000175510) Polyene Antifungal (Code: N0000175498) Polyenes (Code: N0000007672) Amebicides (Code: D000563) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) antiprotozoal drug (Code: CHEBI:35820) 1964-11-12 FDA
Click to view nystatin Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22541068) Nystatin is an antibiotic which is both fungistatic and fungicidal in vitro against a wide variety of yeasts and yeast-like fungi, including Candida albicans, C. parapsilosis, C. tropicalis, C. guilliermondi, C. pseudotropicalis, C. krusei, Torulopsis glabrata, Tricophyton rubrum, T. mentagrophytes. Nystatin acts by binding to sterols in the cell membrane of susceptible species resulting in a change in membrane permeability and the subsequent leakage of intracellular components. Nystatin is used largely to treat skin and oropharyngeal candidiasis. Polyene Antifungal (Code: N0000175498) Polyenes (Code: N0000007672) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Ionophores (Code: D007476) Membrane Transport Modulators (Code: D049990) 1964-07-08 FDA
Click to view atracurium Acetylcholine receptor (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/20551Orig1s026lbl.pdf) Atracurium is a non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents. Atracurium antagonizes the neurotransmitter action of acetylcholine by binding competitively with cholinergic receptor sites on the motor end-plate. This antagonism is inhibited, and neuromuscular block reversed, by acetylcholinesterase inhibitors such as neostigmine, edrophonium, and pyridostigmine. Cisatracurium is a cis-cis isomer of atracurium and five time as potent as atracurium. Atracurium and cisatracurium is indicated as an adjunct to general anesthesia to facilitate tracheal intubation, to provide skeletal muscle relaxation during surgery and for mechanical ventilation in the ICU. Neuromuscular Nondepolarizing Blockade (Code: N0000175732) Nondepolarizing Neuromuscular Blocker (Code: N0000175720) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373) muscle relaxant (Code: CHEBI:51371) nicotinic antagonist (Code: CHEBI:48878) Atracurium: 1983-11-23 FDA Cisatracurium: 1995-12-15 FDA
Click to view cangrelor P2Y purinoceptor 12 (Organism: Homo sapiens, class: GPCR, accessions: Q9H244, gene: P2RY12, swissprot: P2Y12_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204958lbl.pdf) P2Y purinoceptor 13 (Organism: Homo sapiens, class: GPCR, accessions: Q9BPV8, gene: P2RY13, swissprot: P2Y13_HUMAN) antagonist (Source: ) Uracil nucleotide/cysteinyl leukotriene receptor (Organism: Mus musculus, class: Unclassified, accessions: Q6NS65, gene: Gpr17, swissprot: GPR17_MOUSE) antagonist (Source: ) Cangrelor is a direct P2Y12 platelet receptor inhibitor that blocks ADP-induced platelet activation and aggregation. Cangrelor binds selectively and reversibly to the P2Y12 receptor to prevent further signaling and platelet activation. Hematologic Agents (Code: D006401) Neurotransmitter Agents (Code: D018377) Platelet Aggregation Inhibitors (Code: D010975) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P2 Receptor Antagonists (Code: D058919) Purinergic P2Y Receptor Antagonists (Code: D058921) platelet aggregation inhibitor (Code: CHEBI:50427) P2Y12 Platelet Inhibitor (Code: N0000182142) Decreased Platelet Aggregation (Code: N0000008832) P2Y12 Receptor Antagonists (Code: N0000182143) 2015-03-23 EMA
Click to view oxytocin Oxytocin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30559, gene: OXTR, swissprot: OXYR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/018261s031lbl.pdf) Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12036367) Vasopressin V1a receptor (Organism: Homo sapiens, class: GPCR, accessions: P37288, gene: AVPR1A, swissprot: V1AR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/12036367) Vasopressin V1b receptor (Organism: Homo sapiens, class: GPCR, accessions: P47901, gene: AVPR1B, swissprot: V1BR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24874785) Recombinant Oxytocin is a synthetic cyclic peptide form of the naturally occurring posterior pituitary hormone oxytocin. Oxytocin binds to oxytocin receptors in the uterine myometrium. Oxytocin is indicated for the initiation or improvement of uterine contractions, where this is desirable and considered suitable for reasons of fetal or maternal concern, in order to achieve vaginal delivery, to produce uterine contractions during the third stage of labor and to control postpartum bleeding or hemorrhage. Increased Uterine Smooth Muscle Contraction or Tone (Code: N0000009705) Oxytocin (Code: N0000006473) Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102) oxytocic (Code: CHEBI:36063) vasodilator agent (Code: CHEBI:35620) 1980-04-17 FDA
Click to view demoxytocin Oxytocin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30559, gene: OXTR, swissprot: OXYR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24874785) Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24874785) Vasopressin V1a receptor (Organism: Homo sapiens, class: GPCR, accessions: P37288, gene: AVPR1A, swissprot: V1AR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24874785) Vasopressin V1b receptor (Organism: Homo sapiens, class: GPCR, accessions: P47901, gene: AVPR1B, swissprot: V1BR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24874785) Demoxytocin is a synthetic analogue of oxytocin that is used for induction and augmentation of labour. Oxytocics (Code: D010120) Reproductive Control Agents (Code: D012102)
Click to view octreotide Somatostatin receptor type 1 (Organism: Homo sapiens, class: GPCR, accessions: P30872, gene: SSTR1, swissprot: SSR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15103227) Somatostatin receptor type 4 (Organism: Homo sapiens, class: GPCR, accessions: P31391, gene: SSTR4, swissprot: SSR4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15103227) Somatostatin receptor type 5 (Organism: Homo sapiens, class: GPCR, accessions: P35346, gene: SSTR5, swissprot: SSR5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15103227) Somatostatin receptor type 3 (Organism: Homo sapiens, class: GPCR, accessions: P32745, gene: SSTR3, swissprot: SSR3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15103227) Somatostatin receptor type 2 (Organism: Homo sapiens, class: GPCR, accessions: P30874, gene: SSTR2, swissprot: SSR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15103227) Somatostatin receptor type 5 (Organism: Mus musculus, class: GPCR, accessions: O08858, gene: Sstr5, swissprot: SSR5_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10818261) Somatostatin receptor type 2 (Organism: Mus musculus, class: GPCR, accessions: P30875, gene: Sstr2, swissprot: SSR2_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10818261) Octreotide is a potent, long-acting synthetic somatostatin octapeptide analog that inhibits secretion of growth hormone and is used to treat hormone-secreting tumors. Somatostatin Analog (Code: N0000175904) Somatostatin Receptor Agonists (Code: N0000000194) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Gastrointestinal Agents (Code: D005765) hormone agonist (Code: CHEBI:51060) 1988-10-21 FDA
Click to view quinupristin component of RP 59500 Streptogramin Antibacterial (Code: N0000175502) Streptogramins (Code: N0000011418) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1999-09-21 FDA
Click to view mivacurium Acetylcholine receptor (Organism: Homo sapiens, class: Ion channel, accessions: P02708|P11230|Q07001, gene: CHRNA1|CHRNB1|CHRND, swissprot: ACHA_HUMAN|ACHB_HUMAN|ACHD_HUMAN) antagonist Neuronal acetylcholine receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: Q15822, gene: CHRNA2, swissprot: ACHA2_HUMAN) a short-acting nondepolarizing agent; RN from Toxlit 6/88 Neuromuscular Agents (Code: D009465) Neuromuscular Blocking Agents (Code: D009466) Neuromuscular Nondepolarizing Agents (Code: D003473) Peripheral Nervous System Agents (Code: D018373) 1992-01-22 FDA
Click to view sonidegib Smoothened homolog (Organism: Homo sapiens, class: GPCR, accessions: Q99835, gene: SMO, swissprot: SMO_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/22042473) Sonic hedgehog protein (Organism: Mus musculus, class: Enzyme, accessions: Q62226, gene: Shh, swissprot: SHH_MOUSE specific Smoothened/Smo antagonist Hedgehog Pathway Inhibitor (Code: N0000184149) Smoothened Receptor Antagonists (Code: N0000184148) antineoplastic agent (Code: CHEBI:35610) 2015-06-25 EMA
Click to view lumacaftor Cystic fibrosis transmembrane conductance regulator (Organism: Homo sapiens, class: Ion channel, accessions: P13569, gene: CFTR, swissprot: CFTR_HUMAN) pharmacological chaperone (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/206038Orig1s000lbl.pdf) Lumacaftor improves the conformational stability of F508del-CFTR, resulting in increased processing and trafficking of mature protein to the cell surface. Cytochrome P450 3A Inducers (Code: N0000190118) Cytochrome P450 2B6 Inducers (Code: N0000187064) Cytochrome P450 2C8 Inducers (Code: N0000187063) Cytochrome P450 2C9 Inducers (Code: N0000185507) Cytochrome P450 2C19 Inducers (Code: N0000185607) Cytochrome P450 2C8 Inhibitors (Code: N0000187062) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) P-Glycoprotein Inducers (Code: N0000191264) P-Glycoprotein Inhibitors (Code: N0000185503) orphan drug (Code: CHEBI:71031) 2015-07-02 FDA
Click to view desmopressin Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201656lbl.pdf) Oxytocin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30559, gene: OXTR, swissprot: OXYR_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24874785) Vasopressin V1b receptor (Organism: Homo sapiens, class: GPCR, accessions: P47901, gene: AVPR1B, swissprot: V1BR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24874785) Desmopressin is a vasopressin analogue of the natural pituitary hormone 8-arginine vasopressin (ADH), an antidiuretic hormone affecting renal water conservation. The antidiuretic effects of desmopressin are mediated by stimulation of vasopressin 2 (V2) receptors, thereby increasing water re-absorption in the kidney, and hence reducing urine production. Desmopressin is a replacement hormone for antidiuretic hormone in the treatment of central diabetes insipidus. The change in structure of arginine vasopressin to desmopressin acetate resulted in a decreased vasopressor action and decreased actions on visceral smooth muscle relative to the enhanced antidiuretic activity, so that clinically effective antidiuretic doses were usually below threshold levels for effects on vascular or visceral smooth muscle. Desmopressin is indicated as antidiuretic replacement therapy in the management of central diabetes insipidus. Also desmopressin is used to prevent and control excessive thirst, urination, and dehydration caused by injury, surgery, and certain medical conditions. It is also used in the diagnosis of cranial diabetes insipidus and in tests of renal function. vasopressin receptor agonist (Code: CHEBI:59727) renal agent (Code: CHEBI:35846) diagnostic agent (Code: CHEBI:33295) Factor VIII Activator (Code: N0000175916) Increased Coagulation Factor VIII Activity (Code: N0000175914) Increased Coagulation Factor VIII Concentration (Code: N0000175915) Vasopressin Analog (Code: N0000175905) Vasopressins (Code: N0000006320) 1978-02-21 FDA
Click to view vasopressin Vasopressin V2 receptor (Organism: Sus scrofa, class: GPCR, accessions: P32307, gene: AVPR2, swissprot: V2R_PIG Vasopressin V2 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: Q00788, gene: Avpr2, swissprot: V2R_RAT Oxytocin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30559, gene: OXTR, swissprot: OXYR_HUMAN Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) agonist Vasopressin V1a receptor (Organism: Homo sapiens, class: GPCR, accessions: P37288, gene: AVPR1A, swissprot: V1AR_HUMAN) agonist Vasopressin V1b receptor (Organism: Homo sapiens, class: GPCR, accessions: P47901, gene: AVPR1B, swissprot: V1BR_HUMAN) agonist Vasopressin V2 receptor (Organism: Bos taurus, class: GPCR, accessions: P48044, gene: AVPR2, swissprot: V2R_BOVIN Vasopressin V1b receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P48974, gene: Avpr1b, swissprot: V1BR_RAT Vasopressin V1a receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30560, gene: Avpr1a, swissprot: V1AR_RAT Vasopressin V1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30560|P48974, gene: Avpr1a|Avpr1b, swissprot: V1AR_RAT|V1BR_RAT Oxytocin receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P70536, gene: Oxtr, swissprot: OXYR_RAT Vasopressin (argipressin) is a synthetic peptide identical to the endogenous nonapeptide hormone with antidiuretic property. Synthesized in the hypothalamus and stored/released from the posterior lobe of the pituitary, argipressin's primary function is regulating extracellular fluid volume. This agent can also act as a vasoconstrictor, increasing blood pressure and systemic vascular resistance. Vasopressin is indicated to increase blood pressure in adults with vasodilatory shock (e.g., post-cardiotomy or sepsis) who remain hypotensive despite fluids and catecholamines. Antidiuretic Agents (Code: D050034) Cardiovascular Agents (Code: D002317) Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) Natriuretic Agents (Code: D045283) Vasoconstrictor Agents (Code: D014662) 2014-04-17 FDA
Click to view plicamycin DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) other (Source: http://www.ncbi.nlm.nih.gov/pubmed/1828228) A tricyclic pentaglycosidic antibiotic from Streptomyces strains that inhibits RNA and protein synthesis by adhering to DNA. It is used as a fluorescent dye and as an antineoplastic agent, especially in bone and testicular tumors. Plicamycin is also used to reduce hypercalcemia, especially that due to malignancies. Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Coloring Agents (Code: D004396) Enzyme Inhibitors (Code: D004791) Fluorescent Dyes (Code: D005456) Indicators and Reagents (Code: D007202) Luminescent Agents (Code: D049408) Nucleic Acid Synthesis Inhibitors (Code: D019384) Protein Synthesis Inhibitors (Code: D011500) antineoplastic agent (Code: CHEBI:35610) 1970-05-05 FDA
Click to view lypressin Vasopressin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518|P37288|P47901, gene: AVPR1A|AVPR1B|AVPR2, swissprot: V1AR_HUMAN|V1BR_HUMAN|V2R_HUMAN) agonist The porcine antidiuretic hormone (VASOPRESSINS). It is a cyclic nonapeptide that differs from ARG-VASOPRESSIN by one amino acid, containing a LYSINE at residue 8 instead of an ARGININE. Lys-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE. Antidiuretic Agents (Code: D050034) Cardiovascular Agents (Code: D002317) Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) Natriuretic Agents (Code: D045283) Vasoconstrictor Agents (Code: D014662) FDA
Click to view lanreotide Somatostatin receptor type 4 (Organism: Homo sapiens, class: GPCR, accessions: P31391, gene: SSTR4, swissprot: SSR4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7988476) Somatostatin receptor type 5 (Organism: Homo sapiens, class: GPCR, accessions: P35346, gene: SSTR5, swissprot: SSR5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7988476) Somatostatin receptor type 2 (Organism: Homo sapiens, class: GPCR, accessions: P30874, gene: SSTR2, swissprot: SSR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7988476) Somatostatin receptor type 3 (Organism: Homo sapiens, class: GPCR, accessions: P32745, gene: SSTR3, swissprot: SSR3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7988476) Somatostatin receptor type 1 (Organism: Homo sapiens, class: GPCR, accessions: P30872, gene: SSTR1, swissprot: SSR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10433861) Lanreotide is a synthetic cyclic octapeptide analogue of somatostatin. Lanreotide binds to somatostatin receptors, specifically SSTR-2 and also to SSTR-5 with a lesser affinity. Lanreotide is usually given as a prolonged-release microparticle or Autogel formulation for the treatment of acromegaly and to relieve the symptoms of neuroendocrine tumors. Somatostatin Analog (Code: N0000175904) Somatostatin Receptor Agonists (Code: N0000000194) Antineoplastic Agents (Code: D000970) Cardiovascular Agents (Code: D002317) 2007-08-30 FDA
Click to view caspofungin Beta-1,3-glucan synthase catalytic subunit 1 (Organism: Candida albicans, class: Enzyme, accessions: O13428, gene: GSC1, swissprot: O13428_CANAX) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021227s039lbl.pdf) 1,3-beta-glucan synthase component FKS1 (Organism: Aspergillus niger (strain CBS 513.88 / FGSC A1513), class: Enzyme, accessions: A2QLK4, gene: fksA, swissprot: FKS1_ASPNC) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16207161) Caspofungin, an echinocandin, inhibits the synthesis of beta (1,3)-D-glucan, an essential component of the cell wall of susceptible Aspergillus species and Candida species. Beta (1,3)-D-glucan is not present in mammalian cells. Caspofungin has shown activity against Candida species and in regions of active cell growth of the hyphae of Aspergillus fumigatus. Echinocandin Antifungal (Code: N0000175507) Lipopeptides (Code: N0000175508) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) antiinfective agent (Code: CHEBI:35441) 2001-01-26 FDA
Click to view adipiodone A water-soluble radiographic contrast media for cholecystography and intravenous cholangiography. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) 1954-04-27 FDA IDB
Click to view dapagliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202293s018lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202293s018lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202293s018lbl.pdf) Dapagliflozin is a sodium-glucose cotransporter 2 (SGLT2) inhibitor. Dapagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion. Dapagliflozin is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus and to reduce the risk of hospitalization for heart failure in adults with type 2 diabetes mellitus and established cardiovascular disease or multiple cardiovascular risk factors. Sodium-Glucose Cotransporter 2 Inhibitor (Code: N0000187059) Sodium-Glucose Transporter 2 Inhibitors (Code: N0000187058) hypoglycemic agent (Code: CHEBI:35526) 2012-11-12 EMA
Click to view gonadorelin Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) agonist Gonadotropin-releasing hormone receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30969, gene: Gnrhr, swissprot: GNRHR_RAT Lutropin-choriogonadotropic hormone receptor (Organism: Rattus norvegicus, class: Unclassified, accessions: P16235, gene: Lhcgr, swissprot: LSHR_RAT A decapeptide that stimulates the synthesis and secretion of both pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. GnRH is produced by neurons in the septum PREOPTIC AREA of the HYPOTHALAMUS and released into the pituitary portal blood, leading to stimulation of GONADOTROPHS in the ANTERIOR PITUITARY GLAND. gonadotropin releasing hormone agonist (Code: CHEBI:63533) 1982-09-30 FDA
Click to view eledoisin Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) agonist (Source: ) Neuromedin-K receptor (Organism: Homo sapiens, class: GPCR, accessions: P29371, gene: TACR3, swissprot: NK3R_HUMAN A peptide extracted from the posterior salivary glands of certain small octopi (Eledone spp., Mollusca), or obtained by synthesis. Its actions resemble those of SUBSTANCE P; it is a potent vasodilator and increases capillary permeability. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1364) Neurotransmitter Agents (Code: D018377)
Click to view leuprorelin Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021343s033,021379s033,021488s030,021731s029lbl.pdf) A potent synthetic long-acting agonist of gonadotropin-releasing hormone that regulates the synthesis and release of pituitary gonadotropins, luteinizing hormone and follicle stimulating hormone. Gonadotropin Releasing Hormone Receptor Agonist (Code: N0000175655) Gonadotropin Releasing Hormone Receptor Agonists (Code: N0000175654) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Fertility Agents (Code: D005299) Fertility Agents, Female (Code: D005300) Reproductive Control Agents (Code: D012102) antineoplastic agent (Code: CHEBI:35610) gonadotropin releasing hormone agonist (Code: CHEBI:63533) 1985-04-09 FDA
Click to view iotroxic acid Contrast media for intravenous cholecystography
Click to view terlipressin Vasopressin V1a receptor (Organism: Homo sapiens, class: GPCR, accessions: P37288, gene: AVPR1A, swissprot: V1AR_HUMAN) partial agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27586252) Vasopressin V1b receptor (Organism: Homo sapiens, class: GPCR, accessions: P47901, gene: AVPR1B, swissprot: V1BR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27586252) Vasopressin V2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P30518, gene: AVPR2, swissprot: V2R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27586252) Terlipressin is a synthetic peptide composed of one molecule of [Lysine8]Vasopressin (LVP) and three additional glycine residues. It is metabolized via exopeptidases into LVP, the natural vasopressin porcine hormone. Terlipressin is presented as a specific V1A receptor agonist. The vasoactive properties of LVP decreases splanchnic blood flow in order to prevent oesophageal varices haemorrhage or the hepatorenal syndrome complicating liver cirrhosis. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Vasoconstrictor Agents (Code: D014662) 1995-07-22 CDSCO (INDIA)
Click to view mifamurtide Nucleotide-binding oligomerization domain-containing protein 2 (Organism: Homo sapiens, class: Cytosolic other, accessions: Q9HC29, gene: NOD2, swissprot: NOD2_HUMAN) activator (Source: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/000802/WC500026565.pdf) Mifamurtide (muramyl tripeptide phosphatidyl ethanolamine, MTP-PE) is a fully synthetic derivative of muramyl dipeptide (MDP), the smallest naturally-occurring immune stimulatory component of cell walls from Mycobacterium sp. It has similar immunostimulatory effects as natural MDP with the additional advantage of a longer half-life in plasma. Mifamurtide liposomal formulation is specifically designed for in vivo targeting to macrophages by intravenous infusion. MTP-PE is a specific ligand of NOD2, a receptor found primarily on monocytes, dendritic cells and macrophages. MTP-PE is a potent activator of monocytes and macrophages. Activation of human macrophages by mifamurtide is associated with production of cytokines, including tumour necrosis factor (TNF-alfa), interleukin-1 (IL-1beta), IL-6, IL-8, and IL-12 and adhesion molecules, including lymphocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1 (ICAM-1). In vitro-treated human monocytes killed allogeneic and autologous tumour cells (including melanoma, ovarian, colon, and renal carcinoma), but had no toxicity towards normal cells. Adjuvants, Immunologic (Code: D000276) Immunologic Factors (Code: D007155) 2009-03-06 EMA
Click to view buserelin Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/26398856) Buserelin is a synthetic analog of gonadotropin-releasing hormone (GnRH). Buserelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Prolonged administration of buserelin results in sustained inhibition of gonadotropin production, suppression of testicular and ovarian steroidogenesis, and reduced levels of circulating gonadotropin and gonadal steroids. Buserelin is more potent that GnRH. Buserelin is used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction. Fertility Agents (Code: D005299) Fertility Agents, Female (Code: D005300) Reproductive Control Agents (Code: D012102) 1986-04-01 CDSCO (INDIA)
Click to view abarelix Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2003/21320_plenaxis_lbl.pdf) Abarelix is a synthetic decapeptide with potent antagonistic activity against naturally occurring gonadotropin releasing-hormone (GnRH). Abarelix inhibits gonadotropin and related androgen production by directly and competitively blocking GnRH receptors in the pituitary. Abarelix was indicated for the palliative treatment of men with advanced symptomatic prostate cancer. Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) hormone antagonist (Code: CHEBI:49020) antineoplastic agent (Code: CHEBI:35610) 2003-11-25 FDA
Click to view iocarmic acid see also iocarmate meglumine
Click to view dactinomycin DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) binder (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050682s034lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050682s034lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/050682s034lbl.pdf) Solute carrier family 22 member 5 (Organism: Homo sapiens, class: Transporter, accessions: O76082, gene: SLC22A5, swissprot: S22A5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10525100) Multidrug resistance-associated protein 6 (Organism: Homo sapiens, class: Transporter, accessions: O95255, gene: ABCC6, swissprot: MRP6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12414644) Growth factor receptor-bound protein 2 (Organism: Mus musculus, class: Cytosolic other, accessions: Q60631, gene: Grb2, swissprot: GRB2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10888331) Discoidin domain-containing receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: Q16832, gene: DDR2, swissprot: DDR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19122296) Dactinomycin is an actinomycin D which produced by Streptomyces parvullus. Dactinomycin binds DNA and inhibits RNA synthesis. Dactinomycin is indicated for the treatment of Wilms tumor, rhabdomyosarcoma, Ewing sarcoma, metastatic, nonseminomatous testicular cancer, gestational trophoblastic neoplasia, locally recurrent or locoregional solid malignancies. Actinomycin (Code: N0000180850) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Protein Synthesis Inhibitors (Code: D011500) 1964-12-10 FDA PRD_0
Click to view ioxaglic acid Ioxaglic Acid is an ionic tri-iodinated benzoate used as a contrast agent in diagnostic imaging. Like other organic iodine compounds, ioxaglic acid blocks x-rays and appears opaque on x-ray film, thereby enhancing the visibility of structure and organs during angiography, arteriography, arthrography, cholangiography, urography, and computed tomography (CT) scanning procedures. Ioxaglic acid has low osmolarity and is therefore associated with few side effects compared to older contrast agents. Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338) 1985-07-26 FDA
Click to view goserelin Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/019726s059,020578s037lbl.pdf) Goserelin is a synthetic decapeptide analogue of gonadotropin releasing hormone (GnRH) and a GnRH agonist. Goserelin acts as an inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. Goserelin is indicated in combination with flutamide for the management of locally confined carcinoma of the prostate, for palliative treatment of advanced carcinoma of the prostate, for the management of endometriosis and for the palliative treatment of advanced breast cancer in pre- and perimenopausal women. Gonadotropin Releasing Hormone Receptor Agonist (Code: N0000175655) Gonadotropin Releasing Hormone Receptor Agonists (Code: N0000175654) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) 1989-12-29 FDA
Click to view micafungin Beta-1,3-glucan synthase catalytic subunit 1 (Organism: Candida albicans, class: Enzyme, accessions: O13428, gene: GSC1, swissprot: O13428_CANAX) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15101786) 1,3-beta-glucan synthase component FKS1 (Organism: Aspergillus niger (strain CBS 513.88 / FGSC A1513), class: Enzyme, accessions: A2QLK4, gene: fksA, swissprot: FKS1_ASPNC) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15101786) Arylsulfatase A (Organism: Homo sapiens, class: Enzyme, accessions: P15289, gene: ARSA, swissprot: ARSA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15882123) Micafungin is an antifungal drug and exerts its effect by inhibiting the synthesis of 1,3-beta-D-glucan, an integral component of the fungal cell wall. Echinocandin Antifungal (Code: N0000175507) Lipopeptides (Code: N0000175508) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) antiinfective agent (Code: CHEBI:35441) 2005-03-16 FDA
Click to view cetrorelix Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021197s010lbl.pdf) Cetrorelix is a synthetic decapeptide with gonadotropin-releasing hormone antagonistic activity. Cetrorelix acetate is an analog of native GnRH with substitutions of amino acids at positions 1, 2, 3, 6, and 10. Cetrorelix is indicated for the inhibition of premature LH surges in women undergoing controlled ovarian stimulation. Fertility Agents (Code: D005299) Fertility Agents, Female (Code: D005300) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Reproductive Control Agents (Code: D012102) GnRH antagonist (Code: CHEBI:59229) antineoplastic agent (Code: CHEBI:35610) Decreased GnRH Secretion (Code: N0000008638) Gonadotropin Releasing Hormone Antagonist (Code: N0000175839) Gonadotropin Releasing Hormone Receptor Antagonists (Code: N0000175084) 2000-08-11 FDA
Click to view iodoxamic acid radiopaque medium used in the diagnosis of gall bladder & bile duct diseases, usually as meglumine salt; minor descriptor (81-86); on-line & INDEX MEDICUS search TRIIODOBENZOIC ACIDS (81-86) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 1981-08-14 FDA
Click to view suramin P2Y purinoceptor 11 (Organism: Homo sapiens, class: GPCR, accessions: Q96G91, gene: P2RY11, swissprot: P2Y11_HUMAN) antagonist (Source: ) P2Y purinoceptor 13 (Organism: Homo sapiens, class: GPCR, accessions: Q9BPV8, gene: P2RY13, swissprot: P2Y13_HUMAN) antagonist (Source: ) P2Y purinoceptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P47900, gene: P2RY1, swissprot: P2RY1_HUMAN) antagonist (Source: ) P2Y purinoceptor 2 (Organism: Homo sapiens, class: GPCR, accessions: P41231, gene: P2RY2, swissprot: P2RY2_HUMAN) antagonist (Source: ) P2X purinoceptor 4 (Organism: Homo sapiens, class: Ion channel, accessions: Q99571, gene: P2RX4, swissprot: P2RX4_HUMAN) P2X purinoceptor 3 (Organism: Homo sapiens, class: Ion channel, accessions: P56373, gene: P2RX3, swissprot: P2RX3_HUMAN) Nucleoside triphosphate diphosphohydrolase 3 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q80Z26, gene: Entpd3, swissprot: Q80Z26_RAT ATP-dependent 6-phosphofructokinase (Organism: Trypanosoma brucei brucei, class: Kinase, accessions: O15648, gene: pfk, swissprot: PFKA_TRYBB Protein kinase C (PKC) (Organism: Homo sapiens, class: Kinase, accessions: O94806|P05129|P05771|P17252|P24723|P41743|Q02156|Q04759|Q05513|Q05655|Q15139, gene: PRKCA|PRKCB|PRKCD|PRKCE|PRKCG|PRKCH|PRKCI|PRKCQ|PRKCZ|PRKD1|PRKD3, swissprot: KPCA_HUMAN|KPCB_HUMAN|KPCD1_HUMAN|KPCD3_HUMAN|KPCD_HUMAN|KPCE_HUMAN|KPCG_HUMAN|KPCI_HUMAN|KPCL_HUMAN|KPCT_HUMAN|KPCZ_HUMAN RmtA (Organism: Emericella nidulans, class: Enzyme, accessions: Q5VLE3, gene: rmtA, swissprot: Q5VLE3_EMEND Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1 DNA-dependent protein kinase catalytic subunit (Organism: Homo sapiens, class: Kinase, accessions: P78527, gene: PRKDC, swissprot: PRKDC_HUMAN Ectonucleoside triphosphate diphosphohydrolase 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: O35795, gene: Entpd2, swissprot: ENTP2_RAT NAD-dependent protein deacylase sirtuin-5, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9NXA8, gene: SIRT5, swissprot: SIR5_HUMAN Protein arginine N-methyltransferase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q99873, gene: PRMT1, swissprot: ANM1_HUMAN NAD-dependent protein deacetylase sirtuin-2 (Organism: Homo sapiens, class: Enzyme, accessions: Q8IXJ6, gene: SIRT2, swissprot: SIR2_HUMAN NAD-dependent protein deacetylase sirtuin-1 (Organism: Homo sapiens, class: Enzyme, accessions: Q96EB6, gene: SIRT1, swissprot: SIR1_HUMAN P2X purinoceptor 1 (Organism: Rattus norvegicus, class: Unclassified, accessions: P47824, gene: P2rx1, swissprot: P2RX1_RAT) antagonist (Source: ) P2X purinoceptor 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P49653, gene: P2rx2, swissprot: P2RX2_RAT) antagonist (Source: ) P2X purinoceptor 3 (Organism: Rattus norvegicus, class: Unclassified, accessions: P49654, gene: P2rx3, swissprot: P2RX3_RAT) antagonist (Source: ) P2X purinoceptor 5 (Organism: Rattus norvegicus, class: Unclassified, accessions: P51578, gene: P2rx5, swissprot: P2RX5_RAT) antagonist (Source: ) P2Y purinoceptor 6 (Organism: Homo sapiens, class: GPCR, accessions: Q15077, gene: P2RY6, swissprot: P2RY6_HUMAN) antagonist (Source: ) A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties. Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antineoplastic Agents (Code: D000970) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Trypanocidal Agents (Code: D014344) antinematodal drug (Code: CHEBI:35444) trypanocidal drug (Code: CHEBI:36335) SVR
Click to view triptorelin Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020715s040,021288s035,022427s015lbl.pdf) Triptorelin is a synthetic decapeptide agonist analog of gonadotropin releasing hormone (GnRH) that is a potent inhibitor of the synthesis of testosterone (in men) and estrogen (in women) and is used to treat advanced prostate cancer. Triptorelin is also used as a contraceptive drug. Gonadotropin Releasing Hormone Receptor Agonist (Code: N0000175655) Gonadotropin Releasing Hormone Receptor Agonists (Code: N0000175654) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Hormonal (Code: D018931) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Luteolytic Agents (Code: D008186) Reproductive Control Agents (Code: D012102) gonadotropin releasing hormone agonist (Code: CHEBI:63533) antineoplastic agent (Code: CHEBI:35610) contraceptive drug (Code: CHEBI:49323) 2000-06-15 FDA
Click to view eritoran Toll-like receptor 4 (Organism: Homo sapiens, class: Membrane receptor, accessions: O00206, gene: TLR4, swissprot: TLR4_HUMAN) Eritoran is a structural analogue of the lipid A portion of lipopolysaccharide that blocks lipopolysaccharide from binding at the cell surface MD2-TLR4 receptor. It is being developed for the treatment of severe sepsis. E55
Click to view nafarelin Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) agonist A potent synthetic agonist of GONADOTROPIN-RELEASING HORMONE with 3-(2-naphthyl)-D-alanine substitution at residue 6. Nafarelin has been used in the treatments of central PRECOCIOUS PUBERTY and ENDOMETRIOSIS. Gonadotropin Releasing Hormone Receptor Agonist (Code: N0000175655) Gonadotropin Releasing Hormone Receptor Agonists (Code: N0000175654) Fertility Agents (Code: D005299) Fertility Agents, Female (Code: D005300) Reproductive Control Agents (Code: D012102) 1990-02-13 FDA
Click to view histrelin Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) agonist gonadotropin releasing hormone agonist Gonadotropin Releasing Hormone Receptor Agonist (Code: N0000175655) Gonadotropin Releasing Hormone Receptor Agonists (Code: N0000175654) antineoplastic agent (Code: CHEBI:35610) gonadotropin releasing hormone agonist (Code: CHEBI:63533) 1991-12-24 FDA
Click to view depreotide Depreotide is a peptide analogue of a somatostatin receptors. Tc-99m labeled Depreotide is indicated for diagnostic use only, for scintigraphic imaging of suspected malignant tumours in the lung after initial detection, in combination with CT scan or chest X-ray, in patients with solitary pulmonary nodules. 1999-03-08 FDA
Click to view vancomycin Vancomycin is a complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile. Vancomycin is indicated for the treatment of Clostridium difficile-associated diarrhea and enterocolitis caused by Staphylococcus aureus (including methicillin-resistant strains). Glycopeptide Antibacterial (Code: N0000175491) Glycopeptides (Code: N0000007889) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1964-11-06 FDA PRD_0
Click to view peplomycin An antineoplastic agent derived from BLEOMYCIN. Antibiotics, Antineoplastic (Code: D000903) Antineoplastic Agents (Code: D000970)
Click to view fondaparinux Antithrombin-III (Organism: Homo sapiens, class: Secreted, accessions: P01008, gene: SERPINC1, swissprot: ANT3_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021345s035lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021345s035lbl.pdf) Fondaparinux is a synthetic glucopyranoside with antithrombotic activity. Fondaparinux selectively binds to antithrombin III, thereby potentiating the innate neutralization of activated factor X (Factor Xa) by antithrombin. Neutralization of Factor Xa inhibits its activity and interrupts the blood coagulation cascade, thereby preventing thrombin formation and thrombus development. Fondaparinux is used for: prophylaxis of venous thromboembolism, treatment of acute deep vein thrombosis and pulmonary embolism, management of unstable angina pectoris and Non ST Segment Elevation Myocardial Infarction. Factor Xa Inhibitor (Code: N0000175637) Anticoagulants (Code: D000925) Antithrombins (Code: D000991) Enzyme Inhibitors (Code: D004791) Factor Xa Inhibitors (Code: D065427) Hematologic Agents (Code: D006401) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) 2001-12-07 FDA NTO
Click to view betadex Food Additives (Code: D005503) Sequestering Agents (Code: D064449) BCD
Click to view iodixanol Iodixanol is a dimeric iso-osmolar, non-ionic, hydrophilic iodinated radiocontrast agent used in diagnostic imaging. Upon intravascular administration and during computed tomography (CT) imaging, iodixanol blocks x-rays and appears opaque on x-ray images. This allows body structures that absorb iodine to be visualized. The degree of opacity produced by iodixanol is directly proportional to the total amount of the iodinated contrast agent in the path of the x-rays. The visualization of body structures is dependent upon the distribution and elimination of iodixanol. Compared to other iodinated contrast agents, iodixanol appears to exhibit less nephrotoxicity. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338) Radiographic Contrast Agent (Code: N0000180185) X-Ray Contrast Activity (Code: N0000010258) 1996-03-22 FDA
Click to view ganirelix Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021057s010lbl.pdf) Ganirelix is a synthetic decapeptide with high antagonistic activity against naturally occurring gonadotropin-releasing hormone (GnRH). Ganirelix Acetate is derived from native GnRH. Ganirelix acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion. The suppression of pituitary luteinizing hormone secretion by ganirelix is more pronounced than that of follicle-stimulating hormone.Ganirelix is indicated for the inhibition of premature luteinizing hormone surges in women undergoing controlled ovarian hyperstimulation. Decreased GnRH Secretion (Code: N0000008638) Gonadotropin Releasing Hormone Antagonist (Code: N0000175839) Gonadotropin Releasing Hormone Receptor Antagonists (Code: N0000175084) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1999-07-29 FDA
Click to view daptomycin Bacterial outer membrane (Organism: None, class: NOne, accessions: None, gene: None, swissprot: None) destabilizator (Source:https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021572s061lbl.pdf) Daptomycin is a cyclic lipopeptide antibacterial agent derived from the fermentation of Streptomyces roseosporus. Daptomycin binds to bacterial cell membranes and causes a rapid depolarization of membrane potential. This loss of membrane potential causes inhibition of DNA, RNA, and protein synthesis, which results in bacterial cell death. Daptomycin has been shown to be active against Enterococcus faecalis (vancomycin-susceptible isolates only), Staphylococcus aureus (including methicillin-resistant isolates), Streptococcus agalactiae, Streptococcus dysgalactiae subsp. equisimilis, Streptococcus pyogenes. Daptomycin is indicated for the treatment of complicated skin and skin structure infections and Staphylococcus aureus bacteremia. Lipopeptide Antibacterial (Code: N0000175509) Lipopeptides (Code: N0000175508) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 2003-09-12 FDA PRD_0
Click to view iotrolan nonionic, isotonic contrast medium designed for intrathecal use; RN given refers to cpd without isomeric designation; DL-3-117 refers to stereoisomer; structure given in first source Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) FDA
Click to view lercanidipine Voltage-gated L-type calcium channel (Organism: Homo sapiens, class: Ion channel, accessions: Q13936|Q01668, gene: CACNA1C|CACNA1D, swissprot: CAC1C_HUMAN|CAC1D_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/8821512) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11996015) Lercanidipine is antihypertensive drugs which acts by blocking L-type calcium channels. Lercanidipine is also investigated in preclinical models of epilepsy and ischemic stroke. Antihypertensive Agents (Code: D000959) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) 1996-03-22 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view somatostatin Somatostatin receptor type 2 (Organism: Homo sapiens, class: GPCR, accessions: P30874, gene: SSTR2, swissprot: SSR2_HUMAN) agonist Somatostatin receptor type 5 (Organism: Rattus norvegicus, class: GPCR, accessions: P30938, gene: Sstr5, swissprot: SSR5_RAT Somatostatin receptor type 1 (Organism: Homo sapiens, class: GPCR, accessions: P30872, gene: SSTR1, swissprot: SSR1_HUMAN) agonist Somatostatin receptor type 5 (Organism: Homo sapiens, class: GPCR, accessions: P35346, gene: SSTR5, swissprot: SSR5_HUMAN) agonist Somatostatin receptor type 3 (Organism: Mus musculus, class: GPCR, accessions: P30935, gene: Sstr3, swissprot: SSR3_MOUSE Somatostatin receptor type 3 (Organism: Homo sapiens, class: GPCR, accessions: P32745, gene: SSTR3, swissprot: SSR3_HUMAN) agonist Somatostatin receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P28646|P30680|P30936|P30937|P30938, gene: Sstr1|Sstr2|Sstr3|Sstr4|Sstr5, swissprot: SSR1_RAT|SSR2_RAT|SSR3_RAT|SSR4_RAT|SSR5_RAT Somatostatin receptor (Organism: Mus musculus, class: GPCR, accessions: O08858|P30873|P30875|P30935|P49660, gene: Sstr1|Sstr2|Sstr3|Sstr4|Sstr5, swissprot: SSR1_MOUSE|SSR2_MOUSE|SSR3_MOUSE|SSR4_MOUSE|SSR5_MOUSE Somatostatin receptor type 2 (Organism: Mus musculus, class: GPCR, accessions: P30875, gene: Sstr2, swissprot: SSR2_MOUSE Delta-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533, gene: Oprd1, swissprot: OPRD_RAT Mu-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33535, gene: Oprm1, swissprot: OPRM_RAT Somatostatin receptor type 4 (Organism: Homo sapiens, class: GPCR, accessions: P31391, gene: SSTR4, swissprot: SSR4_HUMAN) agonist A 14-amino acid peptide named for its ability to inhibit pituitary GROWTH HORMONE release, also called somatotropin release-inhibiting factor. It is expressed in the central and peripheral nervous systems, the gut, and other organs. SRIF can also inhibit the release of THYROID-STIMULATING HORMONE; PROLACTIN; INSULIN; and GLUCAGON besides acting as a neurotransmitter and neuromodulator. In a number of species including humans, there is an additional form of somatostatin, SRIF-28 with a 14-amino acid extension at the N-terminal. Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730)
Click to view telavancin Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022407s000,022110s003lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022407s000,022110s003lbl.pdf) Telavancin is a semisynthetic, lipoglycopeptide antibiotic. Telavancin inhibits cell wall biosynthesis by binding to late-stage peptidoglycan precursors, including lipid II. Telavancin also binds to the bacterial membrane and disrupts membrane barrier function. Telavancin is indicated for the treatment of the complicated skin and skin structure infections and hospital-acquired and ventilator-associated bacterial pneumonia caused by susceptible isolates of Staphylococcus aureus. Lipoglycopeptide Antibacterial (Code: N0000191281) Lipoglycopeptides (Code: N0000191280) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 2009-09-11 FDA
Click to view artenimol Artenimol is able to reach high concentrations within the parasitized erythrocytes. Its endoperoxide bridge is thought to be essential for its antimalarial activity, causing free-radical damage to parasite membrane systems. Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) 2011-10-27 EMA
Click to view dalbavancin Dalbavancin, a semisynthetic lipoglycopeptide, interferes with cell wall synthesis by binding to the D-alanyl-D-alanine terminus of the stem pentapeptide in nascent cell wall peptidoglycan, thus preventing cross-linking. Dalbavancin is indicated for the treatment of adult patients with acute bacterial skin and skin structure infections, caused by susceptible isolates of the following Gram-positive microorganisms (Staphylococcus aureus (including methicillinsusceptible and methicillin-resistant strains), Streptococcus pyogenes, Streptococcus agalactiae, Streptococcus dysgalactiae, Streptococcus anginosus group (including S. anginosus, S. intermedius, S. constellatus) and Enterococcus faecalis (vancomycin susceptible strains)). Lipoglycopeptide Antibacterial (Code: N0000191281) Lipoglycopeptides (Code: N0000191280) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 2014-05-23 FDA
Click to view alsactide Alsactide is synthesized heptadecapeptide analog of adrenocorticotropic hormone (ACTH) having a C-terminal amide group (butylamide) and the substitution of beta-alanine for serine in position 1 and of lysine for arginine in position 17. Alsactide was used as a diagnostic agent of adrenal insufficiency. Italian Medicines Agency (AIFA)
Click to view bivalirudin Prothrombin (Organism: Homo sapiens, class: Enzyme, accessions: P00734, gene: F2, swissprot: THRB_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020873s039lbl.pdf) Bivalirudin is a synthetic, 20 amino acid peptide. Bivalirudin is a specific and reversible direct thrombin inhibitor. Bivalirudin directly inhibits thrombin by specifically binding both to the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin. Bivalirudin is indicated for use as an anticoagulant in patients undergoing percutaneous coronary intervention including patients with heparin-induced thrombocytopenia or heparin-induced thrombocytopenia and thrombosis syndrome. Anti-coagulant (Code: N0000175980) Direct Thrombin Inhibitor (Code: N0000175518) Thrombin Inhibitors (Code: N0000009963) Anticoagulants (Code: D000925) Antithrombins (Code: D000991) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) anticoagulant (Code: CHEBI:50249) 2000-12-15 FDA PRD_0
PRD_0
Click to view ziconotide Voltage-dependent N-type calcium channel subunit alpha-1B (Organism: Rattus norvegicus, class: Unclassified, accessions: Q02294, gene: Cacna1b, swissprot: CAC1B_RAT) blocker (Source: ) Voltage-dependent N-type calcium channel subunit alpha-1B (Organism: Homo sapiens, class: Ion channel, accessions: Q00975, gene: CACNA1B, swissprot: CAC1B_HUMAN) blocker Voltage-dependent P/Q-type calcium channel subunit alpha-1A (Organism: Rattus norvegicus, class: Unclassified, accessions: P54282, gene: Cacna1a, swissprot: CAC1A_RAT) blocker (Source: ) Ziconotide binds to N-type calcium channels located on the primary nociceptive (A-delta and C) afferent nerves in the superficial layers (Rexed laminae I and II) of the dorsal horn in the spinal cord. Although the mechanism of action of ziconotide has not been established in humans, results in animals suggest that its binding blocks N-type calcium channels, which leads to a blockade of excitatory neurotransmitter release from the primary afferent nerve terminals and antinociception. N-Calcium Channel Receptor Antagonists (Code: N0000020069) N-type Calcium Channel Antagonist (Code: N0000175697) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Calcium Channel Blockers (Code: D002121) Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neuroprotective Agents (Code: D018696) Peripheral Nervous System Agents (Code: D018373) Protective Agents (Code: D020011) Sensory System Agents (Code: D018689) 2004-12-28 FDA
Click to view alpha-tocopherol acetate Alpha-Tocopherol: Alpha-tocopherol transfer protein (Homo sapiens, class: Enzyme, accessions: P49638, gene: TTPA, swissprot: TTPA_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/7887897) Alpha-tocopherol is the primary form of vitamin E that is preferentially used by the human body to meet appropriate dietary requirements. Alpha-tocopherol acetate is a natural tocopherol and one of the most potent antioxidant tocopherols. It exhibits antioxidant activity by virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus. It has four methyl groups on the 6-chromanol nucleus. The natural d form of alpha-tocopherol is more active than its synthetic dl-alpha-tocopherol racemic mixture. Vitamin E is known to be a fat-soluble antioxidant that has the capability to neutralize endogenous free radicals. Alpha-tocopherol acetate is most commonly indicated for dietary supplementation in individuals who may demonstrate a genuine deficiency in vitamin E. 2000-05-18 FDA VIV
Click to view secretin human Secretin receptor (Organism: Homo sapiens, class: GPCR, accessions: P47872, gene: SCTR, swissprot: SCTR_HUMAN) agonist (Source: ) A peptide hormone of about 27 amino acids from the duodenal mucosa that activates pancreatic secretion and lowers the blood sugar level. (USAN and the USP Dictionary of Drug Names, 1994, p597) Secretin (Code: N0000006078) Secretin-class Hormone (Code: N0000175813) Gastrointestinal Agents (Code: D005765) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 2002-04-04 FDA
Click to view carperitide Carperitide is a synthetic, recombinant atrial natriuretic peptide with both vasodilating and diuretic activity. It is used for acute heart failure treatment. 1995-01-20 PMDA
Click to view telotristat ethyl Tryptophan 5-hydroxylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P17752, gene: TPH1, swissprot: TPH1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208794s000lbl.pdf) Telotristat, the active metabolite of telotristat ethyl, is an inhibitor of tryptophan hydroxylase, which mediates the rate limiting step in serotonin biosynthesis. The in vitro inhibitory potency of telotristat towards tryptophan hydroxylase is 29 times higher than that of telotristat ethyl. Serotonin plays a role in mediating secretion, motility, inflammation, and sensation of the gastrointestinal tract, and is over-produced in patients with carcinoid syndrome. Through inhibition of tryptophan hydroxylase, telotristat and telotristat ethyl reduce the production of peripheral serotonin, and the frequency of carcinoid syndrome diarrhea. 2017-02-28 FDA
Click to view beclabuvir Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN 2016-12-19 PMDA 2N7
Click to view thymalfasin Thymalfasin is a synthetic analogue of thymosin-alpha-1, a 28-amino acid protein derived from the precursor protein prothymosin-alpha. Exhibiting a variety of immunoregulating properties, thymosin-alpha-1 induces differentiation of T-cell precursors and human thymocytes and the terminal differentiation of functionally immature cord blood lymphocytes and induces production of IL-2, high affinity IL-2 receptors, and B-cell growth factors by peripheral blood mononuclear cells. T-helper and cytotoxic/suppressor T-cell populations are targets of thymosin activity. Thymosin-alpha-1 has been shown to increase the efficiency of antigen presentation by macrophages and to be an endogenous modulator of alpha-thrombin activity. Thymalfasin is used alone or with interferon as an immunomodulator for the treatment of Chronic Hepatitis B And Hepatitis C. Thymalfasin is also used for the treatment of chemotherapy-induced immunosuppression, and to enhance the efficacy of influenza and hepatitis B vaccines in immunocompromised patients. Adjuvants, Immunologic (Code: D000276) Antineoplastic Agents (Code: D000970) Immunologic Factors (Code: D007155) 1993-04-27 Italian Medicines Agency (AIFA)
Click to view sermorelin Growth hormone-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: Q02643, gene: GHRHR, swissprot: GHRHR_HUMAN) agonist (Source: ) The biologically active fragment of human growth hormone-releasing factor, consisting of GHRH(1-29)-amide. This N-terminal sequence is identical in several mammalian species, such as human, pig, and cattle. It is used to diagnose or treat patients with GROWTH HORMONE deficiency. 1990-12-28 FDA
Click to view ribociclib Cyclin-dependent kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P11802, gene: CDK4, swissprot: CDK4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf) Cyclin-dependent kinase 6 (Organism: Homo sapiens, class: Kinase, accessions: Q00534, gene: CDK6, swissprot: CDK6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf) Ribociclib is an inhibitor of cyclin-dependent kinase (CDK) 4 and 6. The cyclin D-CDK4/6 complex regulates cell cycle progression through phosphorylation of the retinoblastoma protein (pRb). In vitro, ribociclib decreased pRb phosphorylation leading to arrest in the G1 phase of the cell cycle and reduced cell proliferation in breast cancer cell lines. Ribociclib is indicated for the treatment of pre/perimenopausal or postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer, as initial endocrine-based therapy. Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) Cytochrome P450 3A Inhibitors (Code: N0000190114) 2017-03-13 FDA 6ZZ
Click to view naldemedine Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208854s000lbl.pdf) Naldemedine is an opioid antagonist with binding affinities for mu-, delta-, and kappa-opioid receptors. Naldemedine functions as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids. Opioid Antagonist (Code: N0000175691) Opioid Antagonists (Code: N0000000154) 2017-03-23 FDA
Click to view hydrocortisone acetate Hydrocortisone acetate is a synthetic glucocorticoid corticosteroid and corticosteroid ester. It is the C21 acetate ester of hydrocortisone, and acts as a prodrug of hydrocortisone. (See: hydrocortisone) Anti-Inflammatory Agents (Code: D000893) 1951-12-21 FDA
Click to view calcitonin (salmon synthetic) Calcitonin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30988, gene: CALCR, swissprot: CALCR_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/017808s036lbl.pdf) Amylin receptor AMY1 (Organism: Homo sapiens, class: GPCR, accessions: O60894|P30988, gene: CALCR|RAMP1, swissprot: CALCR_HUMAN|RAMP1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10385705) Amylin receptor AMY2 (Organism: Homo sapiens, class: GPCR, accessions: O60895|P30988, gene: CALCR|RAMP2, swissprot: CALCR_HUMAN|RAMP2_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10385705) Amylin receptor AMY3 (Organism: Homo sapiens, class: GPCR, accessions: O60896|P30988, gene: CALCR|RAMP3, swissprot: CALCR_HUMAN|RAMP3_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10385705) Used in the treatment of symptomatic Paget's disease for patients unresponsive to alternate treatments or intolerant to such treatments. Calcitonin inhibits bone resorption by osteoclasts (bone remodeling cells) and promotes bone formation by osteoblasts. Salmon calcitonin was shown to inhibit lactation in animals and is not recommend in nursing mothers. Calcitonin (Code: N0000006509) Bone Density Conservation Agents (Code: D050071) bone density conservation agent (Code: CHEBI:50646) 1978-04-17 FDA
Click to view calcitonin (pork natural) a polypeptide hormone secreted by the parafollicular cells of the thyroid gland in mammals. It inhibits bone resorption and lowers both serum and urinary calcium concentrations.
