| 词条 | Orvepitant |
| 释义 |
| IUPAC_name = (2R,4S)-4-[(8aS)-6-oxo-1,3,4,7,8,8a-hexahydropyrrolo[1,2-a]pyrazin-2-yl]-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-N-methylpiperidine-1-carboxamide | image = Orvepitant_structure.png | width = 240 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | bioavailability = | protein_bound = | metabolism = | excretion = | IUPHAR_ligand = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 579475-18-6 | CAS_supplemental = | ATC_prefix = none | ATC_suffix = | PubChem = 9852175 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | UNII_Ref = {{fdacite|changed|FDA}} | UNII = IIU6V0W3JD | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = | ChemSpiderID = 8027888 | C=31 | H=35 | F=7 | N=4 | O=2 | molecular_weight = 628.623 g/mol | smiles = CC1=C(C=CC(=C1)F)[C@H]2C[C@H](CCN2C(=O)N(C)[C@H](C)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)N4CCN5[C@H](C4)CCC5=O | StdInChI = 1S/C31H35F7N4O2/c1-18-12-23(32)4-6-26(18)27-16-24(40-10-11-41-25(17-40)5-7-28(41)43)8-9-42(27)29(44)39(3)19(2)20-13-21(30(33,34)35)15-22(14-20)31(36,37)38/h4,6,12-15,19,24-25,27H,5,7-11,16-17H2,1-3H3/t19-,24+,25+,27-/m1/s1 | StdInChIKey = XWNBGDJPEXZSQM-VZOBGQTKSA-N }}Orvepitant (GW823296) is a drug developed by GlaxoSmithKline which acts as a selective antagonist for the NK1 receptor.[1] It was under development as a potential antidepressant drug, and early stage human clinical trials showed it to have some antidepressant effects, though not with sufficient efficacy to justify further development for this application. It was however considered a successful proof of concept for NK1 antagonists as potential antidepressants, and efforts are continuing to find more potent compounds which might be more effective.[2] References1. ^Di Fabio R, Alvaro G, Braggio S, Carletti R, Gerrard PA, Griffante C, Marchioro C, Pozzan A, Melotto S, Poffe A, Piccoli L, Ratti E, Tranquillini E, Trower M, Spada S, Corsi M. Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate. Bioorg Med Chem. 2013 Nov 1;21(21):6264-73. doi: 10.1016/j.bmc.2013.09.001. {{PMID|24075145}} {{Neurokinin receptor modulators}}{{nervous-system-drug-stub}}2. ^Ratti E, Bettica P, Alexander R, Archer G, Carpenter D, Evoniuk G, Gomeni R, Lawson E, Lopez M, Millns H, Rabiner EA, Trist D, Trower M, Zamuner S, Krishnan R, Fava M. Full central neurokinin-1 receptor blockade is required for efficacy in depression: evidence from orvepitant clinical studies. J Psychopharmacol. 2013 May;27(5):424-34. doi: 10.1177/0269881113480990. {{PMID|23539641}} 3 : NK1 receptor antagonists|Trifluoromethyl compounds|Fluoroarenes |
| 随便看 |
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。