Click to view chidamide Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22080169) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22080169) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22080169) Histone deacetylase 10 (Organism: Homo sapiens, class: Enzyme, accessions: Q969S8, gene: HDAC10, swissprot: HDA10_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22080169) Histone deacetylase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BY41, gene: HDAC8, swissprot: HDAC8_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22080169) Histone deacetylase 11 (Organism: Homo sapiens, class: Enzyme, accessions: Q96DB2, gene: HDAC11, swissprot: HDA11_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22080169) An orally bioavailable benzamide-type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Chidamide binds to and inhibits HDACs, leading to an increase of acetylation levels of histone proteins. This agent also inhibits the expression of kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. HDACs, a class of enzymes that deacetylate chromatin histone proteins, are upregulated in many tumor types and play key roles in gene expression. Compared to some other benzamide-type HDAC inhibitors, chidamide is more stable, more resistant to degradation and has a longer half-life. 2014-12-23 China Food and Drug Administration (CFDA)
Click to view nesiritide Atrial natriuretic peptide receptor 1 (Organism: Homo sapiens, class: Enzyme, accessions: P16066, gene: NPR1, swissprot: ANPRA_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/20920s033lbl.pdf) Nesiritide is the recombinant form of the 32 amino acid human B-type natriuretic peptide (BNP), which is normally produced by the ventricular myocardium. Human BNP binds to the particulate guanylate cyclase receptor of vascular smooth muscle and endothelial cells, leading to increased intracellular concentrations of guanosine 3'5'-cyclic monophosphate (cGMP) and smooth muscle cell relaxation. Cyclic GMP serves as a second messenger to dilate veins and arteries. Nesiritid is used for the treatment of patients with acutely decompensated congestive heart failure who have dyspnea at rest or with minimal activity. Natriuretic Peptide (Code: N0000175593) Natriuretic Peptides (Code: N0000011465) 2001-08-10 FDA
Click to view isopropanol Isopropanol is an isomer of 1-propanol. It is a colorless liquid having disinfectant properties. It is used in the manufacture of acetone and its derivatives and as a solvent. Topically, it is used as an antiseptic. Solvents (Code: D012997) protic solvent (Code: CHEBI:48356) 1992-07-16 Austrian Medicines and Medical Devices Agency IPA
Click to view deutetrabenazine Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208082s000lbl.pdf) The precise mechanism by which deutetrabenazine exerts its anti-chorea effects is unknown but is believed to be related to its effect as a reversible depletor of monoamines (such as dopamine, serotonin, norepinephrine, and histamine) from nerve terminals. The major circulating metabolites (alpha-dihydrotetrabenazine [HTBZ] and beta-HTBZ) of deutetrabenazine, are reversible inhibitors of VMAT2, resulting in decreased uptake of monoamines into synaptic vesicles and depletion of monoamine stores. 2017-04-03 FDA
Click to view glucagon Glucagon-like peptide 1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P43220, gene: GLP1R, swissprot: GLP1R_HUMAN) agonist (Source: ) Glucagon receptor (Organism: Homo sapiens, class: GPCR, accessions: P47871, gene: GCGR, swissprot: GLR_HUMAN) agonist (Source: ) Glucagon receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30082, gene: Gcgr, swissprot: GLR_RAT Adenylate cyclase (Organism: Rattus norvegicus, class: Enzyme, accessions: D4A3N4|P21932|P26769|P26770|P40146|Q03343|Q04400|Q8CFM9, gene: Adcy1|Adcy2|Adcy3|Adcy4|Adcy5|Adcy6|Adcy8, swissprot: ADCY2_RAT|ADCY3_RAT|ADCY4_RAT|ADCY5_RAT|ADCY6_RAT|ADCY8_RAT|D4A3N4_RAT|Q8CFM9_RAT A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511) Antihypoglycemic Agent (Code: N0000190852) Gastrointestinal Motility Inhibitor (Code: N0000190853) Increased Gluconeogenesis (Code: N0000009340) Increased Glycogenolysis (Code: N0000009345) Decreased GI Smooth Muscle Tone (Code: N0000008636) Decreased GI Motility (Code: N0000008635) Decreased Glycolysis (Code: N0000008652) Gastrointestinal Agents (Code: D005765) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1960-11-14 FDA
Click to view ruxolitinib Tyrosine-protein kinase JAK2 (Organism: Homo sapiens, class: Kinase, accessions: O60674, gene: JAK2, swissprot: JAK2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202192s017lbl.pdf) Tyrosine-protein kinase JAK1 (Organism: Homo sapiens, class: Kinase, accessions: P23458, gene: JAK1, swissprot: JAK1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202192s017lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202192s017lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202192s017lbl.pdf) Tyrosine-protein kinase JAK3 (Organism: Homo sapiens, class: Kinase, accessions: P52333, gene: JAK3, swissprot: JAK3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20130243) Non-receptor tyrosine-protein kinase TYK2 (Organism: Homo sapiens, class: Kinase, accessions: P29597, gene: TYK2, swissprot: TYK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20130243) Ruxolitinib is an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies. Ruxolitinib is indicated for treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera myelofibrosis and post-essential thrombocythemia myelofibrosis, polycythemia vera, steroid-refractory acute graft-versus-host disease. Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) antineoplastic agent (Code: CHEBI:35610) 2011-11-16 FDA RXT
Click to view fesoterodine Fesoterodine is a competitive muscarinic receptor antagonist. After oral administration, fesoterodine is rapidly and extensively hydrolyzed by nonspecific esterases to its active metabolite, 5-hydroxymethyl tolterodine, which is responsible for the antimuscarinic activity of fesoterodine. Fesoterodine is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Urological Agents (Code: D064804) 2008-10-31 FDA
Click to view tafamidis Transthyretin (Organism: Homo sapiens, class: Secreted, accessions: P02766, gene: TTR, swissprot: TTHY_HUMAN) stabilizer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211996s000,212161s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211996s000,212161s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211996s000,212161s000lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211996s000,212161s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211996s000,212161s000lbl.pdf) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211996s000,212161s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211996s000,212161s000lbl.pdf) Tafamidis is a selective stabilizer of TTR. Tafamidis binds to TTR at the thyroxine binding sites, stabilizing the tetramer and slowing dissociation into monomers, the rate-limiting step in the amyloidogenic process. Tafamidis is indicated for the treatment of the cardiomyopathy of wild type or hereditary transthyretin-mediated amyloidosis. central nervous system drug (Code: CHEBI:35470) 2011-11-16 EMA 3MI
Click to view piperaquine The exact mechanism of action of piperaquine is unknown, but it likely mirrors that of chloroquine, a close structural analogue. Chloroquine binds to toxic haeme (derived from the patient??™s haemoglobin) within the malaria parasite, preventing its detoxification via a polymerisation step. Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) antimalarial (Code: CHEBI:38068) 2011-10-27 EMA
Click to view domiphen
Click to view pramlintide Amylin receptor AMY1 (Organism: Homo sapiens, class: GPCR, accessions: O60894|P30988, gene: CALCR|RAMP1, swissprot: CALCR_HUMAN|RAMP1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/24169554) Amylin receptor AMY3 (Organism: Homo sapiens, class: GPCR, accessions: O60896|P30988, gene: CALCR|RAMP3, swissprot: CALCR_HUMAN|RAMP3_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/24169554) Amylin receptor AMY2 (Organism: Homo sapiens, class: GPCR, accessions: O60895|P30988, gene: CALCR|RAMP2, swissprot: CALCR_HUMAN|RAMP2_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/15494035) Pramlintide is an analog of human amylin. Amylin is colocated with insulin in secretory granules and cosecreted with insulin by pancreatic beta cells in response to food intake. Amylin and insulin show similar fasting and postprandial patterns in healthy individuals. In patients with type 1 and type 2 diabetes, there is reduced secretion from pancreatic beta cells of both insulin and amylin in response to food. Amylin affects the rate of postprandial glucose appearance through a variety of mechanisms, as determined by nonclinical studies. Amylin slows gastric emptying (i.e., the rate at which food is released from the stomach to the small intestine) without altering the overall absorption of nutrients. In addition, amylin suppresses glucagon secretion (not normalized by insulin alone), which leads to suppression of endogenous glucose output from the liver. Amylin also regulates food intake due to centrally-mediated modulation of appetite. In human studies, pramlintide, acting as an amylin analog, slows gastric emptying, reduces the postprandial rise in plasma glucagon, and modulates satiety leading to decreased caloric intake. Amylin Agonists (Code: N0000020064) Amylin Analog (Code: N0000177910) Hypoglycemic Agents (Code: D007004) 2005-03-16 FDA
Click to view exenatide Glucagon-like peptide 1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P43220, gene: GLP1R, swissprot: GLP1R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022200s028lbl.pdf) Exenatide is a 39 amino acid peptide and synthetic version of exendin-4, a hormone found in the saliva of the venomous lizard Gila monster, with insulin secretagogue and antihyperglycemic activity. Exenatide is administered subcutaneously and mimics human glucagon-like peptide-1 (GLP-1). Compared to GLP-1, exenatide has a longer half-life of 2.4 hours. Exenatide is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other antidiabetic agents. GLP-1 Receptor Agonist (Code: N0000178480) Glucagon-Like Peptide 1 (Code: N0000170335) Glucagon-like Peptide-1 (GLP-1) Agonists (Code: N0000020058) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Hypoglycemic Agents (Code: D007004) Incretins (Code: D054795) hypoglycemic agent (Code: CHEBI:35526) 2005-04-28 FDA 3C59
3C5T
Click to view enfuvirtide GP41 (Organism: Human immunodeficiency virus 1, class: Unclassified, accessions: Q76270, gene: HIV1 ENV, swissprot: Q76270_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021481s033lbl.pdf) Enfuvirtide interferes with the entry of HIV-1 into cells by inhibiting fusion of viral and cellular membranes. Enfuvirtide binds to the first heptad-repeat (HR1) in the gp41 subunit of the viral envelope glycoprotein and prevents the conformational changes required for the fusion of viral and cellular membranes. Fusion Protein Inhibitors (Code: N0000175615) Human Immunodeficiency Virus 1 Fusion Inhibitor (Code: N0000175616) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) HIV Fusion Inhibitors (Code: D023581) HIV fusion inhibitor (Code: CHEBI:59886) 2003-03-13 FDA
Click to view vitamin A palmitate Retinol-binding protein 4 (Organism: Homo sapiens, class: Secreted, accessions: P02753, gene: RBP4, swissprot: RET4_HUMAN Beta-lactoglobulin (Organism: Bos taurus, class: Unclassified, accessions: P02754, gene: LGB, swissprot: LACB_BOVIN Anticarcinogenic Agents (Code: D016588) Antineoplastic Agents (Code: D000970) Antioxidants (Code: D000975) Protective Agents (Code: D020011) 1949-05-18 FDA
Click to view prazosin Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15258254) Alpha-1D adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P23944, gene: Adra1d, swissprot: ADA1D_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11682453) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15098086) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12110607) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12110607) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16455806) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22004608) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871765) 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9871765) Adrenergic receptor alpha-2 (Organism: Rattus norvegicus, class: GPCR, accessions: P22909|P19328|P22086, gene: Adra2a|Adra2b|Adra2c, swissprot: ADA2A_RAT|ADA2B_RAT|ADA2C_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9822553) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23241029) Prazosin is a nonselective alpha-1-adrenergic antagonist. Prazosin is used in the treatment of heart failure and hypertension. Prazosin is also useful in treating urinary hesitancy associated with prostatic hyperplasia, blocking alpha-1 receptors, which control constriction of both the prostate and urethra. alpha-Adrenergic Blocker (Code: N0000175553) Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) antihypertensive agent (Code: CHEBI:35674) alpha-adrenergic antagonist (Code: CHEBI:37890) 1976-06-23 FDA XRA
Click to view acetic acid Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/14610227) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12724351) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) Free fatty acid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: O15552, gene: FFAR2, swissprot: FFAR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21220428) Acetic acid is an antibacterial and antifungal agent. Although its mechanism of action is not fully known, undissociated acetic acid may enhance lipid solubility allowing increased fatty acid accumulation on the cell membrane or in other cell wall structures. Acetic acid, as a weak acid, can inhibit carbohydrate metabolism resulting in subsequent death of the organism. Acetic acid is used for the treatment of superficial infections of the external auditory canal caused by susceptible organisms. Indicators and Reagents (Code: D007202) food acidity regulator (Code: CHEBI:64049) protic solvent (Code: CHEBI:48356) antimicrobial food preservative (Code: CHEBI:65256) 1960-05-17 FDA ACY
ACT
Click to view migalastat Alpha-galactosidase A (Organism: Homo sapiens, class: Enzyme, accessions: P06280, gene: GLA, swissprot: AGAL_HUMAN) pharmacological chaperone (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208623s001lbl.pdf) Sodium/glucose cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P13866, gene: SLC5A1, swissprot: SC5A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208623s001lbl.pdf) Sodium/glucose cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P13866, gene: SLC5A1, swissprot: SC5A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208623s001lbl.pdf) Sucrase-isomaltase, intestinal (Organism: Rattus norvegicus, class: Enzyme, accessions: P23739, gene: Si, swissprot: SUIS_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20000679) Non-lysosomal glucosylceramidase (Organism: Mus musculus, class: Enzyme, accessions: Q69ZF3, gene: Gba2, swissprot: GBA2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20000679) Lysosomal alpha-glucosidase (Organism: Homo sapiens, class: Enzyme, accessions: P10253, gene: GAA, swissprot: LYAG_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20000679) Migalastat is a pharmacological chaperone that is designed to selectively and reversibly bind with high affinity to the active sites of certain mutant forms of alpha-galactosidase A (alpha-Gal A), the genotypes of which are referred to as amenable mutations. Migalastat binding stabilizes these mutant forms of alpha-Gal A in the endoplasmic reticulum and facilitates their proper trafficking to lysosomes where dissociation of migalastat restores alpha-Gal A activity, leading to the catabolism of GL-3 and related substrates. Migalastat is indicated for the treatment of adults with a confirmed diagnosis of Fabry disease and an amenable galactosidase alpha gene (GLA) variant based on in vitro assay data. 2016-05-26 EMA DGJ
Click to view amfecloral Amfecloral is a phenethylamine derivative. It is an anorectic drug with little to no stimulant activity. Amphecloral is metabolized to both d-(S)- and l-(R)-amphetamine. it was used as an amphetamine pro-drug with prolonged duration of action.
Click to view dexfosfoserine Metabotropic glutamate receptor 8 (Organism: Homo sapiens, class: GPCR, accessions: O00222, gene: GRM8, swissprot: GRM8_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9473604) Metabotropic glutamate receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: Q14831, gene: GRM7, swissprot: GRM7_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9473604) Metabotropic glutamate receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q14833, gene: GRM4, swissprot: GRM4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9473604) Metabotropic glutamate receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: O15303, gene: GRM6, swissprot: GRM6_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9144651) Dexfosfoserine is the most abundant phosphoamino acid. It is the phosphoric acid ester of serine. It is not encoded in the genetic code but synthesized posttranslationally. Dexfosfoserine is an agonist of the group III metabotropic glutamate receptors. This endogenous compound inhibits neural stem cells proliferation and promotes survival of nascent neurons thus it has potential therapeutic value in addition to its basic utility as a probe for dissecting molecular mechanisms underlying neurogenesis. SEP
Click to view lubiprostone Chloride channel protein 2 (Organism: Homo sapiens, class: Ion channel, accessions: P51788, gene: CLCN2, swissprot: CLCN2_HUMAN) opener Member of a bicyclic fatty acid class of compounds derived from PROSTAGLANDIN E1 involved in chloride channel gating. Chloride Channel Agonists (Code: D065101) Membrane Transport Modulators (Code: D049990) Chloride Channel Activator (Code: N0000175573) Chloride Channel Activators (Code: N0000175456) 2006-01-31 FDA
Click to view proline Proline dehydrogenase 1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: O43272, gene: PRODH, swissprot: PROD_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18401543) Proline is a cyclic, nonessential amino acid (actually, an imino acid) in humans (synthesized from glutamic acid and other amino acids), Proline is a constituent of many proteins. Found in high concentrations in collagen, proline constitutes almost a third of the residues. Proline is important for the proper functioning of joints and tendons and also helps maintain and strengthen heart muscles. 1971-09-24 FDA DPR
PRO
Click to view asparagine Sodium-coupled neutral amino acid transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q96QD8, gene: SLC38A2, swissprot: S38A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10930503) Sodium-coupled neutral amino acid transporter 3 (Organism: Homo sapiens, class: Transporter, accessions: Q99624, gene: SLC38A3, swissprot: S38A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10823827) Sodium-coupled neutral amino acid transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q969I6, gene: SLC38A4, swissprot: S38A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11342143) Sodium-coupled neutral amino acid transporter 5 (Organism: Homo sapiens, class: Transporter, accessions: Q8WUX1, gene: SLC38A5, swissprot: S38A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11243884) Asparagine is a non-essential amino acid in humans. Asparagine is a beta-amido derivative of aspartic acid and plays an important role in the biosynthesis of glycoproteins and other proteins. A metabolic precursor to aspartate, Asparagine is a nontoxic carrier of residual ammonia to be eliminated from the body. Asparagine acts as diuretic. L-asparagine is an optically active form of asparagine having L-configuration. Asparagine is used for nutritional supplementation, also for treating dietary shortage or imbalance. nutraceutical (Code: CHEBI:50733) ASN
DSG
Click to view serine Serine racemase (Organism: Homo sapiens, class: Enzyme, accessions: Q9GZT4, gene: SRR, swissprot: SRR_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20106978) Proton-coupled amino acid transporter 2 (Organism: Mus musculus, class: Transporter, accessions: Q8BHK3, gene: Slc36a2, swissprot: S36A2_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11959859) Serine palmitoyltransferase 1 (Organism: Homo sapiens, class: Enzyme, accessions: O15269, gene: SPTLC1, swissprot: SPTC1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19416851) Serine is a non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from glycine or threonine. It is involved in the biosynthesis of purines; pyrimidines; and other amino acids. L-Serine plays a role in cell growth and development (cellular proliferation). The conversion of L-serine to glycine by serine hydroxymethyltransferase results in the formation of the one-carbon units necessary for the synthesis of the purine bases, adenine and guanine. These bases when linked to the phosphate ester of pentose sugars are essential components of DNA and RNA and the end products of energy producing metabolic pathways, ATP and GTP. In addition, L-serine conversion to glycine via this same enzyme provides the one-carbon units necessary for production of the pyrimidine nucleotide, deoxythymidine monophosphate, also an essential component of DNA. D-serine is a selective full agonist at the glycine site of N-methyl-D-aspartate (NMDA)-type glutamate receptor. Serine is used as a natural moisturizing agent in some cosmetics and skin care products. Amino Acid (Code: N0000175780) Amino Acids (Code: N0000006806) 1971-09-24 FDA SER
DSN
Click to view valine Valine is an alpha-amino acid that is used in the biosynthesis of proteins. It is essential in humans, meaning the body cannot synthesize it and thus it must be obtained from the diet. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway. There is a mixed scientivic evidence that as a dietary supplement valine improves training efficacy, delays central fatigue. Valine promotes mental vigor, muscle coordination, and calm emotions. May also be of use in a minority of patients with hepatic encephalopathy and in some with phenylketonuria. nutraceutical (Code: CHEBI:50733) 1971-09-24 FDA VAL
DVA
Click to view isoleucine Large neutral amino acids transporter small subunit 3 (Organism: Homo sapiens, class: Transporter, accessions: O75387, gene: SLC43A1, swissprot: LAT3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/12930836) Isoleucine is an essential alpha-amino acid that is used in the biosynthesis of proteins. It is important in hemoglobin synthesis and regulation of blood sugar and energy levels. L-isoleucine is commonly used in parenteral and enteral nutrition. It is used in combination with the other branched chain amino acids to improve the nutritional status of patients with hepatic diseases. 1971-09-24 FDA ILE
IIL
DIL
28J
Click to view silodosin Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf) Alpha-1B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35368, gene: ADRA1B, swissprot: ADA1B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022206s012lbl.pdf) Potassium voltage-gated channel subfamily H member 6 (Organism: Homo sapiens, class: Ion channel, accessions: Q9H252, gene: KCNH6, swissprot: KCNH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27709945) Silodosin is a selective antagonist of post-synaptic alpha-1 adrenoreceptors, which are located in the human prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra. Blockade of these alpha-1 adrenoreceptors can cause smooth muscle in these tissues to relax, resulting in an improvement in urine flow and a reduction in benign prostatic hyperplasia symptoms. An in vitro study examining binding affinity of silodosin to the three subtypes of the alpha-1 adrenoreceptors (alpha-1A, alpha-1B, and alpha-1D) was conducted. The results of the study demonstrated that silodosin binds with high affinity to the alpha-1A subtype. alpha-Adrenergic Blocker (Code: N0000175553) Adrenergic Agents (Code: D018663) Adrenergic alpha-1 Receptor Antagonists (Code: D058668) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Neurotransmitter Agents (Code: D018377) Urological Agents (Code: D064804) 2008-10-08 FDA
Click to view pyridoxal Aldehyde oxidase (Organism: Mus musculus, class: Enzyme, accessions: O54754, gene: Aox1, swissprot: AOXA_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7365745) Pyridoxal is the 4-carboxyaldehyde form of vitamin B6, it is converted into pyridoxal phosphate, a coenzyme for the synthesis of amino acids, neurotransmitters, sphingolipids and aminolevulinic acid. Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) PXL
Click to view lisdexamfetamine Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) releasing agent (Source: ) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) releasing agent (Source: ) Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) inhibitor (Source: ) A dextroamphetamine drug precursor that also functions as a CENTRAL NERVOUS SYSTEM STIMULANT and DOPAMINE UPTAKE INHIBITOR and is used in the treatment of ATTENTION DEFICIT HYPERACTIVITY DISORDER. Central Nervous System Stimulant (Code: N0000175739) Central Nervous System Stimulation (Code: N0000175729) Central Nervous System Agents (Code: D002491) Central Nervous System Stimulants (Code: D000697) Dopamine Agents (Code: D015259) Dopamine Uptake Inhibitors (Code: D018765) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) 2007-02-23 FDA
Click to view paliperidone Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022043lbl.pdf) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022043lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022043lbl.pdf) Alpha-1A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P35348, gene: ADRA1A, swissprot: ADA1A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022043lbl.pdf) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022043lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022043lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022043lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021999s036lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Paliperidone is the primary active metabolite of the older antipsychotic risperidone. Paliperidone is used for the treatment of schizophrenia. Atypical Antipsychotic (Code: N0000175430) dopaminergic antagonist (Code: CHEBI:48561) serotonergic antagonist (Code: CHEBI:48279) alpha-adrenergic antagonist (Code: CHEBI:37890) H1-receptor antagonist (Code: CHEBI:37955) psychotropic drug (Code: CHEBI:35471) second generation antipsychotic (Code: CHEBI:65191) neuroprotective agent (Code: CHEBI:63726) 2006-12-19 FDA
Click to view gentian violet Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) Adenosine receptor A2a (Organism: Homo sapiens, class: GPCR, accessions: P29274, gene: ADORA2A, swissprot: AA2AR_HUMAN) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) Alpha-2B adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18089, gene: ADRA2B, swissprot: ADA2B_HUMAN) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) Histamine H2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25021, gene: HRH2, swissprot: HRH2_HUMAN) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) Sodium-dependent dopamine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q01959, gene: SLC6A3, swissprot: SC6A3_HUMAN) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) Adenosine receptor A3 (Organism: Homo sapiens, class: GPCR, accessions: P0DMS8, gene: ADORA3, swissprot: AA3R_HUMAN) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) Substance-K receptor (Organism: Homo sapiens, class: GPCR, accessions: P21452, gene: TACR2, swissprot: NK2R_HUMAN) Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Alpha-1B adrenergic receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P15823, gene: Adra1b, swissprot: ADA1B_RAT) A dye that is a mixture of violet rosanilinis with antibacterial, antifungal, and anthelmintic properties. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) histological dye (Code: CHEBI:77178) antiseptic drug (Code: CHEBI:48218) anthelminthic drug (Code: CHEBI:35443) FDA CVI
Click to view nadide A coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage. It is found widely in nature and is involved in numerous enzymatic reactions in which it serves as an electron carrier by being alternately oxidized (NAD+) and reduced (NADH). (Dorland, 27th ed) FDA
Click to view udenafil cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/12510841) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18308836) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/18308836) Udenafil is a benzenesulfonamide derivative with vasodilatory activity. Udenafil selectively inhibits phosphodiesterase type 5 (PDE5), thus inhibiting the degradation of cyclic guanosine monophosphate (cGMP) found in the smooth muscle of the corpus cavernosa and corpus spongiosum of the penis; inhibition of cGMP degradation results in prolonged muscle relaxation, vasodilation, and blood engorgement of the corpus cavernosa, and, so, prolonged penile erection. Enzyme Inhibitors (Code: D004791) Phosphodiesterase 5 Inhibitors (Code: D058986) Phosphodiesterase Inhibitors (Code: D010726) 2005-12-31 Korean Food and Drug Administration (KFDA)
Click to view darunavir Pol polyprotein (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72874, gene: pol, swissprot: Q72874_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021976s056,202895s027lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021976s056,202895s027lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20102298) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20102298) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021976s056,202895s027lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021976s056,202895s027lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily KQT member 1 (Organism: Homo sapiens, class: Ion channel, accessions: P51787, gene: KCNQ1, swissprot: KCNQ1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Potassium voltage-gated channel subfamily D member 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UK17, gene: KCND3, swissprot: KCND3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) Darunavir is an inhibitor of the HIV-1 protease. It selectively inhibits the cleavage of HIV-1 encoded Gag-Pol polyproteins in infected cells, thereby preventing the formation of mature virus particles. Darunavir exhibits activity against laboratory strains and clinical isolates of HIV-1 and laboratory strains of HIV-2. Darunavir demonstrates antiviral activity in cell culture against a broad panel of HIV-1 group M (A, B, C, D, E, F, G), and group O primary isolates. Darunavir is indicated for the treatment of HIV-1 infection. Darunavir must be co-administered with ritonavir and with other antiretroviral agents. Protease Inhibitor (Code: N0000175889) Cytochrome P450 3A Inhibitors (Code: N0000190114) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) HIV Protease Inhibitors (Code: D017320) Protease Inhibitors (Code: D011480) antiviral drug (Code: CHEBI:36044) 2006-06-23 FDA 017
Click to view lutein A xanthophyll found in the major LIGHT-HARVESTING PROTEIN COMPLEXES of plants. Dietary lutein accumulates in the MACULA LUTEA. food colouring (Code: CHEBI:77182) FDA
Click to view testosterone propionate Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT Steroid 17-alpha-hydroxylase/17,20 lyase (Organism: Homo sapiens, class: Enzyme, accessions: P05093, gene: CYP17A1, swissprot: CP17A_HUMAN An ester of TESTOSTERONE with a propionate substitution at the 17-beta position. 1974-05-02 FDA
Click to view epicriptine a sec-butyl group replaces the isobutyl group of dihydroergocryptine FDA
Click to view doripenem Peptidoglycan D,D-transpeptidase MrdA (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P0AD65, gene: mrdA, swissprot: MRDA_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022106lbl.pdf) Peptidoglycan D,D-transpeptidase FtsI (Organism: Pseudomonas aeruginosa, class: Enzyme, accessions: Q51504, gene: pbpB, swissprot: Q51504_PSEAI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022106lbl.pdf) Penicillin-binding protein 1A (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02918, gene: mrcA, swissprot: PBPA_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022106lbl.pdf) Penicillin-binding protein 1B (Organism: Escherichia coli (strain K12), class: Enzyme, accessions: P02919, gene: mrcB, swissprot: PBPB_ECOLI) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022106lbl.pdf) Voltage-dependent L-type calcium channel subunit alpha-1C (Organism: Homo sapiens, class: Ion channel, accessions: Q13936, gene: CACNA1C, swissprot: CAC1C_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25087753) has antibacterial activity; structure given in first source Carbapenems (Code: N0000011294) Penem Antibacterial (Code: N0000175496) 2007-10-12 FDA
Click to view liraglutide Glucagon-like peptide 1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P43220, gene: GLP1R, swissprot: GLP1R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206321s007lbl.pdf) An analog of glucagon-like peptide 1 and agonist of the glucagon-like peptide 1 receptor that is used as a hypoglycemic agent and supplemental therapy in the treatment of diabetes mellitus by patients who do not respond to metformin. GLP-1 Receptor Agonist (Code: N0000178480) Glucagon-Like Peptide 1 (Code: N0000170335) Glucagon-like Peptide-1 (GLP-1) Agonists (Code: N0000020058) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Hypoglycemic Agents (Code: D007004) Incretins (Code: D054795) neuroprotective agent (Code: CHEBI:63726) 2009-06-30 EMA
Click to view permethrin Permethrin is a synthetic pyrethroid and neurotoxin. It acts on the nerve cell membrane to disrupt the sodium channel current by which the polarization of the membrane is regulated. Delayed repolarization and paralysis of the pests are the consequences of this disturbance. It has a role as a pyrethroid ester insecticide, a pyrethroid ester acaricide, an agrochemical, an ectoparasiticide and a scabicide. Permethrin is used to eradicate parasites such as head lice, ticks and scabies from humans and animals. Pyrethrins (Code: N0000006014) Pyrethroid (Code: N0000175847) Enzyme Inhibitors (Code: D004791) Insecticides (Code: D007306) Pesticides (Code: D010575) scabicide (Code: CHEBI:73333) pyrethroid ester insecticide (Code: CHEBI:39116) agrochemical (Code: CHEBI:33286) ectoparasiticide (Code: CHEBI:38956) 1986-03-31 FDA
Click to view rimonabant Cannabinoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P21554, gene: CNR1, swissprot: CNR1_HUMAN) antagonist Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN Cannabinoid receptor 2 (Organism: Mus musculus, class: GPCR, accessions: P47936, gene: Cnr2, swissprot: CNR2_MOUSE G-protein coupled receptor 55 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y2T6, gene: GPR55, swissprot: GPR55_HUMAN Cannabinoid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: P34972, gene: CNR2, swissprot: CNR2_HUMAN N-arachidonyl glycine receptor (Organism: Homo sapiens, class: GPCR, accessions: Q14330, gene: GPR18, swissprot: GPR18_HUMAN Cannabinoid receptor 1 (Organism: Mus musculus, class: GPCR, accessions: P47746, gene: Cnr1, swissprot: CNR1_MOUSE Cannabinoid receptor 1 (Organism: Rattus norvegicus, class: GPCR, accessions: P20272, gene: Cnr1, swissprot: CNR1_RAT a potent & selective antagonist of the brain cannabinoid receptor Cannabinoid Receptor Antagonists (Code: D063387) Cannabinoid Receptor Modulators (Code: D063385) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Neurotransmitter Agents (Code: D018377) 2006-06-19 EMA
Click to view sodium stibogluconate Antimony complex where the metal may exist in either the pentavalent or trivalent states. The pentavalent gluconate is used in leishmaniasis. The trivalent gluconate is most frequently used in schistosomiasis. antineoplastic agent (Code: CHEBI:35610) antileishmanial agent (Code: CHEBI:70868)
Click to view cabazitaxel Tubulin beta (Organism: Homo sapiens, class: Structural, accessions: Q9H4B7|Q13885|Q9BVA1|Q13509|P04350|P68371|P07437|Q9BUF5|Q3ZCM7, gene: TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB|TUBB6|TUBB8, swissprot: TBB1_HUMAN|TBB2A_HUMAN|TBB2B_HUMAN|TBB3_HUMAN|TBB4A_HUMAN|TBB4B_HUMAN|TBB5_HUMAN|TBB6_HUMAN|TBB8_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/23337758) a microtubule inhibitor, cabazitaxel binds to tubulin and promotes its assembly into microtubules while simultaneously inhibiting disassembly. This leads to the stabilization of microtubules, which results in the inhibition of mitotic and interphase cellular functions Microtubule Inhibition (Code: N0000175085) Microtubule Inhibitor (Code: N0000175592) antineoplastic agent (Code: CHEBI:35610) 2010-06-17 FDA
Click to view edaravone reactive chemical species (Organism: None, class: Reactive chemical species, accessions: None, gene: None, swissprot: None) other (Source: http://www.ncbi.nlm.nih.gov/pubmed/19466525) Edaravone protects neurons from oxidative stress by scavenging free radicals that may cause cellular damage, and this mechanism is expected to be effective both in patients with acute cerebral infarction and in those with ALS 2017-05-05 FDA
Click to view cefcapene Cefcapene is a semisynthetic third-generation cephalosporin with antibacterial activity. Cefcapene binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. Cefcapene is active against Staphylococcus spp., Streptococcus spp., Neisseria gonorrhoeae, Moraxella (Branhamella) catarrhalis, Escherichia coli, Citrobacter spp., Klebsiella spp., Enterobacter spp., Proteus spp., Morganella morganii, Providencia spp., Haemophilus influenzae, Peptostreptococcus spp., Bacteroides spp., Prevotella spp. (excluding Prevotella vivia). It is used for the treatment of skin and skin structure infections, respiratory tract infections, urinary tract infections, cholecystitis, cholangitis, otitis externa and media. antibacterial drug (Code: CHEBI:36047) 1997-06-01 PMDA
Click to view carbocisteine Carbocisteine is a mucolytic agent that modifies mucous secretions. It acts during the mucous gel phase, most likely by breaking up the disulfide bonds in glycoproteins, thereby favouring expectoration. Carbocisteine is indicated for the adjunctive therapy of respiratory tract disorders characterised by excessive, viscous mucus, including chronic obstructive airways disease. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Expectorants (Code: D005100) Respiratory System Agents (Code: D019141) mucolytic (Code: CHEBI:77034) 1992 UK Medicines and Healthcare Products Regulatory Agency (MHRA) CCS
Click to view temsirolimus Peptidyl-prolyl cis-trans isomerase FKBP1A (Organism: Homo sapiens, class: Enzyme, accessions: P62942, gene: FKBP1A, swissprot: FKB1A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022088s021s023lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022088s021s023lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022088s021s023lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022088s021s023lbl.pdf) Temsirolimus is an ester analog of rapamycin. Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor. Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) 2007-05-30 FDA
Click to view fampridine Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022250s015lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/fampyra-epar-product-information_en.pdf) Potassium voltage-gated channel subfamily C member 1 (Organism: Mus musculus, class: Unclassified, accessions: P15388, gene: Kcnc1, swissprot: KCNC1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/7517498) Potassium voltage-gated channel subfamily A member 10 (Organism: Homo sapiens, class: Ion channel, accessions: Q16322, gene: KCNA10, swissprot: KCA10_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10836990) Fampridine (dalfampridine) is a potassium channel blocker, used as a research tool in characterizing subtypes of the potassium channel. Fampridine has also been used to manage some of the symptoms of multiple sclerosis, and is indicated for symptomatic improvement of walking in adults with several variations of the disease. The mechanism by which dalfampridine exerts its therapeutic effect has not been fully elucidated. Potassium Channel Blocker (Code: N0000192795) Potassium Channel Antagonists (Code: N0000175448) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Potassium Channel Blockers (Code: D026902) orphan drug (Code: CHEBI:71031) avicide (Code: CHEBI:33289) 2010-01-22 FDA 4AP
Click to view methyldopate Methyldopate is an antihypertensive agent and a prodrug of methyldopa which is administered by intravenous infusion. Methyldopate is hydrolyzed to methyldopa. (See: methyldopa) 1962-12-20 FDA
Click to view alcaftadine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist Alcaftadine is an H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated. Histamine H1 Receptor Antagonists (Code: N0000000190) Histamine-1 Receptor Antagonist (Code: N0000175587) Histamine Agents (Code: D018494) Histamine Antagonists (Code: D006633) Histamine H1 Antagonists (Code: D006634) Neurotransmitter Agents (Code: D018377) H1-receptor antagonist (Code: CHEBI:37955) anti-allergic agent (Code: CHEBI:50857) 2010-07-28 FDA
Click to view ulipristal Progesterone receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P06401, gene: PGR, swissprot: PRGR_HUMAN) agonist/antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022474s010lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022474s010lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022474s010lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022474s010lbl.pdf) Ulipristal is a selective progesterone receptor modulator used for the purposes of emergency contraception and for the treatment of uterine fibroids. It is a derivative of 19-norprogesterone and has both antagonistic and partial agonist activity at the progesterone receptor. It also binds to glucocorticoid receptor. The exact mechanism of action for ulipristal is still currently debated, though there is evidence that it functions by inhibiting ovulation. Progesterone Agonist/Antagonist (Code: N0000191263) Selective Progesterone Receptor Modulators (Code: N0000191262) Contraceptive Agents (Code: D003270) Contraceptive Agents, Female (Code: D003271) Reproductive Control Agents (Code: D012102) contraceptive drug (Code: CHEBI:49323) progesterone receptor modulator (Code: CHEBI:71027) 2009-05-15 EMA 2S0
Click to view fingolimod fingolimod: Sphingosine kinase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q9NYA1, gene: SPHK1, swissprot: SPHK1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022527s029s030lbl.pdf) Cytochrome P450 4F2 (Organism: Homo sapiens, class: Enzyme, accessions: P78329, gene: CYP4F2, swissprot: CYP4F2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022527s029s030lbl.pdf) Transient receptor potential cation channel subfamily M member 7 (Organism: Mus musculus, class: Unclassified, accessions: Q923J1, gene: Trpm7, swissprot: TRPM7_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23145923) fingolimod-phosphate: Sphingosine 1-phosphate receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P21453, gene: S1PR1, swissprot: S1PR1_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022527s029s030lbl.pdf) Sphingosine 1-phosphate receptor 3 (Organism: Homo sapiens, class: GPCR, accessions: Q99500, gene: S1PR3, swissprot: S1PR3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16078855) Sphingosine 1-phosphate receptor 5 (Organism: Homo sapiens, class: GPCR, accessions: Q9H228, gene: S1PR5, swissprot: S1PR5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16078855) Sphingosine 1-phosphate receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: O95977, gene: S1PR4, swissprot: S1PR4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16078855) Sphingosine 1-phosphate receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: O95136, gene: S1PR2, swissprot: S1PR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/16078855) Fingolimod is metabolized by sphingosine kinase to the active metabolite, fingolimod-phosphate. Fingolimodphosphate is a sphingosine 1-phosphate receptor modulator, and binds with high affinity to sphingosine 1-phosphate receptors 1, 3, 4, and 5. Fingolimod-phosphate blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood. The mechanism by which fingolimod exerts therapeutic effects in multiple sclerosis is unknown, but may involve reduction of lymphocyte migration into the central nervous system. Sphingosine 1-Phosphate Receptor Modulators (Code: N0000181815) Sphingosine 1-phosphate Receptor Modulator (Code: N0000181816) Immunologic Factors (Code: D007155) Immunosuppressive Agents (Code: D007166) antineoplastic agent (Code: CHEBI:35610) immunosuppressive agent (Code: CHEBI:35705) prodrug (Code: CHEBI:50266) 2010-09-21 FDA
Click to view lurasidone D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/200603s029lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/200603s029lbl.pdff) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/200603s029lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) partial agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/200603s029lbl.pdf) Alpha-2A adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08913, gene: ADRA2A, swissprot: ADA2A_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/200603s029lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/200603s029lbl.pdf) Alpha-2C adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P18825, gene: ADRA2C, swissprot: ADA2C_HUMAN) modulator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/200603s029lbl.pdf) Lurasidone is used (generally as the hydrochloride salt) as an atypical antipsychotic for the treatment of schizophrenia. It has a role as an adrenergic antagonist, a dopaminergic antagonist, a serotonergic antagonist and a second generation antipsychotic. Atypical Antipsychotic (Code: N0000175430) Adrenergic Agents (Code: D018663) Adrenergic alpha-2 Receptor Antagonists (Code: D058669) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Dopamine D2 Receptor Antagonists (Code: D065127) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin 5-HT2 Receptor Antagonists (Code: D058830) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Tranquilizing Agents (Code: D014149) adrenergic antagonist (Code: CHEBI:37887) dopaminergic antagonist (Code: CHEBI:48561) serotonergic antagonist (Code: CHEBI:48279) second generation antipsychotic (Code: CHEBI:65191) 2010-10-28 FDA
Click to view ceftaroline fosamil Ceftaroline: Penicillin-binding protein 2X (Organism: Streptococcus pneumoniae (strain ATCC BAA-255 / R6), class: Enzyme, accessions: P59676, gene: pbpX, swissprot: PBPX_STRR6) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/200327s022lbl.pdf) Ceftaroline fosamil is a semi-synthetic, prodrug of thefifth-generation cephalosporin derivative ceftaroline. Ceftaroline fosamil is converted into bioactive ceftaroline in plasma by a phosphatase enzyme. The bactericidal action of ceftaroline is mediated through binding to essential penicillin-binding proteins (PBPs). Ceftaroline is bactericidal against S. aureus due to its affinity for PBP2a and against Streptococcus pneumoniae due to its affinity for PBP2x. Ceftaroline has been shown to be active against Staphylococcus aureus, Streptococcus pyogenes, Streptococcus agalactiae, Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Streptococcus pneumoniae, Haemophilus influenzae. Ceftaroline fosamil is indicated for the treatment of Acute Bacterial Skin and Skin Structure Infectionsand Community-Acquired Bacterial Pneumonia. Cephalosporin Antibacterial (Code: N0000175488) Cephalosporins (Code: N0000011161) prodrug (Code: CHEBI:50266) antibacterial drug (Code: CHEBI:36047) 2010-10-29 FDA Cefta
AI8
Click to view droxypropine
Click to view eribulin Tubulin beta (Organism: Homo sapiens, class: Structural, accessions: P04350|P07437|P68371|Q13509|Q13885|Q3ZCM7|Q9BUF5|Q9BVA1|Q9H4B7, gene: TUBB|TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB6|TUBB8, swissprot: TBB1_HUMAN|TBB2A_HUMAN|TBB2B_HUMAN|TBB3_HUMAN|TBB4A_HUMAN|TBB4B_HUMAN|TBB5_HUMAN|TBB6_HUMAN|TBB8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/201532s016lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/201532s016lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/201532s016lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/201532s016lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/201532s016lbl.pdf) Eribulin inhibits the growth phase of microtubules without affecting the shortening phase and sequesters tubulin into nonproductive aggregates. Eribulin exerts its effects via a tubulin-based antimitotic mechanism leading to G2/M cell-cycle block, disruption of mitotic spindles, and, ultimately, apoptotic cell death after prolonged mitotic blockage. In addition, eribulin treatment of human breast cancer cells caused changes in morphology and gene expression as well as decreased migration and invasiveness in vitro. In mouse xenograft models of human breast cancer, eribulin treatment was associated with increased vascular perfusion and permeability in the tumor cores, resulting in reduced tumor hypoxia, and changes in the expression of genes in tumor specimens associated with a change in phenotype. Microtubule Inhibition (Code: N0000175085) Microtubule Inhibitor (Code: N0000175592) antineoplastic agent (Code: CHEBI:35610) 2010-11-15 FDA 6K9
Click to view boceprevir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202258s016lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202258s016lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202258s016lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202258s016lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202258s016lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202258s016lbl.pdf) Cathepsin K (Organism: Homo sapiens, class: Enzyme, accessions: P43235, gene: CTSK, swissprot: CATK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19841155) Cathepsin L2 (Organism: Homo sapiens, class: Enzyme, accessions: O60911, gene: CTSV, swissprot: CATL2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19841155) Cathepsin F (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBX1, gene: CTSF, swissprot: CATF_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19841155) Chymase (Organism: Homo sapiens, class: Enzyme, accessions: P23946, gene: CMA1, swissprot: CMA1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19841155) Cathepsin S (Organism: Homo sapiens, class: Enzyme, accessions: P25774, gene: CTSS, swissprot: CATS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19841155) Cathepsin L1 (Organism: Homo sapiens, class: Enzyme, accessions: P07711, gene: CTSL, swissprot: CATL1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19841155) Cathepsin B (Organism: Homo sapiens, class: Enzyme, accessions: P07858, gene: CTSB, swissprot: CATB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20823284) Aldo-keto reductase family 1 member C2 (Organism: Homo sapiens, class: Enzyme, accessions: P52895, gene: AKR1C2, swissprot: AK1C2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21123164) Aldo-keto reductase family 1 member C3 (Organism: Homo sapiens, class: Enzyme, accessions: P42330, gene: AKR1C3, swissprot: AK1C3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/21123164) Boceprevir is an inhibitor of the HCV NS3/4A protease that is necessary for the proteolytic cleavage of the HCV encoded polyprotein into mature forms of the NS4A, NS4B, NS5A and NS5B proteins. Boceprevir covalently, yet reversibly, binds to the NS3 protease active site serine (S139) through an (alpha)-ketoamide functional group to inhibit viral replication in HCV-infected host cells. Boceprevir is indicated for the treatment of chronic hepatitis C (CHC) genotype 1 infection, in combination with peginterferon alfa and ribavirin, in adult patients with compensated liver disease, including cirrhosis, who are previously untreated or who have failed previous interferon and ribavirin therapy, including prior null responders, partial responders, and relapsers. antiviral drug (Code: CHEBI:36044) HCV NS3/4A Protease Inhibitors (Code: N0000182638) Hepatitis C Virus NS3/4A Protease Inhibitor (Code: N0000182639) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 3A5 Inhibitors (Code: N0000190115) 2011-05-13 FDA HU5
MCX
Click to view telaprevir Genome polyprotein (Organism: Hepatitis C virus genotype 1a (isolate H), class: Polyprotein, accessions: P27958, gene: None, swissprot: POLG_HCVH) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/201917s012lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/201917s012lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/201917s012lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/201917s012lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/201917s012lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/201917s012lbl.pdf) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/201917s012lbl.pdf) Cathepsin K (Organism: Homo sapiens, class: Enzyme, accessions: P43235, gene: CTSK, swissprot: CATK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19841155) Chymotrypsin-like elastase family member 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UNI1, gene: CELA1, swissprot: CELA1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19841155) Chymase (Organism: Homo sapiens, class: Enzyme, accessions: P23946, gene: CMA1, swissprot: CMA1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19841155) Cathepsin S (Organism: Homo sapiens, class: Enzyme, accessions: P25774, gene: CTSS, swissprot: CATS_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19841155) Neutrophil elastase (Organism: Homo sapiens, class: Enzyme, accessions: P08246, gene: ELANE, swissprot: ELNE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20823284) Chronic hepatitis C virus infection antiviral drug (Code: CHEBI:36044) HCV NS3/4A Protease Inhibitors (Code: N0000182638) Hepatitis C Virus NS3/4A Protease Inhibitor (Code: N0000182639) Cytochrome P450 3A Inhibitors (Code: N0000190114) P-Glycoprotein Inhibitors (Code: N0000185503) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 2B1 Inhibitors (Code: N0000190109) 2011-05-23 FDA
Click to view rilpivirine Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72547, gene: pol, swissprot: Q72547_9HIV1) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202022s013lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202022s013lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23428312) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23428312) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23428312) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23428312) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23428312) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23428312) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23428312) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/23428312) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/23428312) Rilpivirine is a diarylpyrimidine. Rilpivirine is a second-generation non-nucleoside reverse transcriptase inhibitor. Rilpivirine is used in combination with other antiretroviral agents in the therapy of human immunodeficiency virus (HIV) infection. Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor (Code: N0000175463) Non-Nucleoside Reverse Transcriptase Inhibitors (Code: N0000009948) Non-Nucleoside Analog (Code: N0000175460) Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Enzyme Inhibitors (Code: D004791) Nucleic Acid Synthesis Inhibitors (Code: D019384) Reverse Transcriptase Inhibitors (Code: D018894) 2011-05-20 FDA T27
Click to view ivacaftor Cystic fibrosis transmembrane conductance regulator (Organism: Homo sapiens, class: Ion channel, accessions: P13569, gene: CFTR, swissprot: CFTR_HUMAN) positive modulator Ivacaftor is a potentiator of the CFTR protein. The CFTR protein is a chloride channel present at the surface of epithelial cells in multiple organs. Ivacaftor facilitates increased chloride transport by potentiating the channel-open probability (or gating) of the CFTR protein. Cystic Fibrosis Transmembrane Conductance Regulator Potentiator (Code: N0000184146) Chloride Channel Activation Potentiators (Code: N0000184145) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) P-Glycoprotein Inhibitors (Code: N0000185503) Cytochrome P450 3A Inhibitors (Code: N0000190114) Chloride Channel Agonists (Code: D065101) Membrane Transport Modulators (Code: D049990) orphan drug (Code: CHEBI:71031) 2012-01-31 FDA
Click to view linagliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206073s019lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206073s019lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Enzyme, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22568694) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Enzyme, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22568694) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Enzyme, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22568694) Prolyl endopeptidase FAP (Organism: Mus musculus, class: Enzyme, accessions: P97321, gene: Fap, swissprot: SEPR_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24617858) Prolyl endopeptidase FAP (Organism: Homo sapiens, class: Enzyme, accessions: Q12884, gene: FAP, swissprot: SEPR_HUMAN) (Source: https://www.ncbi.nlm.nih.gov/pubmed/27190600) Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Linagliptin is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other oral hypoglycemic agents. Linagliptin has been linked to rare instances of clinically apparent liver injury. Dipeptidyl Peptidase 4 Inhibitors (Code: N0000175912) Dipeptidyl Peptidase 4 Inhibitor (Code: N0000175913) Dipeptidyl-Peptidase IV Inhibitors (Code: D054873) Enzyme Inhibitors (Code: D004791) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Hypoglycemic Agents (Code: D007004) Incretins (Code: D054795) Protease Inhibitors (Code: D011480) hypoglycemic agent (Code: CHEBI:35526) 2011-05-02 FDA 356
Click to view abiraterone acetate Abiraterone: Steroid 17-alpha-hydroxylase/17,20 lyase (Organism: Homo sapiens, class: Enzyme, accessions: P05093, gene: CYP17A1, swissprot: CP17A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 11B1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P15538, gene: CYP11B1, swissprot: C11B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18672868) Cytochrome P450 11B2, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P19099, gene: CYP11B2, swissprot: C11B2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18672868) Abiraterone acetate is an antiandrogen. Abiraterone acetate is converted in vivo to abiraterone, an androgen biosynthesis inhibitor, that inhibits 17 alpha-hydroxylase/C17,20-lyase (CYP17). Androgen sensitive prostatic carcinoma responds to treatment that decreases androgen levels. Abiraterone acetate is indicated in combination with methylprednisolone for the treatment of patients with metastatic castration-resistant prostate cancer. (See: abiraterone) Cytochrome P450 17A1 Inhibitors (Code: N0000182632) Cytochrome P450 17A1 Inhibitor (Code: N0000182633) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Cytochrome P450 2C8 Inhibitors (Code: N0000187062) Antineoplastic Agents (Code: D000970) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Metabolic Side Effects of Drugs and Substances (Code: D065606) Steroid Synthesis Inhibitors (Code: D065088) prodrug (Code: CHEBI:50266) antineoplastic agent (Code: CHEBI:35610) 2011-04-28 FDA
Click to view gabapentin enacarbil Sodium-dependent multivitamin transporter (Organism: Homo sapiens, class: Transporter accessions: Q9Y289, gene: SLC5A6, swissprot: SC5A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15146028) Gabapentin enacarbil is a prodrug of gabapentin and, accordingly, its therapeutic effects in restless legs syndrome and postherpetic neuralgia are attributable to gabapentin. After oral administration, gabapentin enacarbil undergoes extensive first-pass hydrolysis by non-specific carboxylesterases primarily in enterocytes and to a lesser extent in the liver, to form gabapentin, carbon dioxide, acetaldehyde, and isobutyric acid. (See: gabapentin) prodrug (Code: CHEBI:50266) anticonvulsant (Code: CHEBI:35623) 2011-04-06 FDA
Click to view vandetanib Vascular endothelial growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P17948, gene: FLT1, swissprot: VGFR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Vascular endothelial growth factor receptor 3 (Organism: Homo sapiens, class: Kinase, accessions: P35916, gene: FLT4, swissprot: VGFR3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Platelet-derived growth factor receptor beta (Organism: Homo sapiens, class: Kinase, accessions: P09619, gene: PDGFRB, swissprot: PGFRB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Macrophage colony-stimulating factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P07333, gene: CSF1R, swissprot: CSF1R_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Cyclin-dependent kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P06493, gene: CDK1, swissprot: CDK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Angiopoietin-1 receptor (Organism: Homo sapiens, class: Kinase, accessions: Q02763, gene: TEK, swissprot: TIE2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Hepatocyte growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P08581, gene: MET, swissprot: MET_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12477352) Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26874741) Protein-tyrosine kinase 6 (Organism: Homo sapiens, class: Kinase, accessions: Q13882, gene: PTK6, swissprot: PTK6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022405s014lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022405s014lbl.pdf) Dimethylaniline monooxygenase [N-oxide-forming] 3 (Organism: Homo sapiens, class: Enzyme, accessions: P31513, gene: FMO3, swissprot: FMO3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022405s014lbl.pdf) Dimethylaniline monooxygenase [N-oxide-forming] 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q01740, gene: FMO1 swissprot: FMO1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022405s014lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022405s014lbl.pdf) Vandetanib is an oral once-daily kinase inhibitor of tumour angiogenesis and tumour cell proliferation with the potential for use in a broad range of tumour types. In vitro studies have shown that vandetanib inhibits the tyrosine kinase activity of the EGFR and VEGFR families, RET, BRK, TIE2, and members of the EPH receptor and Src kinase families. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, and maintenance of the tumor microenvironment. In addition, the N-desmethyl metabolite of the drug, representing 7 to 17.1% of vandetanib exposure, has similar inhibitory activity to the parent compound for VEGF receptors (KDR and Flt-1) and EGFR. In vitro, vandetanib inhibited epidermal growth factor (EGF)-stimulated receptor tyrosine kinase phosphorylation in tumor cells and endothelial cells and VEGF-stimulated tyrosine kinase phosphorylation in endothelial cells. In vivo, vandetanib administration reduced tumor cell-induced angiogenesis, tumor vessel permeability, and inhibited tumor growth and metastasis in mouse models of cancer. Vandetanib is indicated for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease. antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) 2011-04-06 FDA ZD6
Click to view fidaxomicin DNA-directed RNA polymerase (Organism: Peptoclostridium difficile (strain 630), class: Enzyme, accessions: Q182S6|Q18CF1|Q18CF3|Q18CI5, gene: rpoA|rpoB|rpoC|rpoZ, swissprot: RPOA_PEPD6|RPOB_PEPD6|RPOC_PEPD6|RPOZ_PEPD6) inhibitor Fidaxomicin is a fermentation product obtained from the Actinomycete Dactylosporangium aurantiacum. In vitro, fidaxomicin is active primarily against species of clostridia, including Clostridium difficile by inhibiting RNA synthesis by RNA polymerases. Macrolides (Code: N0000007529) Macrolide Antibacterial (Code: N0000175431) antibacterial drug (Code: CHEBI:36047) 2011-05-27 FDA
Click to view retigabine Potassium voltage-gated channel subfamily KQT member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O43526, gene: KCNQ2, swissprot: KCNQ2_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022345s011lbl.pdf) Potassium voltage-gated channel subfamily KQT member 4 (Organism: Homo sapiens, class: Ion channel, accessions: P56696, gene: KCNQ4, swissprot: KCNQ4_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022345s011lbl.pdf) Potassium voltage-gated channel subfamily KQT member 5 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NR82, gene: KCNQ5, swissprot: KCNQ5_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022345s011lbl.pdf) Potassium voltage-gated channel subfamily KQT member 3 (Organism: Homo sapiens, class: Ion channel, accessions: O43525, gene: KCNQ3, swissprot: KCNQ3_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022345s011lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022345s011lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022345s011lbl.pdf) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022345s011lbl.pdf) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022345s011lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022345s011lbl.pdf) Arylamine N-acetyltransferase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P11245, gene: NAT2, swissprot: ARY2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022345s011lbl.pdf) Retigabine is a unique anticonvulsant used largely as an adjunctive agent in the treatment of partial seizures. In vitro studies indicate that retigabine enhances transmembrane potassium currents mediated by the KCNQ (Kv7.2 to 7.5) family of ion channels. By activating KCNQ channels, ezogabine is thought to stabilize the resting membrane potential and reduce brain excitability. Potassium Channel Openers (Code: N0000182728) Potassium Channel Opener (Code: N0000182729) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) anticonvulsant (Code: CHEBI:35623) 2011-03-28 EMA
Click to view rivaroxaban Coagulation factor X (Organism: Homo sapiens, class: Enzyme, accessions: P00742, gene: F10, swissprot: FA10_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202439s029lbl.pdf) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202439s029lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202439s029lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202439s029lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202439s029lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202439s029lbl.pdf) Rivaroxaban is a selective inhibitor of FXa. By inhibiting FXa, rivaroxaban decreases thrombin generation. Rivaroxaban is indicated to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation, treatment and prophylaxis of deep vein thrombosis. Anticoagulants (Code: D000925) Antithrombins (Code: D000991) Enzyme Inhibitors (Code: D004791) Factor Xa Inhibitors (Code: D065427) Hematologic Agents (Code: D006401) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) anticoagulant (Code: CHEBI:50249) Factor Xa Inhibitor (Code: N0000175637) 2011-07-01 FDA RIV
Click to view indacaterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022383s000lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022383s000lbl.pdf) Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022383s000lbl.pdf) D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/25065493) Indacaterol is a beta2-Adrenergic Agonist for the once-daily treatment of asthma and chronic obstructive pulmonary disease. Adrenergic beta2-Agonists (Code: N0000009922) beta2-Adrenergic Agonist (Code: N0000175779) beta-adrenergic agonist (Code: CHEBI:35522) bronchodilator agent (Code: CHEBI:35523) 2011-07-01 FDA
Click to view ticagrelor P2Y purinoceptor 12 (Organism: Homo sapiens, class: GPCR, accessions: Q9H244, gene: P2RY12, swissprot: P2Y12_HUMAN) antagonist (Source: https://www.ema.europa.eu/documents/product-information/brilique-epar-product-information_en.pdf) Equilibrative nucleoside transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q99808, gene: SLC29A1, swissprot: S29A1_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/brilique-epar-product-information_en.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/brilique-epar-product-information_en.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/brilique-epar-product-information_en.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/brilique-epar-product-information_en.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) weak inhibitor (Source: https://www.ema.europa.eu/documents/product-information/brilique-epar-product-information_en.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21177984) Ticagrelor is a platelet aggregation inhibitor which is used for prevention of thromboembolic events in patients with acute coronary syndrome. It has a role as a platelet aggregation inhibitor and a P2Y12 receptor antagonist. P2Y12 Platelet Inhibitor (Code: N0000182142) Phenylalanine Hydroxylase Activators (Code: N0000190482) Decreased Platelet Aggregation (Code: N0000008832) P2Y12 Receptor Antagonists (Code: N0000182143) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) Cytochrome P450 3A5 Inhibitors (Code: N0000190115) P-Glycoprotein Inhibitors (Code: N0000185503) Neurotransmitter Agents (Code: D018377) Purinergic Agents (Code: D058905) Purinergic Antagonists (Code: D058914) Purinergic P2 Receptor Antagonists (Code: D058919) Purinergic P2Y Receptor Antagonists (Code: D058921) platelet aggregation inhibitor (Code: CHEBI:50427) 2010-12-03 EMA TIQ
Click to view vemurafenib Serine/threonine-protein kinase B-raf (Organism: Homo sapiens, class: Kinase, accessions: P15056, gene: BRAF, swissprot: BRAF_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Serine/threonine-protein kinase A-Raf (Organism: Homo sapiens, class: Kinase, accessions: P10398, gene: ARAF, swissprot: ARAF_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Serine/threonine-protein kinase A-Raf (Organism: Homo sapiens, class: Kinase, accessions: P10398, gene: ARAF, swissprot: ARAF_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Tyrosine-protein kinase Srms (Organism: Homo sapiens, class: Kinase, accessions: Q9H3Y6, gene: SRMS, swissprot: SRMS_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Activated CDC42 kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q07912, gene: TNK2, swissprot: ACK1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Mitogen-activated protein kinase kinase kinase kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: O95819, gene: MAP4K4, swissprot: M4K4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Mitogen-activated protein kinase kinase kinase kinase 5 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y4K4, gene: MAP4K5, swissprot: M4K5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Tyrosine-protein kinase Fgr (Organism: Homo sapiens, class: Kinase, accessions: P09769, gene: FGR, swissprot: FGR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/202429s016lbl.pdf) Vemurafenib is a low molecular weight, orally available inhibitor of some mutated forms of BRAF serine- threonine kinase, including BRAF V600E. Vemurafenib also inhibits other kinases in vitro such as CRAF, ARAF, wild-type BRAF, SRMS, ACK1, MAP4K5, and FGR at similar concentrations. Some mutations in the BRAF gene including V600E result in constitutively activated BRAF proteins, which can cause cell proliferation in the absence of growth factors that would normally be required for proliferation. Vemurafenib has anti-tumor effects in cellular and animal models of melanomas with mutated BRAF V600E. Vemurafenib is indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation and for the treatment of patients with Erdheim-Chester Disease with BRAF V600 mutation. Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) antineoplastic agent (Code: CHEBI:35610) Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) Cytochrome P450 1A2 Inhibitors (Code: N0000182138) P-Glycoprotein Inhibitors (Code: N0000185503) 2011-08-17 FDA 032
Click to view vismodegib Smoothened homolog (Organism: Homo sapiens, class: GPCR, accessions: Q99835, gene: SMO, swissprot: SMO_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203388s014lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203388s014lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203388s014lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203388s014lbl.pdf) Vismodegib is a hedgehog (Hh) pathway inhibitor. Vismodegib binds to and inhibits Smoothened, a transmembrane protein involved in Hedgehog signal transduction. Vismodegib is indicated for the treatment of adults with metastatic basal cell carcinoma, or with locally advanced basal cell carcinoma that has recurred following surgery or who are not candidates for surgery and who are not candidates for radiation. Hedgehog Pathway Inhibitor (Code: N0000184149) Smoothened Receptor Antagonists (Code: N0000184148) antineoplastic agent (Code: CHEBI:35610) 2012-01-30 FDA VIS
Click to view sugammadex Sugammadex is a modified gamma cyclodextrin. It forms a complex with the neuromuscular blocking agents rocuronium and vecuronium, and it reduces the amount of neuromuscular blocking agent available to bind to nicotinic cholinergic receptors in the neuromuscular junction. Sugammadex is indicated for reversal of neuromuscular blockade during surgery in adults. gamma-Cyclodextrins (Code: N0000168522) neuromuscular agent (Code: CHEBI:51372) 2015-12-15 FDA
Click to view threonine Threonine is an essential amino acid in humans (provided by food), Threonine is an important residue of many proteins, such as tooth enamel, collagen, and elastin. An important amino acid for the nervous system, threonine also plays an important role in porphyrin and fat metabolism and prevents fat buildup in the liver. Useful with intestinal disorders and indigestion, threonine has also been used to alleviate anxiety and mild depression. FDA DTH
THR
Click to view alanine Alanine is a non-essential amino acid that occurs in high levels in its free state in plasma. It is produced from pyruvate by transamination. It is involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and the central nervous system. Alanine is medically used as a dietary supplement for conditions such as fructose intolerance, muscle atrophy, low birth weight. Amino Acid (Code: N0000175780) Amino Acids (Code: N0000006806) 1971-09-24 FDA ALA
DAL
Click to view bismuth subsalicylate Bismuth Subsalicylate is a bismuth salt of salicylic acid. Little absorbed from the gastrointestinal tract, bismuth subsalicylate exerts a local effect on the gastric mucosa, coating it and protecting it from the corrosive effects of acid and pepsin. This agent also has local antimicrobial properties. Upon oral administration, bismuth subsalicylate is almost completely hydrolyzed in the gastrointestinal tract to bismuth and salicylic acid. Bismuth Subsalicylate is used to treat nausea, heartburn, indigestion, upset stomach, diarrhea, and other temporary discomforts of the stomach and gastrointestinal tract. Bismuth Subsalicylate in combination with metronidazole and tetracycline is indicated for treatment of patients with H. pylori infection and duodenal ulcer disease. (See: salicylic acid) Bismuth (Code: N0000007888) Antidiarrheals (Code: D000930) Gastrointestinal Agents (Code: D005765) 1996-08-15 FDA
Click to view thymol Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/20356305) Thymol is a phenol obtained from thyme oil or other volatile oils used as a stabilizer in pharmaceutical preparations, and as an antiseptic (antibacterial or antifungal) agent. It was formerly used as a vermifuge. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Antifungal Agents (Code: D000935) FDA IPB
Click to view cineole 1,4-cineole is also available; solvent for gutta-percha; main constituent of oil of Eucalyptus (ingalipt) Anti-Infective Agents (Code: D000890) Solvents (Code: D012997) flavouring agent (Code: CHEBI:35617) FDA CNL
Click to view carbamide Carbamide (urea) is a nitrogenous compound containing a carbonyl group attached to two amine groups with osmotic diuretic activity. In vivo, urea is formed in the liver via the urea cycle from ammonia and is the final end product of protein metabolism. Administration of urea elevates blood plasma osmolality, resulting in enhanced flow of water from tissues, including the brain, cerebrospinal fluid and eye, into interstitial fluid and plasma, thereby decreasing pressure in those tissues and increasing urine outflow. flour treatment agent (Code: CHEBI:64577) fertilizer (Code: CHEBI:33287) 1966-10-05 FDA URE
Click to view phenol Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20185318) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20185318) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20185318) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20185318) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20185318) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20185318) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20185318) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20674354) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21332115) Carbonic anhydrase 2 (Organism: Cryptococcus neoformans var. grubii, class: Unclassified, accessions: Q3I4V7, gene: CAN2, swissprot: Q3I4V7_CRYNV) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21332115) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21332115) Phenol is an antiseptic and disinfectant. It is active against a wide range of micro-organisms including some fungi and viruses, but is only slowly effective against spores. Phenol has been used to disinfect skin and to relieve itching. Phenol is also used as an oral analgesic or anesthetic in products such as Chloraseptic to treat pharyngitis. Additionally, phenol and its related compounds are used in surgical ingrown toenail treatment, a process termed phenolization. Phenol is a toxic compound whose vapours are corrosive to the skin, eyes, and respiratory tract. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Cardiovascular Agents (Code: D002317) Disinfectants (Code: D004202) Pharmaceutical Solutions (Code: D019999) Sclerosing Solutions (Code: D012597) antiseptic drug (Code: CHEBI:48218) 1956-02-01 Spanish Agency of Medicines and Medical Products (AEMPS) IPH
Click to view allantoin Allantoin is a diureide of glyoxylic acid that is produced from uric acid. Allantoin is endogenous to the human body and also found as a normal component of human diets Label. In healthy human volunteers, the mean plasma concentration of allantoin is about 2-3 mg/l. During exercise, the plasma allantoin concentration rapidly increases about two fold and remains elevated Label. In human muscle, urate is oxidized to allantoin during such exercise Label. Allantoin is found in OTC cosmetic products and other commercial products such as oral hygiene products, in shampoos, lipsticks, anti-acne products, sun care products, and clarifying lotions. Dermatologic Agents (Code: D003879) vulnerary (Code: CHEBI:73336) FDA 3AL
Click to view Padimate O Padimate O is an active sunscreen agent in cosmetics and over-the-counter sunscreen drug products in concentrations up to 8%. It is a structurally-related compound to Aminobenzoic acid that absorbs UV-B rays to prevent photodamage. It is proposed that simultaneous contact of padimate O with keratinocytes can stimulate the diffusion through human epidermis. Upon photoexcitation, padimate O generates singlet oxygen and forms carbon-centred free radicals. While padimate O attenuates simple and repairable, UV-induced cellular damage, it may also increase complex chemical damage that is more difficult to repair by normal cells. 1960-12-31 Health Canada
Click to view hydroxyproline Hydroxyproline is a nonessential amino acid derivative formed during post-translational protein modification through hydroxylation of the amino acid proline by the enzyme prolyl hydroxylase which requires vitamin C as a co-factor. Hydroxyproline is a major component of the protein collagen and plays a key role in the stability of the collagen triple helix. It can be used as an indicator to determine the amount of collagen. Increased hydroxyproline levels in the urine and/or serum are normally associated with degradation of connective tissue. Vitamin C deficiency decreases the conversion of proline to hydroxyproline, which leads to reduced collagen stability. Therapeutically, hydroxyproline is being studied as an an experimental medicine but is approved in France as a combination topical gel product called Cicactive for small, superficial wounds. 1985-07-19 ANSM (French National Agency for Medicines and Health Products Safety) HYP
HZP
Click to view piperonyl butoxide Cytochrome P450 (Organism: Pediculus humanus subsp. corporis, class: Enzyme, accessions: E0V9R7|E0VAD1|E0VBK5|E0VCA5|E0VCW8|E0VCW9|E0VDM3|E0VDR0|E0VED4|E0VGV6|E0VHL8|E0VHZ1|E0VJJ0|E0VM29|E0VMV6|E0VMV7|E0VMW9|E0VQ45|E0VQ46|E0VQ47|E0VRD2|E0VSD4|E0VSD5|E0VUR0|E0VUR1|E0VV39|E0VV52|E0VV70|E0VV72|E0VXT9|E0VZW4|E0W115|E0W2B1|E0W389|E0W4F7, gene: None, swissprot: E0V9R7_PEDHC|E0VAD1_PEDHC|E0VBK5_PEDHC|E0VCA5_PEDHC|E0VCW8_PEDHC|E0VCW9_PEDHC|E0VDM3_PEDHC|E0VDR0_PEDHC|E0VED4_PEDHC|E0VGV6_PEDHC|E0VHL8_PEDHC|E0VHZ1_PEDHC|E0VJJ0_PEDHC|E0VM29_PEDHC|E0VMV6_PEDHC|E0VMV7_PEDHC|E0VMW9_PEDHC|E0VQ45_PEDHC|E0VQ46_PEDHC|E0VQ47_PEDHC|E0VRD2_PEDHC|E0VSD4_PEDHC|E0VSD5_PEDHC|E0VUR0_PEDHC|E0VUR1_PEDHC|E0VV39_PEDHC|E0VV52_PEDHC|E0VV70_PEDHC|E0VV72_PEDHC|E0VXT9_PEDHC|E0VZW4_PEDHC|E0W115_PEDHC|E0W2B1_PEDHC|E0W389_PEDHC|E0W4F7_PEDHC) inhibitor An insecticide synergist, especially for pyrethroids and ROTENONE. Pesticide Synergists (Code: D010574) Pesticides (Code: D010575) pesticide synergist (Code: CHEBI:25943) 2000-03-07 FDA
Click to view tocofersolan Tocofersolan (d-alpha-tocopherol-polyethylene glycol) is a pro-drug. The active metabolite is the d-alpha-tocopherol. The hydrolysis of tocofersolan occurs in the gut lumen. Taken up by cells, the alpha-tocopherol moiety appears in chylomicrons in the lymph in a manner identical to vitamin E absorbed from the diet. (See: vitamin E) Tocofersolan is indicated in vitamin E deficiency due to digestive malabsorption in paediatric patients with congenital chronic cholestasis or hereditary chronic cholestasis. Antioxidants (Code: D000975) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Protective Agents (Code: D020011) Vitamins (Code: D014815) 2009-07-23 EMA VIV
Click to view tapentadol Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022304s019s021lbl.pdf) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022304s019s021lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022304s019s021lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022304s019s021lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022304s019s021lbl.pdf) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitot (Source: https://www.ncbi.nlm.nih.gov/pubmed/22698264) Tapentadol is a centrally-acting synthetic analgesic. The exact mechanism of action is unknown. Although the clinical relevance is unclear, preclinical studies have shown that tapentadol is a mu-opioid receptor (MOR) agonist and a norepinephrine reuptake inhibitor (NRI). Analgesia in animal models is derived from both of these properties. Tapentadol is indicated for the management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. Opioid Agonist (Code: N0000175690) Opioid Agonists (Code: N0000000174) 2008-11-20 FDA
Click to view Florbetapir F-18 Amyloid beta A4 protein (Organism: Homo sapiens, class: Unclassified, accessions: P05067, gene: APP, swissprot: A4_HUMAN a PET agent for Abeta plaques Radioactive Diagnostic Agent (Code: N0000177914) Positron Emitting Activity (Code: N0000175869) 2012-04-06 FDA
Click to view doconexent Free fatty acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: O14842, gene: FFAR1, swissprot: FFAR1_HUMAN) agonist (Source: ) Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN Prostaglandin G/H synthase 2 (Organism: Ovis aries, class: Enzyme, accessions: P79208, gene: PTGS2, swissprot: PGH2_SHEEP Prostaglandin G/H synthase 1 (Organism: Bos taurus, class: Enzyme, accessions: O62664, gene: PTGS1, swissprot: PGH1_BOVIN Oxoeicosanoid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q8TDS5, gene: OXER1, swissprot: OXER1_HUMAN Transient receptor potential cation channel subfamily A member 1 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q6RI86, gene: Trpa1, swissprot: TRPA1_RAT) activator (Source: ) a mixture of fish oil and primrose oil; used as a high-docosahexaenoic acid fatty acid supplement nutraceutical (Code: CHEBI:50733) antineoplastic agent (Code: CHEBI:35610) FDA HXA
Click to view enzacamene camphor derivative used as sunscreen FDA
Click to view sincalide Cholecystokinin receptor type A (Organism: Homo sapiens, class: GPCR, accessions: P32238, gene: CCKAR, swissprot: CCKAR_HUMAN Cholecystokinin receptor type A (Organism: Cavia porcellus, class: GPCR, accessions: Q63931, gene: CCKAR, swissprot: CCKAR_CAVPO Gastrin/cholecystokinin type B receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P30553, gene: Cckbr, swissprot: GASR_RAT Cholecystokinin receptor (Organism: Mus musculus, class: GPCR, accessions: O08786|P56481, gene: Cckar|Cckbr, swissprot: CCKAR_MOUSE|GASR_MOUSE Cholecystokinin receptor type A (Organism: Rattus norvegicus, class: GPCR, accessions: P30551, gene: Cckar, swissprot: CCKAR_RAT Gastrin/cholecystokinin type B receptor (Organism: Homo sapiens, class: GPCR, accessions: P32239, gene: CCKBR, swissprot: GASR_HUMAN Gastrin/cholecystokinin type B receptor (Organism: Mus musculus, class: GPCR, accessions: P56481, gene: Cckbr, swissprot: GASR_MOUSE An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas. Cholecystokinin (Code: N0000007750) Cholecystokinin Analog (Code: N0000175798) 1976-07-21 FDA
Click to view apixaban Coagulation factor X (Organism: Homo sapiens, class: Enzyme, accessions: P00742, gene: F10, swissprot: FA10_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202155s021lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202155s021lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202155s021lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202155s021lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202155s021lbl.pdf) Cytochrome P450 2J2 (Organism: Homo sapiens, class: Enzyme, accessions: P51589, gene: CYP2J2, swissprot: CP2J2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202155s021lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202155s021lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202155s021lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202155s021lbl.pdf) Apixaban is a selective inhibitor of FXa. It does not require antithrombin III for antithrombotic activity. Apixaban inhibits free and clot-bound FXa, and prothrombinase activity. Apixaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, apixaban decreases thrombin generation and thrombus development. Apixaban is indicated to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation, for the prophylaxis of deep vein thrombosis (DVT), which may lead to pulmonary embolism (PE), in patients who have undergone hip or knee replacement surgery and for the treatment of DVT and PE, and for the reduction in the risk of recurrent DVT and PE following initial therapy. Factor Xa Inhibitor (Code: N0000175637) Anticoagulants (Code: D000925) Antithrombins (Code: D000991) Enzyme Inhibitors (Code: D004791) Factor Xa Inhibitors (Code: D065427) Hematologic Agents (Code: D006401) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) anticoagulant (Code: CHEBI:50249) 2011-05-18 EMA GG2
Click to view cobicistat Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: P08684|P20815|P24462|Q9HB55, gene: CYP3A4|CYP3A43|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/203094s005lbl.pdf) A carbamate and thiazole derivative that functions as a CYTOCHROME P450 CYP3A INHIBITOR to enhance the concentration of ANTI-HIV AGENTS, with which it is used in combination, for the treatment of HIV INFECTIONS. Anti-HIV Agents (Code: D019380) Anti-Infective Agents (Code: D000890) Anti-Retroviral Agents (Code: D044966) Antiviral Agents (Code: D000998) Cytochrome P-450 CYP3A Inhibitors (Code: D065692) Cytochrome P-450 Enzyme Inhibitors (Code: D065607) Enzyme Inhibitors (Code: D004791) Metabolic Side Effects of Drugs and Substances (Code: D065606) Cytochrome P450 3A Inhibitors (Code: N0000190114) Cytochrome P450 3A Inhibitor (Code: N0000191001) P-Glycoprotein Inhibitors (Code: N0000185503) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) 2012-08-27 FDA
Click to view elvitegravir Gag-Pol polyprotein (Organism: Human immunodeficiency virus type 1 group M subtype B (isolate BRU/LAI), class: Polyprotein, accessions: P03367, gene: gag-pol, swissprot: POL_HV1BR) Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q7ZJM1, gene: pol, swissprot: Q7ZJM1_9HIV1) inhibitor Integrase (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q76353, gene: None, swissprot: Q76353_9HIV1 Elvitegravir inhibits the strand transfer activity of HIV-1 integrase (integrase strand transfer inhibitor; INSTI), an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the integration of HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the viral infection. Elvitegravir does not inhibit human topoisomerases I or II. HIV Integrase Inhibitors (Code: N0000000127) Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor (Code: N0000175887) Cytochrome P450 2C9 Inducers (Code: N0000185507) 2012-08-27 FDA ELV
Click to view Flutemetamol (18F) used for PET imaging of brain fibrillar amyloid beta Radioactive Diagnostic Agent (Code: N0000177914) Radiopharmaceutical Activity (Code: N0000000205) 2013-10-25 FDA
Click to view glycopyrronium bromide Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/207923s002lbl.pdf) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/207923s002lbl.pdf) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/207923s002lbl.pdf) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/207923s002lbl.pdf) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/207923s002lbl.pdf) Glycopyrronium bromide is a long-acting muscarinic antagonist, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. Glycopyrronium bromide is indicated for the long-term, maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD). Glycopyrronium is also indicated to reduce chronic severe drooling in patientsn or for topical treatment of primary axillary hyperhidrosis. Adjuvants, Anesthesia (Code: D000759) Central Nervous System Agents (Code: D002491) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Muscarinic Antagonists (Code: D018727) Neurotransmitter Agents (Code: D018377) Anticholinergic (Code: N0000175574) 1961-08-11 FDA
Click to view eslicarbazepine acetate Eslicarbazepine acetate is a third generation antiepileptic drug. Eslicarbazepine acetate is extensively converted to eslicarbazepine, which is considered to be responsible for therapeutic effects in humans. It is indicated for the treatment of partial-onset seizures. (See: eslicarbazepine) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Cytochrome P450 3A4 Inducers (Code: N0000185506) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 2009-04-21 National Authority of Medicines and Health Products (Portugal)
Click to view avanafil cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha' (Organism: Homo sapiens, class: Enzyme, accessions: P51160, gene: PDE6C, swissprot: PDE6C_HUMAN) cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Canis familiaris, class: Enzyme, accessions: O77746, gene: PDE5A, swissprot: PDE5A_CANFA a selective inhibitor of cGMP-specific PDE5 has no direct relaxant effect on isolated human corpus cavernosum, but enhances the effect of NO by inhibiting PDE5, which is responsible for degradation of cGMP in the corpus cavernosum vasodilator agent (Code: CHEBI:35620) Phosphodiesterase 5 Inhibitor (Code: N0000175599) Phosphodiesterase 5 Inhibitors (Code: N0000020026) 2012-04-27 FDA
Click to view lasofoxifene Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist Estrogen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P06211|Q62986, gene: Esr1|Esr2, swissprot: ESR1_RAT|ESR2_RAT Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) agonist a SERM whose biological actions are largely mediated through binding to estrogen receptors, this binding results in the activation of some estrogenic pathways and a blockade of others, Lasofoxifene produces tissue and cell-specific effects in estrogen-responsive tissues 2009-02-24 EMA C3D
Click to view lacosamide Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 13 (Organism: Homo sapiens, class: Enzyme, accessions: Q8N1Q1, gene: CA13, swissprot: CAH13_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20028100) Sodium channel protein type 3 subunit alpha (Organism: Rattus norvegicus, class: Ion channel, accessions: P08104, gene: Scn3a, swissprot: SCN3A_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18378801) Sodium channel protein type X alpha subunit (Organism: Rattus norvegicus, class: Unclassified, accessions: Q62968, gene: Scn10a, swissprot: SCNAA_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18378801) Sodium channel protein type 2 subunit alpha (Organism: Rattus norvegicus, class: Ion channel, accessions: P04775, gene: Scn2a, swissprot: SCN2A_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/24065921) Sodium channel protein type 9 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q15858, gene: SCN9A, swissprot: SCN9A_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18378801) Lacosamide is a functionalized amino acid compound specifically synthesized as an anticonvulsive drug to use as add-on therapy for partial-onset seizures with antinociceptive and neuroprotective activities. Lacosamide selectively enhances slow inactivation of voltage-gated sodium channels without affecting fast inactivation, thereby stabilizing hyperexcitabe neuronal membranes. Anti-epileptic Agent (Code: N0000175753) Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Anticonvulsants (Code: D000927) Central Nervous System Agents (Code: D002491) 2008-08-29 EMA
Click to view olaflur cariostatic agent Cariostatic Agents (Code: D002327) Protective Agents (Code: D020011)
Click to view 4-dimethylaminophenol in combination with SODIUM NITRITE antagonizes experimental cyanide poisoning; RN given refers to parent cpd Antidotes (Code: D000931) Protective Agents (Code: D020011)
Click to view aceclidine Muscarinic acetylcholine receptor M1 (Organism: Mus musculus, class: GPCR, accessions: P12657, gene: Chrm1, swissprot: ACM1_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9464368) Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9111297) Aceclidine is a parasympathomimetic agent. It is a muscarinic acetylcholine receptor agonist with weak anticholinesterase activity. Acting directly on the motor end-plate (cholinergic nerve endings) it decreases intraocular pressure and mediates the contraction of iris muscle. Aceclidine increased outflow facility in human eyes in vitro by a direct stimulation of the outflow tissues in the absence of an intact ciliary muscle. It is used alone or in combination with timolol for the treatment of ocular hypertension and open-angle glaucoma. Autonomic Agents (Code: D001337) Miotics (Code: D008916) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) 1969-11-25 Italian Medicines Agency (AIFA)
Click to view afatinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/201292s015lbl.pdf) Receptor tyrosine-protein kinase erbB-2 (Organism: Homo sapiens, class: Kinase, accessions: P04626, gene: ERBB2, swissprot: ERBB2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/201292s015lbl.pdf) Receptor tyrosine-protein kinase erbB-4 (Organism: Homo sapiens, class: Kinase, accessions: Q15303, gene: ERBB4, swissprot: ERBB4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/201292s015lbl.pdf) Dimethylaniline monooxygenase [N-oxide-forming] 3 (Organism: Homo sapiens, class: Enzyme, accessions: P31513, gene: FMO3, swissprot: FMO3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/201292s015lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/201292s015lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/201292s015lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/201292s015lbl.pdf) Afatinib is a tyrosine kinase inhibitor and a 4-anilinoquinazoline. Afatinib covalently binds to the kinase domains of EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) and irreversibly inhibits tyrosine kinase autophosphorylation, resulting in downregulation of ErbB signaling. Afatinib demonstrated inhibition of autophosphorylation and/or in vitro proliferation of cell lines expressing wild-type EGFR and in those expressing selected EGFR exon 19 deletion mutations, exon 21 L858R mutations, or other less common non-resistant mutations, at afatinib concentrations achieved in patients. In addition, afatinib inhibited in vitro proliferation of cell lines overexpressing HER2. Afatinib is indicated for first-line treatment of patients with metastatic non-small cell lung cancer whose tumors have non-resistant epidermal growth factor receptor mutations and for treatment of patients with metastatic, squamous NSCLC progressing after platinum-based chemotherapy. Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) Radiation-Sensitizing Agents (Code: D011838) antineoplastic agent (Code: CHEBI:35610) 2013-07-12 FDA 0WM
Click to view alanyl glutamine Alanyl glutamine is a dipeptide formed from L-alanyl and L-glutamine residues. Upon oral or enteral administration, alanylglutamine works locally in the gastrointestinal (GI) tract to both protect the integrity of the intestinal mucosa and maintain intestinal barrier functions. This reduces bacterial translocation, the risk of infection, infection-induced inflammatory damage and infection-associated symptoms, such as diarrhea, dehydration, malabsorption and electrolyte imbalances. Alanylglutamine also increases absorption of other chemicals, enhances epithelial repair, and inhibits apoptosis due to cellular damage, and stimulates cellular proliferation. Upon absorption, alanylglutamine may also help inhibit muscle protein catabolism. Alanyl glutamine is used as a supplement to amino acid solutions or an amino acid containing infusion regimen as part of complete nutritional support. 1997-03-13 Italian Medicines Agency (AIFA)
Click to view azilsartan medoxomil Azilsartan: Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/200796s006lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/200796s006lbl.pdf) Azilsartan medoxomil is a prodrug which hydrolyzed to azilsartan in the gastrointestinal tract during absorption. Azilsartan is a selective AT1 subtype angiotensin II receptor antagonist. Azilsartan is indicated for the treatment of hypertension to lower blood pressure alone or in combination with other antihypertensive agents. Angiotensin 2 Type 1 Receptor Antagonists (Code: N0000180999) Angiotensin 2 Receptor Blocker (Code: N0000175561) Decreased Blood Pressure (Code: N0000178477) Angiotensin II Type 1 Receptor Blockers (Code: D047228) Angiotensin Receptor Antagonists (Code: D057911) prodrug (Code: CHEBI:50266) angiotensin receptor antagonist (Code: CHEBI:61016) antihypertensive agent (Code: CHEBI:35674) 2011-02-25 FDA
Click to view laropiprant Prostaglandin D2 receptor (Organism: Homo sapiens, class: GPCR, accessions: Q13258, gene: PTGDR, swissprot: PD2R_HUMAN) antagonist Prostaglandin F2-alpha receptor (Organism: Homo sapiens, class: GPCR, accessions: P43088, gene: PTGFR, swissprot: PF2R_HUMAN Prostacyclin receptor (Organism: Homo sapiens, class: GPCR, accessions: P43119, gene: PTGIR, swissprot: PI2R_HUMAN Prostaglandin E2 receptor EP2 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43116, gene: PTGER2, swissprot: PE2R2_HUMAN Prostaglandin E2 receptor EP3 subtype (Organism: Homo sapiens, class: GPCR, accessions: P43115, gene: PTGER3, swissprot: PE2R3_HUMAN Prostaglandin D2 receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: Q9Y5Y4, gene: PTGDR2, swissprot: PD2R2_HUMAN Thromboxane A2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P21731, gene: TBXA2R, swissprot: TA2R_HUMAN Prostaglandin E2 receptor EP1 subtype (Organism: Homo sapiens, class: GPCR, accessions: P34995, gene: PTGER1, swissprot: PE2R1_HUMAN a potent orally active human prostaglandin D(2) receptor 1 antagonist
Click to view (2-benzhydryloxyethyl)diethyl-methylammonium iodide
Click to view 2-(4-chlorphenoxy)-ethanol 2-(4-Chlorophenyl)ethanol (Chlorophetanol) is an agent known to have antifungal activities. It has been used as a topical antifungal.
Click to view pasireotide Somatostatin receptor type 3 (Organism: Homo sapiens, class: GPCR, accessions: P32745, gene: SSTR3, swissprot: SSR3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf) Somatostatin receptor type 1 (Organism: Homo sapiens, class: GPCR, accessions: P30872, gene: SSTR1, swissprot: SSR1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf) Somatostatin receptor type 5 (Organism: Homo sapiens, class: GPCR, accessions: P35346, gene: SSTR5, swissprot: SSR5_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf) Somatostatin receptor type 2 (Organism: Homo sapiens, class: GPCR, accessions: P30874, gene: SSTR2, swissprot: SSR2_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/200677lbl.pdf) Somatostatin receptor type 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: P30680, gene: Sstr2, swissprot: SSR2_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21493671) Pasireotide is a somatostatin analog with pharmacologic properties mimicking those of the natural hormone somatostatin binds and activates the SSTRs resulting in inhibition of ACTH secretion, which leads to decreased cortisol secretion. Pasireotide is used (as its diaspartate salt) for treatment of Cushing's disease. Somatostatin Analog (Code: N0000175904) Somatostatin Receptor Agonists (Code: N0000000194) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) antineoplastic agent (Code: CHEBI:35610) 2012-12-14 FDA
Click to view pixantrone DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) alkylation (Source: https://www.ema.europa.eu/documents/product-information/pixuvri-epar-product-information_en.pdf) DNA topoisomerase II (Organism: Homo sapiens, class: Enzyme, accessions: P11388|Q02880, gene: TOP2A|TOP2B, swissprot: TOP2A_HUMAN|TOP2B_HUMAN) weak inhibitor (Source: https://www.ema.europa.eu/documents/product-information/pixuvri-epar-product-information_en.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/pixuvri-epar-product-information_en.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ema.europa.eu/documents/product-information/pixuvri-epar-product-information_en.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/pixuvri-epar-product-information_en.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/pixuvri-epar-product-information_en.pdf) Pixantrone is a cytotoxic aza-anthracenedione. Unlike approved anthracyclines and anthracenediones, pixantrone is only a weak inhibitor of topoisomerase II and directly alkylates DNA forming stable DNA adducts and cross-strand breaks. Pixuvri is indicated as monotherapy for the treatment of adult patients with multiply relapsed or refractory aggressive Non-Hodgkin B-cell Lymphomas. Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Topoisomerase II Inhibitors (Code: D059005) Topoisomerase Inhibitors (Code: D059003) 2012-05-10 EMA
Click to view trinitrophenol Trinitrophenol (picric acid) is a C-nitro compound comprising phenol having three nitro substtituents at the 2-, 4- and 6-positions. Trinitrophenol is used as a high explosive, an oxidant in rocket fuels, in matches and leather processing, as a laboratory reagent for serum creatinine analysis in humans and experimental animals. There is not much information related to pharmacological and biological application of picric acid. During the 1920s-30s, it was used either alone or in combination with butyl aminobenzoate as an antiseptic dressing for burn wounds. About 4% of patients treated with picric acid developed sensitization local dermatitis and at least one case of serious central nervous system dysfunction occurred following topical picric acid application. Picric acid does not sensitize directly, but only after conversion to a more reactive compound. Now it is used as a homeopatic drug. Enzyme Inhibitors (Code: D004791) Indicators and Reagents (Code: D007202) Uncoupling Agents (Code: D014475) 1986-12-31 Health Canada TNF
Click to view bazedoxifene Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) modulator Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) modulator an estrogen agonist/antagonist that acts as an agonist in some estrogen-sensitive tissues and an antagonist in others Estrogen Agonist/Antagonist (Code: N0000175826) Bone Density Conservation Agents (Code: D050071) Estrogen Receptor Modulators (Code: D020847) Hormone Antagonists (Code: D006727) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Selective Estrogen Receptor Modulators (Code: D020845) 2013-10-03 FDA 29S
Click to view amifampridine Amifampridine is an organic compound derived from pyridine with potassium channel inhibition activity. Amifampridine blocks voltage-dependent potassium channels, thereby prolonging pre-synaptic cell membrane depolarization. Prolonging the action potential enhances the transport of calcium into the nerve ending. The resulting increase in intracellular calcium concentrations facilitates exocytosis of acetylcholine containing vesicles, which in turn enhances neuromuscular transmission. Amifampridine is used the symptomatic treatment of Lambert-Eaton Myasthenic Syndrome, a rare autoimmune disease with the primary symptoms of muscle weakness. 2009-12-23 EMA L89
Click to view ambrisentan Endothelin B receptor (Organism: Homo sapiens, class: GPCR, accessions: P24530, gene: EDNRB, swissprot: EDNRB_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) Endothelin-1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P25101, gene: EDNRA, swissprot: EDNRA_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) UDP-glucuronosyltransferase 1-3 (Organism: Homo sapiens, class: Enzyme, accessions: P35503, gene: UGT1A3, swissprot: UD13_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) Sodium/bile acid cotransporter (Organism: Homo sapiens, class: Transporter, accessions: Q14973, gene: SLC10A1, swissprot: NTCP_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022081s041lbl.pdf) Ambrisentan is an endothelin receptor antagonist that is selective for the endothelin type-A receptor. Ambrisentan is indicated for the treatment of pulmonary arterial hypertensionto improve exercise ability and delay clinical worsening in combination with tadalafil to reduce the risks of disease progression and hospitalization for worsening PAH, and to improve exercise ability. Endothelin Receptor Antagonist (Code: N0000175581) Endothelin Receptor Antagonists (Code: N0000175364) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) 2007-06-15 FDA
Click to view angiotensinamide
Click to view pyronaridine Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981)
Click to view alogliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022271s012lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022271s012lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022271s012lbl.pdf) Alogliptin is a selective inhibitor of the enzymatic activity of dipeptidyl peptidase-4 (DPP-4) that slows the inactivation of the incretin hormones, thereby increasing their bloodstream concentrations and reducing fasting and postprandial glucose concentrations in a glucose-dependent manner in patients with type 2 diabetes mellitus. Alogliptin exists predominantly as the (R)-enantiomer. Dipeptidyl Peptidase 4 Inhibitors (Code: N0000175912) Dipeptidyl Peptidase 4 Inhibitor (Code: N0000175913) Dipeptidyl-Peptidase IV Inhibitors (Code: D054873) Enzyme Inhibitors (Code: D004791) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) Hypoglycemic Agents (Code: D007004) Incretins (Code: D054795) Protease Inhibitors (Code: D011480) hypoglycemic agent (Code: CHEBI:35526) 2013-01-25 FDA T22
Click to view bibrocathol Bibrocathol is a bismuth derivative of tetrabromopyrocatechol. Bibrocathol is a topical antiseptic. Bibrocathol is used for the treatment of acute eyelid diseases like blepharitis. 1957-01-29 Sweden Medical Products Agency (MPA)
Click to view bilastine Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/16274260) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Sourse: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1568956435371.pdf) Solute carrier organic anion transporter family member 1A2 (Organism: Homo sapiens, class: Transporter, accessions: P46721, gene: SLCO1A2, swissprot: SO1A2_HUMAN) substrate (Sourse: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1568956435371.pdf) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Sourse: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1568956435371.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Sourse: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1568956435371.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Sourse: http://www.mhra.gov.uk/home/groups/spcpil/documents/spcpil/con1568956435371.pdf) Bilastine is a new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action. Bilastine is used for the symptomatic treatment of allergic rhiniti and chronic urticaria. 2010-09-01 PMDA
Click to view bioallethrin Synthetic analogs of the naturally occurring insecticides cinerin, jasmolin, and pyrethrin. (From Merck Index, 11th ed) Insecticides (Code: D007306) Pesticides (Code: D010575) pyrethroid ester insecticide (Code: CHEBI:39116)
Click to view bisoxatin
Click to view anidulafungin Beta-1,3-glucan synthase catalytic subunit 1 (Organism: Candida albicans, class: Enzyme, accessions: O13428, gene: GSC1, swissprot: O13428_CANAX) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021632s026lbl.pdf) Anidulafungin is a semi-synthetic lipopeptide synthesized from a fermentation product of Aspergillus nidulans. Anidulafungin is an echinocandin, a class of antifungal drugs that inhibits the synthesis of 1,3-beta-D-glucan, an essential component of fungal cell walls. Anidulafungin has been shown to be active against Candida albicans, Candida glabrata, Candida parapsilosis and Candida tropicalis. Anidulafungin is indicated in adults for the treatment of candidemia and other forms of Candida infections (intra-abdominal abscess and peritonitis) and esophageal candidiasis. Echinocandin Antifungal (Code: N0000175507) Lipopeptides (Code: N0000175508) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) 2006-02-17 FDA
Click to view bosutinib Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203341s017lbl.pdf) Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203341s017lbl.pdf) Tyrosine-protein kinase Lyn (Organism: Homo sapiens, class: Kinase, accessions: P07948, gene: LYN, swissprot: LYN_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203341s017lbl.pdf) Tyrosine-protein kinase HCK (Organism: Homo sapiens, class: Kinase, accessions: P08631, gene: HCK, swissprot: HCK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203341s017lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203341s017lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203341s017lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24713129) Tyrosine-protein kinase BTK (Organism: Homo sapiens, class: Kinase, accessions: Q06187, gene: BTK, swissprot: BTK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25351958) Serine/threonine-protein kinase SIK1 (Organism: Homo sapiens, class: Kinase, accessions: P57059, gene: SIK1, swissprot: SIK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25351958) Serine/threonine-protein kinase SIK2 (Organism: Homo sapiens, class: Kinase, accessions: Q9H0K1, gene: SIK2, swissprot: SIK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25351958) Serine/threonine-protein kinase SIK3 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y2K2, gene: SIK3, swissprot: SIK3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25351958) Mitogen-activated protein kinase kinase kinase kinase 5 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y4K4, gene: MAP4K5, swissprot: M4K5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase Yes (Organism: Homo sapiens, class: Kinase, accessions: P07947, gene: YES1, swissprot: YES_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Abelson tyrosine-protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P42684, gene: ABL2, swissprot: ABL2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase Fgr (Organism: Homo sapiens, class: Kinase, accessions: P09769, gene: FGR, swissprot: FGR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase Fyn (Organism: Homo sapiens, class: Kinase, accessions: P06241, gene: FYN, swissprot: FYN_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase FRK (Organism: Homo sapiens, class: Kinase, accessions: P42685, gene: FRK, swissprot: FRK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Activated CDC42 kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q07912, gene: TNK2, swissprot: ACK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Serine/threonine-protein kinase 24 (Organism: Homo sapiens, class: Kinase, accessions: Q9Y6E0, gene: STK24, swissprot: STK24_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Ephrin type-B receptor 4 (Organism: Homo sapiens, class: Kinase, accessions: P54760, gene: EPHB4, swissprot: EPHB4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Cytoplasmic tyrosine-protein kinase BMX (Organism: Homo sapiens, class: Kinase, accessions: P51813, gene: BMX, swissprot: BMX_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Mitogen-activated protein kinase kinase kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: Q12851, gene: MAP4K2, swissprot: M4K2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Misshapen-like kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q8N4C8, gene: MINK1, swissprot: MINK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Serine/threonine-protein kinase 10 (Organism: Homo sapiens, class: Kinase, accessions: O94804, gene: STK10, swissprot: STK10_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase SYK (Organism: Homo sapiens, class: Kinase, accessions: P43405, gene: SYK, swissprot: KSYK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase CSK (Organism: Homo sapiens, class: Kinase, accessions: P41240, gene: CSK, swissprot: CSK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Calcium/calmodulin-dependent protein kinase type 1D (Organism: Homo sapiens, class: Kinase, accessions: Q8IU85, gene: CAMK1D, swissprot: KCC1D_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Protein-tyrosine kinase 2-beta (Organism: Homo sapiens, class: Kinase, accessions: Q14289, gene: PTK2B, swissprot: FAK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Calcium/calmodulin-dependent protein kinase type II subunit gamma (Organism: Homo sapiens, class: Kinase, accessions: Q13555, gene: CAMK2G, swissprot: KCC2G_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Serine/threonine-protein kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: Q13043, gene: STK4, swissprot: STK4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase Tec (Organism: Homo sapiens, class: Kinase, accessions: P42680, gene: TEC, swissprot: TEC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Serine/threonine-protein kinase TBK1 (Organism: Homo sapiens, class: Kinase, accessions: Q9UHD2, gene: TBK1, swissprot: TBK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Tyrosine-protein kinase Fer (Organism: Homo sapiens, class: Kinase, accessions: P16591, gene: FER, swissprot: FER_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Focal adhesion kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q05397, gene: PTK2, swissprot: FAK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Serine/threonine-protein kinase TAO3 (Organism: Homo sapiens, class: Kinase, accessions: Q9H2K8, gene: TAOK3, swissprot: TAOK3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) 5'-AMP-activated protein kinase catalytic subunit alpha-1 (Organism: Homo sapiens, class: Kinase, accessions: Q13131, gene: PRKAA1, swissprot: AAPK1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Dual specificity mitogen-activated protein kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q02750, gene: MAP2K1, swissprot: MP2K1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19039322) Bosutinib is a kinase inhibitor. Bosutinib inhibits the BCR-ABL kinase; it is also an inhibitor of Src-family kinases including Src, Lyn, and Hck. Bosutinib inhibited 16 of 18 imatinib-resistant forms of BCR-ABL kinase expressed in murine myeloid cell lines. Bosutinib did not inhibit the T315I and V299L mutant cells. Bosutinib is indicated for the treatment of adult patients with newly-diagnosed chronic phase Ph+ chronic myelogenous leukemia and chronic, accelerated, or blast phase Ph+ chronic myelogenous leukemia with resistance or intolerance to prior therapy. Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) P-Glycoprotein Inhibitors (Code: N0000185503) antineoplastic agent (Code: CHEBI:35610) 2012-09-04 FDA DB8
Click to view vernakalant Potassium voltage-gated channel subfamily A member 5 (Organism: Homo sapiens, class: Ion channel, accessions: P22460, gene: KCNA5, swissprot: KCNA5_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/17872968) Vernakalant is an antiarrhythmic medicine that acts preferentially in the atria to prolong atrial refractoriness and to rate-dependently slow impulse conduction. These anti-fibrillatory actions on refractoriness and conduction are thought to suppress re-entry, and are potentiated in the atria during atrial fibrillation. The relative selectivity of vernakalant on atrial versus ventricular refractoriness is postulated to result from the block of currents that are expressed in the atria, but not in the ventricles, as well as the unique electrophysiologic condition of the fibrillating atria. However, blockade of cationic currents, including hERG channels and cardiac voltage-dependent sodium channels, which are present in the ventricles has been documented. 2010-09-01 EMA
Click to view voclosporin semi-synthetic cyclosporine A analog & calcineurin inhibitor
Click to view xantinol Xanthinol is a very potent water-soluble derivative of niacin that can be found in diet supplements. It is also known as xanthinol nicotinate. Xaninthol is known to be a potent vasodilator that can easily pass through the cell membrane and once inside the cell it causes an increase in glucose metabolism resulting in an increased energy. Cardiovascular Agents (Code: D002317) Vasodilator Agents (Code: D014665) 1979-08-07 Ministry of Health of the Russian Federation
Click to view triaziquone Alkylating antineoplastic agent used mainly for ovarian tumors. It is toxic to skin, gastrointestinal tract, bone marrow and kidneys. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) antineoplastic agent (Code: CHEBI:35610)
Click to view amiloxate Amiloxate (Isoamyl p-Methoxycinnamate) is an organic compound that absorbs ultraviolet light. Amiloxate is a cinnamic acid derivative. Amiloxate is used as an active sunscreen agent.
Click to view lorcaserin 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022529s005s007,208524s001lbl.pdf) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022529s005s007,208524s001lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022529s005s007,208524s001lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022529s005s007,208524s001lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22266842) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22266842) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22266842) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22266842) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22266842) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22266842) Dimethylaniline monooxygenase [N-oxide-forming] 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q01740, gene: FMO1 swissprot: FMO1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/22266842) Lorcaserin is a serotonin 2C receptor agonist. Lorcaserin is believed to decrease food consumption and promote satiety by selectively activating 5-HT2C receptors on anorexigenic pro-opiomelanocortin neurons located in the hypothalamus. The exact mechanism of action is not known. Lorcaserin is indicated as an adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adults with obese or overweight. Serotonin-2c Receptor Agonist (Code: N0000185010) Serotonin 2c Receptor Agonists (Code: N0000185009) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) appetite depressant (Code: CHEBI:50507) 2012-06-27 FDA
Click to view demecolcine An alkaloid isolated from Colchicum autumnale L. and used as an antineoplastic. Antimitotic Agents (Code: D050256) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Phytogenic (Code: D000972) Mitosis Modulators (Code: D050258) Tubulin Modulators (Code: D050257) antineoplastic agent (Code: CHEBI:35610)
Click to view dequalinium E3 ubiquitin-protein ligase XIAP (Organism: Homo sapiens, class: Enzyme, accessions: P98170, gene: XIAP, swissprot: XIAP_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21340509) cGMP-gated cation channel alpha-1 (Organism: Homo sapiens, class: Unclassified, accessions: P29973, gene: CNGA1, swissprot: CNGA1_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/12508052) Cyclic nucleotide-gated olfactory channel (Organism: Homo sapiens, class: Unclassified, accessions: Q16280, gene: CNGA2, swissprot: CNGA2_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/14981138) Small conductance calcium-activated potassium channel protein 3 (Organism: Homo sapiens, class: Ion channel, accessions: Q9UGI6, gene: KCNN3, swissprot: KCNN3_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/11369031) Small conductance calcium-activated potassium channel protein 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q92952, gene: KCNN1, swissprot: KCNN1_HUMAN) blocker https://www.ncbi.nlm.nih.gov/pubmed/10683185) Dequalinium is a quaternary ammonium antiseptic active against many gram-positive and gram-negative bacteria, yeasts and fungi. The primary mechanism of action is an increase in bacterial cell permeability and the subsequent loss of enzyme activity, finally resulting in cell death. Dequalinium is active against: Enterococcus faecalis, Lactobacillus spp., Staphylococcus aureus, Streptococcus agalactiae (Group B streptococci), Streptococcus pyogenes (Group A streptococci), Enterobacter spp., Escherichia coli, Klebsiella spp., Pseudomonas spp., Serratia spp., Atopobium vaginae, Bacteroides spp., Fusobacteria, Gardnerella vaginalis, Prevotella spp., Peptostreptococci, Poryphyromonas spp. Dequalinium is used for the local therapy of most of the common infections of the mouth including: Vincents angina, pharyngitis, sore throats, tonsillitis, stomatitis, aphthous ulcers, thrush, glossitis. Dequalinium is also indicated for the treatment of Bacterial vaginosis. Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) antineoplastic agent (Code: CHEBI:35610) antiseptic drug (Code: CHEBI:48218) 1967-07-27 Austrian Medicines and Medical Devices Agency DEQ
Click to view desaspidin
Click to view decamethrin A synthetic pyrethroid insecticide with contact and residual activity, also used as an acaricide. Insecticides (Code: D007306) Pesticides (Code: D010575) pyrethroid ester insecticide (Code: CHEBI:39116) agrochemical (Code: CHEBI:33286)
Click to view degarelix Gonadotropin-releasing hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: P30968, gene: GNRHR, swissprot: GNRHR_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022201s011lbl.pdf) Degarelix is a synthetic linear decapeptide amide containing seven unnatural amino acids, five of which are D-amino acids. Degarelix is a GnRH receptor antagonist. It binds reversibly to the pituitary GnRH receptors, thereby reducing the release of gonadotropins and consequently testosterone. Degarelix is indicated for treatment of patients with advanced prostate cancer. 2008-12-24 FDA
Click to view desvenlafaxine Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204683s006lbl.pdf) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204683s006lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204683s006lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204683s006lbl.pdf) Desvenlafaxine (O-desmethylvenlafaxine) is the major active metabolite of the antidepressant venlafaxine, a medication used to treat major depressive disorder. The exact mechanism of the antidepressant action of desvenlafaxine is unknown, but is thought to be related to the potentiation of serotonin and norepinephrine in the central nervous system, through inhibition of their reuptake. Non-clinical studies have shown that desvenlafaxine is a potent and selective serotonin and norepinephrine reuptake inhibitor. Desvenlafaxine is indicated for the treatment of adults with major depressive disorder. Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neurotransmitter Agents (Code: D018377) Neurotransmitter Uptake Inhibitors (Code: D014179) Psychotropic Drugs (Code: D011619) Serotonin and Noradrenaline Reuptake Inhibitors (Code: D000068760) antidepressant (Code: CHEBI:35469) Norepinephrine Uptake Inhibitors (Code: N0000000102) Serotonin and Norepinephrine Reuptake Inhibitor (Code: N0000175749) Serotonin Uptake Inhibitors (Code: N0000000109) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) 2008-02-29 FDA 29J
Click to view dapoxetine Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16430636) Dapoxetine is a selective serotonin reuptake inhibitors. Dapoxetine is indicated for the treatment of premature ejaculation in men 18 to 64 years of age. The mechanism of action of dapoxetine in premature ejaculation is presumed to be linked to the inhibition of neuronal reuptake of serotonin and the subsequent potentiation of the neurotransmitter's action at pre- and post-synaptic receptors. 2009-02-19 Austrian Medicines and Medical Devices Agency
Click to view mirabegron Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202611s011lbl.pdf) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202611s011lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202611s011lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202611s011lbl.pdf) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202611s011lbl.pdf) Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202611s011lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202611s011lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202611s011lbl.pdf) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Enzyme, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202611s011lbl.pdf) Mirabegron is a beta-3 adrenergic agonist, relaxes the detrusor smooth muscle during the storage phase of the urinary bladder fill-void cycle by activation of beta-3 AR which increases bladder capacity. beta3-Adrenergic Agonist (Code: N0000185008) Adrenergic beta3-Agonists (Code: N0000185007) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Adrenergic Agents (Code: D018663) Adrenergic Agonists (Code: D000322) Adrenergic beta-3 Receptor Agonists (Code: D058667) Adrenergic beta-Agonists (Code: D000318) Neurotransmitter Agents (Code: D018377) Urological Agents (Code: D064804) beta-adrenergic agonist (Code: CHEBI:35522) 2012-06-28 FDA
Click to view clefamide Clefamide is dichloroacetamide derivative. It was used for the treatment of luminal amoebiasis.
Click to view clevudine Clevudine is a synthetic pyrimidine analogue with activity against hepatitis B virus (HBV). Intracellularly, clevudine is phosphorylated to its active metabolites, clevudine monophosphate and triphosphate. The triphosphate metabolite competes with thymidine for incorporation into viral DNA, thereby causing DNA chain termination and inhibiting the function of HBV DNA polymerase (reverse transcriptase). Clevudine is indicated in patients with chronic hepatitis B virus infection. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998)
Click to view clopenthixol Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://pdf.hres.ca/dpd_pm/00024771.PDF) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20946203) Clopenthixol is a thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. Originally clopenthixol was a mixture of two chemical isomers: cis (Z) - and trans (E) -clopenthixol. The cis (Z) -isomer, called zuclopenthixol, is the active form. It has high affinity for both dopamine D1 and D2 receptors. Zuclopenthixol also has high affinity for alpha1-adrenergic and 5-HT2 receptors. It has weaker histamine H1 receptor blocking activity, and even lower affinity for muscarinic cholinergic and alpha2-adrenergic receptors. Clopenthixol is used for the treatment of psychoses, especially schizophrenia. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) first generation antipsychotic (Code: CHEBI:65190) H1-receptor antagonist (Code: CHEBI:37955) serotonergic antagonist (Code: CHEBI:48279) alpha-adrenergic antagonist (Code: CHEBI:37890) dopaminergic antagonist (Code: CHEBI:48561) 1984-03-28 Austrian Medicines and Medical Devices Agency
Click to view tegafur Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/teysuno-epar-product-information_en.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11095583) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11095583) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11095583) Tegafur is a prodrug of 5-fluorouracil (5-FU )with good oral bioavailability. Following oral administration, tegafur is gradually converted to 5-FU in vivo, mainly by CYP2A6 enzyme activity in the liver. Tegafur is usually given in combination with other drugs that enhance the bioavailability of the 5-FU by blocking the enzyme responsible for its degradation, or serves to limit the toxicity of 5-FU by ensuring high concentrations of 5-FU at a lower dose of tegafur. (See: fluorouracil) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Noxae (Code: D009676) 1992-07-01 PMDA
Click to view eltrombopag Thrombopoietin receptor (Organism: Homo sapiens, class: Membrane receptor, accessions: P40238, gene: MPL, swissprot: TPOR_HUMAN) agonist (Source: ) an oral, nonpeptide thrombopoietin receptor agonist Increased Megakaryocyte Maturation (Code: N0000175969) Increased Platelet Production (Code: N0000175970) Thrombopoietin Receptor Agonist (Code: N0000175973) Thrombopoietin Receptor Agonists (Code: N0000175968) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) UGT1A1 Inhibitors (Code: N0000191272) UGT1A3 Inhibitors (Code: N0000191275) UGT1A4 Inhibitors (Code: N0000191276) UGT1A6 Inhibitors (Code: N0000191277) UGT1A9 Inhibitors (Code: N0000191278) UGT2B7 Inhibitors (Code: N0000191273) UGT2B15 Inhibitors (Code: N0000191274) Thrombopoiesis Stimulating Agent (Code: N0000178368) Thrombopoietin Receptor Interactions (Code: N0000175967) 2008-11-20 FDA
Click to view carisbamate experimental anticonvulsant and neuromodulator
Click to view cyfluthrin effective against mosquitoes Insecticides (Code: D007306) Pesticides (Code: D010575) pyrethroid ester insecticide (Code: CHEBI:39116) agrochemical (Code: CHEBI:33286)
Click to view candicidin A Candicidin A is an antifungal antibiotic drug. Candicidin A is a component of mixture of heptaene macrolides from Streptomyces griseus or Actinomyces levoris. Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935)
Click to view casopitant Sigma non-opioid intracellular receptor 1 (Organism: Homo sapiens, class: Membrane receptor, accessions: Q99720, gene: SIGMAR1, swissprot: SGMR1_HUMAN Substance-P receptor (Organism: Homo sapiens, class: GPCR, accessions: P25103, gene: TACR1, swissprot: NK1R_HUMAN) antagonist Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Neurokinin-1 Receptor Antagonists (Code: D064729) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373)
Click to view ceftobiprole medocaril Ceftobiprole medocaril is a ceftobiprole prodrug. Ceftobiprole medocaril is indicated for the treatment of hospital-acquired or community-acquired pneumonia. Also it is used for the treatment of local skin infection. (See: ceftobiprole) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) prodrug (Code: CHEBI:50266) 2009-03-20 Ministry of Health of the Russian Federation
Click to view cypermethrin Insecticides (Code: D007306) Pesticides (Code: D010575) molluscicide (Code: CHEBI:33904) pyrethroid ester insecticide (Code: CHEBI:39116) agrochemical (Code: CHEBI:33286)
Click to view plerixafor C-X-C chemokine receptor type 4 (Organism: Homo sapiens, class: GPCR, accessions: P61073, gene: CXCR4, swissprot: CXCR4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022311s020lbl.pdf) Atypical chemokine receptor 3 (Organism: Homo sapiens, class: GPCR, accessions: P25106, gene: ACKR3, swissprot: ACKR3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19255243) Plerixafor is an antagonist of the CXCR4 receptor that plays an important role in mobilization of hematopoietic stem and progenitor cells to the stroma of the bone marrow. It had been developed for the treatment of T-tropic HIV-1 infection, but later approved for autologous transplantation in patients with Non-Hodgkin's lymphoma and multiple myeloma. Hematopoietic Stem Cell Mobilizer (Code: N0000178326) Increased Hematopoietic Stem Cell Mobilization (Code: N0000178324) 2008-12-15 FDA
Click to view diamorphine A narcotic analgesic that may be habit-forming. It is a controlled substance (opium derivative) listed in the U.S. Code of Federal Regulations, Title 21 Parts 329.1, 1308.11 (1987). Sale is forbidden in the United States by Federal statute. (Merck Index, 11th ed) Analgesics (Code: D000700) Analgesics, Opioid (Code: D000701) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Narcotics (Code: D009294) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) opioid analgesic (Code: CHEBI:35482) mu-opioid receptor agonist (Code: CHEBI:55322) prodrug (Code: CHEBI:50266)
Click to view dibromotyrosine Dibromotyrosine is an antithyroid drug. It makes use of the competitive effect of bromide on iodine capture and inhibits storage of hypophysial thyrotropic hormone. Dibromotyrosine is used for the treatment of hyperthyroidism. 1951-06-01 Italian Medicines Agency (AIFA) DBY
Click to view dibutylphthalate A plasticizer used in most plastics and found in water, air, soil, plants and animals. It may have some adverse effects with long-term exposure. Plasticizers (Code: D010968) plasticiser (Code: CHEBI:79056) DB7
Click to view dibutylsuccinate Dibutylsuccinate is an insect repellent, which is approved for use on farm animals and livestock.
Click to view diethyl ether Diethyl ether is an organic compound in the ether class, a colorless, highly volatile flammable liquid. It is commonly used as a solvent. It was formerly used as a general anesthetic, until non-flammable drugs were developed, such as halothane. It has been used as a recreational drug to cause intoxication. refrigerant (Code: CHEBI:78433) inhalation anaesthetic (Code: CHEBI:38870) 1846-10-16 YEAR INTRODUCED ETZ
Click to view etybenzatropine Etybenzatropine is a anticholinergic used as an anti-parkinson drug. It is a derivative of benzatropine.
Click to view diethyltoluamide A compound used as a topical insect repellent that may cause irritation to eyes and mucous membranes, but not to the skin. Insect Repellents (Code: D007302) Pesticides (Code: D010575) Protective Agents (Code: D020011) insect repellent (Code: CHEBI:71692) FDA DE3
Click to view difetarsone Difetarsone is an arsenical compound. It was used to treat intestinal amebiasis.
Click to view dihydroergocryptine 5-hydroxytryptamine receptor 7 (Organism: Mus musculus, class: GPCR, accessions: P32304, gene: Htr7, swissprot: 5HT7R_MOUSE) antagonist (Source: ) 5-hydroxytryptamine receptor 7 (Organism: Rattus norvegicus, class: GPCR, accessions: P32305, gene: Htr7, swissprot: 5HT7R_RAT) antagonist (Source: ) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) agonist (Source: ) A 9,10alpha-dihydro derivative of ERGOTAMINE that contains an isopropyl sidechain at the 2' position and an alpha-isobutyl sidechain at 5'alpha position of the molecule. Cardiovascular Agents (Code: D002317) Dopamine Agents (Code: D015259) Dopamine Agonists (Code: D018491) Neurotransmitter Agents (Code: D018377) Vasodilator Agents (Code: D014665) FDA
Click to view diiodohydroxypropane Diiodohydroxypropane (1,3-diiodo-2-propanol) is an iodine products and an antiseptic. It is used externally in oil solution or as an oinment.
Click to view etilevodopa is the ethyl ester of levodopa; an antiparkinson drug
Click to view calcitonin human Calcitonin receptor (Organism: Homo sapiens, class: GPCR, accessions: P30988, gene: CALCR, swissprot: CALCR_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10385705) Amylin receptor AMY1 (Organism: Homo sapiens, class: GPCR, accessions: O60894|P30988, gene: CALCR|RAMP1, swissprot: CALCR_HUMAN|RAMP1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10385705) Amylin receptor AMY2 (Organism: Homo sapiens, class: GPCR, accessions: O60895|P30988, gene: CALCR|RAMP2, swissprot: CALCR_HUMAN|RAMP2_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10385705) Amylin receptor AMY3 (Organism: Homo sapiens, class: GPCR, accessions: O60896|P30988, gene: CALCR|RAMP3, swissprot: CALCR_HUMAN|RAMP3_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/10385705) Human calcitonin is indicated for the treatment of Paget's disease in the cases where the use of salmon calcitonin may provoke the generation of high-titer of antibodies. 1986-10-31 FDA
Click to view diphenadione major descriptor (66-86); on-line search PHENINDIONE (66-74); PHENINDIONE/AA (75-86); INDEX MEDICUS search DIPHENADIONE (66-86); RN given refers to parent cpd
Click to view prednisolone sodium phosphate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021959s004lbl.pdf) 1973-12-19 FDA
Click to view clobetasol propionate Clobetasol propionate is a synthetic corticosteroid for topical dermatologic use. It is a prodrug of clobetasol. Clobetasol propionate is used for the treatment of moderate to severe plaque psoriasis, inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. (See: clobetasol) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) anti-inflammatory drug (Code: CHEBI:35472) 1985-12-27 FDA
Click to view testosterone cypionate Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist cypionate ester of the androgenic hormone testosterone 1978-06-23 FDA
Click to view eosin Eosin is an acidic dye that binds to basic components of a cell, mainly proteins located in the cytoplasm, and gives to proteins a bright pink color. Eosin is the most common dye to stain the cytoplasm in histology. In dermatological therapy eosin is used as a disinfectant because of its bacteriostatic action on Gram-positive bacteria and Candida spp. It constitutes only an adjunct treatment. fluorochrome (Code: CHEBI:51217) histological dye (Code: CHEBI:77178) 1977-04-25 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view fludeoxyglucose (18F) Hexokinase-1 (Organism: Homo sapiens, class: Enzyme, accessions: P19367, gene: HK1, swissprot: HXK1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Solute carrier family 2, facilitated glucose transporter member 4 (Organism: Homo sapiens, class: Enzyme, accessions: P14672, gene: SLC2A4, swissprot: GLUT4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Solute carrier family 2, facilitated glucose transporter member 12 (Organism: Homo sapiens, class: Enzyme, accessions: Q8TD20, gene: SLC2A12, swissprot: GTR12_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Solute carrier family 2, facilitated glucose transporter member 10 (Organism: Homo sapiens, class: Enzyme, accessions: O95528, gene: SLC2A10, swissprot: GTR10_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Solute carrier family 2, facilitated glucose transporter member 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q9NRM0, gene: SLC2A9, swissprot: GTR9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Solute carrier family 2, facilitated glucose transporter member 5 (Organism: Homo sapiens, class: Enzyme, accessions: P22732, gene: SLC2A5, swissprot: GTR5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Solute carrier family 2, facilitated glucose transporter member 7 (Organism: Homo sapiens, class: Enzyme, accessions: Q6PXP3, gene: SLC2A7, swissprot: GTR7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Solute carrier family 2, facilitated glucose transporter member 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9NY64, gene: SLC2A8, swissprot: GTR8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Solute carrier family 2, facilitated glucose transporter member 3 (Organism: Homo sapiens, class: Enzyme, accessions: P11169, gene: SLC2A3, swissprot: GTR3_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Solute carrier family 2, facilitated glucose transporter member 2 (Organism: Homo sapiens, class: Enzyme, accessions: P11168, gene: SLC2A2, swissprot: GTR2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Solute carrier family 2, facilitated glucose transporter member 11 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BYW1, gene: SLC2A11, swissprot: GTR11_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/021870s015lbl.pdf) Fludeoxyglucose (F18) is a glucose analog that concentrates in cells that rely upon glucose as an energy source, or in cells whose dependence on glucose increases under pathophysiological conditions.Fludeoxyglucose (F18) is transported through the cell membrane by facilitative glucose transporter proteins and is phosphorylated within the cell to [F 18] FDG-6-phosphate by the enzyme hexokinase. Once phosphorylated it cannot exit until it is dephosphorylated by glucose-6-phosphatase. Therefore, within a given tissue or pathophysiological process, the retention and clearance of Fludeoxyglucose F 18 reflect a balance involving glucose transporter, hexokinase and glucose-6-phosphatase activities. Fludeoxyglucose (F18) is used to assess glucose metabolism. Radioactive Diagnostic Agent (Code: N0000177914) Radiopharmaceutical Activity (Code: N0000000205) 1994-08-19 FDA
Click to view hydrocortisone succinate Hydrocortisone succinate has the same metabolic and anti-inflammatory actions as hydrocortisone. Hydrocortisone succinate is a prodrug of hydrocortisone. (See: hydrocortisone) 1955-04-27 FDA
Click to view sulfisoxazole acetyl Sulfisoxazole acetyl (N1-acetyl sulfisoxazole) is an ester of sulfisoxazole. Sulfisoxazole acetyl is absorbed as sulfisoxazole due to hydrolyzinf of acetyl group in intestines. Sulfisoxazole acetyl is used in combination with erythromycin for the treatment of acute otitis media. (See: sulfafurazole) 1988-05-20 FDA
Click to view efaproxiral Antisickling Agents (Code: D000986) Hematologic Agents (Code: D006401) Radiation-Sensitizing Agents (Code: D011838) RQ3
Click to view epanolol Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-Antagonists (Code: D000319) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympathomimetics (Code: D013566)
Click to view fosaprepitant Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022023s017lbl.pdf) Fosaprepitant is a prodrug of aprepitant. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. (See: aprepitant) The conversion of fosaprepitant to aprepitant can occur in multiple extrahepatic tissues in addition to the liver. Fosaprepitant is indicated for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy. Neurokinin 1 Antagonists (Code: N0000010262) Substance P/Neurokinin-1 Receptor Antagonist (Code: N0000175786) Antiemetics (Code: D000932) Autonomic Agents (Code: D001337) Central Nervous System Agents (Code: D002491) Gastrointestinal Agents (Code: D005765) Neurokinin-1 Receptor Antagonists (Code: D064729) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) antiemetic (Code: CHEBI:50919) prodrug (Code: CHEBI:50266) 2008-01-25 FDA
Click to view N-Acetyltyrosine N-Acetyltyrosine is an acetylated derivative of the amino acid L-tyrosine with better solubility and stability. It converts to tyrosine and then can be used in neurotransmitter treatment as a precursor of cathecholamine. N-Acetyltyrosine is commonly used in place of tyrosine in parenteral nutrition or nutritional supplements. biomarker (Code: CHEBI:59163) 1984 FDA 3NF
Click to view carfilzomib Proteasome subunit beta type-5 (Organism: Homo sapiens, class: Enzyme, accessions: P28074, gene: PSMB5, swissprot: PSB5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23393020) Proteasome subunit beta type-8 (Organism: Homo sapiens, class: Enzyme, accessions: P28062, gene: PSMB8, swissprot: PSB8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17591945) epoxomicin derivative proteasome inhibitor with antiproliferative and proapoptotic effects on primary human acute myeloid leukaemia cells Proteasome Inhibitors (Code: N0000175075) antineoplastic agent (Code: CHEBI:35610) proteasome inhibitor (Code: CHEBI:52726) 2012-07-20 FDA
Click to view aclidinium bromide Muscarinic acetylcholine receptor M3 (Organism: Homo sapiens, class: GPCR, accessions: P20309, gene: CHRM3, swissprot: ACM3_HUMAN) antagonist (Source: https://www.ema.europa.eu/documents/product-information/bretaris-genuair-epar-product-information_en.pdf) Muscarinic acetylcholine receptor M2 (Organism: Homo sapiens, class: GPCR, accessions: P08172, gene: CHRM2, swissprot: ACM2_HUMAN) antagonist (Source: https://www.ema.europa.eu/documents/product-information/bretaris-genuair-epar-product-information_en.pdf) Muscarinic acetylcholine receptor M1 (Organism: Homo sapiens, class: GPCR, accessions: P11229, gene: CHRM1, swissprot: ACM1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202450s012lbl.pdf) Muscarinic acetylcholine receptor M4 (Organism: Homo sapiens, class: GPCR, accessions: P08173, gene: CHRM4, swissprot: ACM4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202450s012lbl.pdf) Muscarinic acetylcholine receptor M5 (Organism: Homo sapiens, class: GPCR, accessions: P08912, gene: CHRM5, swissprot: ACM5_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202450s012lbl.pdf) Aclidinium bromide is a synthetic, quaternary ammonium compound and an anticholinergic with specificity for muscarinic receptors. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. Aclidinium bromide is indicated for the maintenance treatment of patients with chronic obstructive pulmonary disease. Anticholinergic (Code: N0000175574) Cholinergic Antagonists (Code: N0000175370) muscarinic antagonist (Code: CHEBI:48876) bronchodilator agent (Code: CHEBI:35523) 2012-07-20 EMA
Click to view diflorasone diacetate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) topical corticosteroid has anti-inflammatory, anti-pruritic, and vasoconstrictive actions Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1977-09-14 FDA
Click to view taurine Glycine receptor subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: P23415, gene: GLRA1, swissprot: GLRA1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9009272) Glycine receptor subunit alpha-2 (Organism: Homo sapiens, class: Ion channel, accessions: P23416, gene: GLRA2, swissprot: GLRA2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9009272) Glycine receptor subunit alpha-3 (Organism: Homo sapiens, class: Ion channel, accessions: O75311, gene: GLRA3, swissprot: GLRA3_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9009272) Proton-coupled amino acid transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: Q7Z2H8, gene: SLC36A1, swissprot: S36A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/29038364) Sodium- and chloride-dependent taurine transporter (Organism: Homo sapiens, class: Transporter, accessions: P31641, gene: SLC6A6, swissprot: SC6A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/29038364) Taurine, whose chemical name is 2-aminoethanesulfonic acid, is one of the most abundant amino acids in several organs. It plays important role in essential biological processes. This conditional amino acid can be either be manufactured by the body or obtained in the diet mainly by the consumption of fish and meat. Diet supplements containing taurine is indicated for the nutritional support of infants and young pediatric patients requiring total parenteral nutrition via central or peripheral routes. The usage of diet supplements containing taurine prevents nitrogen and weight loss or to treat negative nitrogen balance in pediatric patients where the alimentary tract cannot be done through oral, gastrostomy or jejunostomy administration, there is impaired gastrointestinal absorption or protein requirements are substantially increased. FDA TAU
Click to view alclometasone dipropionate Alclometasone dipropionate is a synthetic corticosteroid for topical dermatologic use. Alclometasone dipropionate is a prodrug of alclometasone. The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. Alclometasone dipropionate is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. (See: alclometasone) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) anti-inflammatory drug (Code: CHEBI:35472) 1982-12-14 FDA
Click to view haloperidol decanoate Haloperidol decanoate is a prodrug and an ester derivative of haloperidol. When it is administered as an intramuscula depot in sesame oil, esterases present in blood and tissues hydrolyze haloperidol decanoate to provide a slow release of the active neuroleptic haloperidol from the depot into the systemic circulation. (See: haloperidol) Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) 1986-01-14 FDA
Click to view estradiol acetate Estradiol acetate is a pro-drug ester of estradiol. Estradiol acetate is used for the treatment of moderate to severe vasomotor symptoms and vulvovaginal atrophy due to menopause as a vaginal ring. (See: estradiol) 2003-03-20 FDA
Click to view paliperidone palmitate D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022264s013s014lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/022264s013s014lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN A benzisoxazole derivative and active metabolite of RISPERIDONE that functions as a DOPAMINE D2 RECEPTOR ANTAGONIST and SEROTONIN 5-HT2 RECEPTOR ANTAGONIST. It is an ANTIPSYCHOTIC AGENT used in the treatment of SCHIZOPHRENIA. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Dopamine Agents (Code: D015259) Dopamine Antagonists (Code: D018492) Dopamine D2 Receptor Antagonists (Code: D065127) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin 5-HT2 Receptor Antagonists (Code: D058830) Serotonin Agents (Code: D018490) Serotonin Antagonists (Code: D012702) Tranquilizing Agents (Code: D014149) alpha-adrenergic antagonist (Code: CHEBI:37890) dopaminergic antagonist (Code: CHEBI:48561) H1-receptor antagonist (Code: CHEBI:37955) neuroprotective agent (Code: CHEBI:63726) psychotropic drug (Code: CHEBI:35471) second generation antipsychotic (Code: CHEBI:65191) serotonergic antagonist (Code: CHEBI:48279) 2009-07-31 FDA
Click to view hydrocortisone valerate Hydrocortisone valerate is a topical corticosteroid and it has anti-inflammatory, antipruritic and vasoconstrictive properties. It is a prodrug of hydrocortisone. (See: hydrocortisone) 1978-03-17 FDA
Click to view choline fenofibrate Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022418s016lbl.pdf) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022418s016lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022418s016lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) weak inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022418s016lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022418s016lbl.pdf) Choline Fenofibrate is a choline formulation of fenofibrate, a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity. The effects of fenofibric acid seen in clinical practice have been explained in vivo in transgenic mice and in vitro in human hepatocyte cultures by the activation of peroxisome proliferator activated receptor ? (PPAR?). It’s used as adjunctive therapy to diet to reduce elevated LDL-C, Total-C,Triglycerides and Apo B, and to increase HDL-C in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Fredrickson Types IIa and IIb). Anticholesteremic Agents (Code: D000924) Antimetabolites (Code: D000963) Hypolipidemic Agents (Code: D000960) Lipid Regulating Agents (Code: D057847) Peroxisome Proliferator Receptor alpha Agonist (Code: N0000175596) 1993-12-31 FDA
Click to view halcinonide Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist Androgen receptor (Organism: Rattus norvegicus, class: Transcription factor, accessions: P15207, gene: Ar, swissprot: ANDR_RAT) Progesterone receptor (Organism: Bos taurus, class: Transcription factor, accessions: Q690N0, gene: PGR, swissprot: Q690N0_BOVIN) A glucocorticoid used topically in the treatment of DERMATITIS; ECZEMA; or PSORIASIS. It may cause skin irritation. Anti-Inflammatory Agents (Code: D000893) Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) 1974-11-27 FDA
Click to view linolenic acid Fatty acid-binding protein, heart (Organism: Homo sapiens, class: Cytosolic other, accessions: P05413, gene: FABP3, swissprot: FABPH_HUMAN Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN Prostaglandin G/H synthase 2 (Organism: Ovis aries, class: Enzyme, accessions: P79208, gene: PTGS2, swissprot: PGH2_SHEEP Prostaglandin G/H synthase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P23219, gene: PTGS1, swissprot: PGH1_HUMAN Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN Prostaglandin G/H synthase 1 (Organism: Bos taurus, class: Enzyme, accessions: O62664, gene: PTGS1, swissprot: PGH1_BOVIN Peroxisome proliferator-activated receptor delta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q03181, gene: PPARD, swissprot: PPARD_HUMAN Tissue factor (Organism: Homo sapiens, class: Membrane receptor, accessions: P13726, gene: F3, swissprot: TF_HUMAN A fatty acid that is found in plants and involved in the formation of prostaglandins. nutraceutical (Code: CHEBI:50733) FDA LNL
Click to view tetracosactide Adrenocorticotropic hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: Q01718, gene: MC2R, swissprot: ACTHR_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/17877367) Tetracosactide is a synthetic peptide that is identical to the 24-amino acid segment at the N-terminal of adrenocorticotropic hormone. This segment is similar in all speciesand contains the biological activity that stimulates production of corticosteroids in the adrenal cortex. Tetracosactide exhibits the same activity as natural ACTH with regard to all its biological activities. Tetracosactide is used as a diagnostic agent in the screening of patients presumed to have adrenocortical insufficiency. Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) diagnostic agent (Code: CHEBI:33295) Adrenocorticotropic Hormone (Code: N0000006478) 1970-04-22 FDA
Click to view teriparatide Parathyroid hormone/parathyroid hormone-related peptide receptor (Organism: Homo sapiens, class: GPCR, accessions: Q03431, gene: PTH1R, swissprot: PTH1R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021318s036lbl.pdf) Parathyroid hormone 2 receptor (Organism: Homo sapiens, class: GPCR, accessions: P49190, gene: PTH2R, swissprot: PTH2R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021318s036lbl.pdf) Teriparatide is a polypeptide that consists of the 1-34 amino-acid fragment of human parathyroid hormone, the biologically active N-terminal region. Teriparatide is indicated for the treatment of postmenopausal osteoporosis, osteoporosis associated with sustained systemic glucocorticoid therapy and for increase of bone mass in men with primary or hypogonadal osteoporosis. Parathyroid Hormone (Code: N0000011221) Parathyroid Hormone Analog (Code: N0000180852) Bone Density Conservation Agents (Code: D050071) 2002-11-26 FDA
Click to view quinine Purine nucleoside phosphorylase (Organism: Plasmodium falciparum, class: Unclassified, accessions: Q8T9Z7, gene: PNP, swissprot: Q8T9Z7_PLAFA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/30602534) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/211226s000lbl.pdf) Solute carrier family 22 member 1 (Organism: Mus musculus, class: Unclassified, accessions: O08966, gene: Slc22a1, swissprot: S22A1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12176030) Solute carrier family 22 member 2 (Organism: Mus musculus, class: Transporter, accessions: O70577, gene: Slc22a2, swissprot: S22A2_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12176030) Potassium voltage-gated channel subfamily B member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q92953, gene: KCNB2, swissprot: KCNB2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9612272) Equilibrative nucleoside transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q7RTT9, gene: SLC29A4, swissprot: S29A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16099839) Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23062825) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21300721) Potassium voltage-gated channel subfamily A member 5 (Organism: Homo sapiens, class: Ion channel, accessions: P22460, gene: KCNA5, swissprot: KCNA5_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17506538) Potassium voltage-gated channel subfamily D member 2 (Organism: Rattus norvegicus, class: Unclassified, accessions: Q63881, gene: Kcnd2, swissprot: KCND2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17506538) Potassium channel subfamily T member 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q5JUK3, gene: KCNT1, swissprot: KCNT1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24591078) Potassium voltage-gated channel subfamily H member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O95259, gene: KCNH1, swissprot: KCNH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11943152) Quinine is an alkaloid derived from the bark of the cinchona tree. Quinine inhibits nucleic acid synthesis, protein synthesis, and glycolysis in P. falciparum and can bind with hemazoin in parasitized erythrocytes. The mechanisms of its antimalarial effects are not well understood. It is used as an antimalarial drug, and is the active ingredient in extracts of the cinchona. Quinine is also a mild antipyretic and analgesic and has been used in common cold preparations for that purpose. It was used commonly and as a bitter and flavoring agent, and is still useful for the treatment of babesiosis. Quinidine is the d-isomer of quinine. Quinidine is an antiarrhythmic agent with Class Ia activity. In cardiac muscle and in Purkinje fibers, quinidine depresses the rapid inward depolarizing sodium current. The result is slowed conduction and reduced automaticity in all parts of the heart, with increase of the effective refractory period. Quinidine also raises the fibrillation thresholds of the artria and ventricles, and it raises the ventricular defibrillation threshold as well. Quinidine is used for the conversion of artrial fibrillation/flutter, for the reduction of frequency of relapse into atrial fibrillation/flutter, for the suppression of ventricular arrhythmias. Antiarrhythmic (Code: N0000175426) Cytochrome P450 2D6 Inhibitor (Code: N0000182135) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Anti-Arrhythmia Agents (Code: D000889) muscarinic antagonist (Code: CHEBI:48876) Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Infective Agents (Code: D000890) Antimalarials (Code: D000962) Antiparasitic Agents (Code: D000977) Antiprotozoal Agents (Code: D000981) Central Nervous System Agents (Code: D002491) Muscle Relaxants, Central (Code: D009125) Neuromuscular Agents (Code: D009465) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) non-narcotic analgesic (Code: CHEBI:35481) antimalarial (Code: CHEBI:38068) muscle relaxant (Code: CHEBI:51371) quinine: 2005-08-12 FDA quinidine: 1950-07-12 FDA QI9
QDN
Click to view bismuth subgallate Bismuth subgallate is a compound of bismuth and gallic acid. Bismuth subgallate is a soothing agents. The mechanism of action of bismuth subgallate is unknown but may involve inhibition of bacterial fermentation. Bismuth subgallate is used for eliminating or reducing odor from flatulence and stool. Also bismuth subgallate is used for the symptomatic treatment of haemorrhoids and anal pruritus. Anti-Infective Agents (Code: D000890) Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) astringent (Code: CHEBI:74783) 1967-06-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view fazadinium FAZADINIUM BROMIDE was heading 1991-94; was FAZADINIUM see under PYRIDINIUM COMPOUNDS 1979-90; was AH 8165 see under PYRIDINIUM COMPOUNDS 1975-78; AH 8165 was see FAZADINIUM BROMIDE 1979-94; use PYRIDINIUM COMPOUNDS to search FAZADINIUM BROMIDE 1991-94, FAZADINIUM 1979-90 & AH 8165 1975-78; a rapid-acting, short-lasting, competitive nondepolarizing neuromuscular blocking agent; its action is rapidly and completely reversed by neostigmine
Click to view fluclorolone
Click to view fenbendazole Tubulin beta chain (Organism: Encephalitozoon intestinalis, class: Structural, accessions: Q9GSR5, gene: TUB2, swissprot: TBB_ENCIN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15500920) Fenbendazole is a broad-spectrum benzimidazole antiparasitic drug currently used for treatment in numerous animal species, including rodents. The molecular mode of fenbendazole action consists in binding of beta-tubulin monomer prior to dimerisation with alfa-tubulin which blocks subsequent microtubule formation. These microtubules are important organelles involved in the motility, the division and the secretion processes of cells in all living organisms. In the worms the blocking of microtubules perturbs the uptake of glucose, which eventually empties the glycogen reserves. This blocks the whole energy management mechanism of the worms that are paralyzed and die or are expelled. Fenbendazole also is indicated for use in other animal species against a wide spectrum of nematodes, tapeworms, flukes, and protozoa (Giardia duodenalis, Encephalitozoon intestinalis). Anthelmintics (Code: D000871) Anti-Infective Agents (Code: D000890) Antinematodal Agents (Code: D000969) Antiparasitic Agents (Code: D000977) antinematodal drug (Code: CHEBI:35444)
Click to view fluprednidene
Click to view flumedroxone used for treatment of migraine & premenstrual tension; RN given refers to parent cpd; structure
Click to view flumetasone An anti-inflammatory glucocorticoid used in veterinary practice. Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) anti-inflammatory drug (Code: CHEBI:35472)
Click to view fluorodopa (18F) Aromatic-L-amino-acid decarboxylase (Organism: Homo sapiens, class: Enzyme, accessions: P20711, gene: DDC, swissprot: DDC_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/200655s000lbl.pdf) Monoamine oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P21397|P27338, gene: MAOA|MAOB, swissprot: AOFA_HUMAN|AOFB_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/200655s000lbl.pdf) Catechol O-methyltransferase (Organism: Homo sapiens, class: Enzyme, accessions: P21964, gene: COMT, swissprot: COMT_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/200655s000lbl.pdf) Fluorodopa (18F) is a radioactive diagnostic agent. In dopaminergic nerve terminals in the brain, Fluorodopa (FDOPA) F 18 is decarboxylated by amino acid decarboxylase to Fluorodopamine F18 (F 18 FDA) and stored in presynaptic vesicles in the brain. The accumulation of F 18 FDA in the striatum is visually detected in the PET scan. Fluorodopa (18F) isindicated for use in positron emission tomography to visualize dopaminergic nerve terminals in the striatum for the evaluation of adult patients with suspected Parkinsonian syndromes. 2019-10-10 FDA
Click to view fluoroethylcholine (18F) Fluoroethylcholine (18F) is an 18F-labeled choline analog which was initially synthesized as positron emission tomography tracer. Fluoroethylcholine (18F) phosphorylated by choline kinase (which overexpressed in malignant lesions) can be incorporated into phospholipids. Fluoroethylcholine (18F) is used for the diagnosis of prostate carcinoma and metastatic lymph nodes in patients at risk for metastases.
Click to view gepirone 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN Adrenergic receptor alpha-1 (Organism: Rattus norvegicus, class: GPCR, accessions: P15823|P23944|P43140, gene: Adra1a|Adra1b|Adra1d, swissprot: ADA1A_RAT|ADA1B_RAT|ADA1D_RAT Serotonin 1 (5-HT1) receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19327|P28564|P28565|P30940, gene: Htr1a|Htr1b|Htr1d|Htr1f, swissprot: 5HT1A_RAT|5HT1B_RAT|5HT1D_RAT|5HT1F_RAT 5-hydroxytryptamine receptor 1A (Organism: Rattus norvegicus, class: GPCR, accessions: P19327, gene: Htr1a, swissprot: 5HT1A_RAT Anti-Anxiety Agents (Code: D014151) Antidepressive Agents (Code: D000928) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Neurotransmitter Agents (Code: D018377) Psychotropic Drugs (Code: D011619) Serotonin Agents (Code: D018490) Serotonin Receptor Agonists (Code: D017366) Tranquilizing Agents (Code: D014149)
Click to view fluticasone furoate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205625s007lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/205625s007lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205625Orig1s000ClinPharmR.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205625Orig1s000ClinPharmR.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205625Orig1s000ClinPharmR.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2014/205625Orig1s000ClinPharmR.pdf) Fluticasone furoate is a synthetic trifluorinated corticosteroid with anti-inflammatory activity. Fluticasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor that is approximately 29.9 times that of dexamethasone and 1.7 times that of fluticasone propionate. The precise mechanism of fluticasone furoate action on asthma is not known. Fluticasone furoate is indicated for the treatment of asthma and upper respiratory allergy. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Anti-Allergic Agents (Code: D018926) Anti-Asthmatic Agents (Code: D018927) Anti-Inflammatory Agents (Code: D000893) Autonomic Agents (Code: D001337) Bronchodilator Agents (Code: D001993) Dermatologic Agents (Code: D003879) Peripheral Nervous System Agents (Code: D018373) Respiratory System Agents (Code: D019141) prodrug (Code: CHEBI:50266) anti-allergic agent (Code: CHEBI:50857) anti-asthmatic drug (Code: CHEBI:49167) 2007-04-27 FDA GW6
Click to view gestonorone
Click to view guanoclor Guanoclor is an adrenergic neurone-blocking agent. It also interferes with noradrenaline synthesis by inhibition of the enzyme dopamine beta-hydroxylase. It was used alone or in combination with thiazide diuretic for the treatment of hypertension.
Click to view nomegestrol Nomegestrol is derivative of 19-norprogesterone. Nomegestrol is a potent progestin, acts as a selective full progesterone receptor agonist. It was never marketed, but it is a parent compound of nomegestrol acetate. (See: nomegestrol acetate)
Click to view hydrocortisone probutate Hydrocortisone probutate is a topical synthetic corticosteroid. It is a prodrug of hydrocortisone. (See: hydrocortisone) 1997-02-28 FDA
Click to view hydroquinine
Click to view hydroxyethylpromethazine Hydroxyethylpromethazine is a phenothiazine derivative and an antihistamine agent. Hydroxyethylpromethazine is a first-generation phenothiazine H1-antihistamine. Hydroxyethylpromethazine is also a potent anti-acetylcholine drug. This action may be due to the fact that a choline- like structure exists in the side chain of hydroxyethylpromethazine and may enable this drug to compete effectively with acetylcholine for receptor sites. Hydroxyethylpromethazine is used to treat allergy symptoms such as itching, runny nose, sneezing, itchy or watery eyes, hives, and itchy skin rashes.
Click to view iclaprim Dihydrofolate reductase (Organism: Pneumocystis carinii, class: Enzyme, accessions: P16184, gene: None, swissprot: DYR_PNECA Dihydrofolate reductase (Organism: Homo sapiens, class: Enzyme, accessions: P00374, gene: DHFR, swissprot: DYR_HUMAN Dihydrofolate reductase (Organism: Escherichia coli, class: Unclassified, accessions: B0BL08, gene: dfrA17, swissprot: B0BL08_ECOLX Dihydrofolate reductase (Organism: Staphylococcus aureus, class: Enzyme, accessions: P0A017, gene: folA, swissprot: DYR_STAAU has antiviral activity Enzyme Inhibitors (Code: D004791) Folic Acid Antagonists (Code: D005493) I2H
XCF
Click to view idanpramine
Click to view indigo carmine Indolesulfonic acid used as a dye in renal function testing for the detection of nitrates and chlorates, and in the testing of milk. Coloring Agents (Code: D004396) food colouring (Code: CHEBI:77182) histological dye (Code: CHEBI:77178) two-colour indicator (Code: CHEBI:50412) FDA
Click to view iobenguane (131I) Iobenguane is a synthetic, aralkylguanidine analogue of the adrenergic neurotransmitter norepinephrine (NE) and adrenergic neuron blocking agent with potential diagnostic imaging or antineoplastic activity when radiolabeled. Iobenguane accumulates in adrenergically innervated tissues such as the adrenal medulla, salivary glands, heart, liver, spleen and lungs as well as tumors derived from the neural crest. Iobenguane is taken up and accumulates within pheochromocytoma and paraganglioma cells, and radiation resulting from radioactive decay of I 131 causes cell death and tumor necrosis. Iobenguane (131I) is indicated for the treatment of patients with iobenguane scan positive, unresectable, locally advanced or metastatic pheochromocytoma or paraganglioma who require systemic anticancer therapy. 1994-03-25 FDA
Click to view iodocholesterol (131I)
Click to view ioglicic acid Ioglicic acid is an ionic monomeric iodinated radiographic contrast medium that was used, as the meglumine and sodium salts, for X-RAY diagnostic procedures.
Click to view testosterone enantate Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) agonist Androgens (Code: D000728) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1953-12-24 FDA
Click to view iopydol Iopydol is an X-ray contrast medium used in conjunction with iopydone as the proprietary preparation, for the examination of the bronchial tract.
Click to view ioxitalamic acid Iooxitalamic acid is used as a contrast medium. It has a role as a xenobiotic, an environmental contaminant and a radioopaque medium. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338) 1995-12-31 Health Canada
Click to view itramin tosilate Itramin tosilate (p-toluolsulfonate, nitrolamine tosylate) is a general vasodilator. Its coronaro-dilator and hypotensive effects are less market but are more prolonged than is the case with nitroglycerin. Itramin tosilate was withdrawn from the market.
Click to view levoverbenone Levoverbenone or (1S)-(-)-Verbenone is an enantiomer of verbenone, a bicyclic monoterpene ketone, naturally occurring in insect pheromones, and in certain plant essential oils. It exerts acaricidal activity against Dermatophagoides spp. and Tyrophagus putrescentiae. It is used as an expectorant. expectorant (Code: CHEBI:77035)
Click to view linopirdine Potassium voltage-gated channel subfamily KQT member 5 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NR82, gene: KCNQ5, swissprot: KCNQ5_HUMAN) blocker (Source: ) Potassium voltage-gated channel subfamily KQT member 4 (Organism: Homo sapiens, class: Ion channel, accessions: P56696, gene: KCNQ4, swissprot: KCNQ4_HUMAN) blocker (Source: ) Potassium voltage-gated channel subfamily KQT member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O43526, gene: KCNQ2, swissprot: KCNQ2_HUMAN) blocker (Source: ) Potassium voltage-gated channel subfamily KQT member 3 (Organism: Rattus norvegicus, class: Unclassified, accessions: O88944, gene: Kcnq3, swissprot: KCNQ3_RAT) inhibitor (Source: ) Potassium voltage-gated channel subfamily KQT member 1 (Organism: Mus musculus, class: Unclassified, accessions: P97414, gene: Kcnq1, swissprot: KCNQ1_MOUSE) inhibitor (Source: ) acetylcholine releasing drug Cardiovascular Agents (Code: D002317) Central Nervous System Agents (Code: D002491) Membrane Transport Modulators (Code: D049990) Neuroprotective Agents (Code: D018696) Potassium Channel Blockers (Code: D026902) Protective Agents (Code: D020011)
Click to view linsidomine Linsidomine is an active metabolite of molsidomine and an unstable compound that releases endothelial NO upon decay. Linsidomine is used as a vasodilator and antianginal drug for the treatment of Prinzmetal Angina and for Vasodilation during dynamic coronary diagnostic. Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Hematologic Agents (Code: D006401) Nitric Oxide Donors (Code: D020030) Platelet Aggregation Inhibitors (Code: D010975) Vasodilator Agents (Code: D014665) 1987-12-29 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view diazolidinylurea Diazolidinylurea is a formaldehyde releasing substance. Diazolidinylurea is a heterocyclic-substituted urea used as a preservative in a variety of cosmetic products. Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131)
Click to view mannosulfan minor descriptor (75-84); on-line & Index Medicus search METHANESULFONATES (75-84)
Click to view diosmetin Multidrug resistance-associated protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P33527, gene: ABCC1, swissprot: MRP1_HUMAN) Cytochrome P450 1B1 (Organism: Homo sapiens, class: Enzyme, accessions: Q16678, gene: CYP1B1, swissprot: CP1B1_HUMAN) a 5,7-dihydroxyflavone antineoplastic agent (Code: CHEBI:35610) FDA
Click to view diethylamino hydroxybenzoyl hexyl benzoate a UV filtering agent FDA
Click to view morniflumate
Click to view xylitol Xylitol is a five-carbon sugar alcohol that is obtained through the diet. It is not endogenously produced by humans. Xylitol is used as a diabetic sweetener which is roughly as sweet as sucrose with 33% fewer calories. Xylitol is naturally found in many fruits and vegetables. Xylitol is produced starting from xylose, the isomaltose, by enzymatic transposition of the saccharose. Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Sweetening Agents (Code: D013549) sweetening agent (Code: CHEBI:50505) 1983-08-24 ANSM (French National Agency for Medicines and Health Products Safety) RB0
XYL
Click to view tonzonium Insulin-degrading enzyme (Organism: Homo sapiens, class: Enzyme, accessions: P14735, gene: IDE, swissprot: IDE_HUMAN Dual specificity tyrosine-phosphorylation-regulated kinase 1A (Organism: Rattus norvegicus, class: Unclassified, accessions: Q63470, gene: Dyrk1a, swissprot: DYR1A_RAT a surfactant with antifungal activity; also inhibits osteoclast formation 1962-05-17 FDA
Click to view clocortolone pivalate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist topical, anti-inflammatory glucocorticoid; structure Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1977-08-22 FDA
Click to view ubidecarenone Ubidecarenone is a coenzyme Q10, where Q refers to the quinone chemical group, and 10 refers to the number of isoprenyl chemical subunits in its tail. It is a powerful antioxidant, a lipid-soluble and essential cofactor in mitochondrial oxidative phosphorylation. The ubidecarenone is the coenzyme destined for mitochondrial enzyme complexes involved in oxidative phosphorylation in the production of ATP. It is fundamental for cells that have a high metabolic demand. 1987-12-31 Health Canada
Click to view trypan blue Tyrosine-protein phosphatase non-receptor type 1 (Organism: Homo sapiens, class: Enzyme, accessions: P18031, gene: PTPN1, swissprot: PTN1_HUMAN Tyrosine-protein phosphatase 1 (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P25044, gene: PTP1, swissprot: PTP1_YEAST A diazo-naphthalene sulfonate that is widely used as a stain. Diagnostic Dye (Code: N0000175536) Dyes (Code: N0000175533) Coloring Agents (Code: D004396) dye (Code: CHEBI:37958) 2004-12-16 FDA
Click to view sucrose A nonreducing disaccharide composed of GLUCOSE and FRUCTOSE linked via their anomeric carbons. It is obtained commercially from SUGARCANE, sugar beet (BETA VULGARIS), and other plants and used extensively as a food and a sweetener. Flavoring Agents (Code: D005421) Food Additives (Code: D005503) Sweetening Agents (Code: D013549) sweetening agent (Code: CHEBI:50505) FDA
Click to view stearic acid Carbonyl reductase [NADPH] 1 (Organism: Homo sapiens, class: Enzyme, accessions: P16152, gene: CBR1, swissprot: CBR1_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/28450226/) Stearic Acid is a typical fatty acid, which are essentially long hydrocarbon chains containing a carboxyl group at one end and a methyl group at the other. Stearic acid is found in various animal and plant fats, and is a major component of cocoa butter and shea butter. Stearic acid is used in the manufacturing of skin and hair care products. Stearic Acid is mainly used in the production of detergents, soaps, and cosmetics such as shampoos and shaving cream products. Stearic acid is used along with castor oil for preparing softeners in textile sizing. Stearic acid is known antidiabetic and antioxidant agent. STE
Click to view protocatechualdehyde Protocatechualdehyde is a kind of phenolic acid compound extracted from roots of the Salva miltiorrhiza. Protocatechualdehyde possesses antiproliferative and pro-apoptotic properties against human breast cancer cells and colorectal cancer cells by reducing the expression of pro-oncogenes ?-catenin and cyclin D1. Protocatechualdehyde is one of the major active components of the traditional Chinese medicine. Protocatechualdehyde is used to treat angina and heart coronary disease. In USA it was used in some cosmetic products for a whitening skin. Anticoagulants (Code: D000925) Hematologic Agents (Code: D006401) H6N
Click to view 1-Octacosanol FDA O8N
Click to view polydatin from Polygonum cuspidatum anti-arrhythmia drug (Code: CHEBI:38070) hepatoprotective agent (Code: CHEBI:62868) nephroprotective agent (Code: CHEBI:76595) FDA
Click to view N-Acetylglucosamine N-Acetylglucosamine (N-acetyl-D-glucosamine, or GlcNAc,) is a monosaccharide and a derivative of glucose. It is part of a biopolymer in the bacterial cell wall, built from alternating units of GlcNAc and N-acetylmuramic acid (MurNAc), cross-linked with oligopeptides at the lactic acid residue of MurNAc. It was shown, that GlcNAc was promising substance for treatment of chronic inflammatory bowel disease, with a mode of action which is distinct from conventional treatments. In experiments on rabbits with osteoarthritis, was found chondroprotective effects of aminomonosaccharide glucosamine, but no statistically significant difference was found between study groups. It was also investigated for the treatment of Multiple sclerosis, however, as a drug development target, GlcNAc had significant limitations. GlcNAc has poor membrane permeability, requiring high concentrations for biological effects.
Click to view methylnaltrexone Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021964s019,208271s003lbl.pdf) Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19282177) Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19282177) Methylnaltrexone is a selective antagonist of opioid binding at the mu-opioid receptor. As a quaternary amine, the ability of methylnaltrexone to cross the blood-brain barrier is restricted. This allows methylnaltrexone to function as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids without impacting opioid-mediated analgesic effects on the central nervous system. Opioid Antagonist (Code: N0000175691) Opioid Antagonists (Code: N0000000154) Quaternary Ammonium Compounds (Code: N0000166489) Central Nervous System Agents (Code: D002491) Narcotic Antagonists (Code: D009292) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) 2008-04-24 FDA
Click to view levomenol drug combination containing chamomile and bisabolol; used to treat dermatitis FDA
Click to view diacetyl benzoyl lathyrol FDA
Click to view levomefolic acid Thymidylate synthase (Organism: Homo sapiens, class: Enzyme, accessions: P04818, gene: TYMS, swissprot: TYSY_HUMAN) an ingredient in Contraceptives, Oral, Combined 2010-09-24 FDA C2F
Click to view linaclotide Heat-stable enterotoxin receptor (Organism: Homo sapiens, class: Enzyme, accessions: P25092, gene: GUCY2C, swissprot: GUC2C_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/20863829) Heat-stable enterotoxin receptor (Organism: Rattus norvegicus, class: Unclassified, accessions: P23897, gene: Gucy2c, swissprot: GUC2C_RAT) agonist (Source: ) Linaclotide is a guanylate cyclase-C (GC-C) agonist. Both linaclotide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation in intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit. In animal models, linaclotide has been shown to both accelerate GI transit and reduce intestinal pain. The linaclotide-induced reduction in visceral pain in animals is thought to be mediated by increased extracellular cGMP, which was shown to decrease the activity of pain-sensing nerves. Guanylate Cyclase-C Agonist (Code: N0000185500) Guanylate Cyclase Activators (Code: N0000185499) Enzyme Activators (Code: D020536) Gastrointestinal Agents (Code: D005765) Guanylyl Cyclase C Agonists (Code: D000074268) 2012-08-30 FDA
Click to view panobinostat Histone deacetylase 10 (Organism: Homo sapiens, class: Enzyme, accessions: Q969S8, gene: HDAC10, swissprot: HDA10_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Histone deacetylase 11 (Organism: Homo sapiens, class: Enzyme, accessions: Q96DB2, gene: HDAC11, swissprot: HDA11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Histone deacetylase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q9BY41, gene: HDAC8, swissprot: HDAC8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Histone deacetylase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UKV0, gene: HDAC9, swissprot: HDAC9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Histone deacetylase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UBN7, gene: HDAC6, swissprot: HDAC6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Histone deacetylase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q13547, gene: HDAC1, swissprot: HDAC1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Histone deacetylase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P56524, gene: HDAC4, swissprot: HDAC4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Histone deacetylase 3 (Organism: Homo sapiens, class: Enzyme, accessions: O15379, gene: HDAC3, swissprot: HDAC3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Histone deacetylase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q92769, gene: HDAC2, swissprot: HDAC2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Histone deacetylase 5 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UQL6, gene: HDAC5, swissprot: HDAC5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Histone deacetylase 7 (Organism: Homo sapiens, class: Enzyme, accessions: Q8WUI4, gene: HDAC7, swissprot: HDAC7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/205353s000lbl.pdf) Panobinostat is a histone deacetylase inhibitor used (as its lactate salt) in combination with bortezomib and dexamethasone for the treatment of multiple myeloma. Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Histone Deacetylase Inhibitors (Code: D056572) angiogenesis modulating agent (Code: CHEBI:50926) antineoplastic agent (Code: CHEBI:35610) Histone Deacetylase Inhibitor (Code: N0000175588) Cytochrome P450 2D6 Inhibitors (Code: N0000182137) 2015-02-23 FDA LBH
Click to view phenylacetic acid Phenylacetic acid is an organic compound containing a phenyl functional group and acarboxylic acid functional group. It reduces the amounts of ammonia in a patient's bloodstream by forming phenylacetyl-CoA, which then reacts with nitrogen-rich glutamine to form phenylacetylglutamine. Phenylacetate conjugates with glutamine in the liver and kidneys to form phenylacetylglutamine, via acetylation. Phenylacetylglutamine is excreted by the kidneys via glomerular filtration and tubular secretion. The nitrogen content of phenylacetylglutamine per mole is identical to that of urea (both contain two moles of nitrogen). Two moles of nitrogen are removed per mole of phenylacetate when it is conjugated with glutamine. Phenylacetic acid is used as adjunctive therapy for the treatment of acute hyperammonemia and associated encephalopathy in patients with deficiencies in enzymes of the urea cycle. It is also used in penicillin G production. Ammonium Ion Binding Activity (Code: N0000175806) Nitrogen Binding Agent (Code: N0000175807) Antimetabolites (Code: D000963) Antimetabolites, Antineoplastic (Code: D000964) Antineoplastic Agents (Code: D000970) Noxae (Code: D009676) 1987-12-23 FDA PAC
Click to view enzalutamide Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/203415Orig1s014lbl.pdf) Enzalutamide is an androgen receptor inhibitor that acts on different steps in the androgen receptor signaling pathway. Enzalutamide has been shown to competitively inhibit androgen binding to androgen receptors and inhibit androgen receptor nuclear translocation and interaction with DNA. A major metabolite, N??‘desmethyl enzalutamide, exhibited similar in vitro activity to enzalutamide. Enzalutamide decreased proliferation and induced cell death of prostate cancer cells in vitro, and decreased tumor volume in a mouse prostate cancer xenograft model. antineoplastic agent (Code: CHEBI:35610) androgen antagonist (Code: CHEBI:35497) Androgen Receptor Inhibitor (Code: N0000175560) Androgen Receptor Antagonists (Code: N0000000243) Cytochrome P450 3A4 Inducers (Code: N0000185506) Cytochrome P450 2C9 Inducers (Code: N0000185507) Cytochrome P450 2C19 Inducers (Code: N0000185607) 2012-08-31 FDA
Click to view trabectedin DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) alkylating agent (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207953s005lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207953s005lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/yondelis-epar-product-information_en.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16162970) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16162970) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16162970) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16162970) Trabectedin is a tetrahydroisoquinoline alkaloid isolated from the marine tunicate Ecteinascidia turbinata with potential antineoplastic activity. Binding to the minor groove of DNA, trabectedin interferes with the transcription-coupled nucleotide excision repair machinery to induce lethal DNA strand breaks and blocks the cell cycle in the G2 phase. Trabectedin is used for the treatment of soft tissue sarcoma and relapsed ovarian cancer. Alkylating Activity (Code: N0000000236) Alkylating Drug (Code: N0000175558) Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) angiogenesis modulating agent (Code: CHEBI:50926) antineoplastic agent (Code: CHEBI:35610) anti-inflammatory agent (Code: CHEBI:67079) 2007-09-17 EMA
Click to view teriflunomide Dihydroorotate dehydrogenase (quinone), mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q02127, gene: DHODH, swissprot: PYRD_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202992s008lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202992s008lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) weak inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202992s008lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202992s008lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202992s008lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202992s008lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202992s008lbl.pdf) Dihydroorotate dehydrogenase (Organism: Plasmodium falciparum, class: Unclassified, accessions: Q54A96, gene: dhod, swissprot: Q54A96_PLAFA) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24801997) Teriflunomide, an immunomodulatory agent with anti-inflammatory properties, inhibits dihydroorotate dehydrogenase, a mitochondrial enzyme involved in de novo pyrimidine synthesis. Teriflunomide is used in the treatment of relapsing forms of multiple sclerosis. non-steroidal anti-inflammatory drug (Code: CHEBI:35475) Pyrimidine Synthesis Inhibitor (Code: N0000185502) Dihydroorotate Dehydrogenase Inhibitors (Code: N0000185501) 2012-09-12 FDA A26
Click to view Choline C-11 Choline C-11 is an analog of choline. It is a positron emitting radiopharmaceutical that is used for diagnostic purposes in conjunction with PET imaging of patients with suspected prostate cancer recurrence and non-informative bone scintigraphy, computerized tomography (CT) or magnetic resonance imaging. In these patients, 11 C-choline PET imaging may help identify potential sites of prostate cancer recurrence for subsequent histologic confirmation. (See: choline) Radioactive Diagnostic Agent (Code: N0000177914) Radiopharmaceutical Activity (Code: N0000000205) radioactive tracer (Code: CHEBI:35207) 2012-09-12 FDA
Click to view oxabolone cipionate
Click to view eugenol Transient receptor potential cation channel subfamily V member 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q8NER1, gene: TRPV1, swissprot: TRPV1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/22075131) Transient receptor potential cation channel subfamily V member 1 (Organism: Mus musculus, class: Unclassified, accessions: Q704Y3, gene: Trpv1, swissprot: TRPV1_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15046718) Androgen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P10275, gene: AR, swissprot: ANDR_HUMAN) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20226658) Eugenol is a phenylpropanoid formally derived from guaiacol with an allyl chain substituted para to the hydroxy group. Eugenol, also called clove oil, is an aromatic oil extracted from cloves that is used widely as a flavoring for foods and teas and as an herbal oil used topically to treat toothache and more rarely to be taken orally to treat gastrointestinal and respiratory complaints. Eugenol also demonstrates antifungal and antimicrobial activity, showing efficacy against Candida albicans biofilms, Listeria monocytogenes and Escherichia coli. Eugenol is used in combination with other agents for adjunctive treatment of oral cavity infections. Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) Anti-Infective Agents (Code: D000890) Solvents (Code: D012997) 1994-07-05 Lithuania State Medicines Control Agency (VVKT) EOL
Click to view dipyrithione Dipyrithione (pyrithione disulfide) is a pyrithione derivate used as bactericide and fungicide. Dipyrithione was used in the form of shampoo for the treatment of dandruff, however it is no longer available. Also dipyrithione was used in combination with sulfur for washing of the face during the dermal infectiuos. Dermatologic Agents (Code: D003879) Keratolytic Agents (Code: D007641) 1994-12-31 Health Canada
Click to view dimyristoylphosphatidylglycerol Dimyristoylphosphatidylglycerol is a phospholipid used in commercially available pharmaceutical preparations to solubilize drugs for injection.
Click to view Padimate A combined with PABA in Spectraban 15 lotion & with indomethacin in Spectraban 5.6 lotion FDA
Click to view oftasceine Coloring Agents (Code: D004396) Fluorescent Dyes (Code: D005456) Indicators and Reagents (Code: D007202) Luminescent Agents (Code: D049408) fluorochrome (Code: CHEBI:51217) FDA
Click to view octyltriethoxysilane Octyltriethoxysilane is an organosilicon compound. Octyltriethoxysilane is used as a surface modifier to generate hydrophobicity or in the formulation of water repellent products. Octyltriethoxysilane can be found in hair styling products, suncreens cosmetic, face cream, eye liners.
Click to view dodecanoic acid Free fatty acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: O14842, gene: FFAR1, swissprot: FFAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27074625) Dodecanoic acid (lauric acid) is a saturated medium-chain fatty acid with a 12-carbon backbone. Lauric acid is found naturally in various plant and animal fats and oils, and is a major component of coconut oil and palm kernel oil. Dodecanoic acid is believed to have antimicrobial properties. Lauric acid is used in the manufacture of soaps, detergents, cosmetics, and lauryl alcohol. DAO
Click to view glycolic acid Glycolic acid (or hydroxyacetic acid) is the smallest alpha-hydroxy acid. Due to its excellent capability to penetrate skin, glycolic acid is often used in skin care products, most often as a chemical peel. It may reduce wrinkles, acne scarring, and hyperpigmentation and improve many other skin conditions, including actinic keratosis, hyperkeratosis, and seborrheic keratosis. Once applied, glycolic acid reacts with the upper layer of the epidermis, weakening the binding properties of the lipids that hold the dead skin cells together. This allows the outer skin to dissolve, revealing the underlying skin. It is thought that this is due to the reduction of calcium ion concentrations in the epidermis and the removal of calcium ions from cell adhesions, leading to desquamation. Acute doses of glycolic acid on skin or eyes leads to local effects that are typical of a strong acid (e. g. dermal and eye irritation). Glycolate is a nephrotoxin if consumed orally. Glycolic acid's renal toxicity is due to its metabolism to oxalic acid. Glycolic acid does exhibit some inhalation toxicity and can cause respiratory, thymus, and liver damage if present in very high levels over long periods of time. Dermatologic Agents (Code: D003879) Keratolytic Agents (Code: D007641) keratolytic drug (Code: CHEBI:50176) GOA
Click to view fluorometholone acetate Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist 1986-02-11 FDA
Click to view dimyristoylphosphatidylcholine A synthetic phospholipid used in liposomes and lipid bilayers for the study of biological membranes. Indicators and Reagents (Code: D007202) 2002-05-31 FDA MC3
Click to view chloramphenicol succinate inactive precursor (PRODRUGS) of chloramphenicol; used for parenteral administration of chloramphenicol; RN given refers to (R-(R*,R*))-isomer Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) 1950-12-08 FDA
Click to view benzoic acid Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/10579682) D-amino-acid oxidase (Organism: Homo sapiens, class: Enzyme, accessions: P14920, gene: DAO, swissprot: OXDA_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23391306) Solute carrier organic anion transporter family member 2B1 (Organism: Homo sapiens, class: Transporter, accessions: O94956, gene: SLCO2B1, swissprot: SO2B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12724351) Solute carrier family 22 member 8 (Organism: Rattus norvegicus, class: Transporter, accessions: Q9R1U7, gene: Slc22a8, swissprot: S22A8_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12358729) Benzoic acid is a fungistatic compound that is widely used as a food preservative. Benzoic acid occurs naturally free and bound as benzoic acid esters in many plant and animal species. Appreciable amounts have been found in most berries. Benzoic acid is a commonly used antimicrobial preservative in food and beverages. Benzoic acid in combination with salicylic acid is used to treat skin irritation and inflammation caused by burns, insect bites, fungal infections, or eczema. Ammonium Ion Binding Activity (Code: N0000175806) Nitrogen Binding Agent (Code: N0000175807) Anti-Infective Agents (Code: D000890) Antifungal Agents (Code: D000935) Food Additives (Code: D005503) Food Preservatives (Code: D005520) antimicrobial food preservative (Code: CHEBI:65256) drug allergen (Code: CHEBI:88188) 1953-10-01 Spanish Agency of Medicines and Medical Products (AEMPS) BEZ
Click to view brilliant green Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) Coloring Agents (Code: D004396) FDA
Click to view betiatide Betiatide is the active pharmaceutical ingredient in a diagnostic radiopharmaceutical - a kit for the preparation of technetium Tc 99m mertiatide. It is a renal imaging agent for use in the diagnosis of congenital and acquired abnormalities, renal failure, urinary tract obstruction, and calculi in adults and pediatric patients. It is a diagnostic aid in providing renal function, split function, renal angiograms, and renogram curves for whole kidney and renal cortex. 1990-06-15 FDA
Click to view methylrosaniline
Click to view metizoline Metizoline is an adrenergic agent with vasoconstrictor properties. It was used as the active component of nasal decongestant spray.
Click to view nalfurafine Nociceptin receptor (Organism: Homo sapiens, class: GPCR, accessions: P41146, gene: OPRL1, swissprot: OPRX_HUMAN) Kappa-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P41144, gene: OPRK1, swissprot: OPRK_CAVPO Kappa-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41145, gene: OPRK1, swissprot: OPRK_HUMAN) agonist Delta-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P32300, gene: Oprd1, swissprot: OPRD_MOUSE Mu-type opioid receptor (Organism: Cavia porcellus, class: GPCR, accessions: P97266, gene: OPRM1, swissprot: OPRM_CAVPO Mu-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P42866, gene: Oprm1, swissprot: OPRM_MOUSE Delta-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P41143, gene: OPRD1, swissprot: OPRD_HUMAN Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN Delta-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33533, gene: Oprd1, swissprot: OPRD_RAT Kappa-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P33534, gene: Oprk1, swissprot: OPRK_MOUSE 2009-01-21 PMDA
Click to view naproxcinod a nitric oxide-releasing NSAID derivative non-steroidal anti-inflammatory drug (Code: CHEBI:35475) non-narcotic analgesic (Code: CHEBI:35481) prodrug (Code: CHEBI:50266)
Click to view obidoxime Acetylcholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P22303, gene: ACHE, swissprot: ACES_HUMAN) Cholinesterase reactivator occurring in two interchangeable isomeric forms, syn and anti. Cholinergic Agents (Code: D018678) Cholinesterase Reactivators (Code: D002801) Enzyme Reactivators (Code: D004793) Neurotransmitter Agents (Code: D018377) OBI
Click to view omacetaxine mepesuccinate The mechanism of action of omacetaxine mepesuccinate has not been fully elucidated but includes inhibition of protein synthesis and is independent of direct Bcr-Abl binding. Omacetaxine mepesuccinate binds to the A-site cleft in the peptidyl-transferase center of the large ribosomal subunit from a strain of archaeabacteria. In vitro, omacetaxine mepesuccinate reduced protein levels of the Bcr-Abl oncoprotein and Mcl-1, an anti-apoptotic Bcl-2 family member. Omacetaxine mepesuccinate showed activity in mouse models of wild-type and T315I mutated Bcr-Abl CML. Angiogenesis Inhibitors (Code: D020533) Angiogenesis Modulating Agents (Code: D043924) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Phytogenic (Code: D000972) Growth Inhibitors (Code: D006131) Growth Substances (Code: D006133) antineoplastic agent (Code: CHEBI:35610) 2012-10-26 FDA HMT
Click to view oritavancin Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206334s005lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206334s005lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206334s005lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206334s005lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206334s005lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206334s005lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206334s005lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/206334s005lbl.pdf) Oritavancin is an glycopeptide antibiotic with bactericidal activity effective in treating infections caused by Gram-positive organisms. Oritavancin has three mechanisms of action: (i) inhibition of the transglycosylation (polymerization) step of cell wall biosynthesis by binding to the stem peptide of peptidoglycan precursors; (ii) inhibition of the transpeptidation (crosslinking) step of cell wall biosynthesis by binding to the peptide bridging segments of the cell wall; and (iii) disruption of bacterial membrane integrity, leading to depolarization, permeabilization, and cell death. These multiple mechanisms contribute to the concentration-dependent bactericidal activity of oritavancin. Oritavancin has been shown to be active against Staphylococcus aureus (including methicillin-resistant isolates), Streptococcus agalactiae, Streptococcus anginosus group (includes S. anginosus, S. intermedius, and S. constellatus), Streptococcus dysgalactiae, Streptococcus pyogenes, Enterococcus faecalis (vancomycin-susceptible isolates only). Oritavancin is indicated for the treatment of acute bacterial skin and skin structure infections. Lipoglycopeptide Antibacterial (Code: N0000191281) Lipoglycopeptides (Code: N0000191280) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) Cytochrome P450 2C9 Inhibitors (Code: N0000185504) Cytochrome P450 3A4 Inducers (Code: N0000185506) Cytochrome P450 2D6 Inducers (Code: N0000191267) Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) antibacterial drug (Code: CHEBI:36047) 2014-08-06 FDA
Click to view ornipressin A synthetic analog of vasopressin with ORNITHINE substitution at residue 8 of the cyclic nonapeptide. It is used as a local vasoconstrictor and hemostatic. Cardiovascular Agents (Code: D002317) Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) Vasoconstrictor Agents (Code: D014662)
Click to view paraoxon Lysophosphatidylserine lipase ABHD12 (Organism: Mus musculus, class: Enzyme accessions: Q99LR1, gene: Abhd12, swissprot: ABD12_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16310817) Fatty-acid amide hydrolase 1 (Organism: Mus musculus, class: Enzyme, accessions: O08914, gene: Faah, swissprot: FAAH1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11350214) Acetylcholinesterase (Organism: Mus musculus, class: Enzyme, accessions: P21836, gene: Ache, swissprot: ACES_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11350214) Cholinesterase (Organism: Mus musculus, class: Enzyme, accessions: Q03311, gene: Bche, swissprot: CHLE_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11350214) Liver carboxylesterase (Organism: Sus scrofa, class: Enzyme, accessions: Q29550, gene: None, swissprot: EST1_PIG) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10561082) Paraoxon is an acetylcholinesterase inhibitor. It is an organophosphate oxon, and the active metabolite of the insecticide parathion. Paraoxon is one of the most potent acetylcholinesterase-inhibiting insecticides available, around 70% as potent as the nerve agent sarin, and so is now rarely used as an insecticide due to the risk of poisoning to humans and other animals. It was also used as an opthamological drug against glaucoma. Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Insecticides (Code: D007306) Neurotransmitter Agents (Code: D018377) Pesticides (Code: D010575)
Click to view perampanel Glutamate receptor 1 (Organism: Homo sapiens, class: Ion channel, accessions: P42261, gene: GRIA1, swissprot: GRIA1_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Glutamate receptor 2 (Organism: Homo sapiens, class: Ion channel, accessions: P42262, gene: GRIA2, swissprot: GRIA2_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Glutamate receptor 3 (Organism: Homo sapiens, class: Ion channel, accessions: P42263, gene: GRIA3, swissprot: GRIA3_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Glutamate receptor 4 (Organism: Homo sapiens, class: Ion channel, accessions: P48058, gene: GRIA4, swissprot: GRIA4_HUMAN) antagonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) UDP-glucuronosyltransferase 1-9 (Organism: Homo sapiens, class: Enzyme, accessions: O60656, gene: UGT1A9, swissprot: UD19_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) UDP-glucuronosyltransferase 2B7 (Organism: Homo sapiens, class: Enzyme, accessions: P16662, gene: UGT2B7, swissprot: UD2B7_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) UDP-glucuronosyltransferase 1-4 (Organism: Homo sapiens, class: Enzyme, accessions: P22310, gene: UGT1A4, swissprot: UD14_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208277s000lbl.pdf) Perampanel is a non-competitive AMPA glutamate receptor antagonist. Perampanel is indicated as adjunctive therapy for the treatment of partial-onset seizures with or without secondarily generalized seizures and for the treatment of primary generalized tonic-clonic seizures. Noncompetitive AMPA Glutamate Receptor Antagonist (Code: N0000186106) AMPA Receptor Antagonists (Code: N0000020016) anticonvulsant (Code: CHEBI:35623) 2012-10-22 FDA 6ZP
Click to view pleconaril Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/21907579/) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://pubmed.ncbi.nlm.nih.gov/21907579/) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://pubmed.ncbi.nlm.nih.gov/16467135/) Pleconaril is an antiviral drug from viral capsid inhibitor class. It acts by inhibiting viral replication. it was used for the prevention of acute asthma exacerbations and common cold symptoms in asthmatic patients who have had exposure to picornavirus. Anti-Infective Agents (Code: D000890) Antiviral Agents (Code: D000998) W11
Click to view phenothrin Phenothrin is a synthetic pyrethroid compound which used to eliminate human louse infestation. Phenothrin acts on the membrane of nerve cells of insects blocking the closure of the ion gates of the sodium channel during re-polarization. This strongly disrupts the transmission of nervous impulses. At low concentrations insects suffer from hyperactivity. At high concentrations they are paralyzed and die. Insecticides (Code: D007306) Pesticides (Code: D010575) pyrethroid ester insecticide (Code: CHEBI:39116) 1989-06-19 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view phenylmercuric nitrate Phenylmercuric nitrate is an organomercury compound with powerful antiseptic and antifungal effects. It is bactericidal against many Gram-positive and Gram-negative species. Phenylmercuric nitrate is also an effective spermicide, although its use in vaginal contraceptives is no longer recommended. It is used as antimicrobial preservative mainly in ophthalmic preparations. Patients who used eye drops containing the preservative, phenylmercuric nitrate for from 3 to 15 years, developed a brownish pigmentation of the anterior capsule of the pupillary area.
Click to view picodralazine Picodralazine is a member of phthalazines. Picodralazine is a peripheral vasodilator, sympatholytic agent exerting antihypertensive properties.
Click to view remikiren Renin (Organism: Homo sapiens, class: Enzyme, accessions: P00797, gene: REN, swissprot: RENI_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/1830563) renin inhibitor under development for the treatment of hypertension Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Enzyme Inhibitors (Code: D004791) Protease Inhibitors (Code: D011480) REM
Click to view semustine Semustine is a methylated derivative of carmustine with antineoplastic activity. As an alkylating agent, semustine forms covalent linkages with nucleophilic centers in DNA, causing depurination, base-pair miscoding, strand scission, and DNA-DNA cross-linking, which may result in cytotoxicity. Isolated cases of pulmonary toxicity have been reported. Alkylating Agents (Code: D000477) Antineoplastic Agents (Code: D000970) Antineoplastic Agents, Alkylating (Code: D018906) Noxae (Code: D009676) antineoplastic agent (Code: CHEBI:35610) China Food and Drug Administration (CFDA)
Click to view ritiometan Ritiometan is an antiseptic used in an aerosol preparation for the treatment of rhinopharyngitis. 1996-08-06 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view tofacitinib Tyrosine-protein kinase JAK3 (Organism: Homo sapiens, class: Kinase, accessions: P52333, gene: JAK3, swissprot: JAK3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203214s023,208246s011lbl.pdf) Tyrosine-protein kinase JAK2 (Organism: Homo sapiens, class: Kinase, accessions: O60674, gene: JAK2, swissprot: JAK2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203214s023,208246s011lbl.pdf) Tyrosine-protein kinase JAK1 (Organism: Homo sapiens, class: Kinase, accessions: P23458, gene: JAK1, swissprot: JAK1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203214s023,208246s011lbl.pdf) JAK2/JAK1 (Organism: Homo sapiens, class: Kinase, accessions: P23458|O60674, gene: JAK1|JAK2, swissprot: JAK1_HUMAN|JAK2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203214s023,208246s011lbl.pdf) JAK3/JAK1 (Organism: Homo sapiens, class: Kinase, accessions: P23458|P52333, gene: JAK1|JAK3, swissprot: JAK1_HUMAN|JAK3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203214s023,208246s011lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203214s023,208246s011lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/203214s023,208246s011lbl.pdf) Rho-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: O75116, gene: ROCK2, swissprot: ROCK2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14593182) Tyrosine-protein kinase Lck (Organism: Homo sapiens, class: Kinase, accessions: P06239, gene: LCK, swissprot: LCK_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/14593182) Tofacitinib is a Janus kinase (JAK) inhibitor. Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1/JAK3, JAK1/JAK2, JAK1/TyK2, JAK2/JAK2). Tofacitinib inhibited the in vitro activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations. Tofacitinib is indicated for the treatment of rheumatoid arthritis, psoriatic arthritis and ulcerative colitis. Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) antirheumatic drug (Code: CHEBI:35842) Janus Kinase Inhibitor (Code: N0000190858) Janus Kinase Inhibitors (Code: N0000190857) 2012-11-06 FDA MI1
Click to view cabozantinib Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor Hepatocyte growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P08581, gene: MET, swissprot: MET_HUMAN) inhibitor Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor Angiopoietin-1 receptor (Organism: Homo sapiens, class: Kinase, accessions: Q02763, gene: TEK, swissprot: TIE2_HUMAN) inhibitor Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor Macrophage-stimulating protein receptor (Organism: Homo sapiens, class: Kinase, accessions: Q04912, gene: MST1R, swissprot: RON_HUMAN) inhibitor Cabozantinib inhibits the tyrosine kinase activity of MET, VEGFR-1, -2 and -3, AXL, RET, ROS1, TYRO3, MER, KIT, TRKB, FLT-3, and TIE-2. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, drug resistance, and maintenance of the tumor microenvironment. Kinase Inhibitor (Code: N0000175605) Protein Kinase Inhibitors (Code: N0000175076) antineoplastic agent (Code: CHEBI:35610) prodrug (Code: CHEBI:50266) 2012-11-29 FDA
Click to view ponatinib Tyrosine-protein kinase ABL1 (Organism: Homo sapiens, class: Kinase, accessions: P00519, gene: ABL1, swissprot: ABL1_HUMAN) inhibitor Tyrosine-protein kinase CSK (Organism: Homo sapiens, class: Kinase, accessions: P41240, gene: CSK, swissprot: CSK_HUMAN) inhibitor Tyrosine-protein kinase Lyn (Organism: Homo sapiens, class: Kinase, accessions: P07948, gene: LYN, swissprot: LYN_HUMAN) inhibitor Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor Vascular endothelial growth factor receptor 2 (Organism: Homo sapiens, class: Kinase, accessions: P35968, gene: KDR, swissprot: VGFR2_HUMAN) inhibitor Fibroblast growth factor receptor 1 (Organism: Homo sapiens, class: Kinase, accessions: P11362, gene: FGFR1, swissprot: FGFR1_HUMAN) inhibitor Platelet-derived growth factor receptor alpha (Organism: Homo sapiens, class: Kinase, accessions: P16234, gene: PDGFRA, swissprot: PGFRA_HUMAN) inhibitor Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN Proto-oncogene tyrosine-protein kinase Src (Organism: Gallus gallus, class: Kinase, accessions: P00523, gene: SRC, swissprot: SRC_CHICK Breakpoint cluster region protein (Organism: Homo sapiens, class: Kinase, accessions: P11274, gene: BCR, swissprot: BCR_HUMAN) inhibitor Bcr/Abl fusion protein (Organism: Homo sapiens, class: Kinase, accessions: P00519|P11274, gene: ABL1|BCR, swissprot: ABL1_HUMAN|BCR_HUMAN Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN Proto-oncogene tyrosine-protein kinase Src (Organism: Homo sapiens, class: Kinase, accessions: P12931, gene: SRC, swissprot: SRC_HUMAN Cyclin-dependent kinase 8 (Organism: Homo sapiens, class: Kinase, accessions: P49336, gene: CDK8, swissprot: CDK8_HUMAN) inhibitor (Source: ) Cyclin-dependent kinase 19 (Organism: Homo sapiens, class: Kinase, accessions: Q9BWU1, gene: CDK19, swissprot: CDK19_HUMAN) inhibitor (Source: ) a pan-Bcr-Abl protein kinase Inhibitor Kinase Inhibitor (Code: N0000175605) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) antineoplastic agent (Code: CHEBI:35610) 2012-12-14 FDA 0LI
Click to view teduglutide Glucagon-like peptide 2 receptor (Organism: Homo sapiens, class: GPCR, accessions: O95838, gene: GLP2R, swissprot: GLP2R_HUMAN) agonist an analogue of human glucagon-like peptide-2 (GLP-2) preserves mucosal integrity by promoting repair and normal growth of the intestine through an increase of villus height and crypt depth GLP-2 Analog (Code: N0000190992) Glucagon-like Peptide-2 (GLP-2) Agonists (Code: N0000190990) Glucagon-Like Peptide 2 (Code: N0000175140) Analogs/Derivatives (Code: N0000175452) Gastrointestinal Agents (Code: D005765) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) protective agent (Code: CHEBI:50267) 2012-08-30 EMA
Click to view daunorubicinol main metabolite of daunomycin 1964-01-01 YEAR INTRODUCED
Click to view lomitapide Microsomal triglyceride transfer protein large subunit (Organism: Homo sapiens, class: Cytosolic other, accessions: P55157, gene: MTTP, swissprot: MTP_HUMAN) inhibitor an anticholesteremic agent and microsomal triglycide transfer protein inhibitor anticholesteremic drug (Code: CHEBI:35821) Microsomal Triglyceride Transfer Protein Inhibitor (Code: N0000186779) Microsomal Triglyceride Transfer Protein Inhibitors (Code: N0000186778) Cytochrome P450 3A4 Inhibitors (Code: N0000182141) P-Glycoprotein Inhibitors (Code: N0000185503) 2012-12-21 FDA
Click to view succinimide Succinimide is a cycle imide of succinic acid that is present in numerous biologically active compounds including anticonvulsants, antitremor, anti-Parkinson`s agents. Also succinimide is used as adjunt treatment of urolithiasis. 1997-12-31 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view tacalcitol Vitamin D3 receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P11473, gene: VDR, swissprot: VDR_HUMAN) agonist (Source: )
Click to view tenidap Prostaglandin G/H synthase 1 (Organism: Rattus norvegicus, class: Enzyme, accessions: Q63921, gene: Ptgs1, swissprot: PGH1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10821716) Prostaglandin G/H synthase 2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P35355, gene: Ptgs2, swissprot: PGH2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10821716) Inward rectifier potassium channel 4 (Organism: Homo sapiens, class: Ion channel, accessions: P48050, gene: KCNJ4, swissprot: KCNJ4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/11821021) Tenidap is an oxindole derivative, a COX/5-LOX inhibitor and cytokine-modulating anti-inflammatory drug candidate. It lowers circulating C-reactive protein (CRP) concentrations. It was under development as a promising potential treatment for rheumatoid arthritis. Its marketing approval was rejected by the FDA in 1996 due to liver and kidney toxicity, which was attributed to metabolites of the drug with a thiophene moiety that caused oxidative damage. Analgesics (Code: D000700) Analgesics, Non-Narcotic (Code: D018712) Anti-Inflammatory Agents (Code: D000893) Anti-Inflammatory Agents, Non-Steroidal (Code: D000894) Antirheumatic Agents (Code: D018501) Cyclooxygenase Inhibitors (Code: D016861) Enzyme Inhibitors (Code: D004791) Peripheral Nervous System Agents (Code: D018373) Sensory System Agents (Code: D018689) non-steroidal anti-inflammatory drug (Code: CHEBI:35475)
Click to view trimethyldiphenylpropylamine Trimethyldiphenylpropylamine (Recipavrin) is a methadon analog with antispasmodic properties. It exerts both musculotropic (antibarium) and anticholinergic action, relieves smooth muscle spasms, e.g. dysmenorrhea and pains associated with gallstones. It was used in the 1960s as a spasmolytic drug.
Click to view tetragalacturonic acid hydroxymethylester
Click to view tetramethrin Insecticides (Code: D007306) Pesticides (Code: D010575) pyrethroid ester insecticide (Code: CHEBI:39116)
Click to view thiocolchicoside GABA A receptor alpha-2/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P18507|P47869|P47870, gene: GABRA2|GABRB2|GABRG2, swissprot: GBRA2_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) negative modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/17234181) GABA A receptor alpha-1/beta-1/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18505|P18507, gene: GABRA1|GABRB1|GABRG2, swissprot: GBRA1_HUMAN|GBRB1_HUMAN|GBRG2_HUMAN) negative modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/17234181) GABA-A receptor alpha-1/beta-2/gamma-2 (Organism: Homo sapiens, class: Ion channel, accessions: P14867|P18507|P47870, gene: GABRA1|GABRB2|GABRG2, swissprot: GBRA1_HUMAN|GBRB2_HUMAN|GBRG2_HUMAN) negative modulator (Source: http://www.ncbi.nlm.nih.gov/pubmed/17234181) GABA-A receptor; anion channel (Organism: Rattus norvegicus, class: Ion channel, accessions: O09028|P15431|P18506|P18508|P19969|P20236|P23574|P23576|P28471|P28473|P30191|P62813|P63079|P63138|Q91ZM7|Q9ES14, gene: Gabra1|Gabra2|Gabra3|Gabra4|Gabra5|Gabra6|Gabrb1|Gabrb2|Gabrb3|Gabrd|Gabre|Gabrg1|Gabrg2|Gabrg3|Gabrp|Gabrq, swissprot: GBRA1_RAT|GBRA2_RAT|GBRA3_RAT|GBRA4_RAT|GBRA5_RAT|GBRA6_RAT|GBRB1_RAT|GBRB2_RAT|GBRB3_RAT|GBRD_RAT|GBRE_RAT|GBRG1_RAT|GBRG2_RAT|GBRG3_RAT|GBRP_RAT|Q91ZM7_RAT used in combination with glafenine and meprobamate to tranquilize patients undergoing hysterosalpingography; structure
Click to view thioctic acid NADPH--cytochrome P450 reductase (Organism: Homo sapiens, class: Enzyme, accessions: P16435, gene: POR, swissprot: NCPR_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16391466) Thioctic Acid (also known as alpha-lipoic acid) is a naturally occurring micronutrient, synthesized in small amounts by plants and animals (including humans), with antioxidant and potential chemopreventive activities. Thioctic acid acts as a free radical scavenger and assists in repairing oxidative damage and regenerates endogenous antioxidants, including vitamins C and E and glutathione. This agent also promotes glutathione synthesis. In addition, thioctic acid exerts metal chelating capacities and functions as a cofactor in various mitochondrial enzyme complexes involved in the decarboxylation of alpha-keto acids. Antioxidants (Code: D000975) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Protective Agents (Code: D020011) Vitamin B Complex (Code: D014803) Vitamins (Code: D014815) FDA LPA
LPB
Click to view ticlatone Ticlatone is an antifungal for topical use.
Click to view trimegestone ligand for progesterone receptor
Click to view bedaquiline ATP synthase (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPU7|P9WPV7|P9WPV1|P9WPU5|P9WPS1|P9WPV5|P9WPV3|P9WPU9, gene: atpA|atpB|atpC|atpD|atpE|atpF|atpFH|atpG, swissprot: ATPA_MYCTU|ATP6_MYCTU|ATPE_MYCTU|ATPB_MYCTU|ATPL_MYCTU|ATPF_MYCTU|ATPFD_MYCTU|ATPG_MYCTU) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204384s010lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204384s010lbl.pdf) Bedaquiline is a diarylquinoline antimycobacterial drug that inhibits mycobacterial ATP (adenosine 5'-triphosphate) synthase, by binding to subunit c of the enzyme that is essential for the generation of energy in M. tuberculosis. Bedaquiline is a part of combination therapy in the treatment of pulmonary multi-drug resistant tuberculosis (MDR-TB). Anti-Bacterial Agents (Code: D000900) Anti-Infective Agents (Code: D000890) Antitubercular Agents (Code: D000995) antitubercular agent (Code: CHEBI:33231) Diarylquinoline Antimycobacterial (Code: N0000186775) Diarylquinolines (Code: N0000186774) 2012-12-28 FDA BQ1
Click to view etallobarbital Etallobarbital (ethallymal) is a drug that belongs to the class barbiturates. Etallobarbital was used for insomnia.
Click to view biphenylol Biphenylol (2-biphenylol) is found in lemon. It is an antifungal agent and preservative. 2-Biphenylol is used for post-harvest control of storage disease in apples, citrus fruit, stone fruit, tomatoes, cucumber and peppers through the use of impregnated wrapping materials or by direct application in a wax. 2-Biphenylol is used in food seasonings. CH9
Click to view dimethylaminopropionylphenothiazine Dimethylaminopropionylphenothiazine is a member of phenothiazines. It has anesthetic and antispasmodic activities.
Click to view dimethylcarbate Dimethylcarbate is a dicarboxylic acid. It was used as an insecticides and repellents.
Click to view dimethylphthalate used as plasticizer in computer mouse; structure Fixatives (Code: D005404) Insect Repellents (Code: D007302) Pesticides (Code: D010575) Protective Agents (Code: D020011)
Click to view dipiperonylaminoethanol Dipiperonylaminoethanol is tertiary amine derivative. It was used as a hypnotic and sedative agent.
Click to view ethyl hydroxybenzoate Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/22668600) Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23608764) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/23608764) Ethyl hydroxybenzoate (ethylparaben) is an antimicrobial agent which is produced naturally and found in several fruits and insects. Ethylparaben is mainly used as antiseptics in cosmetics, food and medicine (E number E214). It is also can be used as feed preservatives and antiseptic for bacteria. Standardized Chemical Allergen (Code: N0000185508) Increased Histamine Release (Code: N0000175629) Cell-mediated Immunity (Code: N0000184306) Allergens (Code: N0000171131) E4B
Click to view etohexadiol Etohexadiol is an insect repellent, moderately irritating to eyes, mucous membranes, but not to skin.
Click to view fluoromethylcholine (18F) Fluoromethylcholine (18F) is a radiotracer consisting of methylcholine labeled with the positron-emitting radioisotope fluorine F 18. Upon administration, 18F-fluoromethylcholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase to phosphoryl 18F-fluoromethylcholine. Phosphoryl 18F-fluoromethylcholine is integrated into phospholipids in the cell membrane as part of phosphatidylcholine. As the proliferation of cancer cells is much higher than normal cells, tumor cells exhibit an increased rate of 18F-FMCH uptake and incorporation, allowing tumor imaging with positron emission tomography. (See: choline) 2010-04-02 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view vilanterol Beta-2 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P07550, gene: ADRB2, swissprot: ADRB2_HUMAN) agonist Beta-3 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P13945, gene: ADRB3, swissprot: ADRB3_HUMAN) Beta-1 adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P08588, gene: ADRB1, swissprot: ADRB1_HUMAN) Vilanterol is a long-acting beta2-adrenergic agonist. The clinical relevance of this in vitro finding is unknown. Although beta2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors in the heart, there are also beta2-receptors in the human heart comprising 10% to 50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective beta2-agonists may have cardiac effects. The pharmacologic effects of beta2-adrenergic agonist drugs, including vilanterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. beta-adrenergic agonist (Code: CHEBI:35522) bronchodilator agent (Code: CHEBI:35523) Adrenergic beta2-Agonists (Code: N0000009922) beta2-Adrenergic Agonist (Code: N0000175779) 2013-05-10 FDA
Click to view ridaforolimus Serine/threonine-protein kinase mTOR (Organism: Homo sapiens, class: Kinase, accessions: P42345, gene: MTOR, swissprot: MTOR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21482695) an mTOR inhibitor for the treatment of cancer antineoplastic agent (Code: CHEBI:35610)
Click to view dabrafenib Serine/threonine-protein kinase B-raf (Organism: Homo sapiens, class: Kinase, accessions: P15056, gene: BRAF, swissprot: BRAF_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) RAF proto-oncogene serine/threonine-protein kinase (Organism: Homo sapiens, class: Kinase, accessions: P04049, gene: RAF1, swissprot: RAF1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Serine/threonine-protein kinase SIK1 (Organism: Homo sapiens, class: Kinase, accessions: P57059, gene: SIK1, swissprot: SIK1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Serine/threonine-protein kinase Nek11 (Organism: Homo sapiens, class: Kinase, accessions: Q8NG66, gene: NEK11, swissprot: NEK11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) LIM domain kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: P53667, gene: LIMK1, swissprot: LIMK1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Nuclear receptor subfamily 1 group I member 3 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q14994, gene: NR1I3, swissprot: NR1I3_HUMAN) activator (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/202806s012lbl.pdf) Dabrafenib is an inhibitor of some mutated forms of BRAF kinases (BRAF V600E, BRAF V600K, and BRAF V600D enzymes). Dabrafenib also inhibits wild-type BRAF and CRAF kinases and other kinases such as SIK1, NEK11, and LIMK1 at higher concentrations. Dabrafenib is indicated as a single agent or in combination with trametinib for the treatment of patients with unresectable or metastatic melanoma, metastatic non-small cell lung cancer or metastatic anaplastic thyroid cancer with BRAF V600E or V600K mutation. Kinase Inhibitor (Code: N0000175605) Cytochrome P450 3A4 Inducers (Code: N0000185506) Cytochrome P450 2B6 Inducers (Code: N0000187064) Cytochrome P450 2C8 Inducers (Code: N0000187063) Cytochrome P450 2C9 Inducers (Code: N0000185507) Cytochrome P450 2C19 Inducers (Code: N0000185607) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Organic Anion Transporter 1 Inhibitors (Code: N0000190110) Organic Anion Transporter 3 Inhibitors (Code: N0000190111) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) antineoplastic agent (Code: CHEBI:35610) 2013-05-29 FDA P06
Click to view trametinib Dual specificity mitogen-activated protein kinase kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: P36507, gene: MAP2K2, swissprot: MP2K2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204114s013lbl.pdf) Dual specificity mitogen-activated protein kinase kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q02750, gene: MAP2K1, swissprot: MP2K1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204114s013lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204114s013lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204114s013lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204114s013lbl.pdf) Bile salt export pump (Organism: Homo sapiens, class: Transporter, accessions: O95342, gene: ABCB11, swissprot: ABCBB_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/204114s013lbl.pdf) Trametinib is a dual-kinase inhibitor that is used in the treatment of advanced malignant melanoma, usually in combination with darbafenib. Trametinib specifically binds to and inhibits MEK 1 and 2, resulting in an inhibition of growth factor-mediated cell signaling and cellular proliferation in various cancers. Trametinib is used for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations, and who have not received prior BRAF inhibitor treatment. Kinase Inhibitor (Code: N0000175605) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) antineoplastic agent (Code: CHEBI:35610) 2013-05-29 FDA
Click to view sequifenadine Sequifenadine is a H1-receptor antagonist, it also moderately inhibits HT1 receptors of serotonin, thus decreasing the activity of allergy mediators histamine and serotonin. Sequifenadine activates enzyme diaminoxidase that splits endogenous histamine due to this decreasing quantity of histamine in tissues. Sequifenadine prevents or decreases the histamine and serotonin intoxication, bronchoconstrictive activity of histamine and spasmogenic effect of histamine on smooth musculature of bronchus, intestines, vessels; disturbances of vascular permeability and oedema development. Sequifenadine has pronounced prolonged antipruritic and antiexudative qualities. Insignificant quantity of sequifenadine crosses blood-brain barrier. It does not have pronounced CNS inhibiting effect, though there could be observed a moderate sedative effect in separate cases of individual increased sensitivity. 1984-08-02 Ministry of Health of the Russian Federation
Click to view corticotropin Melanocyte-stimulating hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: Q01726, gene: MC1R, swissprot: MSHR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7774675) Melanocortin receptor 3 (Organism: Homo sapiens, class: GPCR, accessions: P41968, gene: MC3R, swissprot: MC3R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7774675) Melanocortin receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: P32245, gene: MC4R, swissprot: MC4R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8884876) Adrenocorticotropic hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: Q01718, gene: MC2R, swissprot: ACTHR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17877367) Corticotropin (ACTH or adrenocorticotropic hormone) is a polypeptide hormone produced and secreted by the pituitary gland. Corticotropin acts through the stimulation of cell surface ACTH receptors, which are primarily located on the adrenocortical cells. As a diagnostic aid (adrenocortical function), corticotropin combines with a specific receptor on the adrenal cell plasma membrane. In patients with normal adrenocortical function, it stimulates the initial reaction involved in the synthesis of adrenal steroids from cholesterol by increasing the quantity of cholesterol within the mitochondria. The mechanism of action of corticotropin in the treatment of infantile myoclonic seizures is unknown. Seractide is a synthetic form of human corticotropin. Seractide is used as acetate salt for the as monotherapy for the treatment of infantile spasms in infants and children under 2 years of age, for the treatment of exacerbations of multiple sclerosis in adults, for the following disorders and diseases: rheumatic; collagen; dermatologic; allergic states; ophthalmic; respiratory; and edematous state. Adrenocorticotropic Hormone (Code: N0000006478) diagnostic agent (Code: CHEBI:33295) 1950-07-03 FDA
Click to view afamelanotide Melanocyte-stimulating hormone receptor (Organism: Homo sapiens, class: GPCR, accessions: Q01726, gene: MC1R, swissprot: MSHR_HUMAN) agonist (Source: ) Melanocortin receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: P32245, gene: MC4R, swissprot: MC4R_HUMAN) agonist (Source: ) Melanocortin receptor 3 (Organism: Homo sapiens, class: GPCR, accessions: P41968, gene: MC3R, swissprot: MC3R_HUMAN) agonist (Source: ) Melanocortin receptor 5 (Organism: Homo sapiens, class: GPCR, accessions: P33032, gene: MC5R, swissprot: MC5R_HUMAN) agonist (Source: ) observations suggest that afamelanotide has beneficial effects in patients with erythropoietic protoporphyria, induces epidermal melanin formation Dermatologic Agents (Code: D003879) 2014-12-12 EMA
Click to view vorapaxar Proteinase-activated receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P25116, gene: F2R, swissprot: PAR1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/18447380) has antiplatelet activity Protease-activated Receptor-1 Antagonist (Code: N0000190996) Protease-activated Receptor-1 Antagonists (Code: N0000190995) Hematologic Agents (Code: D006401) Platelet Aggregation Inhibitors (Code: D010975) platelet aggregation inhibitor (Code: CHEBI:50427) cardiovascular drug (Code: CHEBI:35554) 2014-05-08 FDA VPX
Click to view albiglutide Glucagon-like peptide 1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P43220, gene: GLP1R, swissprot: GLP1R_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/125431s000lbl.pdf) Glucagon-like peptide 1 receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P32301, gene: Glp1r, swissprot: GLP1R_RAT) agonist (Source: ) A long-acting glucagon-like peptide-1 (GLP-1) receptor agonist, with antihyperglycemic activity. Albiglutide is composed of a GLP-1 (7-36) dimer fused to recombinant human albumin. Upon subcutaneous administration, this agent has a half-life of 4-7 days and resists degradation by dipeptidyl peptidase-4 (DPP-4). GLP-1 Receptor Agonist (Code: N0000178480) Glucagon-like Peptide-1 (GLP-1) Agonists (Code: N0000020058) 2014-04-15 FDA
Click to view glycobiarsol Glycobiarsol is a pentavalent arsenical combined with the metal bismuth. Glycobiarsol have been used for the treatment of amebiasis, but it is no longer available due to its potential toxicity.
Click to view levomilnacipran Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/204168s005lbl.pdf) Sodium-dependent noradrenaline transporter (Organism: Homo sapiens, class: Transporter, accessions: P23975, gene: SLC6A2, swissprot: SC6A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/204168s005lbl.pdf) Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q9R1M7|Q8VHN2, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3A_RAT|NMD3B_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9719604) Levomilnacipran is a selective serotonin and norepinephrine reuptake inhibitor, mechanism of the antidepressant action of levomilnacipran is unknown, but is thought to be related to the potentiation of serotonin and norepinephrine in the central nervous system. Norepinephrine Uptake Inhibitors (Code: N0000000102) Serotonin and Norepinephrine Reuptake Inhibitor (Code: N0000175749) Serotonin Uptake Inhibitors (Code: N0000000109) 2013-07-25 FDA
Click to view cridanimod Cridanimod is a small-molecule immunomodulator and interferon inducer. 1995-05-15 Ministry of Health of the Russian Federation 1K5
Click to view sodium thiosalicylate Sodium thiosalicylate is an salicylic acid derivative with analgetic and anti-inflammatory properties. It is used to relieve pain and other symptoms from musculoskeletal conditions, osteoarthritis, rheumatic fever, acute gout. JKE
Click to view estrone sulphate Estrogen receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P03372, gene: ESR1, swissprot: ESR1_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2005/083220s041lbl.pdf) Estrogen receptor beta (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q92731, gene: ESR2, swissprot: ESR2_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2005/083220s041lbl.pdf) Steryl-sulfatase (Organism: Homo sapiens, class: Enzyme, accessions: P08842, gene: STS, swissprot: STS_HUMAN Solute carrier family 22 member 20 (Organism: Mus musculus, class: Transporter, accessions: Q80UJ1, gene: Slc22a20, swissprot: S22AK_MOUSE used therapeutically in menopausal patients Contraceptive Agents (Code: D003270) Reproductive Control Agents (Code: D012102) 1977-05-19 FDA
Click to view corticorelin Corticotropin-releasing factor receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: P34998, gene: CRHR1, swissprot: CRFR1_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/7692441) Corticorelin is a synthetic peptide that is used for the determination of pituitary corticotroph responsiveness. In medicine corticorelin ovine is used. Corticorelin ovine has an amino acid sequence identical to ovine corticotropin-releasing hormone (oCRH)), which is an analogue of the naturally occurring human CRH (hCRH) peptide. Both peptides are potent stimulators of adrenocorticotropic hormone (ACTH) release from the anterior pituitary. Corticorelin is indicated for use in differentiating pituitary and ectopic production of ACTH in patients with ACTH-dependent Cushing’s syndrome. 1996-05-23 FDA
Click to view mebicar Mebicar is an anxiolytic, non-benzodizepam tranquilizers with nootropic and stress-protective characteristics. Mebicar increases serotonin levels, decreases noradrenaline level with no effect on dopamine and no anticholinergic activity. It acts on hypothalamus emotional zone, thus providing moderate tranquilizing effect. Mebicar is used for the treatment of anxiety, awareness, fear, emotional density, irritability. Analgesics (Code: D000700) Anti-Anxiety Agents (Code: D014151) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Peripheral Nervous System Agents (Code: D018373) Psychotropic Drugs (Code: D011619) Sensory System Agents (Code: D018689) Tranquilizing Agents (Code: D014149) 1978-09-18 Ministry of Health of the Russian Federation
Click to view nicotinyl methylamide Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23047651) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23047651) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/23047651) Nicotinyl methylamide (N-methylnicotinamide) is a metabolite of niacinamide/nicotinamide and niacin/nicotinic acid (vitamin B3). N-methylnicotinamide is known to inhibit choline transport and reduce choline clearance out of the brain. N-methylnicotinamide is used to diagnose niacin deficiency by measuring N-methylnicotinamide in the urine.
Click to view phenibut GABA-B receptor (Organism: Homo sapiens, class: GPCR, accessions: O75899|Q9UBS5, gene: GABBR1|GABBR2, swissprot: GABR1_HUMAN|GABR2_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/11830761) Phenibut is a neuropsychotropic drug that has anxiolytic and nootropic (cognition enhancing) effects. It acts as a GABA-mimetic, primarily at GABA(B) receptors. Pharmacological activity of racemic phenibut relies on R-phenibut and this correlates to the binding affinity of enantiomers of phenibut to the GABAB receptor. In addition R-phenibut binds to the ?2-? subunit of voltage-dependent calcium channels. It is highly effective in treating anxiety, post-traumatic stress disorder, depression, asthenia, insomnia, alcoholism, stuttering, and vestibular disorders. It also improves mental performance (attention, memory, speed and accuracy of sensory-motor reactions), physical performance, reduces sleep disorders as well as movement and speech disorders. 1974-12-18 Ministry of Health of the Russian Federation
Click to view tofogliflozin Sodium/glucose cotransporter 2 (Organism: Homo sapiens, class: Transporter, accessions: P31639, gene: SLC5A2, swissprot: SC5A2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22889351) Sodium/glucose cotransporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P13866, gene: SLC5A1, swissprot: SC5A1_HUMAN) inhibits sodium-glucose cotransporter 2 2014-03-24 PMDA
Click to view tipiracil Thymidine phosphorylase (Organism: Homo sapiens, class: Enzyme, accessions: P19971, gene: TYMP, swissprot: TYPH_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/207981s008lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/lonsurf-epar-product-information_en.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) substrate (Source: https://www.ema.europa.eu/documents/product-information/lonsurf-epar-product-information_en.pdf) Tipiracil is a thymidine phosphorylase inhibitor. Trifluridine is incorporated into DNA via phosphorylation, ultimately inhibiting cell proliferation. Tipiracil increases systemic exposure of trifluridine when coadministered. Tipiracil is used in combination with trifluridine for the treatment of metastatic colorectal cancer. Thymidine Phosphorylase Inhibitor (Code: N0000191870) Thymidine Phosphorylase Inhibitors (Code: N0000191869) antineoplastic agent (Code: CHEBI:35610) 2014-03-24 PMDA CMU
Click to view iguratimod a methanesulfonanilide disease-modifying antirheumatic drug that has been developed exclusively in Japan and China 2012-06-29 PMDA
Click to view teneligliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22959556) Dipeptidyl peptidase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q6V1X1, gene: DPP8, swissprot: DPP8_HUMAN) Dipeptidyl peptidase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q86TI2, gene: DPP9, swissprot: DPP9_HUMAN) Dipeptidyl peptidase 4 (Organism: Rattus norvegicus, class: Enzyme, accessions: P14740, gene: Dpp4, swissprot: DPP4_RAT A long-acting, orally bioavailable, pyrrolidine-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Teneligliptin may also reduce plasma triglyceride levels through a sustained increase in GLP-1 levels. 2012-06-29 PMDA M51
Click to view anagliptin Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/22019046) Dipeptidyl peptidase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q6V1X1, gene: DPP8, swissprot: DPP8_HUMAN) Dipeptidyl peptidase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q86TI2, gene: DPP9, swissprot: DPP9_HUMAN) Prolyl endopeptidase FAP (Organism: Homo sapiens, class: Enzyme, accessions: Q12884, gene: FAP, swissprot: SEPR_HUMAN anagliptin hydrochloride salt is the active compound Dipeptidyl-Peptidase IV Inhibitors (Code: D054873) Enzyme Inhibitors (Code: D004791) Hypoglycemic Agents (Code: D007004) Protease Inhibitors (Code: D011480) 2012-09-28 PMDA SKK
Click to view edoxaban Coagulation factor X (Organism: Homo sapiens, class: Enzyme, accessions: P00742, gene: F10, swissprot: FA10_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20503967) An orally active inhibitor of coagulation factor Xa (activated factor X) with anticoagulant activity. Edoxaban is administered as edoxaban tosylate. This agent has an elimination half-life of 9-11 hours and undergoes renal excretion. Factor Xa Inhibitor (Code: N0000175637) Anticoagulants (Code: D000925) Antithrombins (Code: D000991) Enzyme Inhibitors (Code: D004791) Factor Xa Inhibitors (Code: D065427) Hematologic Agents (Code: D006401) Protease Inhibitors (Code: D011480) Serine Proteinase Inhibitors (Code: D015842) anticoagulant (Code: CHEBI:50249) platelet aggregation inhibitor (Code: CHEBI:50427) 2011-04-22 PMDA
Click to view fimasartan Type-1 angiotensin II receptor (Organism: Homo sapiens, class: GPCR, accessions: P30556, gene: AGTR1, swissprot: AGTR1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/22264484) Fimasartan is an angiotensin II receptor antagonist employed in the treatment of both hypertension and heart failure. 2010-09-01 Korean Food and Drug Administration (KFDA)
Click to view olaparib Poly [ADP-ribose] polymerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P09874, gene: PARP1, swissprot: PARP1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Poly [ADP-ribose] polymerase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UGN5, gene: PARP2, swissprot: PARP2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Poly [ADP-ribose] polymerase 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y6F1, gene: PARP3, swissprot: PARP3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Cytochrome P450 2B6 (Organism: Homo sapiens, class: Enzyme, accessions: P20813, gene: CYP2B6, swissprot: CP2B6_HUMAN) inducer Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inducer Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) inhibitor UDP-glucuronosyltransferase 1-1 (Organism: Homo sapiens, class: Enzyme, accessions: P22309, gene: UGT1A1, swissprot: UD11_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Solute carrier family 22 member 1 (Organism: Homo sapiens, class: Transporter, accessions: O15245, gene: SLC22A1, swissprot: S22A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Solute carrier family 22 member 8 (Organism: Homo sapiens, class: Transporter, accessions: Q8TCC7, gene: SLC22A8, swissprot: S22A8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Multidrug and toxin extrusion protein 1 (Organism: Homo sapiens, class: Transporter, accessions: Q96FL8, gene: SLC47A1, swissprot: S47A1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Multidrug and toxin extrusion protein 2 (Organism: Homo sapiens, class: Transporter, accessions: Q86VL8, gene: SLC47A2, swissprot: S47A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/206162s011lbl.pdf) Tankyrase-1 (Organism: Homo sapiens, class: Enzyme, accessions: O95271, gene: TNKS, swissprot: TNKS1_HUMAN) (Source: https://www.ncbi.nlm.nih.gov/pubmed/26546219) Tankyrase-2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9H2K2, gene: TNKS2, swissprot: TNKS2_HUMAN) (Source: https://www.ncbi.nlm.nih.gov/pubmed/26546219) Poly [ADP-ribose] polymerase 6 (Organism: Homo sapiens, class: Enzyme, accessions: Q2NL67, gene: PARP6, swissprot: PARP6_HUMAN) (Source: https://www.ncbi.nlm.nih.gov/pubmed/26546219) Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. PARP enzymes are involved in normal cellular homeostasis, such as DNA transcription, cell cycle regulation, and DNA repair. Olaparib has been shown to inhibit growth of select tumor cell lines in vitro and decrease tumor growth in mouse xenograft models of human cancer both as monotherapy or following platinum-based chemotherapy. Increased cytotoxicity and anti-tumor activity following treatment with olaparib were noted in cell lines and mouse tumor models with deficiencies in BRCA. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complex, resulting in disruption of cellular homeostasis and cell death. Olaparib is indicated for treatment of gBRCA-mutated advanced ovarian cancer. Poly(ADP-Ribose) Polymerase Inhibitor (Code: N0000191623) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Poly(ADP-ribose) Polymerase Inhibitors (Code: D000067856) antineoplastic agent (Code: CHEBI:35610) 2014-10-23 EMA 09L
Click to view paritaprevir inhibits HCV NS3 protease antiviral drug (Code: CHEBI:36044) HCV NS3/4A Protease Inhibitors (Code: N0000182638) Hepatitis C Virus NS3/4A Protease Inhibitor (Code: N0000182639) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) UGT1A1 Inhibitors (Code: N0000191272) P-Glycoprotein Inhibitors (Code: N0000185503) 2014-11-20 EMA
Click to view dasabuvir Dasabuvir is a non-nucleoside inhibitor of the HCV RNA-dependent RNA polymerase encoded by the NS5B gene, which is essential for replication of the viral genome. In a biochemical assay, dasabuvir inhibited a panel of genotype 1a and 1b NS5B polymerases. Based on drug resistance mapping studies of HCV genotypes 1a and 1b, dasabuvir targets the palm domain of the NS5B polymerase, and is therefore referred to as a non-nucleoside NS5B-palm polymerase inhibitor. Hepatitis C Virus Non-Nucleoside NS5B Palm Polymerase Inhibitor (Code: N0000191257) RNA Replicase Inhibitors (Code: N0000191258) UGT1A1 Inhibitors (Code: N0000191272) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) antiviral drug (Code: CHEBI:36044) 2014-11-20 EMA
Click to view alectinib Proto-oncogene tyrosine-protein kinase receptor Ret (Organism: Homo sapiens, class: Kinase, accessions: P07949, gene: RET, swissprot: RET_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208434s000lbl.pdf) ALK tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: Q9UM73, gene: ALK, swissprot: ALK_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208434s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208434s004lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208434s000lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/208434s000lbl.pdf) Alectinib is a tyrosine kinase inhibitor that targets ALK and RET. In nonclinical studies, alectinib inhibited ALK phosphorylation and ALK-mediated activation of the downstream signaling proteins STAT3 and AKT, and decreased tumor cell viability in multiple cell lines harboring ALK fusions, amplifications, or activating mutations. The major active metabolite of alectinib, M4, showed similar in vitro potency and activity. Alectinib is indicated for the treatment of patients with ALK-positive metastatic non-small cell lung cancer. Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) antineoplastic agent (Code: CHEBI:35610) 2014-07-04 PMDA EMH
Click to view ripasudil Rho-associated protein kinase 2 (Organism: Homo sapiens, class: Kinase, accessions: O75116, gene: ROCK2, swissprot: ROCK2_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/25414122) Rho-associated protein kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q13464, gene: ROCK1, swissprot: ROCK1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/25414122) Rho-associated kinase inhibitor for the treatment of glaucoma and ocular hypertension 2014-09-26 PMDA
Click to view vaniprevir Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20163176) Genome polyprotein (Organism: Hepatitis C virus genotype 2a (isolate JFH-1), class: Polyprotein, accessions: Q99IB8, gene: None, swissprot: POLG_HCVJF) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/20163176) Cathepsin S (Organism: Homo sapiens, class: Enzyme, accessions: P25774, gene: CTSS, swissprot: CATS_HUMAN Nonstructural protein NS3-4A (Organism: Hepatitis C virus, class: Unclassified, accessions: A0A0K1CY61, gene: None, swissprot: A0A0K1CY61_9HEPC inhibits hepatitis C virus NS3/4a protease 2014-09-26 PMDA
Click to view vonoprazan Potassium-transporting ATPase (Organism: Homo sapiens, class: Transporter, accessions: P20648|P51164, gene: ATP4A|ATP4B, swissprot: ATP4A_HUMAN|ATP4B_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/21828261) a potassium-competitive proton pump blocker for the treatment of acid-related disorders 2014-12-26 PMDA HKT
Click to view mirodenafil cGMP-specific 3',5'-cyclic phosphodiesterase (Organism: Homo sapiens, class: Enzyme, accessions: O76074, gene: PDE5A, swissprot: PDE5A_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/18638004) phosphodiesterase type V inhibitor Enzyme Inhibitors (Code: D004791) Phosphodiesterase 5 Inhibitors (Code: D058986) Phosphodiesterase Inhibitors (Code: D010726) 2007-07-18 Korean Food and Drug Administration (KFDA)
Click to view cariprazine D(3) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P35462, gene: DRD3, swissprot: DRD3_HUMAN) partial agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/20093397) D(2) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P14416, gene: DRD2, swissprot: DRD2_HUMAN) partial agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) partial agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf) 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) antagonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/204370lbl.pdf) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/20093397) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/20093397) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) Histamine H1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P35367, gene: HRH1, swissprot: HRH1_HUMAN) antagonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/20093397) Alpha-1D adrenergic receptor (Organism: Homo sapiens, class: GPCR, accessions: P25100, gene: ADRA1D, swissprot: ADA1D_HUMAN) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN D(3) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P19020, gene: Drd3, swissprot: DRD3_RAT D(2) dopamine receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P61169, gene: Drd2, swissprot: DRD2_RAT The efficacy of cariprazine could be mediated through a combination of partial agonist activity at central dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at serotonin 5-HT2A receptors. Antipsychotic Agents (Code: D014150) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) Psychotropic Drugs (Code: D011619) Tranquilizing Agents (Code: D014149) dopamine agonist (Code: CHEBI:51065) second generation antipsychotic (Code: CHEBI:65191) serotonergic antagonist (Code: CHEBI:48279) Atypical Antipsychotic (Code: N0000175430) 2015-09-17 FDA
Click to view ozenoxacin Ozenoxacin is a quinolone antimicrobial drug. The mechanism of action involves the inhibition of bacterial DNA replication enzymes, DNA gyrase A and topoisomerase IV. Ozenoxacin has been shown to be bactericidal against S. aureus and S. pyogenes organisms. Ozenoxacin is used as topical treatment for impetigo and other infectious dermatological conditions. Quinolone Antimicrobial (Code: N0000175937) Quinolones (Code: N0000007606) 2015-09-28 PMDA
Click to view lusutrombopag Thrombopoietin receptor (Organism: Homo sapiens, class: Membrane receptor, accessions: P40238, gene: MPL, swissprot: TPOR_HUMAN) agonist (Source: http://dx.doi.org/10.1016/S0168-8278(14)61094-1) a thrombopoietin receptor agonist 2015-09-28 PMDA
Click to view osimertinib Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) Receptor tyrosine-protein kinase erbB-2 (Organism: Homo sapiens, class: Kinase, accessions: P04626, gene: ERBB2, swissprot: ERBB2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) Receptor tyrosine-protein kinase erbB-3 (Organism: Homo sapiens, class: Kinase, accessions: P21860, gene: ERBB3, swissprot: ERBB3_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) Receptor tyrosine-protein kinase erbB-4 (Organism: Homo sapiens, class: Kinase, accessions: Q15303, gene: ERBB4, swissprot: ERBB4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) Activated CDC42 kinase 1 (Organism: Homo sapiens, class: Kinase, accessions: Q07912, gene: TNK2, swissprot: ACK1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) Tyrosine-protein kinase Blk (Organism: Homo sapiens, class: Kinase, accessions: P51451, gene: BLK, swissprot: BLK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) Cytochrome P450 3A (Organism: Homo sapiens, class: Enzyme, accessions: Q9HB55|P08684|P20815|P24462, gene: CYP3A43|CYP3A4|CYP3A5|CYP3A7, swissprot: CP343_HUMAN|CP3A4_HUMAN|CP3A5_HUMAN|CP3A7_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208065s011lbl.pdf) Potassium voltage-gated channel subfamily H member 2 (Organism: Homo sapiens, class: Ion channel, accessions: Q12809, gene: KCNH2, swissprot: KCNH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25271963) Osimertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR), which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletion) at approximately 9-fold lower concentrations than wild-type. In cultured cells and animal tumor implantation models, osimertinib exhibited anti-tumor activity against NSCLC lines harboring EGFR-mutations (T790M/L858R, L858R, T790M/exon 19 deletion, and exon 19 deletion) and, to a lesser extent, wild-type EGFR amplifications. Its use is indicated for the treatment of metastatic non-small cell lung cancer (NSCLC) in cases where tumour EGFR expression is positive for the T790M mutation. Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) Cytochrome P450 3A Inhibitors (Code: N0000190114) Cytochrome P450 3A4 Inducers (Code: N0000185506) Cytochrome P450 1A2 Inducers (Code: N0000191266) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Protein Kinase Inhibitors (Code: D047428) 2015-11-13 FDA YY3
Click to view lesinurad Solute carrier family 22 member 12 (Organism: Homo sapiens, class: Transporter, accessions: Q96S37, gene: SLC22A12, swissprot: S22AC_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207988lbl.pdf) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207988lbl.pdf) Lesinurad reduces serum uric acid levels by inhibiting the function of transporter proteins involved in uric acid reabsorption in the kidney. Lesinurad inhibited the function of two apical transporters responsible for uric acid reabsorption, uric acid transporter 1 (URAT1) and organic anion transporter 4 (OAT4), with IC50 values of 7.3 and 3.7 ??M, respectively. URAT1 is responsible for the majority of the reabsorption of filtered uric acid from the renal tubular lumen. OAT4 is a uric acid transporter associated with diuretic-induced hyperuricemia. Urate Transporter 1 Inhibitor (Code: N0000192341) Urate Transporter 1 Inhibitors (Code: N0000192340) Cytochrome P450 3A Inducers (Code: N0000190118) Antirheumatic Agents (Code: D018501) Gout Suppressants (Code: D006074) Renal Agents (Code: D012076) Uricosuric Agents (Code: D014528) uricosuric drug (Code: CHEBI:35841) 2016-02-18 EMA 2015-12-22 FDA
Click to view selexipag Prostacyclin receptor (Organism: Homo sapiens, class: GPCR, accessions: P43119, gene: PTGIR, swissprot: PI2R_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207947s000lbl.pdf) Prostacyclin receptor (Organism: Rattus norvegicus, class: Unclassified, accessions: P43253, gene: Ptgir, swissprot: PI2R_RAT) agonist (Source: ) an oral prostacyclin receptor (IP receptor) agonist that is structurally distinct from prostacyclin, indicated for the treatment of pulmonary arterial hypertension, selexipag is hydrolyzed by carboxylesterase 1 to yield its active metabolite, which is approximately 37-fold as potent as selexipag, selexipag and the active metabolite are selective for the IP receptor versus other prostanoid receptors (EP1-4, DP, FP and TP) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) orphan drug (Code: CHEBI:71031) platelet aggregation inhibitor (Code: CHEBI:50427) vasodilator agent (Code: CHEBI:35620) prodrug (Code: CHEBI:50266) Prostacyclin Receptor Agonist (Code: N0000192339) Prostacyclin Receptor Agonists (Code: N0000020068) 2015-12-21 FDA
Click to view lobeglitazone Peroxisome proliferator-activated receptor gamma (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P37231, gene: PPARG, swissprot: PPARG_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/22047812) Peroxisome proliferator-activated receptor alpha (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: Q07869, gene: PPARA, swissprot: PPARA_HUMAN) agonist (Source: http://www.ncbi.nlm.nih.gov/pubmed/22047812) putative antidiabetic agent for type 2 diabetes 2013-07-04 Korean Food and Drug Administration (KFDA) 8LX
Click to view nemonoxacin Streptococcus pneumoniae (Organism: None, class: Bacteria, accessions: None, gene: None, swissprot: None) minimum inhibitory concentration (Source: http://www.ncbi.nlm.nih.gov/pubmed/19833635) Staphylococcus aureus subsp. aureus (Organism: None, class: Bacteria, accessions: None, gene: None, swissprot: None) minimum inhibitory concentration (Source: http://www.ncbi.nlm.nih.gov/pubmed/19833635) has antibacterial activity
Click to view arterolane Arterolane is an anti-malarial drug. Arterolane belongs to peroxidic antimalarial compounds. Upon administration, the drug is activated by heme of hemoglobin digested by malarial parasite. Activation produces free radicals, leading to alkylation of heme and proteins, critical for the survival of the parasite. Arterolane is used for the treatment of malaria. 2012-03-09 CDSCO (INDIA)
Click to view hydracarbazine Hydracarbazine is a hydrazinopyridazine-based diuretic with antihypertensive activity. Hydracarbazine is no longer marketed.
Click to view cytisine Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11553677) Neuronal acetylcholine receptor; alpha4/beta2 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P17787, gene: CHRNA4|CHRNB2, swissprot: ACHA4_HUMAN|ACHB2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11553677) Neuronal acetylcholine receptor; alpha4/beta4 (Organism: Homo sapiens, class: Ion channel, accessions: P43681|P30926, gene: CHRNA4|CHRNB4, swissprot: ACHA4_HUMAN|ACHB4_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11553677) Cytisine is an alkaloid naturally derived from the Fabaceae family of plants including the genera Laburnum and Cytisus. Cytisine is an acetylcholine agonist, it is widely used throughout Eastern Europe as an aid to giving up smoking. nicotinic acetylcholine receptor agonist (Code: CHEBI:47958) 2002-11-06 Bulgarian Drug Agency (BDA) C5E
Click to view valbenazine Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209241lbl.pdf) Synaptic vesicular amine transporter (Organism: Rattus norvegicus, class: Transporter, accessions: Q01827, gene: Slc18a2, swissprot: VMAT2_RAT) inhibitor (Source: ) The mechanism of action of valbenazine in the treatment of tardive dyskinesia is unknown, but is thought to be mediated through the reversible inhibition of vesicular monoamine transporter 2 (VMAT2), a transporter that regulates monoamine uptake from the cytoplasm to the synaptic vesicle for storage and release. Vesicular Monoamine Transporter 2 Inhibitor (Code: N0000190856) Vesicular Monoamine Transporter 2 Inhibitors (Code: N0000190855) 2017-04-11 FDA
Click to view plecanatide Heat-stable enterotoxin receptor (Organism: Homo sapiens, class: Enzyme, accessions: P25092, gene: GUCY2C, swissprot: GUC2C_HUMAN) agonist (Source: http://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208745lbl.pdf) Tumor necrosis factor (Organism: Homo sapiens, class: Cytokine, accessions: P01375, gene: TNF, swissprot: TNFA_HUMAN Plecanatide is structurally related to human uroguanylin, and similar to uroguanylin, plecanatide functions as a guanylate cyclase-C (GC-C) agonist. Both plecanatide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation of intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit. Enzyme Activators (Code: D020536) Gastrointestinal Agents (Code: D005765) Guanylyl Cyclase C Agonists (Code: D000074268) Guanylate Cyclase-C Agonist (Code: N0000185500) Guanylate Cyclase Activators (Code: N0000185499) 2017-01-19 FDA
Click to view niraparib Poly [ADP-ribose] polymerase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P09874, gene: PARP1, swissprot: PARP1_HUMAN) inhibitor (Source: ) Poly [ADP-ribose] polymerase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UGN5, gene: PARP2, swissprot: PARP2_HUMAN) inhibitor (Source: ) Tankyrase-1 (Organism: Homo sapiens, class: Enzyme, accessions: O95271, gene: TNKS, swissprot: TNKS1_HUMAN Poly [ADP-ribose] polymerase 4 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UKK3, gene: PARP4, swissprot: PARP4_HUMAN Poly [ADP-ribose] polymerase 3 (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y6F1, gene: PARP3, swissprot: PARP3_HUMAN Niraparib is an inhibitor of poly(ADP-ribose) polymerase (PARP) enzymes, PARP-1 and PARP-2, which play a role in DNA repair. In vitro studies have shown that niraparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis and cell death. Increased niraparib-induced cytotoxicity was observed in tumor cell lines with or without deficiencies in BRCA1/2. Niraparib decreased tumor growth in mouse xenograft models of human cancer cell lines with deficiencies in BRCA1/2 and in human patient-derived xenograft tumor models with homologous recombination deficiency that had either mutated or wild type BRCA1/2. Antineoplastic Agents (Code: D000970) Enzyme Inhibitors (Code: D004791) Poly(ADP-ribose) Polymerase Inhibitors (Code: D000067856) Poly(ADP-Ribose) Polymerase Inhibitor (Code: N0000191623) 2017-03-27 FDA 3JD
Click to view abaloparatide Parathyroid hormone/parathyroid hormone-related peptide receptor (Organism: Homo sapiens, class: GPCR, accessions: Q03431, gene: PTH1R, swissprot: PTH1R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208743lbl.pdf) Abaloparatide is a PTHrP(1-34) analog which acts as an agonist at the PTH1 receptor (PTH1R). This results in activation of the cAMP signaling pathway in target cells. In rats and monkeys, abaloparatide had an anabolic effect on bone, demonstrated by increases in BMD and bone mineral content (BMC) that correlated with increases in bone strength at vertebral and/or nonvertebral sites. Parathyroid Hormone-Related Peptide Analog (Code: N0000193453) Parathyroid Hormone-Related Protein (Code: N0000170963) Analogs/Derivatives (Code: N0000175452) Bone Density Conservation Agents (Code: D050071) 2017-04-28 FDA
Click to view brigatinib ALK tyrosine kinase receptor (Organism: Homo sapiens, class: Kinase, accessions: Q9UM73, gene: ALK, swissprot: ALK_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208772lbl.pdf) Proto-oncogene tyrosine-protein kinase ROS (Organism: Homo sapiens, class: Kinase, accessions: P08922, gene: ROS1, swissprot: ROS1_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/27780853) Receptor-type tyrosine-protein kinase FLT3 (Organism: Homo sapiens, class: Kinase, accessions: P36888, gene: FLT3, swissprot: FLT3_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/27780853) Epidermal growth factor receptor (Organism: Homo sapiens, class: Kinase, accessions: P00533, gene: EGFR, swissprot: EGFR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/27780853) Insulin-like growth factor 1 receptor (Organism: Homo sapiens, class: Kinase, accessions: P08069, gene: IGF1R, swissprot: IGF1R_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/27780853) Insulin receptor (Organism: Homo sapiens, class: Kinase, accessions: P06213, gene: INSR, swissprot: INSR_HUMAN) inhibitor (Source: http://www.ncbi.nlm.nih.gov/pubmed/27780853) Brigatinib is a tyrosine kinase inhibitor with in vitro activity at clinically achievable concentrations against multiple kinases including ALK, ROS1, insulin-like growth factor-1 receptor (IGF-1R), and FLT-3 as well as EGFR deletion and point mutations. Brigatinib inhibited autophosphorylation of ALK and ALK-mediated phosphorylation of the downstream signaling proteins STAT3, AKT, ERK1/2, and S6 in in vitro and in vivo assays. Brigatinib also inhibited the in vitro proliferation of cell lines expressing EML4-ALK and NPM-ALK fusion proteins and demonstrated dose-dependent inhibition of EML4-ALK-positive NSCLC xenograft growth in mice. At clinically achievable concentrations (<= 500 nM), brigatinib inhibited the in vitro viability of cells expressing EML4-ALK and 17 mutant forms associated with resistance to ALK inhibitors including crizotinib, as well as EGFR-Del (E746-A750), ROS1-L2026M, FLT3-F691L, and FLT3-D835Y. Brigatinib exhibited in vivo anti-tumor activity against 4 mutant forms of EML4-ALK, including G1202R and L1196M mutants identified in NSCLC tumors in patients who have progressed on crizotinib. Brigatinib also reduced tumor burden and prolonged survival in mice implanted intracranially with an ALK-driven tumor cell line. Kinase Inhibitor (Code: N0000175605) Tyrosine Kinase Inhibitors (Code: N0000020001) Cytochrome P450 3A Inducers (Code: N0000190118) 2017-04-28 FDA 6GY
Click to view voxilaprevir Genome polyprotein (Organism: Hepatitis C virus genotype 1b (isolate BK), class: Polyprotein, accessions: P26663, gene: None, swissprot: POLG_HCVBK) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209195s000lbl.pdf) Genome polyprotein (Organism: Hepatitis C virus genotype 3a (isolate k3a) (HCV), class: Polyprotein, accessions: Q81495, gene: None, swissprot: POLG_HCVK3) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209195s000lbl.pdf) Voxilaprevir is a noncovalent, reversible inhibitor of the NS3/4A protease, which is necessary for the proteolytic cleavage of the HCV encoded polyprotein (into mature forms of the NS3, NS4A, NS4B, NS5A, and NS5B proteins) and is essential for viral replication. In a biochemical inhibition assay, voxilaprevir inhibited the proteolytic activity of recombinant NS3/4A enzymes from clinical isolates of HCV genotypes 1b and 3a with Ki values of 38 and 66 pM, respectively. Hepatitis C Virus NS3/4A Protease Inhibitor (Code: N0000182639) HCV NS3/4A Protease Inhibitors (Code: N0000182638) P-Glycoprotein Inhibitors (Code: N0000185503) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) 2017-07-18 FDA
Click to view glecaprevir Glecaprevir is an inhibitor of the HCV NS3/4A protease, which is necessary for the proteolytic cleavage of the HCV encoded polyprotein (into mature forms of the NS3, NS4A, NS4B, NS5A, and NS5B proteins) and is essential for viral replication. In a biochemical assay, glecaprevir inhibited the proteolytic activity of recombinant NS3/4A enzymes from clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a with IC50 values ranging from 3.5 to 11.3 nM. Hepatitis C Virus NS3/4A Protease Inhibitor (Code: N0000182639) HCV NS3/4A Protease Inhibitors (Code: N0000182638) P-Glycoprotein Inhibitors (Code: N0000185503) Breast Cancer Resistance Protein Inhibitors (Code: N0000190113) Organic Anion Transporting Polypeptide 1B1 Inhibitors (Code: N0000190107) Organic Anion Transporting Polypeptide 1B3 Inhibitors (Code: N0000190108) Cytochrome P450 3A Inhibitors (Code: N0000190114) Cytochrome P450 1A2 Inhibitors (Code: N0000182138) UGT1A1 Inhibitors (Code: N0000191272) 2017-07-26 EMA
Click to view butylphthalide Potassium channel subfamily K member 2 (Organism: Homo sapiens, class: Ion channel, accessions: O95069, gene: KCNK2, swissprot: KCNK2_HUMAN) blocker (Source: http://www.ncbi.nlm.nih.gov/pubmed/21293470) 3-N-Butylphthalide (NBP) is a compound found in Chinese celery seed extracts that can improve cognitive functions and may decrease Amyloid-beta levels in Alzheimer???s disease. NBP has antioxidant activities and may protect against oxidative/nitrosative stress, mitochondrial impairment and apoptosis. 2002-09-30 China Food and Drug Administration (CFDA)
Click to view halothane Potassium channel subfamily K member 12 (Organism: Homo sapiens, class: Ion channel, accessions: Q9HB15, gene: KCNK12, swissprot: KCNKC_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25148687) Potassium channel subfamily K member 13 (Organism: Homo sapiens, class: Ion channel, accessions: Q9HB14, gene: KCNK13, swissprot: KCNKD_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/25148687) Potassium channel subfamily K member 5 (Organism: Homo sapiens, class: Ion channel, accessions: O95279, gene: KCNK5, swissprot: KCNK5_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10839924) Potassium channel subfamily K member 3 (Organism: Homo sapiens, class: Ion channel, accessions: O14649, gene: KCNK3, swissprot: KCNK3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/11886861) Potassium channel subfamily K member 9 (Organism: Homo sapiens, class: Ion channel, accessions: Q9NPC2, gene: KCNK9, swissprot: KCNK9_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/11886861) Potassium channel subfamily K member 10 (Organism: Homo sapiens, class: Ion channel, accessions: P57789, gene: KCNK10, swissprot: KCNKA_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/10880510) Cytochrome P450 2A6 (Organism: Homo sapiens, class: Enzyme, accessions: P11509, gene: CYP2A6, swissprot: CP2A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9103523) Cytochrome P450 2E1 (Organism: Homo sapiens, class: Enzyme, accessions: P05181, gene: CYP2E1, swissprot: CP2E1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/9103523) Calcium-activated potassium channel subunit alpha-1 (Organism: Homo sapiens, class: Ion channel, accessions: Q12791, gene: KCNMA1, swissprot: KCMA1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/10794813) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8886607) Halothane is an inhalation anesthetic. It does not increase the production of saliva which can be particularly useful in those who are difficult to intubate. Side effects include an irregular heartbeat, decreased effort to breath (respiratory depression), and liver problems. It should not be used in people with porphyria or a history of malignant hyperthermia either in themselves or their family members. Halothane is used for the induction and maintenance of general anesthesia. inhalation anaesthetic (Code: CHEBI:38870) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Inhalation (Code: D018685) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) 1958-03-12 FDA HLT
Click to view abemaciclib Cyclin-dependent kinase 4 (Organism: Homo sapiens, class: Kinase, accessions: P11802, gene: CDK4, swissprot: CDK4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208716Orig1s000lbl.pdf) Cyclin-dependent kinase 6 (Organism: Homo sapiens, class: Kinase, accessions: Q00534, gene: CDK6, swissprot: CDK6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208716Orig1s000lbl.pdf) Abemaciclib is an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases are activated upon binding to D-cyclins. In estrogen receptor-positive (ER+) breast cancer cell lines, cyclin D1 and CDK4/6 promote phosphorylation of the retinoblastoma protein (Rb), cell cycle progression, and cell proliferation. In vitro, continuous exposure to abemaciclib inhibited Rb phosphorylation and blocked progression from G1 into S phase of the cell cycle, resulting in senescence and apoptosis. In breast cancer xenograft models, abemaciclib dosed daily without interruption as a single agent or in combination with antiestrogens resulted in reduction of tumor size. Kinase Inhibitor (Code: N0000175605) Kinase Inhibitors (Code: N0000175082) 2017-09-28 FDA 6ZV
Click to view semaglutide Glucagon-like peptide 1 receptor (Organism: Homo sapiens, class: GPCR, accessions: P43220, gene: GLP1R, swissprot: GLP1R_HUMAN) agonist (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209637lbl.pdf) Semaglutide is a GLP-1 analogue with 94% sequence homology to human GLP-1. Semaglutide acts as a GLP-1 receptor agonist that selectively binds to and activates the GLP-1 receptor, the target for native GLP-1. GLP-1 is a physiological hormone that has multiple actions on glucose, mediated by the GLP-1 receptors. The principal mechanism of protraction resulting in the long half-life of semaglutide is albumin binding, which results in decreased renal clearance and protection from metabolic degradation. Furthermore, semaglutide is stabilized against degradation by the DPP-4 enzyme. Semaglutide reduces blood glucose through a mechanism where it stimulates insulin secretion and lowers glucagon secretion, both in a glucose-dependent manner. Thus, when blood glucose is high, insulin secretion is stimulated and glucagon secretion is inhibited. The mechanism of blood glucose lowering also involves a minor delay in gastric emptying in the early postprandial phase. GLP-1 Receptor Agonist (Code: N0000178480) Glucagon-Like Peptide 1 (Code: N0000170335) Glucagon-like Peptide-1 (GLP-1) Agonists (Code: N0000020058) 2017-12-05 FDA
Click to view guaiazulen Cytochrome P450 1A2 (Organism: Rattus norvegicus, class: Enzyme, accessions: P04799, gene: Cyp1a2, swissprot: CP1A2_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9112807) Guaiazulen is a sesquiterpene. It is a derivative of azulene. Guaiazulen is a cosmetic color additive. Guaiazulene is used in the formulation of bath products, cleansing products, depilatories, hair bleaches, hair conditioners, hair dyes and colors, hair straighteners, permanent waves, skin care products and skin fresheners. Guaiazulen has antioxidant, antifungal, antimicrobial, anti-inflammatory, anti-spasmodic, anti-ulcer, antitumoral activities and relaxant properties. Guaiazulen is used for the treatment of minor eye injuries and eczema. Also it is used as sodium gualenate hydrate for the treatment of pharyngitis, tonsillitis, stomatitis, acute gingivitis, glossitis and oral wounds. 1969-09-01 State Institute for Drug Control (SUKL) Czech Republic
Click to view hexamethonium Hexamethonium is a nicotinic cholinergic antagonist often referred to as the prototypical ganglionic blocker. It was used forthe treatment of hypertension but, like the other ganglionic blockers, it has been replaced by more specific drugs for most purposes, although it is widely used a research tool. Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Cholinergic Agents (Code: D018678) Cholinergic Antagonists (Code: D018680) Ganglionic Blockers (Code: D005730) Neurotransmitter Agents (Code: D018377) Nicotinic Antagonists (Code: D018733) Peripheral Nervous System Agents (Code: D018373)
Click to view hexafluronium Cholinesterase (Organism: Homo sapiens, class: Enzyme, accessions: P06276, gene: BCHE, swissprot: CHLE_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/948350) Hexafluronium is a quaternary ammonium salt. Hexafluorenium inhibits the enzyme cholinesterase in the plasms, but apparently not at the neuromuscular juntion. It also has some nondepolarizing activity (tubocurarine-like) at the postjunctional membrane. In man hexafluorenium potentiates the muscle relaxant effects of succinylcholine. As such, smaller doses of succinylcholine are required and fewer side effects like fasciculations, twitching and postoperative muscle pain are experienced. 1955 FDA
Click to view chloroform Chloroform is a colorless liquid with a pleasant, nonirritating odor and a slightly sweet taste. It was previously used as an anesthetic, but was banned from use due to its suspected carcinogenicity. Today, chloroform is used to make other chemicals and can also be formed in small amounts when chlorine is added to water. Other names for chloroform are trichloromethane and methyl trichloride. Solvents (Code: D012997) refrigerant (Code: CHEBI:78433) central nervous system drug (Code: CHEBI:35470) inhalation anaesthetic (Code: CHEBI:38870) MCH
Click to view iodoform Iodoform is an organoiodine compound. Due to its antimicrobial properties iodoform is used as an antiseptic wound powder. Iodoform is also used in dental paste, root canal filling materials and as radiopacifier for primary tooth root canal fllling, but its use in endodontics is controversial because of its potential for causing toxic effects. 1973-12-31 Health Canada
Click to view lycopene Lycopene is the fat-soluble pigment that gives tomatoes, watermelon, pink grapefruit, and other foods their red color. Bioavailability of lycopene is enhanced in the presence of lipids and thermal processing. Lycopene is a tetraterpene assembled from eight isoprene units that are solely composed of carbon and hydrogen. Lycopene may undergo extensive isomerization that allows 1056 theoretical cis-trans configurations; however the all-trans configuration of lycopene is the most predominant isomer found in foods that gives the red hue. Lycopene is a non-essential human nutrient that is classified as a non-provitamin A carotenoid pigment since it lacks a terminal beta ionone ring and does not mediate vitamin A activity. However lycopene is a potent antioxidant molecule that scavenges reactive oxygen species (ROS) singlet oxygen. Anticarcinogenic Agents (Code: D016588) Antineoplastic Agents (Code: D000970) Antioxidants (Code: D000975) Protective Agents (Code: D020011) Radiation-Protective Agents (Code: D011837) LYC
Click to view perflenapent Perflenapent is a fluorocarbon-based ultrasound contrast agent which has been approved as a transpulmonary echocardiographic contrast agent for use in patients with suspected or established cardiovascular disease who have had previous inconclusive non-contrast studies. Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) radioopaque medium (Code: CHEBI:37338)
Click to view 1-Chlormethyl-2,8,9-trioxa-5-aza-1-silabicyclo[3.3.3] undecanum 1-Chlormethyl-2,8,9-trioxa-5-aza-1-silabicyclo[3.3.3] undecanum (Chloromethylsilatrane) is a silicon organic compound. It stimulates of hair growth which is manifested by an increase in permeability of connective tissues, blood vessels and hair follicles in skin at the site of drug application. It is used for the treatment of alopecia. Also chloromethylsilatrane is used in agriculture as a broad-spectrum plants growth regulator. 2011-07-19 Ministry of Health of the Russian Federation
Click to view azamethonium bromide Azamethonium is a substance with the ganglia-blocking effect. It is used for the treatment of acute pulmonary embolism and hypertension. Also it is used for the induction of hypotension in surgery. 1970-08-04 Ministry of Health of the Russian Federation
Click to view alclometasone Alclometasone is synthetic glucocorticoid steroid for topical use in dermatology as anti-inflammatory, antipruritic, antiallergic, antiproliferative and vasoconstrictive agent. The mechanism of the anti-inflammatory activity of the topical steroids, in general, is unclear. Alclometasone is indicated for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Italian Medicines Agency (AIFA)
Click to view aminophylline Aminophylline is a drug combination that contains theophylline and ethylenediamine in a 2:1 ratio. It is used for the treatment of chronic obstructive pulmonary disease, such as asthma and emphysema. (See: theophylline) 1964-04-30 Ministry of Health of the Russian Federation
Click to view anabasine Aromatase (Organism: Homo sapiens, class: Enzyme, accessions: P11511, gene: CYP19A1, swissprot: CP19A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/3711333) Anabasine is a pyridine and piperidine alkaloid found in the Solanaceae plant Nicotiana glauca that is a close relative to Nicotiana tabacum, historically used as an insecticide. Now it is used for the assistance of smoking cessation. 1986-08-14 Ministry of Public Health USSR
Click to view aspartame Transient receptor potential cation channel subfamily V member 1 (Organism: Homo sapiens, class: Ion channel, accessions: Q8NER1, gene: TRPV1, swissprot: TRPV1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/17567713) Solute carrier family 22 member 11 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSA0, gene: SLC22A11, swissprot: S22AB_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/12063169) Aspartame (L-alpha-aspartyl-L-phenylalanine methyl ester) is a low-calorie sweetener used to sweeten a wide variety of low- and reduced-calorie foods and beverages, including low-calorie tabletop sweeteners. Aspartame is composed of two amino acids, aspartic acid and phenylalanine, as the methyl ester. Aspartic acid and phenylalanine are also found naturally in protein containing foods, including meats, grains and dairy products. Methyl esters are also found naturally in many foods such as fruits and vegetable and their juices. Upon digestion, aspartame breaks down into three components (aspartic acid, phenylalanine and methanol), which are then absorbed into the blood and used in normal body processes. (See: aspartic acid) (See: phenylalanine) 2006-09-15 Ministry of Health of the Russian Federation PME
Click to view atracurium besylate Atracurium besylate is the bisbenzenesulfonate salt of atracurium. It is used for the skeletal muscle relaxation during general anesthesia. (See: atracurium) Atracurium Besylate: 1983-11-23 FDA Cisatracurium Besylate: 1995-12-15 FDA
Click to view auranofin An oral chrysotherapeutic agent for the treatment of rheumatoid arthritis. Its exact mechanism of action is unknown, but it is believed to act via immunological mechanisms and alteration of lysosomal enzyme activity. Its efficacy is slightly less than that of injected gold salts, but it is better tolerated, and side effects which occur are potentially less serious.
Click to view acetylaminosuccinic acid Acetylaminosuccinic acid is a synthetic analog of aspartic acid. Acetylaminosuccinic acid is used for the treatment of patients with asthenic conditions and fatigue, which is accompanied or not accompanied by a decrease in mood. Acetylaminosuccinic acid is recommended to appoint as an aid to patients receiving antidepressants. 2006-04-14 Ministry of Health of the Russian Federation
Click to view lysine acetylsalicylate Lysine acetylsalicylate is the lysine salt form of acetylsalicylic acid, a nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic and anti-inflammatory activities. In blood lysine acetylsalicylate is hydrolyzed to acetylsalicylic acid and lysine. (See: acetylsalicylic acid) (See: lysine) 1994-11-10 Ministry of Health of the Russian Federation
Click to view acetomepregenol Acetomepregenol is a progestin. Acetomepregenol is a prodrug of megestrol acetate. It is used for the treatment of menopausal and perimenopausal disorder and as a method of contraception in combination with an estrogen. (See: megestrol acetate) 1986-06-13 Ministry of Health of the Russian Federation
Click to view beclometasone Multidrug resistance protein 1 (Organism: Homo sapiens, class: Transporter, accessions: P08183, gene: ABCB1, swissprot: MDR1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/22464980) ATP-binding cassette sub-family G member 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9UNQ0, gene: ABCG2, swissprot: ABCG2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/15365089) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20448812) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/20448812) Beclomethasone is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, beclomethasone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production. Beclomethasone is indicated for the treatment of nasal symptoms associated with seasonal and perennial allergic rhinitis. Also it is used for the treatment of asthma.
Click to view benzathine benzylpenicillin Semisynthetic antibiotic prepared by combining the sodium salt of penicillin G with N,N'-dibenzylethylenediamine.
Click to view beta carotene Beta carotene is a carotenoid, weak antioxidant, precursor of vitamin A which can be found in many foods and is sold as a dietary supplement. Used to reduce the severity of photosensitivity reactions in patients with erythropoietic protoporphyria. It is used in high-dose antioxidant supplements containing ascorbic acid and vitamin E with zinc in high-risk patients with age-related macular degeneration. 1975 FDA BCR
Click to view betamecil Betamicil is the beta-form of 6-methyluracil. Betamicil is a stimulant of corneal repair regeneration. It is used as ointment for the treatment of keratitis and corneal degeneration. 1995-10-27 Ministry of Health of the Russian Federation
Click to view bleomycin A complex of related glycopeptide antibiotics from Streptomyces verticillus consisting of bleomycin A2 and B2. It inhibits DNA metabolism and is used as an antineoplastic, especially for solid tumors.
Click to view bonafton Bonafton (bromonaphthoquinone) is an antiviral drug used for the treatmrnt of herpesviral ocular disease, herpesviral gingivostomatitis and pharyngotonsillitis. Bonafton inhibitions of synthesis of cytoplasmatic proteins incorporated into the capsids. 1982-06-25 Ministry of Public Health USSR
Click to view butylated hydroxytoluene Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231207) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231207) Butylated hydroxytoluene (BHT) is an organic compound that is used in the food, cosmetic, and pharmaceutical industry as an antioxidant. BHT is a substituted derivative of phenol. BHT helps to prevent the formation of free radicals and oxidation. The ability of oral BHT to lead to cancer is a controversial topic, but most food industries have replaced it with butylated hydroxyanisole (BHA). It currently permits its use in concentrations of about 0.01% to 0.02% in most foods. Also it has been used for the treatment of burns, superficial frostbite and bladder cancer due to its ability to prevent the formation of free radicals and oxidation. 1999-06-11 Ministry of Health of the Russian Federation
Click to view butiroxan Butyroxan has peripheral and central adrenoblocking properties. It was used for the treatment of withdrawal syndrome, allergic dermatoses, hypertension. 1982-06-25 Ministry of Health of the Russian Federation
Click to view verteporfin Verteporfin is a light activated drug used in photodynamic therapy. Once verteporfin is activated by light in the presence of oxygen, highly reactive, short-lived singlet oxygen and reactive oxygen radicals are generated. Light activation of verteporfin results in local damage to neovascular endothelium, resulting in vessel occlusion. Verteporfin appears to somewhat preferentially accumulate in neovasculature, including choroidal neovasculature. Verteporfin is indicated for the treatment of patients with predominantly classic subfoveal choroidal neovascularization due to age-related macular degeneration, pathologic myopia or presumed ocular histoplasmosis. photosensitizing agent (Code: CHEBI:47868) antineoplastic agent (Code: CHEBI:35610) Photoenhancer (Code: N0000175540) Photoabsorption (Code: N0000010217) Photosensitizing Activity (Code: N0000009801) Dermatologic Agents (Code: D003879) Photosensitizing Agents (Code: D017319) Radiation-Sensitizing Agents (Code: D011838) 200-04-12 FDA
Click to view bismuthate tripotassium dicitrate Bismuthate tripotassium dicitrate is an anti-ulcer drug with bactericidal activity against Helicobacter pylori. In the acidic environment of the stomach it acts by causing coagulation at the base of the ulcer and thus protecting it and promoting healing. Bismuthate tripotassium dicitrate is used for the treatment of peptic ulcer and gastritis. 1984-08-27 Ministry of Health, Welfare and Sport (Netherlands)
Click to view gadobutrol Gadobutrol is indicated for use with magnetic resonance imaging (MRI) in adult and pediatric patients (including term neonates) to detect and visualize areas with disrupted blood brain barrier and/or abnormal vascularity of the central nervous system.
Click to view gadodiamide Gadodiamide is the formulation of the gadolinium complex of diethylenetriamine pentaacetic acid bismethylamide, and is an injectable, nonionic extracellular enhancing agent for magnetic resonance imaging. Gadodiamide is a paramagnetic agent with unpaired electron spins which generate a local magnetic field. Gadodiamide is used for diagnostic magnetic resonance imaging (MRI) to visualize lesions with abnormal vascularity in the brain, spine, and associated tissues, to facilitate the visualization of lesions with abnormal vascularity within the thoracic, abdominal, pelvic cavities, and the retroperitoneal space. Paramagnetic Contrast Agent (Code: N0000180184) Magnetic Resonance Contrast Activity (Code: N0000175862) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 1993-01-08 FDA
Click to view gadopentetic acid Gadopentetic acid is a complex of gadolinium with a chelating agent, diethylenetriamine penta-acetic acid. It is used for contrast enhancement in direct magnetic resonance arthrography. MRI contrast agent (Code: CHEBI:37335) 1993-03-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view halazone Halazone is a disinfectant with the general properties of chlorine. Halazone is similar to hipochlorite in its mode of action. Halazone is used to disinfect water for drinking and for antiseptic treatment hands and wounds. 1967-07-11 Ministry of Health of the Russian Federation
Click to view gidazepam Gidazepam is an anxiolytic and atypical benzodiazepine derivative. Gidazepam is a prodrug of desalkylgidazepam which has anxiolytic, antiepileptic and vegeto-stabilizing properties. It is used for the treatment of anxiety, alcohol withdrawal syndrome, phobias, insomnia and other neurotic disorders. 1992-07-24 Ministry of Health of the Russian Federation
Click to view hydroxymethylquinoxalindioxyde Hydroxymethylquinoxalindioxyde (dioxidine) is an antibacterial agent with a wide spectrum of activity. It also stimulates tissue regeneration, re-epithelization and facilitates wound healing processes. It has been show to be active against Proteus vulgaris, Pseudomonas aeruginosa, Escherichia coli, Shigella dysenteria spp., Shigella flexneri, Shigella boydii, Shigella sonnei, Salmonella spp., Klebsiella pneumoniae, Staphylococcus spp., Streptococcus spp., Clostridium perfringens. It is used for the treatment of skin and skin structure infections, joint infections, wound infections and respiratory tract infections. 1976-06-29 Ministry of Public Health USSR
Click to view hydroxyprogesterone Hydroxyprogesterone is a physiological progestin that is produced during glucocorticoid and steroid hormone synthesis and is increased during the third trimester of pregnancy. Hydroxyprogesterone binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression. 1997-09-25 ANSM (French National Agency for Medicines and Health Products Safety) 3QZ
Click to view hyoscine butylbromide Hyoscine butylbromide is an orally available bromide salt form of butylscopolamine, a quaternary ammonium derivative of the alkaloid scopolamine, with anticholinergic property. It is a natural substance extracted from Duboisia plant species as Scopolamine (hyoscine). Hyoscine butylbromide has a high affinity for muscarinic receptors located on the smooth-muscle cells of the GI tract. Its anticholinergic action exerts a smooth-muscle relaxing/spasmolytic effect. Hyoscine butylbromide is used to treat spasm of the gastrointestinal tract, biliary spasm, renal spasm, diagnostic aid in radiology. 1998-12-17 Ministry of Health of the Russian Federation
Click to view glaucine Glaucine is an aporphine alkaloid from Glaucium flavum Crantz, a species of Papaveraceae. Glaucine is a non-narcotic antitussive agent with anti-inflammatory action. It is used for the treatment non-productive (dry) cough. 2006-07-28 Ministry of Health of the Russian Federation
Click to view gramicidin s Gramicidin S molecule is amphiphilic, with hydrophobic amino acids (D-Phe, Val, Leu side chains) and charged aminoacid (L-Orn). It exhibits strong antibiotic activity towards Gram-negative and Gram-positive and even several pathogenic fungi. Unfortunately, being hemolytic at even low concentrations, gramicidin S is only used as topical applications at present. Gramicidin S is used for the treatment of pharyngitis, tonsillitis, gingivitis, periodontosis, stomatitis, pyoderma and burns. 1964-04-30 Ministry of Health of the Russian Federation
Click to view dalargin Mu-type opioid receptor (Organism: Mus musculus, class: GPCR, accessions: P42866, gene: Oprm1, swissprot: OPRM_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10516634) Mu-type opioid receptor (Organism: Rattus norvegicus, class: GPCR, accessions: P33535, gene: Oprm1, swissprot: OPRM_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10516634) Dalargin (tyrosine-D-alanyl-glycyl-phenylalanyl-leucyl-arginine diacetate) is the synthetic opioid peptide agent. It has antisecretory activity. Dalargin is used for the treatment of stomach and duodenum ulcer, acute and chronic pancreatitis and necrosis of pancreas. 1988-06-09 Ministry of Health of the Russian Federation
Click to view deanol aceglumate Deanol aceglumate is combination of deanol and N-acetyl-L-glutamic acid. Deanol aceglumate is a nootropic. It is used in asthenia (chronic fatigue), depression, alcohol withdrawal syndrome, organic psychosyndrome, schizophrenia. Also deanol aceglumate has a hepatoprotective activity and is used in chronic hepatitis and cirrhosis of liver. (See: deanol) 1989-02-02 National Authority of Medicines and Health Products (Portugal)
Click to view dibrospidium chloride Dibrospidium chloride (Spyrobromin) is a dispirotripiperazine derivative and alkylating agent with potential antineoplastic and anti-inflammatory activities. It was noted that spirobromin exerted the most pronounced toxic action on erythrocytes. Dibrospidium chloride is used for the treatment of acute leukemias (mainly in combination therapy), malignant lymphomas, laryngeal cancer and skin reticulosis and fungoid mycosis. 1982-08-25 Ministry of Health of the Russian Federation
Click to view dicarbine Dicarbine has neuroleptic, antidepressant and activating effects. Dicarbine blocks dopamine receptors in various brain parts, which leads to a reduction in the productive symptoms of psychosis: delusions and hallucinations. Dicarbine is used for the treatment patients with schizophrenia and alcoholic psychosis. 1970-06-01 Ministry of Health of the Russian Federation
Click to view didecyldimethylammonium chloride Didecyldimethylammonium chloride (DDAC) is a dialkyl-quaternary ammonium compound. It shows a broad spectrum of activity against both gram-positive and gram-negative bacteria and is also effective on fungi and viruses, including those that are enveloped. Didecyldimethylammonium chloride is used in many types of biocidal products including tableware, carpets, humidifiers, and swimming pools. Ministry of Health of the Russian Federation
Click to view dimebone Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18939977) Acetylcholinesterase (Organism: Rattus norvegicus, class: Enzyme, accessions: P37136, gene: Ache, swissprot: ACES_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11462798) Butyrylcholinesterase (Organism: Rattus norvegicus, class: Enzyme, accessions: Q9JKC1, gene: Bche, swissprot: Q9JKC1_RAT) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/11462798) Glutamate NMDA receptor (Organism: Rattus norvegicus, class: Ion channel, accessions: P35439|Q00959|Q00960|Q00961|Q62645|Q9R1M7|Q8VHN2, gene: Grin1|Grin2a|Grin2b|Grin2c|Grin2d|Grin3a|Grin3b, swissprot: NMDZ1_RAT|NMDE1_RAT|NMDE2_RAT|NMDE3_RAT|NMDE4_RAT|NMD3A_RAT|NMD3B_RAT) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11462798) Dimebone (latrepirdine) is a gamma carboline derivative. Dimebone inhibits alpha-Adrenergic receptors (alpha1A, alpha1B, alpha1D, and alpha2A), Histamine H1 and H2 receptors and Serotonin 5-HT2c, 5-HT5A, 5-HT6 receptors with high affinity. Dimebon may act by blocking NMDA receptors or voltage-gated Ca2+ channels and by preventing mitochondrial permeability pore transition. It is used for the treatment of allergy conditions. 1994-07-26 Ministry of Health of the Russian Federation
Click to view dimenhydrinate A drug combination that contains diphenhydramine and theophylline. It is used for treating VERTIGO, MOTION SICKNESS, and NAUSEA associated with PREGNANCY.
Click to view dimeticone Dimeticone is a poly(dimethylsiloxane) which is a polymer of 200-350 units of dimethylsiloxane, along with added silica gel. It has viscoelastic properties. When applied topically, dimethicone forms a layer to delay the evaporation of water. Dimeticone is used as a surfactant, antifoaming agent, carminative in various products such as medical devices, food products, and lubricants. Dimeticone is used as an anti-foaming agent, a hair and skin conditioner, and in the treatment of head lice and, as an anti-bloating/anti-flatulence agent. 1964-12-01 PMDA
Click to view dimethyloxobutylphosphonylmethylate Dimethyloxobutylphosphonylmethylate (dimephosphon) is an antiacidosis drug. It has anti-oxidant and anti-inflammatory activities. It is used in pneumonia, acute respiratory disease, influenza, infection pulmonary disease, diabetes mellitus, and other pathologic processes accompanied by acidosis. 1993-12-08 Ministry of Health of the Russian Federation
Click to view ferrous fumarate Ferrous Fumarate is the fumarate salt form of the mineral iron. Administration of ferrous fumarate results in elevation of serum iron concentration, which is then assimilated into hemoglobin, required for the transport of oxygen, or trapped in the reticuloendothelial cells for storage. This agent is used as a dietary supplement, and to prevent or treat iron deficiency related syndromes. 1986-07-18 FDA FE2
Click to view inosine pranobex An alkylamino-alcohol complex of inosine used in the treatment of a variety of viral infections. Unlike other antiviral agents, it acts by modifying or stimulating cell-mediated immune processes rather than acting on the virus directly.
Click to view iodophenazone Iodophenazone (iodoantipyrine) belongs to the group of nonsteroid anti-inflammatory compounds. It is used for the treatment and prevention of tick-borne encephalitis. 1996-08-13 Ministry of Health of the Russian Federation
Click to view potassium aspartate and magnesium aspartate Potassium aspartate and magnesium aspartate is a recovery-promoting anti-fatigue composition. It acts as a source of potassium and magnesium ions. It is used for the treatment and prevention of cardiac disruptions caused by electrolytic disturbances, primarily low potassium and magnesium levels. 1975-03-12 Ministry of Health of the Russian Federation
Click to view calcium glycerophosphate Calcium glycerophosphate is a Calcium salt of glycerophosphoric acid that forms a white, fine, slightly hygroscopic powder. The commercial product is a mixture of calcium beta-, and D-, and L -alpha-glycerophosphate. Calcium glycerophosphate in combination with sodium monofluorophosphate was found to reduce the acid solubility of enamel. Calcium glycerophosphate reduces the decrease in plaque pH produced by sucrose solutions. Calcium glycerophosphate donates Calcium and inorganic phosphate resulting in elevated levels of the ions in plaque. These ions are important components of the mineral structure of teeth. As such, their presence supports maintenance of healthy tooth structure and mineralization. Calcium glycerophosphate is considered a generally recognized as safe (GRAS) food ingredient as a nutrient supplement (source of calcium or phosphorus), or in food products such as gelatins, puddings, and fillings. It is also present in dental or oral hygiene products due to its cariostatic effects. It is also used as adjunct treatment of the rickets or disorders of calcium metabolism. 1970-09-28 Ministry of Health of the Russian Federation
Click to view calcium gluconate Calcium gluconate is a calcium salt of gluconic acid. The compound has a variety of uses, including its use as a calcium replenisher in hypocalcemic states. Calcium gluconate is used as mineral supplement and medication when there is insufficient calcium in the diet. Supplementation may be done to treat or prevent osteoporosis or rickets, consequences of hypocalcemia. Calcium gluconate is the antidote for magnesium sulfate toxicity. 93 mg elemental calcium is equivalent to 1 g of calcium gluconate. 1951-12-31 Health Canada
Click to view calcium dobesilate Calcium dobesilate is a veno-tonic drug. It was suggested, that the inhibitory effect of calcium dobesilate on platelet function is mediated through the cyclic AMP pathway, and probably through activation of adenyl cyclase. It is used for the treatment of chronic venous disease, diabetic retinopathy and the symptoms of haemorrhoidal attack. Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) 1980-03-16 Hungary National Institute of Pharmacy and Nutrition
Click to view calcium lactate Calcium lactate is a salt that consists of two lactate anions for each calcium cation (Ca2+). In aqueous environments such as the gastrointestinal (GI) tract, calcium lactate will dissociate into calcium cation and lactic acid anions, the conjugate base of lactic acid. Lactic acid is a naturally-occurring compound that serves as fuel or energy in mammals by acting as an ubiquitous intermediate in the metabolic pathways. Lactic acid diffuses through the muscles and is transported to the liver by the bloodstream to participate in gluconeogenesis. Both components of calcium lactate, calcium ion and lactic acid, play essential roles in the human body as a skeletal element an energy source, respectively. It is prepared commercially by the neutralization of lactic acid with calcium carbonate or calcium hydroxide. Calcium lactate is used as a firming agent, flavoring agent, leavening agent, stabilizer, and thickener. Calcium lactate is also found in daily dietary supplements as a source of calcium. It is also available in various hydrate forms, where calcium lactate pentahydrate is the most common. 1952-04-01 PMDA
Click to view calcium pangamate controversial variable preparation containing CALCIUM GLUCONATE and either dimethylglycine or diisopropylamine so the literature is divided among these; was MH 1975-97 (see under VITAMIN B COMPLEX 1975-90); use PANGAMIC ACID (NM) to search PANGAMIC ACID 1975-97; has been called vitamin B15
Click to view calcium pantothenate A butyryl-beta-alanine that can also be viewed as pantoic acid complexed with BETA ALANINE. It is incorporated into COENZYME A and protects cells against peroxidative damage by increasing the level of GLUTATHIONE.
Click to view calcium trisodium pentetate Calcium trisodium pentetate (Ca-DTPA) is a sodium salt of calcium diethylenetriaminepentaacetate. Ca-DTPA forms stable chelates with metal ions by exchanging calcium for a metal of greater binding capacity. The radioactive chelates are then excreted by glomerular filtration into the urine. In animal studies, Ca-DTPA forms less stable chelates with uranium and neptunium in vivo resulting in the deposition of these elements in tissues including the bone. Ca-DTPA treatments are not expected to be effective for uranium and neptunium. Calcium trisodium pentetate is indicated for treatment of individuals with known or suspected internal contamination with plutonium, americium, or curium to increase the rates of elimination. Also Ca-DTPA is used in lead and zinc poisoning. 1970-08-04 Ministry of Health of the Russian Federation
Click to view calcium folinate Calcium folinate is the calcium salt of folinic acid. It is used as detoxifying agents for antineoplastic treatment. (See: folinic acid) Folate Analog (Code: N0000178369) Folic Acid (Code: N0000007151) Antidotes (Code: D000931) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) Protective Agents (Code: D020011) Vitamin B Complex (Code: D014803) Analogs/Derivatives (Code: N0000175452) 1990-06-19 Ministry of Health of the Russian Federation
Click to view camphor bromatic Camphor bromatic (bromocamphor) has a depressive activity on the central nervous system. Also camphor bromatic improves cardiatic function. It is used for the treatment of hypotension, anxiety, malaise and fatigue, neurasthenia as a sedative agent. 1970-03-30 Ministry of Health of the Russian Federation
Click to view carbendazim Carbendazim is a broad-spectrum benzimidazole antifungal with potential antimitotic and antineoplastic activities. Although the exact mechanism of action is unclear, carbendazim appears to binds to an unspecified site on tubulin and suppresses microtubule assembly dynamic. This results in cell cycle arrest at the G2/M phase and an induction of apoptosis. Carbendazim is used as a fungicide in agriculture and home gardening, and as an antihelminthic for the treatment of hookworm diseases, ascariasis, strongyloidiasis, tichuriasis, and enterobiasis. 2005-04-15 Ministry of Health of the Russian Federation
Click to view carboplatin DNA (Organism: None, class: DNA, accessions: None, gene: None, swissprot: None) cross-linking agent (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020452s005lbl.pdf) High affinity copper uptake protein 1 (Organism: Homo sapiens, class: Transporter, accessions: O15431, gene: SLC31A1, swissprot: COPT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15634647) Probable low affinity copper uptake protein 2 (Organism: Mus musculus, class: Transporter, accessions: Q9CPU9, gene: Slc31a2, swissprot: COPT2_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/19509135) Copper-transporting ATPase 1 (Organism: Homo sapiens, class: Enzyme, accessions: Q04656, gene: ATP7A, swissprot: ATP7A_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/15213293) Carboplatin is an organoplatinum compound that possesses antineoplastic activity. Carboplatin, like cisplatin, produces predominantly interstrand DNA cross-links rather than DNA-protein cross-links. The differences in potencies for carboplatin and cisplatin appear to be directly related to the difference in aquation rates. Carboplatinis used for the treatment of initial or secondary treatment of advanced ovarian carcinoma. antineoplastic agent (Code: CHEBI:35610) Platinum-containing Compounds (Code: N0000175073) Platinum-based Drug (Code: N0000175413) Antineoplastic Agents (Code: D000970) Cross-Linking Reagents (Code: D003432) Indicators and Reagents (Code: D007202) 1989-03-03 FDA
Click to view clobetasol Clobetasol is a derivative of prednisolone. It has high glucocorticoid activity and low mineralocorticoid activity. The mechanism of the anti-inflammatory activity of topical steroids is unclear. It is used topically in the treatment of psoriasis, dermatoses, eczema but may cause marked adrenocortical suppression. Corticosteroid (Code: N0000175576) Corticosteroid Hormone Receptor Agonists (Code: N0000175450) Adrenal Cortex Hormones (Code: D000305) Anti-Inflammatory Agents (Code: D000893) Glucocorticoids (Code: D005938) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) anti-inflammatory drug (Code: CHEBI:35472)
Click to view cobamamide Cobamamide is one of the active forms of vitamin B12 that is also known as adenosylcobalamin or dibencozide. This drug is available as a nutritional supplement to prevent the vitamin B12 deficiency. Vitamin B 12 (Code: N0000006276) Vitamin B12 (Code: N0000175951) 1969-11-27 Italian Medicines Agency (AIFA) B1Z
Click to view cocarboxylase Cocarboxylase (tiamine pyrophosphate) is an organic chloride salt of thiamine(1+) diphosphate. It is a coenzyme form of Vitamin B1 present in many animal tissues. It is a required intermediate in the pyruvate dehydrogenase complex and the ketoglutarate dehydrogenase complex. It is used in the vitamin B deficiency states. Also it is used for the treatment of acidosis, neuralgia, neuritis, miocardial infarction, stroke. 1969-04-08 Ministry of Health of the Russian Federation
Click to view colestyramine Colestyramine (cholestyramine) is the chloride salt of a basic anion exchange resin, a cholesterol-lowering agent. Colestyramine resin is quite hydrophilic, but insoluble in water. Colestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. This results in a partial removal of bile acids from the enterohepatic circulation by preventing their absorption. Colestyramine is indicated as adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia. Colestyramine may be useful to lower LDL cholesterol in patients who also have hypertriglyceridemia. Bile Acid Sequestrant (Code: N0000180292) Bile-acid Binding Activity (Code: N0000175365) 1973-08-03 FDA
Click to view xantinol nicotinate Xantinol nicotinate is a nicotinic acid salt of xantinol. Xantinol nicotinate is used for cerebrovascular disorders, peripheral vascular disease and other conditions. (See: xantinol) 1979-08-07 Ministry of Health of the Russian Federation
Click to view lappaconitine hydrobromide Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.ncbi.nlm.nih.gov/pubmed/11160852) Acetylcholinesterase (Organism: Electrophorus electricus, class: Enzyme, accessions: O42275, gene: ache, swissprot: ACES_ELEEL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28463565) Butyrylcholinesterase (Organism: Equus caballus, class: Enzyme, accessions: Q9N1N9, gene: BCHE, swissprot: Q9N1N9_HORSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/28463565) Lappaconitine is an alkaloid isolated from the root of Aconltitum sinomantanum Nakai. It has a analgesic activity. It was shown to have class-I antiarrhythmic action and irreversibly blocks cloned human heart channels by binding to the site 2 receptor. It is noncompetitive inhibitor of AChE. It is used in hydrobromide form for the treatment of supraventricular and ventricular tachycardia, atrial fibrillation and flutter, junctional and ventricular premature depolarization. 1986-12-15 Ministry of Health of the Russian Federation
Click to view levodropropizine Levodropropizine is a non-opioid cough suppressant whose peripheral antitussive action may result from its modulation of sensory neuropeptide levels within the respiratory tract. Levodropropizine exerts its antitussive effect through an inhibitory action at the level of the airway sensory nerves and it has been shown to be able to inhibit in vitro the release of neuropeptides from C-fibers. Levodropropizine is used for the symptomatic therapy of cough. antitussive (Code: CHEBI:51177) 1987-07-30 Italian Medicines Agency (AIFA)
Click to view leucogen Leucogen enhances leukocyte level. It is used for the treatment of leukopenia, including chemotherapy-, radiotherapy-induced leukemia, alimentary toxic aleukia. 1964-04-30 Ministry of Health of the Russian Federation
Click to view magnesium orotate Magnesium orotate is a magnesium salt of orotic acid. It is indicated as a source of magnesium (Mg) for the oral treatment of extracellular Mg deficiency. (See: orotic acid) 1991-07-31 Hungary National Institute of Pharmacy and Nutrition
Click to view magnesium citrate Magnesium Citrate is the citrate salt of the element magnesium with cathartic activity. The cathartic action of magnesium cations appears to result, in part, from osmotically mediated water retention, which subsequently stimulates peristalsis. In addition, magnesium ions may also stimulate the activity of nitric oxide (NO) synthase and increase the biosynthesis of the phospholipid proinflammatory mediator platelet activating factor (PAF) in the gut. Magnesium Citrate is used for the treatment and prevention of magnesium deficiency. 1996-08-30 Ministry of Health of the Russian Federation
Click to view megestrol Megestrol is a synthetic derivative of progesterone with antiestrogenic activity. Megestrol binds to and activates nuclear receptors which subsequently bind to and activate target genes for transcription. As an antiestrogen, this agent may inhibit the growth-stimulating effects of estrogen on estrogen-sensitive tumor cells. In addition, megestrol stimulates appetite in cachectic subjects. Megestrol is indicated for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Also it is used for the palliative management of recurrent, inoperable, or metastatic breast cancer, endometrial cancer, and prostate cancer.
Click to view mesocarb Mesocarb is a central nervous system stimulant. It is an amphetamine derivative. Mesocarb has a two optical isomers, only levo-isomer has a CNS stimulant activity. Mesocarb produces locomotor stimulation, anorectic activity, enhancement of conditioned reflexes and shortening of the period of action of hypnotic agents. Mesocarb is used for the treatment of neurastenia, asthenia, schizophrenia. It has however been added to the list of drugs under international control and is a scheduled substance in most countries. 1971-12-31 Ministry of Health of the Russian Federation
Click to view menthol Transient receptor potential cation channel subfamily M member 8 (Organism: Homo sapiens, class: Ion channel, accessions: Q7Z2W7, gene: TRPM8, swissprot: TRPM8_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15931068) Transient receptor potential cation channel subfamily A member 1 (Organism: Homo sapiens, class: Ion channel, accessions: O75762, gene: TRPA1, swissprot: TRPA1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/15931068) Transient receptor potential cation channel subfamily A member 1 (Organism: Mus musculus, class: Unclassified, accessions: Q8BLA8, gene: Trpa1, swissprot: TRPA1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16829128) Transient receptor potential cation channel subfamily V member 3 (Organism: Mus musculus, class: Unclassified, accessions: Q8NET8, gene: Trpv3, swissprot: TRPV3_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16829128) Kappa-type opioid receptor (Organism: Mus musculus, class: Unclassified, accessions: P33534, gene: Oprk1, swissprot: OPRK_MOUSE) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11897159) Menthol is an organic compound made synthetically or obtained from peppermint or other mint oils. (-)-Menthol (levomenthol) is the naturally-occurring,main form and optically active of menthol, and is assigned the (1R,2S,5R) configuration. Menthol mediates anesthetic properties and anti-irritating properties locally, thus it is widely used to relieve minor throat irritations. Menthol primarily activates the cold-sensitive TRPM8 receptors in the skin. Menthol, after topical application, causes a feeling of coolness due to stimulation of 'cold' receptors by inhibiting Ca++ currents of neuronal membranes. It may also yield analgesic properties via kappa-opioid receptor agonism. Menthol is used to treat occasional minor irritation, pain, sore mouth, and sore throat as well as cough associated with a cold or inhaled irritants. antitussive (Code: CHEBI:51177) antispasmodic drug (Code: CHEBI:53784) antipruritic drug (Code: CHEBI:59683) Antipruritics (Code: D000982) Dermatologic Agents (Code: D003879) 2008-02-20 FDA
Click to view metadoxine Metadoxine is an ion pair salt of pyridoxine and pyroglutamic acid. Pyroglutamic acid (2-Pyrrolidone-5-carboxylic acid, PCA) is transformed into glutathione. It is a cyclic derivative of glutamic acid, physiologically present in mammalian tissues. It has been shown that PCA releases GABA from the cerebral cortex and displays anti-anxiety effects in a simple approach-avoidance conflict situation in the rat. In clinical pharmacology experiments, PCA significantly shortens the plasma half-life of ethanol during acute intoxication.Pyridoxine is a precursor of coenzymes such as pyridoxal phosphate. Metadoxine is predominantly used for acute alcohol intoxication, alcoholism or alcohol withdrawal syndrome. (See: pyridoxine) 1984-07-01 Italian Medicines Agency (AIFA)
Click to view metazide Metazide is an anti-tuberculosis agent and a derivative of isoniazid. Metazide has activity against Mycobacterium tuberculosis. Metazide causes damage to the membrane of Mycobacterium tuberculosis, inhibits metabolic and oxidative processes, inhibits the synthesis of nucleic acids, suppressing the multiplication of bacteria both inside the cell and outside it. Metazide is used for the treatment of pulmonary tuberculosis, CNS tuberculosis, miliary tuberculosis and of tuberculosis of other organs. 1964-04-30 Ministry of Health of the Russian Federation
Click to view methyltestosterone A synthetic hormone used for androgen replacement therapy and as an hormonal antineoplastic agent (ANTINEOPLASTIC AGENTS, HORMONAL).
Click to view methyluracil Methyluracil (dioxomethyltetrahydropyrimidine) stimulates the process of regeneration and promotes the activation of metabolic processes in tissues and the improvement of trophism. It is used as oinment for the treatment of wounds, burns, dermatitis and as injection for the treatment of anemia, thrombocytopenia, hepatitis. 1976-06-29 Ministry of Health of the Russian Federation
Click to view metocinium iodide Metocinium iodide is a spasmolytic agent. It acts as antagonist of muscarinic acetylcholine receptors. Metocinium iodide is used in patients with irritable bowel syndrome, peptic ulcer and renal colic. 1967-07-11 Ministry of Health of the Russian Federation
Click to view mometasone
Click to view sodium calcium edetate Sodium calcium edetate is an agent used as a chelator of lead and some other heavy metals. Sodium calcium edetate mobilizes lead from bone. It enhances removal of lead from the body by forming a stable water-soluble lead complex in which calcium is replaced by divalent and trivalent metals, especially any available lead. This complex is readily excreted by the kidneys. (See: edetic acid) 1993-12-31 Health Canada
Click to view sodium nitroprusside Sodium nitroprusside is disodium pentacyanonitrosylferrate(2-) dihydrate, a hypotensive agent. Sodium nitroprusside interacts with oxyhemoglobin to produce methemoglobin, cyanide, and nitric oxide (NO). NO then reacts with guanylate cyclase in vascular smooth muscle to produce cGMP that reduces intracellular calcium concentrations resulting in relaxation of vascular smooth muscle and consequent dilatation of peripheral arteries and veins. Sodium nitroprusside is more active on veins than on arteries, but this selectivity is much less marked than that of nitroglycerin. Dilatation of the veins promotes peripheral pooling of blood and decreases venous return to the heart, thereby reducing left ventricular end diastolic pressure and pulmonary capillary wedge pressure (preload). Arteriolar relaxation reduces systemic vascular resistance, systolic arterial pressure, and mean arterial pressure (afterload). Dilatation of the coronary arteries also occurs. Sodium nitroprusside is indicated for the immediate reduction of blood pressure, for the producing controlled hypotension to reduce bleeding during surgery and for the treatment of acute heart failure to reduce, left ventricular end-diastolic pressure, pulmonary capillary wedge pressure, peripheral vascular resistance and mean arterial blood pressure. Vasodilator (Code: N0000175940) Vasodilation (Code: N0000009909) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Indicators and Reagents (Code: D007202) Nitric Oxide Donors (Code: D020030) Vasodilator Agents (Code: D014665) 1974-05-10 FDA
Click to view iodohippurate sodium i123 Iodohippurate sodium I123 is an isotopically modified compound, an organic sodium salt and a sodium 2-iodohippurate. It derives from a N-benzoylglycine. It is used as a radiopharmaceutical. It is used for evaluating effective renal plasma flow by means of either in vivo scintigraphy and/or plasma clearance curves. It has been used to evaluate renal functioning in patients with obstructive uropathy, vesicorenal reflux, hypertensiion due to renal artery stenosis. 1984 FDA
Click to view sodium oxybate Gamma-hydroxybutyric acid: Hydroxycarboxylic acid receptor 1 (Organism: Homo sapiens, class: GPCR, accessions: Q9BXC0, gene: HCAR1, swissprot: HCAR1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/19047060) Monocarboxylate transporter 1 (Organism: Rattus norvegicus, class: Transporter, accessions: P53987, gene: Slc16a1, swissprot: MOT1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16707723) Monocarboxylate transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: P53985, gene: SLC16A1, swissprot: MOT1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9786900) Monocarboxylate transporter 1 (Organism: Homo sapiens, class: Transporter, accessions: O60669, gene: SLC16A7, swissprot: MOT2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/9786900) Hydroxyacid-oxoacid transhydrogenase, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q8IWW8, gene: ADHFE1, swissprot: HOT_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16435184) Sodium oxybate is a CNS depressant. The mechanism of action of sodium oxybate in the treatment of narcolepsy is unknown. Sodium oxybate is the sodium salt of gamma-hydroxybutyrate (GHB), an endogenous compound and metabolite of the neurotransmitter GABA. It is hypothesized that the therapeutic effects of sodium oxybate on cataplexy and excessive daytime sleepiness are mediated through GABAB actions at noradrenergic and dopaminergic neurons, as well as at thalamocortical neurons. Sodium oxybate is indicated for the treatment of cataplexy in narcolepsy and excessive daytime sleepiness (EDS) in narcolepsy. Adjuvants, Anesthesia (Code: D000759) Anesthetics (Code: D000777) Anesthetics, General (Code: D018681) Anesthetics, Intravenous (Code: D018686) Central Nervous System Agents (Code: D002491) Central Nervous System Depressants (Code: D002492) 2002-07-17 FDA
Click to view sodium picosulfate Sodium picosulfate is a locally acting laxative from the triarylmethane group, which after bacterial cleavage in the colon, has the dual action of stimulating the mucosa of both the large intestine causing peristalsis and of the rectum causing increased motility and a feeling of rectal fullness. Sodium picosulfate is a prodrug. It has no significant direct physiological effect on the intestine. But it is hydrolyzed by colonic bacteria to form an active metabolite: bis-(p-hydroxy-phenyl)-pyridyl-2-methane, BHPM, which acts directly on the colonic mucosa to stimulate colonic peristalsis. Sodium picosulfate is indicated for the treatment of constipation of any aetiology and bowel clearance before surgery, childbirth or radiological investigations. 1934-05-01 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view nicotinoyl gamma-aminobutyric acid Nicotinoyl gamma-aminobutyric acid (picamilon) is a synthetic combination of niacin and GABA. It permeated the blood-brain barrier and then is hydrolyzed into GABA and niacin. The released GABA, in theory, would activate GABA receptors potentially producing an anxiolytic response. The second released component, niacin, is a vasodilator. It is used for the treatment of depression, migraine, neuro infections, senile psychosis, certain types of glaucoma, acute alcohol intoxication, cerebral infraction and other cerebral circulatory disorders. (See: aminobutyric acid) (See: nicotinic acid) 1986-12-22
Click to view nitrosomethylurea Nitrosomethylurea (N-methyl-N-nitrosourea) is a nitrosamine compound. Nitrosomethylurea was once widely used to synthesize diazomethane in the laboratory. N-Nitroso-N-methylurea is reasonably anticipated to be a human carcinogen based on sufficient evidence from studies in experimental animals. Nitrosomethylurea was used as a chemotherapeutic agent in cancer treatment, either alone or in combination with cyclophosphamide. 2000-01-26 Ministry of Health of the Russian Federation
Click to view nonoxinol Nonionic surfactant mixtures varying in the number of repeating ethoxy (oxy-1,2-ethanediyl) groups. They are used as detergents, emulsifiers, wetting agents, defoaming agents, etc. Nonoxynol-9, the compound with 9 repeating ethoxy groups, is a spermatocide, formulated primarily as a component of vaginal foams and creams.
Click to view oxaliplatin Oxaliplatin is an organoplatinum complex in which the platinum atom is complexed with 1,2-diaminocyclohexane (DACH) and with an oxalate ligand as a leaving group. Oxaliplatin is an antineoplastic agent. Oxaliplatin undergoes nonenzymatic conversion in physiologic solutions to active derivatives via displacement of the labile oxalate ligand. Several transient reactive species are formed, including monoaquo and diaquo DACH platinum, which covalently bind with macromolecules. Both inter-and intrastrand Pt-DNA crosslinks are formed. Crosslinks are formed between the N7 positions of two adjacent guanines (GG), adjacent adenine-guanines (AG), and guanines separated by an intervening nucleotide (GNG). These crosslinks inhibit DNA replication and transcription. Cytotoxicity is cell-cycle nonspecific. Oxaliplatin is used in combination with infusional 5-fluorouracil /leucovorin for adjuvant treatment of stage III colon cancer in patients who have undergone complete resection of the primary tumor and for the treatment of advanced colorectal cancer. antineoplastic agent (Code: CHEBI:35610) Platinum-containing Compounds (Code: N0000175073) Platinum-based Drug (Code: N0000175413) Antineoplastic Agents (Code: D000970) 2002-08-09 FDA
Click to view pantogam Pantogam is a calcium salt of hopantenic acid. Pantogam has a unique spectrum of pharmacological effects (nootropic, anticonvulsant, mild activating). Pantogam is used to treat a variety of neurological, psychological and psychiatric conditions. (See: hopantenic acid)
Click to view pentoxyl Pentoxyl (hydroxymethylmethyluracil) is a derivative of pyrimidine and chemically related to metacil. Pentoxyl stimulates leukopoiesis. Pentoxyl is indicated in various leukopenic conditions, agranulocytary angina of unknown etiology, alimentary-toxic aleukia, chronic effects of benzene and agranulocytoses caused by drugs. 1952 Ministry of Public Health USSR
Click to view pipofezine Pipofezine is a tricyclic antidepressant. Pipofezine has been shown to act as a potent inhibitor of the reuptake of serotonin. In addition to its antidepressant action, pipofezine has sedative effects as well, suggesting antihistamine activity. The main advantage of pipofezine compared with other tricyclic antidepressants is that this drug has a low toxic effect on the body, including the heart, and it does not block cholinergic receptors and does not change the activity of monoamine oxidase. Pipofezine is used for the treatment of depression. 1970-06-01 Ministry of Health of the Russian Federation
Click to view pyrithione zinc Pyrithione zinc is a coordination complex consisted of pyrithione ligands chelated to zinc (2+) ions via oxygen and sulfur centers. In the crystalline state, it exists as a centrosymmetric dimer. Due to its dynamic fungistatic and bacteriostatic properties, pyrithione zinc is used to treat dandruff and seborrheic dermatitis. It has antibacterial properties and is effective against many pathogens from the Streptococcus and Staphylococcus genera. Pyrithione zinc`s other medical applications include treatments of psoriasis, eczema, ringworm, fungus, athletes foot, dry skin, atopic dermatitis, tinea, and vitiligo. It was shown that Pyrithione zinc inhibits fungal growth through increased cellular levels of copper, damaging iron-sulphur clusters of proteins essential for fungal metabolism. Dermatologic Agents (Code: D003879) Keratolytic Agents (Code: D007641) 1981-12-31 Health Canada
Click to view platyphylline Platyphylline is a pyrrolizidine alkaloid. Platyphylline has an antimuscarinic action. Platyphylline has typical atropine-like properties. It causes mydriasis and antagonism of pilocarpine and physostigmine induced miosis. Platyphylline inhibits acetylcholine induced cantraction of smooth muscle preparation from the gastrointestinal tract and inhibits pilocarpine induced salivatory secretion. Platyphylline is used for the treatment of spasm due to stomach and duodenal ulcers, intestinal colic, renal colic, biliary colic. Also it is used for the treatment of bronchial asthma, hypertension, poisoning by acetone, boric acid, strong acids or arsenic. In ophtalmology it is used for the pupil dilation. 1971-08-23 Ministry of Health of the Russian Federation
Click to view povidone Providone (polyvinylpyrrolidone (PVP) or polyvidone) is a synthetic water-soluble polymer made from the monomer N-vinylpyrrolidone that is used as a binder in many pharmaceutical tablets and lubricant in eye drops. It is also used in many technical applications with various roles as an adhesive, additive, and emulsifier. Providone in combination with polyvinyl alcohol used for the temporary relief of burning, irritation, and discomfort due to dryness of the eye or exposure to wind or sun. May be used as a protectant against further irritation. 1985-09-12 FDA
Click to view povidone-iodine Povidone-iodine is a stable chemical complex of polyvinylpyrrolidone (povidone, PVP) and elemental iodine. Povidone-Iodine is a broad-spectrum microbicide with in vitro activity against bacteria, viruses, fungi and protozoans. It is used for topical application in the treatment and prevention of infection in wounds. Iodine (Code: N0000007196) Antiseptic (Code: N0000175486) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 1985-11-29 FDA
Click to view polyvinox Polyvinox is a potent antiseptic compound. With external use, it promotes epithelization, cleansing wounds, tissue regeneration. It is used for the treatment of infected wounds as an antiseptic. Also it is used for the treatment of peptic ulcer and heartburn. 1964-04-30 Ministry of Health of the Russian Federation
Click to view polidocanol polyethylene glycol monododecyl ether (average polymer n=9); RN in Chemline for nonaethyleneglycol monododecyl ether: 3055-99-0
Click to view policresulen anti-infective agent (vaginal); condensation product of meta-cresolsulfonic acid and formaldehyde
Click to view polyestradiol phosphate polymeric phosphoric acid ester of estradiol Estrogens (Code: D004967) Hormones (Code: D006728) Hormones, Hormone Substitutes, and Hormone Antagonists (Code: D006730) 1957-04-17 FDA
Click to view proxifeine Proxifeine is an antitumor agent. It inhibits biosynthesis of nucleic acids. It was used for the treatment of malignant neoplasms of brain, breast, gastrointestinal tract, ovaries, thyroid gland, neuroblastoma and melanoma. Also it was used in lymphogranulomatosis, non-Hodgkin lymphomas. 1997-10-03 Ministry of Health of the Russian Federation
Click to view proxodolol Proxodolol (butylaminohydroxypropoxyphenoxymethyl methyloxadiazole) is an oxadiazolo-2-propanol. Proxodolol acts as a specific competitive antagonist at both beta- and alpha-adrenoceptors. Proxodolol is used for the treatment of open-angle, angle-closure glaucoma, hypertension, angina pectoris and heart failure. 1993-05-31 Ministry of Health of the Russian Federation
Click to view proroxan Proroxan is a non-selective alpha-adrenergic blocker. Proroxan was found to prevent the development of hypertensive crises. Proroxan is used for the treatment of hypertension, Meniere’s disease, motion sickness, and allergic dermatitis. 1969-11-06 Ministry of Health of the Russian Federation
Click to view propionilphenyletoxyethylpiperidine Propionilphenyletoxyethylpiperidine (prosidol) is a narcotic analgesic. It is used for treatment of chronic pain in oncology patients, pain due to myocardial infarction and acute pancreatitis, renal colic, hepatic colic, pain in postoperative period. Prosidol is included in list of narcotic drugs and psychotropic substances. 1993-05-31 Ministry of Health of the Russian Federation
Click to view prospidium chloride Prospidium is a diazoniadispiro(5.2.5.2)hexadecane derivative. It is an antitumor agent that does not inhibit hematopoiesis. It is used for the treatment of acute leukemia, laryngeal cancer, skin reticulosis, papillomatosis of the upper respiratory tract, lung cancer, lymphosarcoma, lymphogranulomatosis, retinoblastoma. 1970-06-01 Ministry of Health of the Russian Federation
Click to view saccharin Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17705204) Carbonic anhydrase 2 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ9, gene: mtcA2, swissprot: MTCA2_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Beta-carbonic anhydrase 1 (Organism: Mycobacterium tuberculosis (strain ATCC 25618 / H37Rv), class: Enzyme, accessions: P9WPJ7, gene: mtcA1, swissprot: MTCA1_MYCTU) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19338333) Carbonic anhydrase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P53615, gene: NCE103, swissprot: CAN_YEAST) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19124253) Carbonic anhydrase 2 (Organism: Cryptococcus neoformans var. grubii, class: Unclassified, accessions: Q3I4V7, gene: CAN2, swissprot: Q3I4V7_CRYNV) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Carbonic anhydrase (Organism: Candida albicans (strain SC5314 / ATCC MYA-2876), class: Enzyme, accessions: Q5AJ71, gene: NCE103, swissprot: CAN_CANAL) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19450983) Saccharin, ammonium salt is used as a food additive. Saccharin is the most established of the artificial sweeteners on the market. It is 300-500 times sweeter than sugar and contains zero calories. While saccharin has no food energy, it can trigger the release of insulin in humans due to its sweet taste. The T1R2/R3 sweet taste receptor exist on the surface of pancreatic beta cells. Saccharin is a unique in that it inhibits glucose-stimulated insulin secretion (GSIS) at submaximal and maximal glucose concentrations, with the other sweeteners having no effect. Saccharin is used as a artificial sweeteners for patients with diabetes mellitus. 1964-04-30 Ministry of Health of the Russian Federation LSA
Click to view plumbous acetate Plumbous acetate (lead acetate) is a toxic agent, which can lead to irritation to skin, eyes, and respiratory tract. Its oxidising nature can indirectly lead to many diseases. Plumbous acetate has a sweet taste, which led to its historical use as a sugar substitute. In 1980 lead acetate was permanently listed as a color additive for the safe use in cosmetics for hair coloring. However, since 2017 no longer provide for the use of lead acetate in cosmetics intended for coloring hair on the scalp. It also used as an antiseptic. 1973-06-15 Ministry of Health of the Russian Federation PB
Click to view sennosides a & b Reverse transcriptase/RNaseH (Organism: Human immunodeficiency virus 1, class: Enzyme, accessions: Q72549, gene: pol, swissprot: Q72549_9HIV1) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27765358) Sennosides are hydroxyanthracene glycosides derived from Senna leaves. The phytoconstituents principally responsible for its characteristic action are two anthraquinone glycosides namely; Sennoside A and Sennoside B. Sennoside A has being shown to be a dual HIV-1 inhibitor effective on HIV-1 replication. Sennoside B has reported that it has inhibitory effects on PDGF receptor signaling and cell proliferation induced by PDGF-BB in human osteosarcoma cells. Sennoside A and B together are responsible for up to 40 – 60% activity of crude senna. Sennosides A and B are used for the treatment of constipation. It is also used for colonoscopy preparation. 1985-07-30 Ministry of Health of the Russian Federation
Click to view serotonin 5-hydroxytryptamine receptor 2A (Organism: Homo sapiens, class: GPCR, accessions: P28223, gene: HTR2A, swissprot: 5HT2A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15322733) 5-hydroxytryptamine receptor 2B (Organism: Homo sapiens, class: GPCR, accessions: P41595, gene: HTR2B, swissprot: 5HT2B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15322733) 5-hydroxytryptamine receptor 2C (Organism: Homo sapiens, class: GPCR, accessions: P28335, gene: HTR2C, swissprot: 5HT2C_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/15322733) 5-hydroxytryptamine receptor 1A (Organism: Homo sapiens, class: GPCR, accessions: P08908, gene: HTR1A, swissprot: 5HT1A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10431754) 5-hydroxytryptamine receptor 1B (Organism: Homo sapiens, class: GPCR, accessions: P28222, gene: HTR1B, swissprot: 5HT1B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10431754) 5-hydroxytryptamine receptor 1D (Organism: Homo sapiens, class: GPCR, accessions: P28221, gene: HTR1D, swissprot: 5HT1D_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10431754) 5-hydroxytryptamine receptor 1E (Organism: Homo sapiens, class: GPCR, accessions: P28566, gene: HTR1E, swissprot: 5HT1E_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8380639) 5-hydroxytryptamine receptor 4 (Organism: Homo sapiens, class: GPCR, accessions: Q13639, gene: HTR4, swissprot: 5HT4R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11218067) 5-hydroxytryptamine receptor 5A (Organism: Homo sapiens, class: GPCR, accessions: P47898, gene: HTR5A, swissprot: 5HT5A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/7988681) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27475109) 5-hydroxytryptamine receptor 6 (Organism: Homo sapiens, class: GPCR, accessions: P50406, gene: HTR6, swissprot: 5HT6R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9730917) 5-hydroxytryptamine receptor 7 (Organism: Homo sapiens, class: GPCR, accessions: P34969, gene: HTR7, swissprot: 5HT7R_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/27475109) 5-hydroxytryptamine receptor 3A (Organism: Homo sapiens, class: Ion channel, accessions: P46098, gene: HTR3A, swissprot: 5HT3A_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/9463477) 5-hydroxytryptamine receptor 3B (Organism: Homo sapiens, class: Ion channel, accessions: O95264, gene: HTR3B, swissprot: 5HT3B_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/10521471) Sodium-dependent serotonin transporter (Organism: Homo sapiens, class: Transporter, accessions: P31645, gene: SLC6A4, swissprot: SC6A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17913921) Carbonic anhydrase 1 (Organism: Homo sapiens, class: Enzyme, accessions: P00915, gene: CA1, swissprot: CAH1_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 12 (Organism: Homo sapiens, class: Enzyme, accessions: O43570, gene: CA12, swissprot: CAH12_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 2 (Organism: Homo sapiens, class: Enzyme, accessions: P00918, gene: CA2, swissprot: CAH2_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 9 (Organism: Homo sapiens, class: Enzyme, accessions: Q16790, gene: CA9, swissprot: CAH9_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18294854) Carbonic anhydrase 5A, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P35218, gene: CA5A, swissprot: CAH5A_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17174092) Carbonic anhydrase 5B, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: Q9Y2D0, gene: CA5B, swissprot: CAH5B_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17174092) Carbonic anhydrase 14 (Organism: Homo sapiens, class: Enzyme, accessions: Q9ULX7, gene: CA14, swissprot: CAH14_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 7 (Organism: Homo sapiens, class: Enzyme, accessions: P43166, gene: CA7, swissprot: CAH7_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17540561) Carbonic anhydrase 3 (Organism: Homo sapiens, class: Enzyme, accessions: P07451, gene: CA3, swissprot: CAH3_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18627905) Carbonic anhydrase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P22748, gene: CA4, swissprot: CAH4_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/18627905) D(1A) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21728, gene: DRD1, swissprot: DRD1_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1826762) D(1B) dopamine receptor (Organism: Homo sapiens, class: GPCR, accessions: P21918, gene: DRD5, swissprot: DRD5_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/1826762) Carbonic anhydrase 6 (Organism: Homo sapiens, class: Enzyme, accessions: P23280, gene: CA6, swissprot: CAH6_HUMAN) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/17499996) Carbonic anhydrase 13 (Organism: Mus musculus, class: Enzyme, accessions: Q9D6N1, gene: Ca13, swissprot: CAH13_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/16730978) Carbonic anhydrase 15 (Organism: Mus musculus, class: Enzyme, accessions: Q99N23, gene: Ca15, swissprot: CAH15_MOUSE) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/19464888) Carbonic anhydrase (Organism: Saccharomyces cerevisiae (strain ATCC 204508 / S288c), class: Enzyme, accessions: P53615, gene: NCE103, swissprot: CAN_YEAST) activator (Source: https://www.ncbi.nlm.nih.gov/pubmed/19231177) Solute carrier family 22 member 1 (Organism: Rattus norvegicus, class: Transporter, accessions: Q63089, gene: Slc22a1, swissprot: S22A1_RAT) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8898084) Chromaffin granule amine transporter (Organism: Homo sapiens, class: Transporter, accessions: P54219, gene: SLC18A1, swissprot: VMAT1_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8643547) Synaptic vesicular amine transporter (Organism: Homo sapiens, class: Transporter, accessions: Q05940, gene: SLC18A2, swissprot: VMAT2_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/8643547) Solute carrier family 22 member 3 (Organism: Homo sapiens, class: Transporter, accessions: O75751, gene: SLC22A3, swissprot: S22A3_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/20402963) Equilibrative nucleoside transporter 4 (Organism: Homo sapiens, class: Transporter, accessions: Q7RTT9, gene: SLC29A4, swissprot: S29A4_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/16099839) Solute carrier family 26 member 6 (Organism: Mus musculus, class: Transporter, accessions: Q8CIW6, gene: Slc26a6, swissprot: S26A6_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/16126914) Serotonin (5-Hydroxytryptamine) is a biochemical messenger and regulator, synthesized from the essential amino acid L-Tryptophan. Serotonin in the nervous system acts as a local transmitter at synapses, and as a paracrine or hormonal modulator of circuits upon diffusion, allowing a wide variety of "state-dependent" behavioral responses to different stimuli. Such is the case of aggressive behavior and rhythmic motor patterns, including those responsible for feeding. Serotonin also modulates sleep, the arousal state , sexual behavior, and others, and deficiencies of the serotonergic system causes disorders such as depression, obsessive-compulsive disorder, phobias, posttraumatic stress disorder, epilepsy, and generalized anxiety disorder. Serotonin has three different modes of action in the nervous system: as transmitter, acting locally at synaptic boutons; upon diffusion at a distance from its release sites, producing paracrine (also called volume) effects, and by circulating in the blood stream, producing hormonal effects. The three modes can affect a single neuronal circuit. Synthetic serotonin is used for temporary relief of nervousness, anxiety, mood swings, joint pains, weakness, drowsiness, itching and lethargy as a homeopathic product. SRO
Click to view silabolin Silabolin is an anabolic drug. It is a steroid containing a trimethylsilyl group. Silabolin was used for the treatment of cachexia, unspecified protein-energy malnutrition, delayed puberty, Turner syndrome, muscular dystrophy and other protein-wasting disorders. Anabolic 1980-06-04 Ministry of Health of the Russian Federation
Click to view silibinin Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19934397) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/17920288) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/17920288) Silibinin is the major active constituent of silymarin, a standardized extract of the milk thistle seeds, containing a mixture of flavonolignans consisting of silibinin, isosilibinin, silicristin, silidianin and others. Silibinin is presented as a mixture of two diastereomers, silybin A and silybin B, which are found in an approximately equimolar ratio. Both in vitro and animal research suggest that silibinin has hepatoprotective (antihepatotoxic) properties that protect liver cells against toxins. Silibinin has also demonstrated in vitro anti-cancer effects against human prostate adenocarcinoma cells, estrogen-dependent and -independent human breast carcinoma cells, human ectocervical carcinoma cells, human colon cancer cells, and both small and nonsmall human lung carcinoma cells. Silibinin is used as a hepatoprotor. 1987-01-01 Hungary National Institute of Pharmacy and Nutrition
Click to view Cymarin Potassium-transporting ATPase (Organism: Sus scrofa, class: Enzyme, accessions: P18434|P19156, gene: ATP4A|ATP4B, swissprot: ATP4A_PIG|ATP4B_PIG) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/6146536) Cymarin (Strophanthin-K, K-strophanthidin-alpha) is a cardiac glycoside from strophanthus, the seeds of Strophanthus kombe (Apocynaceae) or other spp. Its mechanism of action is similar to ouabain and digitoxin. It works as an inhibitor of Na+ /K+-ATPase. Strophanthin-K is used for the treatment of supraventricular tachycardia, atrial fibrillation and flutter and heart failure. 1967-07-11 Ministry of Health of the Russian Federation
Click to view sucralfate Sucralfate is an alpha-D-glucopyranoside, beta-Dfructofuranosyl-, octakis-(hydrogen sulfate), aluminum complex. Sucralfate’s antiulcer activity is the result of formation of an ulcer-adherent complex that covers the ulcer site and protects it against further attack by acid, pepsin, and bile salts. Sucralfate is indicated fir short-term treatment and maintenance of duodenal ulcer. Sucralfate is also used in the prevention and treatment of gastro-esophageal reflux disease, gastritis, peptic ulcer disease, stress ulcer, in addition to dyspepsia. Organometallic Compounds (Code: N0000007683) Aluminum Complex (Code: N0000175801) Anti-Ulcer Agents (Code: D000897) Gastrointestinal Agents (Code: D005765) 1981-10-30 FDA
Click to view suxamethonium iodide Suxamethonium iodide is the iodide salt form of suxamethonium, a quaternary ammonium compound and depolarizing agent with short-term muscle relaxant properties. Suxamethonium iodide has about two-thirds the potency of the cloride salt form. (See: suxamethonium) 1964-04-30 Ministry of Health of the Russian Federation
Click to view suxamethonium chloride Suxamethonium chloride is the chloride salt form of suxamethonium, a quaternary ammonium compound and depolarizing agent with short-term muscle relaxant properties. (See: suxamethonium) 1990-09-04 UK Medicines and Healthcare Products Regulatory Agency (MHRA)
Click to view tebrofen Tebrofen is a polyphenol and an antiviral drug. Tebrofen has activity against an arbovirus.
Click to view tetraxolin Tetraxolin (dioxotetrahydrooxytetrahydronaphthaline) has antiviral activity. Tetraxolin has been shown to be active against Herpes simplex, Herpes zoster, adenoviruses, infectious wart viruses and molluscum contagiosum. It is used as 0.25% ointment and aqueous solutions for the treatment of viral rhinitis, keratoconjunctivitis,and for the prophylaxis of influenza. 1970-11-12 Ministry of Health of the Russian Federation
Click to view tilorone Neuronal acetylcholine receptor subunit alpha-7 (Organism: Homo sapiens, class: Ion channel, accessions: P36544, gene: CHRNA7, swissprot: ACHA7_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/18157163) Tilorone is the first recognized synthetic, small molecular weight compound that is an orally active interferon inducer. Tilorone induces the formation of interferons (alpha, beta, gamma) by intestinal epithelial cells, hepatocytes, T-lymphocytes, and granulocytes. The mechanism of antiviral action is associated with the inhibition of translation of virus-specific proteins in infected cells, thereby suppressing the replication of the virus. Effective against influenza viruses and viruses that cause ARVI, hepato- and herpesviruses, incl. CMV and others. Tilorone is indicated for the treatment of hepatitis B and C virus infections, influenza, herpes simplex virus infections and acute respiratory tract infections. 1996-06-18 Ministry of Health of the Russian Federation
Click to view trimeperidine Trimeperidine (promedol) is a narcotic analgesic similar to meperidine. It exists in four stereoisomers, two of which, the beta (isopromedol) and the gamma (trimeperidine) are active. It has been used to treat shock (low blood pressure and heartbeat abnormality). Currently it is used for the relief of pain. Also trimeperidine is used for the treatment of left ventricular failure, pulmonary oedema, poisoning by barbiturates, toxic effect of carbon monoxide, and formaldehyde. 1998-04-09 Ministry of Health of the Russian Federation
Click to view troclosene Troclosene is chlorinated hydroxytriazine and it is used as a source of free available chlorine, in the form of hypochlorous acid, for the disinfection of water. Troclosene is used for the preparation of a wide spectrum disinfectant solution effective against vegetative bacteria, fungi, viruses and bacterial spores for disinfection of hard surfaces. In addition, efficacy has been demonstrated against Clostridium difficile, Methicillin Resistant Staphylococcus aureus, Canine Parvovirus and Feline Panleukopenia virus. 1968-12-31 Health Canada
Click to view trospium chloride Trospium chloride is an organic chloride salt of trospium. Trospium chloride is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. (See: trospium) 2004-05-28 FDA
Click to view bromdihydrochlorphenylbenzodiazepine GABA-A receptor; anion channel (Organism: Rattus norvegicus, class: Ion channel, accessions: P62813|P23576|P20236|P28471|P19969|P30191|P15431|P63138|P63079|P18506|P23574|P18508|P28473|Q9ES14|O09028|Q91ZM7, gene: Gabra1|Gabra2|Gabra3|Gabra4|Gabra5|Gabra6|Gabrb1|Gabrb2|Gabrb3|Gabrd|Gabrg1|Gabrg2|Gabrg3|Gabre|Gabrp|Gabrq, swissprot: GBRA1_RAT|GBRA2_RAT|GBRA3_RAT|GBRA4_RAT|GBRA5_RAT|GBRA6_RAT|GBRB1_RAT|GBRB2_RAT|GBRB3_RAT|GBRD_RAT|GBRG1_RAT|GBRG2_RAT|GBRG3_RAT|GBRE_RAT|GBRP_RAT|Q91ZM7_RAT) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/11485032) Bromdihydrochlorphenylbenzodiazepine (phenazepam) belongs to the 1,4-benzodiazepines. Phenazepam and its metabolites potentiate GABA responses. In vivo, phenazepam induces pronounced myorelaxation. Both phenazepam and its metabolite 3-hydroxyphenazepam are full GABAA receptor agonists. Bromdihydrochlorphenylbenzodiazepine is used as an anxiolytic for the treatment of insomnia, anxiety, phobias, epilepy, neurasthenia. 1977-11-10 Ministry of Health of the Russian Federation
Click to view ferramid Ferramid is a complex of nicotinamide with FeCl2. It is used for the treatment of iron deficiency anaemia. 1974-07-29 Ministry of Health of the Russian Federation
Click to view flakosid Flakosid (Glucopyranosidemethylbuteniltrihydroxyflavanol) is a herbal substance (from the leaves of the Amur velvet, Phellodendron amurensis Rupr., and leaves velvet Laval, Phellodendron amurensis var. Lavallei Sprague, SEM. Rutaceae (Rutaceae)). Flakosid has antiviral, hepatoprotect and antioxidant actions. It was used for the treatment of herpes simplex virus infections. Also it was used for the treatment of herpes zoster and hepatitis infections. 1990-06-19 Ministry of Health of the Russian Federation
Click to view fludarabine Fludarabine is a purine analogue and antineoplastic agent used in the therapy of chronic lymphocytic leukemia and in immunosuppressive regimens in preparation of hematopoietic cell transplantation. (See: fludarabine phosphate)
Click to view fludrocortisone Mineralocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P08235, gene: NR3C2, swissprot: MCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8282004) Glucocorticoid receptor (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: P04150, gene: NR3C1, swissprot: GCR_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/8282004) Fludrocortisone is a mineralocorticoid receptor and glucocorticoid receptor agonist that binds to cytoplasmic receptors, translocates to the nucleus and subsequently initiates the transcription of glucocorticoid-responsive genes such as lipocortins to inhibit phospholipase A2. This prevents the release of arachidonic acid, a precursor to important mediators in the pro-inflammatory response mechanism. This agent exerts its mineralocorticoid effect on the distal tubules and collecting ducts of the kidney by inducing permease, an enzyme that regulates Na+ permeability in cells, thereby enhancing Na+ reabsorption and water retention as well as increasing K+, H+ excretion. Fludrocortisone is used for partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison’s disease and for the treatment of salt losing adrenogenital syndrome. Anti-Inflammatory Agents (Code: D000893) 1991 Hungary National Institute of Pharmacy and Nutrition ZK5
Click to view fluorescein sodium Multidrug resistance-associated protein 1 (Organism: Mus musculus, class: Transporter, accessions: O35379, gene: Abcc1, swissprot: MRP1_MOUSE) substrate (Source: https://www.ncbi.nlm.nih.gov/pubmed/11409873) Fluorescein sodium is a xanthene dye that is highly fluorescent, detectable even when present in minute quantities. Fluorescein sodium responds to electromagnetic radiation and light between the wavelengths of 465-490 nm and fluoresces, i.e., emits light at wavelengths of 520-530 nm. Following intravenous injection of fluorescein sodium in an aqueous solution, the unbound fraction of the fluorescein can be excited with a blue light flash from a fundus camera as it circulates through the ocular vasculature, and the yellowish green fluorescence of the dye is captured by the camera. In the fundus, the fluorescence of the dye demarcates the retinal and/or choroidal vasculature under observation, distinguishing it from adjacent areas/structures. Fuorescein sodium is used intravenously in diagnostic fluorescein angiography or angioscopy of the retina and iris vasculature. fluorescent dye (Code: CHEBI:51121) radioopaque medium (Code: CHEBI:37338) Diagnostic Dye (Code: N0000175536) Dyes (Code: N0000175533) Coloring Agents (Code: D004396) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) Fluorescent Dyes (Code: D005456) 1976-11-10 FDA FLU
Click to view fluticasone Fluticasone is a medium-potency synthetic trifluorinated corticosteroid which is used in some countries to manage nasal symptoms of allergic and non-allergic rhinitis. Fluticasone binds and activates glucocorticoid receptor, resulting in the activation of lipocortin. Fluticasone isused in the form of its propionate ester or furoate ester to manage nasal symptoms of allergic and non-allergic rhinitis. (See: fluticasone propionate) (See: fluticasone furoate) 1999-12-01 Ministry of Health of the Russian Federation
Click to view fosenazide Fosenazide is a tranquilizer. It possesses the central N-cholinolytic, antiadrenergic and antiserotonin effects. Fosenazide is used for the treatment of alcohol withdrawal state with delirium and alcohol psychotic disorder. 1995-07-20 Ministry of Health of the Russian Federation
Click to view chinifuryl Chinifuryl (quinifuryl) is an antiseptic agent. Quinifuryl is active against gram-positive and gram-negative bacteria. It is used for the treatment of wounds burns, and skin and skin structure infections. 1991-11-29 Ministry of Health of the Russian Federation
Click to view chlornitrophenol Chloronitrophenol is an antifungal agent for topical use. Chloronitrophenol is active against Microsporum canis, Trichophyton gypseum, Candida albicans. In high concentrations, it is active against gram-positive and gram-negative bacteria. 2007-08-17 Ministry of Health of the Russian Federation P9P
Click to view choline salicylate Choline salicylate is an anti-inflammatory pain reliever agent. Choline salicylate has actions similar to those of aspirin, i.e. analgesic, antiinflammatory and anti-pyretic actions considered to be due to inhibition of the biosynthesis of prostaglandins. Choline Salicylate is the choline salt of salicylic acid, used as an analgesic, antipyretic and antirheumatic. It is used to decrease swelling and to treat mild-moderate pain. It is used for the symptomatic relief of pain in infant teething, otitis externa, mouth ulcers. (See: salicylic acid) 1981-07-31 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view chondroitin sulfate Chondroitin sulfate belongs to the group of glycosaminoglycans. Chondroitin sulfate is a major component of the extracellular matrix of many connective tissues, including cartilage, bone, skin, ligaments and tendons. Chondroitin sulfate is usually manufactured from animal sources, such as shark and cow cartilage. Chondroitin sulfate is used for osteoarthritis. It is often used in combination with other ingredients, including manganese ascorbate, glucosamine sulfate, glucosamine hydrochloride, or N-acetyl glucosamine. Chondroitin sulfate is available as an eye drop for dry eyes. In addition, it is used during cataract surgery, and as a solution for preserving corneas used for transplants. 1972-02-01 PMDA
Click to view cianamid Cyanamide is a nitrile that is hydrogen cyanide in which the hydrogen has been replaced by a methyl group. This white solid is widely used in agriculture and the production of pharmaceuticals and other organic compounds. It is also used as an alcohol-deterrent drug. Cyanamide exists as two tautomers. Cyanamide is used in the treatment of alcoholism. 2010-03-26 Ministry of Health of the Russian Federation
Click to view cyanocobalamin Cyanocobalamin is a synthetic form of vitamin B12 with equivalent vitamin B12 activity. Cyanocobalamin is a cobalt-containing coordination compound generated by intestinal microbes, and a natural water-soluble vitamin of the B-complex family that must combine with Intrinsic Factor for absorption by the intestine. Cyanocobalamin is necessary for hematopoiesis, neural metabolism, DNA and RNA production, and carbohydrate, fat, and protein metabolism. Cyanocobalamin improves iron functions in the metabolic cycle and assists folic acid in choline synthesis. Cyanocobalamin metabolism is interconnected with that of folic acid. Vitamin B12 deficiency causes pernicious anemia, megaloblastic anemia, and neurologic lesions. Cyanocobalamin as nasal spray is indicated for the maintenance of vitamin B12 concentrations after normalization with intramuscular vitamin B12 therapy in patients with deficiency of this vitamin who have no nervous system involvement. Injection forms of cyanocobalamin are indicated for vitamin B12 deficiencies due to various causes, with or without neurologic manifestations. Vitamin B12 tabletes are indicated in patients who require supplementation for various reasons. Dose requirements for vitamin B12 which are higher than normal (caused by pregnancy, thyrotoxicosis, hemolytic anemia, hemorrhage, malignancy, hepatic and renal disease) can usually be achieved with oral supplementation. Oral products of vitamin B12 are not recommended in patients with malabsorption, as these forms are primarily absorbed in the gastrointestinal tract. Vitamin B 12 (Code: N0000006276) Vitamin B12 (Code: N0000175951) 1949-09-15 FDA
Click to view cyproterone Cyproterone is a steroidal antiandrogen. It suppresses testosterone and its metabolites. Cyproterone, in its acetate form, binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation and inhibiting the growth of testosterone-sensitive tumor cells. It has approximately three-fold lower potency as an antagonist of the androgen receptor relative to cyproterone acetate. (See: cyproterone acetate)
Click to view cisplatin An inorganic and water-soluble platinum complex. After undergoing hydrolysis, it reacts with DNA to produce both intra and interstrand crosslinks. These crosslinks appear to impair replication and transcription of DNA. The cytotoxicity of cisplatin correlates with cellular arrest in the G2 phase of the cell cycle.
Click to view cystamine Cysteamine is an organic disulfide obtained by oxidative dimerisation of cysteamine. Cystamine dihydrochloride is a useful reagent to derivatize various polymer monoliths for hydrophilic interaction liquid chromatography, as a crosslinking agent in the development of polymer hydrogels, and as a functional group in nanoparticles developed for siRNA and DNA delivery. In medicine cysteamine is used as a radioprotective agent. 2005-05-20 Ministry of Health of the Russian Federation
Click to view citrulline malate Citrulline malate is a mixture of citrulline which is involved in the urea cycle, and malate which improves muscle performance of patients suffering from asthenia. It is used as a nutritional supplement for the symptomatic relief of asthenia. (See: citrulline) 2000-03-15 Spanish Agency of Medicines and Medical Products (AEMPS)
Click to view exametazime Exametazime is known as hexamethylpropylene amine oxime. Exametazime is a diagnostic radiopharmaceutical agent commonly used for the preparation of Tc99m Exametazime injection. It acts as a chelating agent for the radioisotope technetium-99m to form a cationic lipophilic complex which is able to cross the blood-brain barrier as well as penetrate cell membranes to label leukocytes. It is used in leukocyte labeled scintigraphy (as an adjunct in the localization of intraabdominal infection and inflammatory bowel disease) and cerebral scintigraphy (as an adjunct in the detection of altered regional cerebral perfusion in stroke). Radioactive Diagnostic Agent (Code: N0000177914) Radiopharmaceutical Activity (Code: N0000000205) Diagnostic Uses of Chemicals (Code: D064907) Indicators and Reagents (Code: D007202) Radiopharmaceuticals (Code: D019275) 1988-12-30 FDA
Click to view emoxipin Emoxipin (methylethylpiridinol) is a 3-oxypyridine derivative and an anti-oxidant and an anti-hypoxant . It reduces permeability of vascular wall, viscosity and coagulability of blood, agglutination ability of erythrocytes, increases process of fibrinolysis and mproves microcirculation. Emoxipin inhibits free-radical oxidation of biomembranes lipids, increases activity of antioxidative enzymes. It is used in ophthalmology for the treatment of dystrophic changes of retina, diabetic retinopathy, glaucoma, hemophthalmias, hyphemas, keratites, keratoconus, uveites. As a part of complex therapy it is used for the treatment of insult, chronic failure of cerebral circulation, myocardial infarction, angina pectoris and in postoperative period in patients with the craniocerebral trauma, arterial aneurysms and arteriovenous malformations of brain vessels. 2006-09-08 Ministry of Health of the Russian Federation
Click to view escin Pentacyclic triterpene saponins, biosynthesized from protoaescigenin and barringtogenol, occurring in the seeds of AESCULUS. It inhibits edema formation and decreases vascular fragility.
Click to view etamsylate Etamsylate is a sulfonic acid derivative and an organosulfur compound. Etamsylate is a veno-tonic drug. It was suggested, that the inhibitory effect of etamsylate on platelet function is mediated through the cyclic AMP pathway, and probably through activation of adenyl cyclase. It is used for the treatment and prevention of hemorrhages and for the control of haemorrhage after surgery. Coagulants (Code: D003029) Hematologic Agents (Code: D006401) Hemostatics (Code: D006490) 1987-04-22 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view ethacizine Ethacizine (Diaethylaminopropyonylaethoxycarbonylaminophenothiazin) is a class Ic antiarrhythmic agent, related to moracizine. It is used for the treatment of severe and/or refractory ventricular and supraventricular arrhythmias, especially those accompanied by organic heart disease. It is also indicated as a treatment of refractory tachycardia associated with Wolff–Parkinson–White syndrome. 1984-06-14 Ministry of Health of the Russian Federation
Click to view ethylthiobenzymidazol Ethylthiobenzymidazol (bemethyl) is an antihypoxant. Bemethyl increases physical performance. It is a tranquilizer and psyhostimulant. Bemethyl has positive influence on mental as well as physical work capacity under both normal and extreme conditions. Bemethyl is used for the treatment asthenic disorders. 1983-05-30 Ministry of Health of the Russian Federation
Click to view etimizol Etimizol (methylamide ethylimidazoledicarbonate) is a cognitive enhancer and nootropic drug, the molecular target of which is a multifunctional protein kinase casein kinase II. Etimizol activates casein kinase II. Etimizol excites respiratory center. It is indicated as a respiratory analeptic for the prevention and for the treatment of respiratory depression of various etiology. 1972-04-26 Ministry of Public Health USSR
Click to view abiraterone Steroid 17-alpha-hydroxylase/17,20 lyase (Organism: Homo sapiens, class: Enzyme, accessions: P05093, gene: CYP17A1, swissprot: CP17A_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 1A2 (Organism: Homo sapiens, class: Enzyme, accessions: P05177, gene: CYP1A2, swissprot: CP1A2_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 2C8 (Organism: Homo sapiens, class: Enzyme, accessions: P10632, gene: CYP2C8, swissprot: CP2C8_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 2C9 (Organism: Homo sapiens, class: Enzyme, accessions: P11712, gene: CYP2C9, swissprot: CP2C9_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 2D6 (Organism: Homo sapiens, class: Enzyme, accessions: P10635, gene: CYP2D6, swissprot: CP2D6_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 3A5 (Organism: Homo sapiens, class: Enzyme, accessions: P20815, gene: CYP3A5, swissprot: CP3A5_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) substrate (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/210308s000lbl.pdf) Cytochrome P450 11B1, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P15538, gene: CYP11B1, swissprot: C11B1_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18672868) Cytochrome P450 11B2, mitochondrial (Organism: Homo sapiens, class: Enzyme, accessions: P19099, gene: CYP11B2, swissprot: C11B2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/18672868) Abiraterone is an androgen biosynthesis inhibitor, that inhibits 17 alpha-hydroxylase/C17,20-lyase (CYP17). This enzyme is expressed in testicular, adrenal, and prostatic tumor tissues and is required for androgen biosynthesis. Inhibition of CYP17 by abiraterone can also result in increased mineralocorticoid production by the adrenals. Androgen sensitive prostatic carcinoma responds to treatment that decreases androgen levels. AER
Click to view imidazolyl ethanamide pentandioic acid Imidazolyl ethanamide pentandioic acid is an orally bioavailable small molecule, with potential hematopoiesis inducing and antiviral activities. Its exact mechanism of action is unknown. It is used for the treatment and prevention of influenza. 2007-03-27 Ministry of Health of the Russian Federation
Click to view 2-hydroxybutanedioic acid 2-hydroxybutanedioic acid (malic acid) is a 2-hydroxydicarboxylic acid that is succinic acid in which one of the hydrogens attached to a carbon is replaced by a hydroxy group. Malic acid is a tart-tasting organic dicarboxylic acid that plays a role in many sour or tart foods. In its ionised form it is malate, an intermediate of the TCA cycle along with fumarate. It can also be formed from pyruvate as one of the anaplerotic reactions. Malic Acid has been used in trials studying the treatment of xerostomia, depression, and hypertension. 2015-07-22 Ministry of Health of the Russian Federation LMR
MLT
Click to view bromanilidediethylaminopropanic acid Bromanilidediethylaminopropanic acid is used for the local anesthesia. 1997-10-03 Ministry of Health of the Russian Federation
Click to view folinic acid Folinic Acid (also known as 5-formyl tetrahydrofolic acid or leucovorin) is the 5-formyl derivative of tetrahydrofolic acid, a necessary co-factor in the body. Commercially available leucovorin is composed of a 1:1 racemic mixture of the dextrorotary and levorotary isomers, while levoleucovorin contains only the pharmacologically active levo-isomer. It is indicated for use as rescue therapy following use of high-dose methotrexate in the treatment of osteosarcoma or for diminishing the toxicity associated with inadvertent overdosage of folic acid antagonists. Injectable forms are also indicated for use in the treatment of megaloblastic anemias due to folic acid deficiency when oral therapy is not feasible and for use in combination with 5-fluorouracil to prolong survival in the palliative treatment of patients with advanced colorectal cancer. Antidotes (Code: D000931) Protective Agents (Code: D020011) antineoplastic agent (Code: CHEBI:35610) Folate Analog (Code: N0000178369) Folic Acid (Code: N0000007151) Antidotes (Code: D000931) Growth Substances (Code: D006133) Micronutrients (Code: D018977) Vitamins (Code: D014815) Protective Agents (Code: D020011) Vitamin B Complex (Code: D014803) Analogs/Derivatives (Code: N0000175452) leucovorin: 1952-06-20 FDA folinic acid: 2008-03-07 FDA FFO
FON
Click to view formic acid Free fatty acid receptor 2 (Organism: Homo sapiens, class: GPCR, accessions: O15552, gene: FFAR2, swissprot: FFAR2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/21220428) Formic acid is the simplest carboxylic acid, containing a single carbon. Occurs naturally in various sources including the venom of bee and ant stings, and is a useful organic synthetic reagent. Principally used as a preservative and antibacterial agent in livestock feed. Induces severe metabolic acidosis and ocular injury in human subjects. In medicine 85% formic acid application is a safe, economical, and effective alternative in the treatment of common warts with few side-effects and good compliance. 1973-06-15 Ministry of Health of the Russian Federation FMT
Click to view gadobenic acid used in MR imaging of liver
Click to view hyaluronic acid Hyaluronic acid is an anionic, nonsulfated glycosaminoglycan distributed widely throughout connective, epithelial, and neural tissues. It is unique among glycosaminoglycans in that it is nonsulfated, forms in the plasma membrane instead of the Golgi, and can be very large, with its molecular weight often reaching the millions. One of the chief components of the extracellular matrix, hyaluronic acid contributes significantly to cell proliferation and migration, and may also be involved in the progression of some malignant tumors. It is naturally synthesized by a class of integral membrane proteins called hyaluronan synthases, and degraded by a family of enzymes called hyaluronidases. Exogenous hyaluronic acid enhances chondrocyte HA and proteoglycan synthesis, reduces the production and activity of proinflammatory mediators and matrix metalloproteinases, and alters the behavior of immune cells. Hyaluronic acid is used as a sodium hyaluronate to treat knee pain in patients with osteoarthritis. Hyaluronic acid may also be used in plastic surgery to reduce wrinkles on the face or as a filler in other parts of the body. May be used in ophthalmology to assist in the extraction of cataracts, the implantation of intraocular lenses, corneal transplants, glaucoma filtration, retinal attachment and in the treatment of dry eyes. Finally, hyaluronic acid is also used to coat the bladder lining in treating interstitial cystitis.
Click to view adamantilbromphenylamine Adamantilbromphenylamine (bromantane) is an atypical psychostimulant and anxiolytic drug of the adamantane family. Adamantilbromphenylamine has stimulatory and selective anxiolytic effects. adamantilbromphenylamine's effect manifested in the increase in physical and mental activity, deceleration of fatigue, rapid recovery of activity and improvenet of mnesic performance and learning. adamantilbromphenylamine has a positive effect on cognitive functions. Adamantilbromphenylamine is used for the treatment of neurasthenia and asthenia. 2008-11-21 Ministry of Health of the Russian Federation
Click to view ethonium Ethonium is an antimicrobial drug of the group of cationic surface-active substances. Ethonium is used as an antimicrobial agent for wound healing in surgical and stomatological practice. 1998-06-01 Ministry of Health of the Russian Federation
Click to view ethylbromisovalerinate Ethylbromisovalerinate (ethyl alpha-bromoisovalerate) has a sedative, hypnotic and spasmolytic effect. Ethylbromisovalerinate is used in combination with phenobarbital and menthol for the treatment of functional disorders of the cardiovascular system, neuroses accompanied by irritability, anxiety, fear, insomnia. 1972-04-26 Ministry of Health of the Russian Federation
Click to view ethylmethylhydroxypyridine malate Ethylmethylhydroxypyridine malate is a 3-hydroxypyridine derivative. It is used as cardioprotective drug due to its antihypoxic and antioxidant actions. 2010-02-03 Ministry of Health of the Russian Federation
Click to view ethylmethylhydroxypyridine succinate Ethylmethylhydroxypyridine succinate is a derivative of 3-oxopyridine. It has cerebroprotective and endotheliotropic activities. It is used for the treatment of post-stroke conditions, coronary heart disease, heart failure, stroke, abstinence syndrome and encephalopathy. 1996-12-31 Ministry of Health of the Russian Federation
Click to view allyloxyethanol Allyloxyethanol (lioxasol) is an ethyl alcohol based product. It helps decrease local pain sensation, control skin cell disintegration and stimulate skin-cell regeneration. It was used for the topical treatment of local radiation injuries. 2006-12-08 Ministry of Health of the Russian Federation
Click to view alfa-glutamyl-triptophan Alfa-glutamyl-triptophan (oglufanide) is a synthetic dipeptide immunomodulator composed of glutamate and tryptophan. It belongs to the family of N-acyl-alpha amino acids and derivatives. Alfa-glutamyl-triptophan works as a regulator of the body's immune response and is being given by intranasal administration to patients with chronic hepatitis C viral infection. It is used for the treatment of severe infectious disease (such as acute respiratory tract infections). Also it is used in immunosuppressed conditions, after chemo- and radio-therapy. 1990-06-19 Ministry of Health of the Russian Federation
Click to view aminodihydrophthalasindione sodium Aminodihydrophthalasindione sodium (luminol) is an immunomodulator. Aminodihydrophthalasindione is a monosodium alpha-luminol. Galavit reduces production of inflammatory cytokines such as TNF-alpha, IL-1, inhibits hyperactivity of macro-phages. Aminodihydrophthalasindione is used for the treatment of gastrointestinal infections, herpes infections and surgical infections. 2005-08-05 Ministry of Health of the Russian Federation
Click to view aminostigmin Aminostigmin is a reversible inhibitor of cholinesterase which is used as an antidote in cholinolytic poisoning. 1984-06-16 Ministry of Health of the Russian Federation
Click to view ammonium glycyrrhizinate Ammonium glycyrrhizinate is an ammonium salt of glycyrrhizic acid. It is used for the treatment of respiratory tract disease. Also it is used as a nutritional supplement. (See: glycyrrhizic acid) Anti-Inflammatory Agents (Code: D000893) 1976-03-15 Ministry of Health of the Russian Federation
Click to view amylnitrite Amylnitrite is an antihypertensive medicine. Amylnitrite's antianginal action is thought to be the result of a reduction in systemic and pulmonary arterial pressure (afterload) and decreased cardiac output because of peripheral vasodilation, rather than coronary artery dilation. Amyl nitrite is a source of nitric oxide, which accounts for the mechanism described above. As an antidote (to cyanide poisoning), amyl nitrite promotes formation of methemoglobin, which combines with cyanide to form nontoxic cyanmethemoglobin. Amylnitrite is used medically to treat heart diseases such as angina and to treat cyanide poisoning. As an inhalant, it also has psychoactive effect which has led to illegal drug use. 1951-12-31 Health Canada
Click to view aprofene Aprofene is an antagonist of muscarinic and nicotinic acetylcholine receptors. It has been used for the treatment of peptic ulcer, spastic colitis, cholecystitis until was included in the list of psychotropic substances. 1970-03-17 Ministry of Health of the Russian Federation
Click to view sulfathiazole silver Sulfathiazole silver (argosulfan) is used as an ointment for the treatment of infection in burns, bedsores and leg ulcers. (See: sulfathiazole) 1990-03-08 The Office for Registration of Medicinal Products, Medical Devices and Biocidal Products (Poland)
Click to view arginine aspartate Arginine Aspartate is a salt composed of L-arginine combined with aspartic acid. Arginine combined with aspartate is used for better absorption. It is used for the treatment of asthenia and in statural delays. (See: arginine) (See: aspartic acid) 1984-04-02 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view arginine glutamate Arginine glutamate is a mixture of two amino acids, arginine and glutamic acid. It is used in liver therapy for the treatment of cirrhosis, hepatitis, poisoning by alcohol, drugs and other substances. Also it is used for the treatment of asthenia. 1992-05-13 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view atorvastatin calcium Atorvastatin calcium is an organic calcium salt composed of calcium cations and atorvastatin anions in a 1:2 ratio. Atorvastatin calcium is used as an adjunct therapy to diet to reduce the risk of miocardial infarction, stroke, revascularization procedures, and angina. Also it is used to reduce total-C, LDL-C, apo B, and TG levels and increase HDLC in adult patients with primary hyperlipidemia, mixed dyslipidemia, primary dysbetalipoproteinemia or homozygous familial hypercholesterolemia, heterozygous familial hypercholesterolemia. (See: atorvastatin)
Click to view azapentacene Azapentacene has been used for the treatment of cataract. 2004-11-10 Ministry of Health of the Russian Federation
Click to view aziridinylmethylthiazolidinylphosphineoxide Aziridinylmethylthiazolidinylphosphineoxide (imiphos) is one of the phosphor-organic compounds of alkali type which contains the active mutagen aziridine. Imiphos has an antitumor activity. It suppresses erythropoiesis. It was used for the treatment of erythremia (polycythemia vera). 1975-09-19 Ministry of Public Health USSR
Click to view benzobarbital Benzobarbital is a barbiturate derivative. It is used to treat convulsive forms of epilepsy, newborn hemolytic disease, and insomnia. 1970-03-30 Ministry of Health of the Russian Federation
Click to view benzoclidine Benzoclidine has tranquilizing and hypotensive actions. It reduces the excitability of the central nervous system, enhances the effect of hypnotic drugs, analgesics and local anesthetics, has a moderate antihypertensive effect, reduces the excitability of the vasomotor centers, has anti-arrhythmic activity. Benzoclidine was used for the treatment of insomnia, hypertension, depression of various origins (particularly mild expressed and associated with cerebrovascular insufficiency), neurosis, personality disorder. 1971-07-14 Ministry of Health of the Russian Federation
Click to view beta-alanine Sodium- and chloride-dependent GABA transporter 3 (Organism: Homo sapiens, class: Transporter, accessions: P48066, gene: SLC6A11, swissprot: S6A11_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23886812) Sodium- and chloride-dependent GABA transporter 2 (Organism: Homo sapiens, class: Transporter, accessions: Q9NSD5, gene: SLC6A13, swissprot: S6A13_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/23886812) Sodium- and chloride-dependent GABA transporter 1 (Organism: Mus musculus, class: Transporter, accessions: P31648, gene: Slc6a1, swissprot: SC6A1_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21353350) Sodium- and chloride-dependent GABA transporter 2 (Organism: Mus musculus, class: Unclassified, accessions: P31649, gene: Slc6a13, swissprot: S6A13_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21353350) Sodium- and chloride-dependent GABA transporter 3 (Organism: Mus musculus, class: Unclassified, accessions: P31650, gene: Slc6a11, swissprot: S6A11_MOUSE) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/21353350) Beta-alanine is the only naturally occurring beta-amino acid formed in vivo by the degradation of dihydrouracil and carnosine and an endogenous agonist of glycine receptor. Beta-alanine has been shown to enhance muscular endurance and its supplementation appears to be most effective for exercise tasks that rely heavily on ATP synthesis from anaerobic glycolysis. Chronically high levels of beta-alanine are associated with at least three inborn errors of metabolism, including GABA-transaminase deficiency, hyper-beta-alaninemia, and methylmalonate semialdehyde dehydrogenase deficiency. Beta-Alanine is a biomarker for the consumption of meat. 1991-09-23 ANSM (French National Agency for Medicines and Health Products Safety) BAL
Click to view biclotymol Biclotymol is a phenolic antiseptic. It has bacteriostatic, bactericidal, anti-inflammatory and analgesic activity. Biclotymol is recommended as a prompt, effective and safe first-line option for the treatment of sore throat. Also it is indicated for the treatment of pharyngitis, gingivitis, stomatitis. 1991-08-30 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view bretylium tosylate Bretylium tosylate is the tosylate salt form of bretylium, a quaternary ammonium salt and non-selective adrenergic neuronal blocking agent with anti-arrhythmic properties. Bretylium tosylate is selectively taken up into peripheral nerve terminals and initially causes a release of norepinephrine from sympathetic nerve endings, thereby causing a sympathomimetic effect. This is followed by a prolonged anti-adrenergic action which prevents further discharge of neurotransmitter from sympathetic nerve endings. Its myocardial effects include a prolongation of action potential as well as refractory period. Bretylium tosylate is used to treat and suppress ventricular arrhythmias, particularly ventricular fibrillation and ventricular tachycardia. (See: bretylium) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Anti-Arrhythmia Agents (Code: D000889) Antihypertensive Agents (Code: D000959) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) 1978 FDA
Click to view gamma-oxybutyric acid, calcium salt Gamma-oxybutyric acid, calcium salt is a nootropic. lt exerts moderate tranquillizing action, increases the thershold of emotional reaction. It has sedative and muscle-relaxing actions. Gamma-oxybutyric acid (4-hydroxybutyric acid, GHB) is a precursor and a metabolite of gamma-aminobutyric acid (GABA). GHB acts as a central nervous system neuromodulator, mediating its effects through GABA and GHB-specific receptors, or by affecting dopamine transmission. In high doses, GHB inhibits the CNS, inducing sleep and inhibiting the respiratory drive. Gamma-oxybutyric acid, calcium salt was used in mental and behavioural disorders due to use of alcohol, for the treatment of insomnia and other disorders of autonomic nervous system. GHB is labeled as an illegal drug in most countries, but it also is used as a legal drug (Xyrem) in patients with narcolepsy. (See: sodium oxybate)
Click to view valproate calcium Valproate calcium is a calcium salt of valproic acid. Valproate calcium is a tablet form of valproic acid. (See: valproic acid)
Click to view capreomycin Cyclic peptide antibiotic similar to VIOMYCIN. It is produced by Streptomyces capreolus.
Click to view carbocisteine lysine salt Carbocisteine lysine salt restores the viscosity and elasticity of the mucous secretions at the upper and lower airways. Its efficacy seems to be due to the capacity of increasing the synthesis of sialomucins. Carbocisteine lysine salt stimulates the secretion of chloride ions in the epithelium of the airways. Carbocisteine lysine salt increases the concentration of lactoferrin, lisozyme and alpha1-antichymotrypsin. Carbocisteine lysine salt is used as a mucolytic drug, fluidifying agent in the acute and chronic diseases of the respiratory system. (See: carbocisteine) 2008-11-01 Italian Medicines Agency (AIFA)
Click to view cefditoren Cefditoren is a cephalosporin with antibacterial activity against gram-positive and gram-negative pathogens. The bactericidal activity of cefditoren results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). Cefditoren is stable in the presence of a variety of beta-lactamases, including penicillinases and some cephalosporinases. Cefditoren has been shown to be active against Staphylococcus aureus (methicillin-susceptible strains, including beta-lactamase-producing strains), Streptococcus pneumoniae (penicillin-susceptible strains only), Streptococcus pyogenes, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis. Cefditoren is indicated for the treatment of Acute Bacterial Exacerbation of Chronic Bronchitis, Community-Acquired Pneumonia, Pharyngitis/Tonsillitis, Uncomplicated Skin and Skin-Structure Infections. Bound
Click to view cefpodoxime Cefpodoxime is a bactericidal agent that acts by inhibition of bacterial cell wall synthesis. Cefpodoxime has activity in the presence of some beta-lactamases, both penicillinases and cephalosporinases. Cefpodoxime has been shown to be active against Staphylococcus aureus (methicillin-susceptible strains), Staphylococcus saprophyticus, Streptococcus pneumoniae (excluding penicillin-resistant isolates), Streptococcus pyogenes, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae. Cefpodoxime proxetil is indicated for the treatment of acute otitis media (due to S. pneumoniae (excluding penicillin-resistant strains), S. pyogenes, H. influenzae, or M. catarrhalis), pharyngitis/tonsillitis (due to S. pyogenes), community-acquired pneumonia (due to S. pneumoniae or H. Influenzae), acute bacterial exacerbation of chronic bronchitis (due to S. pneumoniae, H. influenzae (non-beta-lactamase-producing strains only), or M. catarrhalis) , gonorrhea (due to Neisseria gonorrhoeae), skin and skin structure infections (due to S. aureus or S. pyogenes) and acute maxillary sinusitis (due to H. influenzae, S. pneumoniae, and M. catarrhalis). 1990-08-02 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view ceftobiprole Pencillin binding protein 2a (Organism: Staphylococcus aureus, class: Unclassified, accessions: O54286, gene: mecA, swissprot: O54286_STAAU) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200217/2c5ec323a1bde44f86f30f430636416fbd31f0c5) Penicillin-binding protein 2B (Organism: Streptococcus pneumoniae (strain ATCC BAA-255 / R6), class: Enzyme, accessions: P0A3M6, gene: penA, swissprot: PBP2_STRR6) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200217/2c5ec323a1bde44f86f30f430636416fbd31f0c5) Solute carrier organic anion transporter family member 1B1 (Organism: Homo sapiens, class: Transporter, accessions: Q9Y6L6, gene: SLCO1B1, swissprot: SO1B1_HUMAN) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200217/2c5ec323a1bde44f86f30f430636416fbd31f0c5) Solute carrier organic anion transporter family member 1B3 (Organism: Homo sapiens, class: Transporter, accessions: Q9NPD5, gene: SLCO1B3, swissprot: SO1B3_HUMAN) inhibitor (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200217/2c5ec323a1bde44f86f30f430636416fbd31f0c5) Solute carrier family 22 member 2 (Organism: Homo sapiens, class: Transporter, accessions: O15244, gene: SLC22A2, swissprot: S22A2_HUMAN) substrate (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200217/2c5ec323a1bde44f86f30f430636416fbd31f0c5) Solute carrier family 22 member 6 (Organism: Homo sapiens, class: Transporter, accessions: Q4U2R8, gene: SLC22A6, swissprot: S22A6_HUMAN) substrate (Source: https://mhraproductsprod.blob.core.windows.net/docs-20200217/2c5ec323a1bde44f86f30f430636416fbd31f0c5) Ceftobiprole is a fifth-generation cephalosporin antibiotic. Ceftobiprole exerts bactericidal activity through binding to important penicillin-binding proteins (PBPs) in susceptible species. In Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), Ceftobiprole binds to PBP2a. Ceftobiprole has demonstrated in vitro activity against strains with divergent mecA homolog (mecC or mecALGA251). Ceftobiprole also binds to PBP2b in Streptococcus pneumoniae (penicillinintermediate), PBP2x in S. pneumoniae (penicillin resistant), and to PBP5 in Enterococcus faecalis. Ceftobiprole is indicated for the treatment of hospital-acquired or community-acquired pneumonia. Also it is used for the treatment of local skin infection. 2009-03-20 Ministry of Health of the Russian Federation
Click to view chinoxydin Chinoxydin is a quinoxaline derivative. It has an antibacterial activity. It was used for the treatment of cystitis, cholecystitis, cholangitis, lung abscess, pleural empyema, sepsis caused by gram-negative microorganisms resistant to other antibiotics. 1976-05-18 Ministry of Health of the Russian Federation
Click to view chlorhexidine bigluconate Chlorhexidine bigluconate is a water-soluble form of chlorhexidine. Chlorhexidine bigluconate is used in water-based formulations as an antiseptic. (See: chlorhexidine)
Click to view choline theophyllinate Choline theophyllinate (oxtriphylline) is the choline salt of theophylline with an anti-asthmatic property. Its pharmacologic action is the same as that of theophylline. Its pharmacologic effects include stimulation of respiration, augmentation of cardiac inotropy and chronotropy, relaxation of smooth muscle, including that in the bronchi and blood vessels other than cerebral vessels, and diuresis. It appears to inhibit phosphodiesterase and prostaglandin production, regulates calcium flux and intracellular calcium distribution, and antagonizes adenosine. Oxtriphylline is reported to be more soluble, more stable, better absorbed from the GI tract and less irritating to the gastric mucosa than theophylline. (See: theophylline) 1951-12-31 Health Canada
Click to view neostigmine methylsulfate Neostigmine methylsulfate is a parenteral form of neostigmine. (See: neostigmine) Cholinesterase Inhibitor (Code: N0000175723) Autonomic Agents (Code: D001337) Cholinergic Agents (Code: D018678) Cholinesterase Inhibitors (Code: D002800) Enzyme Inhibitors (Code: D004791) Neurotransmitter Agents (Code: D018377) Parasympathomimetics (Code: D010277) Peripheral Nervous System Agents (Code: D018373) 1964-04-30 Ministry of Health of the Russian Federation
Click to view diaethylbensimidasolium tryiodide Diethylbenzimidazolium triiodide has local and system wide spectrum antibacterial activity, anti-inflammation and regenerating properties. It is used as a part of complex therapy for the treatment of bedsores, trophic ulcers, burns, postoperative and other wounds to speed up the regeneration processes. 2009-01-16 Ministry of Health of the Russian Federation
Click to view diglycidyl methylphosphonate Diglycidyl methylphosphonate (Glyciphon) is diglycidyl ether of methylphosphonic acid, which belongs to a class of organophosphors epoxides. It has antiblastoma activity, relatively low toxicity, and high safety when it was used long. Diglycidyl methylphosphonate inhibits DNA synthesis, retards all mitotic phases, and blocks the entry of cells into S and M phases. It is used for the treatment of Stage I squamous cell carcinoma, as well as basaliomas (including recurrences after surgery and radiotherapy), Bowen's disease, senile keratosis. 2011-10-18 Ministry of Health of the Russian Federation
Click to view dihydroergotoxine Dihydroergotoxine (ergoloid mesylate) is a mixture of three different hydrogenated derivatives of ergotamine (dihydroergocornine, dihydroergocristine, and dihydroergocryptine). All these components are produced by the fungus Claviceps purpurea and are all derivatives of the tetracyclic compound 6-methylergonovine. Dihydroergotoxine has been proposed to be a neuroprotective agent and a nootropic agent. The mechanism of its therapeutic actions is not clear, but it can act as an alpha-adrenergic antagonist and a dopamine agonist. It is used as a dihydroergotoxine mesylate (a mixture of the methanesulfonate salts of ergotamine) for the treatment of for the treatment of symptoms of an idiopathic decline in the mental capacity not related to a potentially reversible condition as well as for age-related cognitive impairment. Also it is used for the treatment of cerebrovascular disorders and migraine. alpha-adrenergic antagonist (Code: CHEBI:37890) vasodilator agent (Code: CHEBI:35620) sympatholytic agent (Code: CHEBI:66991) nootropic agent (Code: CHEBI:66980) Adrenergic Agents (Code: D018663) Adrenergic alpha-Antagonists (Code: D000317) Adrenergic Antagonists (Code: D018674) Cardiovascular Agents (Code: D002317) 1953-05-11 FDA
Click to view dihydroquercetin Amyloid beta A4 protein (Organism: Homo sapiens, class: Unclassified, accessions: P05067, gene: APP, swissprot: A4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26719209) Mast/stem cell growth factor receptor Kit (Organism: Homo sapiens, class: Kinase, accessions: P10721, gene: KIT, swissprot: KIT_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/26807861) Dihydroquercetin (taxifolin) is a natural phenolic compound found in Agrimonia pilosa Ledeb and in the plants of coniferae. Dihydroquercetin is a potent flavonoid. It was reported that dihydroquercetin can act as a scavenger of myeloperoxidase (MPO)-derived reactive nitrogen species. Also dihydroquercetin was able to downregulate the collagenase I (MMP-1) in UVB-treated skin cells. Dihydroquercetin is used for the treatment of respiratory tract infections (such as pneumonia, bronchitis), asthma. As a part of complex therapy dihydroquercetin is used for the treatment of ischaemic heart disease, arrhythmia. 1996-07-29 Ministry of Health of the Russian Federation DQH
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Click to view diindolylmethane Cyclin-dependent kinase inhibitor 1 (Organism: Mus musculus, class: Cytosolic other, accessions: P39689, gene: Cdkn1a, swissprot: CDN1A_MOUSE) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/20068155) Diindolylmethane is a natural product from cruciferous vegetables. Diindolylmethane has inhibitory effects on some tumors. Diindolylmethane selectively induced proteasome-mediated degradation of the class I histone deacetylases (HDAC1, HDAC2, HDAC3, and HDAC8) without affecting the class II HDAC proteins (HDAC4, 5, 6, 7, and 10). Diindolylmethane is used for supporting a more favorable metabolism of estrogen and supporting the production of 2 hydroxyestrone and 2-methoxyestrone, key metabolites in men and women. Diindolylmethane is used to treat cervical intraepithelial neoplasia. 2010-08-18 Ministry of Health of the Russian Federation
Click to view diphenyltropine Diphenyltropine (tropacine) is closely related to atropine in chemical structure and pharmacological properties. Diphenyltropine has a central cholinolytic effect. Diphenyltropine was used for the treatment of Parkinson's disease. Also it was indicated for the treatment of peptic ulcer, bronchial asthma, phosphorganic compounds poisoning and other cases os smooth muscle spasm. 1971-12-31 Ministry of Health of the Russian Federation
Click to view enisamium iodide Enisamium iodide is an isonicotinic acid derivative, that used as an antiviral agent. Enisamium iodide suppresses the effect of influenza viruses and other pathogens of acute respiratory viral infections due to a direct inhibitory effect on the penetration of viruses through the cell membrane. Enisamium has interferonogenic properties, promotes an increase in the concentration of endogenous interferon (interferon alfa and gamma) in blood plasma by 3-4 times. Enisamium iodide is used for the treatment and prevention of influenza. 1998-12-21 Ministry of Health of the Russian Federation
Click to view eslicarbazepine Sodium channel protein type 2 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q99250, gene: SCN2A, swissprot: SCN2A_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022416s011lbl.pdf) Sodium channel protein type 3 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9NY46, gene: SCN3A, swissprot: SCN3A_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022416s011lbl.pdf) Sodium channel protein type 4 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: P35499, gene: SCN4A, swissprot: SCN4A_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022416s011lbl.pdf) Sodium channel protein type 5 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q14524, gene: SCN5A, swissprot: SCN5A_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022416s011lbl.pdf) Sodium channel protein type 7 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q01118, gene: SCN7A, swissprot: SCN7A_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022416s011lbl.pdf) Sodium channel protein type 8 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q9UQD0, gene: SCN8A, swissprot: SCN8A_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022416s011lbl.pdf) Sodium channel protein type 9 subunit alpha (Organism: Homo sapiens, class: Ion channel, accessions: Q15858, gene: SCN9A, swissprot: SCN9A_HUMAN) blocker (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022416s011lbl.pdf) Cytochrome P450 2C19 (Organism: Homo sapiens, class: Enzyme, accessions: P33261, gene: CYP2C19, swissprot: CP2CJ_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022416s011lbl.pdf) Cytochrome P450 3A4 (Organism: Homo sapiens, class: Enzyme, accessions: P08684, gene: CYP3A4, swissprot: CP3A4_HUMAN) inducer (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022416s011lbl.pdf) Eslicarbazepine is an aromatic anticonvulsant similar to oxcarbazepine that is used in combination with other antiepileptic agents as therapy of partial onset seizures. The precise mechanism by which eslicarbazepine exerts anticonvulsant activity is unknown but is thought to involve inhibition of voltage-gated sodium channels. Decreased Central Nervous System Disorganized Electrical Activity (Code: N0000008486) Cytochrome P450 3A4 Inducers (Code: N0000185506) Cytochrome P450 2C19 Inhibitors (Code: N0000182140) Cardiovascular Agents (Code: D002317) Membrane Transport Modulators (Code: D049990) Sodium Channel Blockers (Code: D026941) Voltage-Gated Sodium Channel Blockers (Code: D061567) 2011-11-24 Ministry of Health of the Russian Federation
Click to view ethyl ether n-phenilacethyl-l-propylglycine Ethyl ether n-phenilacethyl-l-propylglycine (Noopept) is a synthetic peptide Noopept exhibits a combined neuroprotector effect both in vitro and in vivo. Noopept decreases the extent of necrotic damage caused by photoinduced thrombosis of cortical blood vessels. Noopept reduces neurotoxic effects of excess extracellular calcium, glutamate, and free radicals. It is used for the treatment of cognitive deficits, encephalopathies, asthenia. 2006-03-24 Ministry of Health of the Russian Federation
Click to view ferrous gluconate Ferrous gluconate is a form of mineral iron for oral administration. Ferrous gluconate is absorbed in the stomach and small intestine and combines with apoferritin to form ferritin, which is stored in the liver, spleen, red bone marrow, and intestinal mucosa. Important in transport of oxygen by hemoglobin to the tissues, iron is also found in myoglobin, transferrin, and ferritin, and is as a component of many enzymes such as catalase, peroxidase, and cytochromes. It is used for the treatment and prevention of iron deficiency anemia, anemia of prematurity. Iron (Code: N0000006237) Parenteral Iron Replacement (Code: N0000177913) Hematinics (Code: D006397) Hematologic Agents (Code: D006401) 1957-12-31 Health Canada
Click to view fonturacetam Fonturacetam (Phenylpiracetam) is a phenylated analog of the piracetam. Fonturacetam is a nootropic drug. Fonturacetam acts on most neurotransmitter systems and has been used for its cognitive and physical enhancing properties, and also as an antidepressant. Fonturacetam is used for the treatment of cerebrovascular deficiency, depression, apathy, attention and memory decline, and it is recommended for cosmonauts for increasing physical and mental/cognitive activities in space. 2008-07-18 Ministry of Health of the Russian Federation
Click to view fusafungine antibiotic from Fusarium lateririum; for treatment of respiratory infections
Click to view gadoteridol Gadoteridol is the gadolinium complex of 10-(2-hydroxy-propyl)-1,4,7,10tetraazacyclododecane-1,4,7-triacetic acid. Gadoteridol is a paramagnetic agent and, as such, develops a magnetic moment when placed in a magnetic field. Abnormal vascularity or disruption of the blood-brain barrier allows accumulation of gadoteridol in lesions such as neoplasms, abscesses, and subacute infarcts. Gadoteridol is indicated for use in magnetic resonance imaging (MRI) to visualize lesions with abnormal vascularity in the brain (intracranial lesions), spine and associated tissues and the head and neck. Paramagnetic Contrast Agent (Code: N0000180184) Magnetic Resonance Contrast Activity (Code: N0000175862) Contrast Media (Code: D003287) Diagnostic Uses of Chemicals (Code: D064907) 1992-11-16 FDA GD
DO3
Click to view gadoversetamide nonionic, linear chelate used for magnetic resonance imaging of brain and spine
Click to view gamma-d-glutamyl-l-tryptophan Gamma-d-glutamyl-l-tryptophan (golotimod) is containing the amino acids D-glutamine and L-tryptophan connected by a gamma-glutamyl linkage with potential immunostimulating, antimicrobial and antineoplastic activities. Gamma-d-glutamyl-l-tryptophan is a synthetic dipeptide that acts broadly on the Toll-like receptor pathway. It has been shown to stimulate T-lymphocyte differentiation, macrocytic phagocytosis, and specific immune responses, and enhance IL-2 and INF-g production. It is used as an immunomodulator for the treatment of viral infection diseases (tuberculosis, hepatitis), sepsis. Also it is used after extensive operations. 2000-07-19 Ministry of Health of the Russian Federation
Click to view glucosamine sulfate Glucosamine sulfate is a normal component of glycosaminoglycans in the cartilage matrix and synovial fluid. Glucosamine sulfate disassociates within the stomach. It is used as nutritional supplement to ease the pain and discomfort of arthritis in humans and animals. (See: glucosamine)
Click to view gosogliptin Dipeptidyl peptidase 2 (Organism: Homo sapiens, class: Enzyme, accessions: Q9UHL4, gene: DPP7, swissprot: DPP2_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19275964) Dipeptidyl peptidase 4 (Organism: Homo sapiens, class: Enzyme, accessions: P27487, gene: DPP4, swissprot: DPP4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19275964) Dipeptidyl peptidase 8 (Organism: Homo sapiens, class: Enzyme, accessions: Q6V1X1, gene: DPP8, swissprot: DPP8_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/19275964) Gosogliptin is a potent, selective and orally bioavailable, difluoropyrrolidine-based inhibitor of dipeptidyl peptidase 4, with hypoglycemic activity. It is used for the treatment of type 2 diabetes mellitus. 2016-05-04 Ministry of Health of the Russian Federation PF2
Click to view heliomycin Heliomycin is an antibiotic substance produced by Streptomyces resistomycificus. Heliomycin has been shown to demonstrate antibacterial activity against gram-positive bacteria and mycobacteria. Heliomycin preferentially inhibits RNA synthesis in comparison to DNA and protein synthesis in intact bacterial cells. Heliomycin is indicated for the treatment of various dermatological diseases, including pyoderma, pemphigus, pemphigus neonatorum, infected trophic ulcers, eczema, pseudofurunculosis. 1969-08-21 Ministry of Health of the Russian Federation
Click to view hemin Chloro(7,12-diethenyl-3,8,13,17-tetramethyl-21H,23H-porphine-2,18-dipropanoato(4-)-N(21),N(22),N(23),N(24)) ferrate(2-) dihydrogen.
Click to view hydroxyethylaminoadenine Hydroxyethylaminoadenine is a stimulant of reparative processes. Hydroxyethylaminoadenine activates protein synthesis. It is used for the treatment of gastric and duodenal ulcer, wounds, burns and disorders of cornea, such as bullous keratopathy, corneal degeneration. 2006-07-28 Ministry of Health of the Russian Federation
Click to view hydroxiethyldimethyldihydropyrimidine Hydroxiethyldimethyldihydropyrimidine (xymedone) is a pyrimidinone derivative, which stimulates cell-mediated immunity and decreases the total serum Ig E. It is used for the treatment of deep and superficial burns. Also it is used for the prevention and for the treatment of post-operative infections of skin and skin structure. 2004-05-11 Ministry of Health of the Russian
Click to view indolcarbinol E3 ubiquitin-protein ligase NEDD4 (Organism: Homo sapiens, class: Enzyme, accessions: P46934, gene: NEDD4, swissprot: NEDD4_HUMAN) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/27979631) Cytochrome P450 1A1 (Organism: Homo sapiens, class: Enzyme, accessions: P04798, gene: CYP1A1, swissprot: CP1A1_HUMAN) inducer (Source: https://www.ncbi.nlm.nih.gov/pubmed/27451867) Indolcarbinol (indole-3-carbinol) is produced by members of the family Cruciferae and particularly members of the genus Brassica, for example, cabbage, radishes, cauliflower, broccoli, Brussels sprouts, and daikon). Indolcarbinol is metabolized to a number of products, including the dimeric 3, 3'-diindolylmethane. Indolcarbinol is a natural chemopreventive compound. It has multiple anticarcinogenic and antitumorigenic properties by suppressing the proliferation of certain cancer cells, including breast cancer, prostate cancer, endometrial cancer, colon cancer, and leukemic cells. Indole-3-carbinol scavenges free radicals and induces various hepatic cytochrome P450 monooxygenases. Specifically, this agent induces the hepatic monooxygenase cytochrome P4501A1 (CYP1A1), resulting in increased 2-hydroxylation of estrogens and increased production of the chemoprotective estrogen 2-hydroxyestrone. Indolcarbinol is used for the prevention of breast cancer in patient with benign breast hyperplasia. 2010-08-18 Ministry of Health of the Russian Federation
Click to view isodibut Isodibut is a homolog of alrestatin and an aldose reductase inhibitor. It was used for the treatment of diabetic retinopathy and neuropathy. 1998-03-17 Ministry of Health of the Russian Federation
Click to view l-ornithine-l-aspartate L-ornithine-L-aspartate (LOLA) is a stable salt of two natural nonessential L-amino acids: ornithine and aspartic acid. acts through the mechanism of substrate activation to detoxify ammonia. LOLA is a substrate for the urea cycle. LOLA also activates glutamine production by activating glutamine synthetase in perivenous hepatocytes and skeletal muscles. It is used as a nutritional supplement or to lower blood ammonia concentration and to eliminate symptoms of hepatic encephalopathy associated with liver cirrhosis. (See: ornithine) (See: aspartic acid)
Click to view lanthanum carbonate phosphate (Organism: None, class: Metabolite, accessions: None, gene: None, swissprot: None) sequestering agent (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021468s019lbl.pdf) Lanthanum carbonate is a phosphate binder commonly used in clinical practice. Lanthanum carbonate chewable tablet is a phosphate binder that reduces absorption of phosphate by forming insoluble lanthanum phosphate complexes that pass through the gastrointestinal (GI) tract unabsorbed. Both serum phosphate and calcium phosphate product are reduced as a consequence of the reduced dietary phosphate absorption. It is prescribed for treating high phosphate levels, mainly found in patients with chronic kidney disease. 2004-10-26 FDA LA
Click to view levorin Levorin (Candicidin D) is an antifungal antibiotic drug. Levorin is a major component of mixture of heptaene macrolides from Streptomyces griseus or Actinomyces levoris. Candicidin inhibits cell membrane of Candida albicans, resulting in disruption of membrane integrity and ultimately cell death. It is used for the topical treatment of candidasis. 1968-11-28 Ministry of Health of the Russian Federation
Click to view lithium oxybate Lithium oxybate is the lithium salt of gamma-hydroxybutyrate (GHB), an endogenous metabolite of gamma-aminobutyric acid (GABA) a major inhibitory neurotransmitter. Lithium oxybate is the chemical structure is a lithium analogue of sodium oxybutyrate . The therapeutic effect of the drug is mainly associated with the presence of lithium ion in its molecule, however, the drug also has elements of the activity characteristic of sodium oxybutyrate, it has a sedative effect. Compared to lithium carbonate, oxybutyrate is less toxic and more active. Lithium oxybate is used for the treatment of neurosis, psychoses (including manic-depressive psychosis) and schizophrenia. (See: sodium oxybate) 1980-11-28 Ministry of Health of the Russian Federation
Click to view magnesium aspartate Magnesium aspartate is a magnesium salt of aspartic acid that is commonly used as a mineral supplement. It displays high oral bioavailability and water solubiltiy compared to other magnesium salts such as magnesium citrate, magnesium carbonate and magnesium oxide. (See: aspartic acid) 1984-03-29 Austrian Medicines and Medical Devices Agency
Click to view mepartricin Mepartricin is a polyene macrolide antibiotic. It is obtained from Streptomyces aureofaciens. It is used for the treatment of benign prostatic hypertrophy. Also it is used for the treatment of vulvovaginal candidiasis. 1974-02-28 Italian Medicines Agency (AIFA)
Click to view mesodiethylethylendibenzosulfonate Mesodiethylethylendibenzosulfonate (sygethin) is an anti-climacteric drug. It affects the hypothalamic centers and the pituitary gonadotropic activity. It is used for the treatment of menopausal and female climacteric states, prolonged pregnancy, and other uterine inertia. 1973-05-15 Ministry of Health of the Russian Federation
Click to view mesulfamide Mesulfamide ((p-Sulfamoylanilino)methanesulfonic acid) is a drug from the group of sulfonamides,. It is an antibacterial agent. Mesulfamide has been shown to be active against Escherichia coli, Shigella spp., Vibrio cholerae, Clostridium perfringens, Bacillus anthracis, Corynebacterium diphtheriae, Yersinia pestis, Chlamydia spp., Actinomyces israelii, Toxoplasma gondii. Mesulfamide is used for the topical treatment of tonsillitis, infected wounds, infected burns, acne vulgaris, impetigo and other bacterial skin infections. 2007-05-22 Ministry of Health of the Russian Federation
Click to view metoprolol tartrate Metoprolol tartrate is an injectable form of metoprolol. It is used for the treatment of hypertension, angina pectoris and arrhythmia. (See: metoprolol) beta-Adrenergic Blocker (Code: N0000175556) Adrenergic Agents (Code: D018663) Adrenergic Antagonists (Code: D018674) Adrenergic beta-1 Receptor Antagonists (Code: D058671) Adrenergic beta-Antagonists (Code: D000319) Anti-Arrhythmia Agents (Code: D000889) beta-adrenergic antagonist (Code: CHEBI:35530) antihypertensive agent (Code: CHEBI:35674) Antihypertensive Agents (Code: D000959) Autonomic Agents (Code: D001337) Cardiovascular Agents (Code: D002317) Neurotransmitter Agents (Code: D018377) Peripheral Nervous System Agents (Code: D018373) Sympatholytics (Code: D013565)
Click to view miristalkonium chloride Miristalkonium chloride is a quaternary ammonium antiseptic with actions and uses similar to those of other cationic surfactants. Miristalkonium chloride is used as spermicide in vaginal contraceptives. It has antiseptic properties also. 1980-02-18 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view monophosphothiamine Monophosphothiamine is an organic chloride salt of thiamine(1+) monophosphate.
Click to view narlaprevir NS3 (Organism: Hepatitis C virus, class: Enzyme, accessions: A3EZI9, gene: NS3, swissprot: A3EZI9_9HEPC) inhibitor (Source: https://www.ncbi.nlm.nih.gov/pubmed/24900178) Narlaprevir is a NS3 protease inhibitor. It is used for the treatment of a chronic hepatitis C (genotype 1). 2016-05-12 Ministry of Health of the Russian Federation
Click to view sodium methylthionitrooxodihydrotriazolotriazinide Sodium methylthionitrooxodihydrotriazolotriazinide (trade name: Triazavirin) is a broad-spectrum antiviral drug developed in Russia. It has a novel triazolotriazine core, which represents a new structural class of non-nucleoside antiviral drugs. It is used for the treatment of influenza. 2014-08-28 Ministry of Health of the Russian Federation
Click to view neomycin Antibiotic complex produced by Streptomyces fradiae. It is composed of neomycins A, B, and C. It acts by inhibiting translation during protein synthesis.
Click to view phthalylsulfapyridazine Phthalylsulfapyridazine is a prodrug of long-acting sulfonamide antibiotic sulfamethoxypyridazine. It was used for the treatment of infectious diarrhea. (See: sulfamethoxypyridazine) 1972 Ministry of Health of the Russian Federation
Click to view nitrophenyldiethylaminopentilbenzamidine Nitrophenyldiethylaminopentilbenzamidine (nibentan) is a class III antiarrhythmic drug. However, its mechanism of action remains unclear. Nibentan is used for the treatment of supraventricular tachycardia and atrial fibrillation and flutter. 2002-09-18 Ministry of Health of the Russian Federation
Click to view pentahydroxyethylnaphtoquinone Pentahydroxyethylnaphtoquinone is a naphthoquinoid pigment from sea urchins that possesses antioxidant, antimicrobial, anti-inflammatory and chelating abilities. Pentahydroxyethylnaphtoquinone captures free radicals and stabilizes cell membranes. Also pentahydroxyethylnaphtoquinone neutralizes ferrous cations cations and prevents myocardium from toxic peroxides. It is used for the treatment of ischemia and myocardial infarction. Also it is used for the treatment of retinopathies and of cornea diseases. 1999-03-18 Ministry of Health of the Russian Federation
Click to view phosphazide Phosphazide is an antiretroviral agent of the class of inhibitors of type 1 HIV reverse transcriptase. It was designed in Russia. Now phosphazide is used for the treatment of HIV infection as the monotherapy or as a component of the combined therapy. 1999-10-05 Ministry of Health of the Russian Federation
Click to view piperazine adipinate Piperazine adipinate is a piperazinium salt obtained by combining equimolar amounts of piperazine and adipic acid. It has a role as an anthelminthic drug and an antinematodal drug. It is used for the treatment of ascaridosis and enterobiasis. (See: piperazine) 1964-04-30 Ministry of Health of the Russian Federation
Click to view pipotiazine Pipotiazine is a typical antipsychotic of the phenothiazine class. Pipotiazine has actions similar to those of other phenothiazines. Among the different phenothiazine derivatives, it appears to be less sedating and to have a weak propensity for causing hypotension or potentiating the effects of CNS depressants and anesthetics. However, it produces a high incidence of extra pyramidal reactions. It is used for the maintenance treatment of chronic non-agitated schizophrenic patients. Also it is used for the treatment of nonorganic psychosis and anxiety. 1994-07-12 Ministry of Health of the Russian Federation
Click to view prajmalium bitartrate Prajmalium bitartrate is the salt of the quartary ajmalium base, isolated from Rauwolfia serpentina and has potent antiarrhythmic effects. It is used for the treatment of angina pectoris, Wolff–Parkinson–White Syndrome, paroxysmal atrial fibrillation, atrioventricular tachycardia and coronary artery disease. (See: prajmalium) Anti-Arrhythmia Agents (Code: D000889) Cardiovascular Agents (Code: D002317) 1998-02-05 Ministry of Health of the Russian Federation
Click to view pyrvinium embonate Pyrvinium embonate is one of pyrvinium forms. Pyrvinium embonate is used in the treatment of enterobiasis caused by Enterobius vermicularis (pinworm). (See: pyrvinium)
Click to view riodipine Nuclear receptor subfamily 1 group I member 2 (Organism: Homo sapiens, class: Nuclear hormone receptor, accessions: O75469, gene: NR1I2, swissprot: NR1I2_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/20966043) Riodipine is the blocker of calcium channels of L-type. Also riodipine has an antiepileptic effect which is manifested by a decreased frequency and amplitude of interictal discharges and a less frequent appearance of ictal discharges. Riodipine is indicated for the treatment of arterial hypertension, prevention of attacks of angina pectoris or a recurrent myocardial infarction. 1987-10-28 Ministry of Health of the Russian Federation
Click to view roxatidine Histamine H2 receptor (Organism: Cavia porcellus, class: GPCR, accessions: P47747, gene: HRH2, swissprot: HRH2_CAVPO) antagonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/2861823) Roxatidine is an histamine H2-receptor antagonist. Roxatidine is a potent and selective inhibitor of basal and stimulated gastric acid secretion through competitive blockade of H2-receptors. Total pepsin secretion is reduced in a dose-dependent manner. There is an independent mucosal protection action. Roxatidine is indicated for the treatment of peptic ulcer, gastro-oesophageal reflux disease, gastritis, upper gastrointestinal haemorrhage and Zollinger-Ellison syndrome. roxatidine acetate: 1991-12-17 Italian Medicines Agency (AIFA)
Click to view selenopyrane Selenopyrane has a antioxidant, antiatherosclerotic, immunomodulating activity. It is used for prevention and management of radiotherapy-induced toxicity. 2010-04-27 Ministry of Health of the Russian Federation
Click to view strontium ranelate Strontium ranelate is a strontium (II) salt of ranelic acid. Strontium ranelate increases bone formation in bone tissue culture as well as osteoblast precursor replication and collagen synthesis in bone cell culture, and reduces bone resorption by decreasing osteoclast differentiation and resorbing activity. This results in a rebalance of bone turnover in favour of bone formation. Strontium ranelate is used for the treatment of severe osteoporosis in postmenopausal women and adult men, at high risk of fracture, for whom treatment with other medicinal products approved for the treatment of osteoporosis is not possible due to, for example, contraindications or intolerance. In postmenopausal women, strontium ranelate reduces the risk of vertebral and hip fractures. Bone Density Conservation Agents (Cede: D050071) 2004-09-21 EMA
Click to view sulfadiazine, silver salt Sulfadiazine, silver salt is a sulfa derivative topical antibacterial. Silver sulfadiazine may act through a combination of the activity of silver and sulfadiazine. When this agent interacts with sodium chloride-containing body fluids, silver ions are released slowly and sustainably into wounded areas. Ionized silver atoms catalyze the formation of disulfide bonds leading to protein structural changes and inactivating thiol-containing enzymes; silver ions may also intercalate DNA thereby interfering with replication and transcription of bacteria. As a competitive inhibitor of para-aminobenzoic acid (PABA), sulfadiazine inhibits bacterial dihydropteroate synthase, thereby resulting in disruption of folic acid metabolism and ultimately DNA synthesis. Sulfadiazine, silver salt is used for the treatment and prevention of wound sepsis in patients with second- and third-degree burns. (See: sulfadiazine) antibacterial drug (Code: CHEBI:36047) Sulfonamides (Code: N0000008048) Sulfonamide Antibacterial (Code: N0000175503) Anti-Infective Agents (Code: D000890) Anti-Infective Agents, Local (Code: D000891) 1973-11-26 FDA
Click to view tebaine Mu-type opioid receptor (Organism: Homo sapiens, class: GPCR, accessions: P35372, gene: OPRM1, swissprot: OPRM_HUMAN) agonist (Source: https://www.ncbi.nlm.nih.gov/pubmed/17616524) Tebaine is an alkaloid opiate that is used as an intermediate in the biosynthesis of other opioids. Tebaine is controlled under international law. 2008-08-18 Ministry of Health of the Russian Federation
Click to view teicoplanin Teicoplanin is a glycopeptide antibiotic complex from Actinoplanes teichomyceticus active against gram-positive bacteria. Teicoplanin inhibits the growth of susceptible organisms by interfering with cell-wall biosynthesis at a site different from that affected by beta-lactams. Peptidoglycan synthesis is blocked by specific binding to D-alanyl-D-alanine residues. Teicoplanin is active against Corynebacterium jeikeium, Enterococcus faecalis, Staphylococcus aureus (including methicillin-resistant strains), Streptococcus agalactiae, Streptococcus dysgalactiae subsp. equisimilis, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococci in the viridans group a b, Clostridium difficile and Peptostreptococcus spp. Teicoplanin is indicated for the treatment of complicated skin and soft tissue infections, bone and joint infections, hospital acquired pneumonia, community acquired pneumonia, complicated urinary tract infections, infective endocarditis, peritonitis associated with continuous ambulatory peritoneal dialysis (CAPD), bacteraemia that occurs in association with any of the indications listed above. Teicoplanin is also indicated as an alternative oral treatment for Clostridium difficile infection-associated diarrhoea and colitis. 1988-02-12 ANSM (French National Agency for Medicines and Health Products Safety)
Click to view tercuronium Tercuronium is p',p"-bis-triethylammonium-p-terphenyl dibenzosulfonate and a bisquaternary-p-terphenyl derivative. Tercuronium has neuromuscular blocking activity. Tercuronium possesses a cumulative property similar to that of tubocurarine and pancuronium. Tercuronium was used for skeletal muscle relaxantion during general anesthesia. 1984-12-11 Ministry of Health of the Russian Federation
Click to view tetrahydroxyglucopyranosilxanten Tetrahydroxyglucopyranosilxanten (alpisarin) is an antiviral agent. It is active against herpes simplex virus I and II, Varicella zoster virus, and Cytomegalovirus. Alpisarin has a moderate bacteriostatic effect on certain types of gram-positive and gram-negative bacteria. It is used for the treatment of herpes simplex virus infections, herpes zoster, varicella. 1985-04-17 Ministry of Health of the Russian Federation
Click to view troventolum Troventolum is an anticholinergic substance that acts primarily on muscarinic cholinergic receptors. Troventolum as a very active bronchodilator is used for chronic obstructive bronchitis, mild to moderate bronchial asthma attacks. 1988-08-29 Ministry of Health of the Russian Federation
Click to view zuclopenthixol decanoate Zuclopenthixol decanoate is a prodrug of zuclopenthixol. Decanoate form is used for long-acting intramuscular injection. (See: clopenthixol) 1976-09-27 Austrian Medicines and Medical Devices Agency
Click to view silibinin Silibinin is the major active constituent of silymarin, a standardized extract of the milk thistle seeds (silybi mariani fructuum extract), containing a mixture of flavonolignans consisting of silibinin, isosilibinin, silicristin, silidianin and others. Silibinin is presented as a mixture of two diastereomers, silybin A and silybin B, which are found in an approximately equimolar ratio. Both in vitro and animal research suggest that silibinin has hepatoprotective (antihepatotoxic) properties that protect liver cells against toxins. Silibinin has also demonstrated in vitro anti-cancer effects against human prostate adenocarcinoma cells, estrogen-dependent and -independent human breast carcinoma cells, human ectocervical carcinoma cells, human colon cancer cells, and both small and nonsmall human lung carcinoma cells. Silibinin has been used traditionally for the treatment of liver and gallbladder disorders. 1977-09-15 Austrian Medicines and Medical Devices Agency
Click to view belatacept T-lymphocyte activation antigen CD80 (Organism: Homo sapiens, class: Unclassified, accessions: P33681, gene: CD80, swissprot: CD80_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/125288s075lbl.pdf) T-lymphocyte activation antigen CD86 (Organism: Homo sapiens, class: Unclassified, accessions: P42081, gene: CD86, swissprot: CD86_HUMAN) inhibitor (Source: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/125288s075lbl.pdf) Belatacept, a selective costimulation blocker, is a soluble fusion protein consisting of a modified extracellular domain of human cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) fused to a portion (hinge-CH2-CH3 domains) of the Fc domain of a human immunoglobulin G1 antibody. Belatacept is produced by recombinant DNA technology in a mammalian cell expression system. Two amino acid substitutions (L104 to E; A29 to Y) were made in the ligand binding region of CTLA-4. Belatacept binds to CD80 and CD86 on antigen presenting cells. As a result, belatacept blocks CD28 mediated co-stimulation of T cells inhibiting their activation. Belatacept, a modified form of CTLA4-Ig, binds CD80 and CD86 more avidly than the parent CTLA4-Ig molecule from which it is derived. This increased avidity provides a level of immunosuppression that is necessary for preventing immune-mediated allograft failure and dysfunction. Belatacept, in combination with corticosteroids and a mycophenolic acid (MPA), is indicated for prophylaxis of graft rejection in adults receiving a renal transplant. It is recommended to add an interleukin (IL)-2 receptor antagonist for induction therapy to this belatacept-based regimen. Selective T Cell Costimulation Blocker (Code: N0000182830) CD80-directed Antibody Interactions (Code: N0000182830) CD86-directed Antibody Interactions (Code: N0000182151) T Lymphocyte Costimulation Activity Blockade (Code: N0000182829) 2011-06-15 FDA