| 词条 | Vofopitant |
| 释义 |
| IUPAC_name = (2S,3S)-N-[(2-methoxy-5-[5-(trifluoromethyl)tetrazol-1-yl]phenyl)methyl]-2-phenylpiperidin-3-amine | image = Vofopitant.svg | tradename = | pregnancy_category = | legal_status = | routes_of_administration = Oral | bioavailability = | metabolism = | elimination_half-life = | excretion = | IUPHAR_ligand = 5752 | CAS_number = 168266-90-8 | ATC_prefix = none | ATC_suffix = | PubChem = 6918331 | ChemSpiderID = 5293535 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = | ChEMBL = | C=21 | H=23 | F=3 | N=6 | O=1 | molecular_weight = 432.442 g/mol | smiles = COC1=C(C=C(C=C1)N2C(=NN=N2)C(F)(F)F)CN[C@H]3CCCN[C@H]3C4=CC=CC=C4 | StdInChI = 1S/C21H23F3N6O/c1-31-18-10-9-16(30-20(21(22,23)24)27-28-29-30)12-15(18)13-26-17-8-5-11-25-19(17)14-6-3-2-4-7-14/h2-4,6-7,9-10,12,17,19,25-26H,5,8,11,13H2,1H3/t17-,19-/m0/s1 | StdInChIKey = XILNRORTJVDYRH-HKUYNNGSSA-N }}Vofopitant (GR-205,171) is a drug which acts as an NK1 receptor antagonist. It has antiemetic effects as with other NK1 antagonists,[1] and also shows anxiolytic actions in animals.[2] It was trialled for applications such as the treatment of social phobia and post-traumatic stress disorder, but did not prove sufficiently effective to be marketed.[3][4] See also
References1. ^Gardner CJ, Armour DR, Beattie DT, Gale JD, Hawcock AB, Kilpatrick GJ, Twissell DJ, Ward P. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53. {{PMID|8876035}} {{Neurokinin receptor modulators}}{{pharm-stub}}2. ^Heldt SA, Davis M, Ratti E, Corsi M, Trist D, Ressler KJ. Anxiolytic-like effects of the neurokinin 1 receptor antagonist GR-205171 in the elevated plus maze and contextual fear-potentiated startle model of anxiety in gerbils. Behav Pharmacol. 2009 Oct;20(7):584-95. doi: 10.1097/FBP.0b013e32832ec594 {{PMID|19675456}} 3. ^Furmark T, Appel L, Michelgård A, Wahlstedt K, Ahs F, Zancan S, Jacobsson E, Flyckt K, Grohp M, Bergström M, Pich EM, Nilsson LG, Bani M, Långström B, Fredrikson M. Cerebral blood flow changes after treatment of social phobia with the neurokinin-1 antagonist GR205171, citalopram, or placebo. Biol Psychiatry. 2005 Jul 15;58(2):132-42. {{PMID|16038684}} 4. ^Mathew SJ, Vythilingam M, Murrough JW, Zarate CA Jr, Feder A, Luckenbaugh DA, Kinkead B, Parides MK, Trist DG, Bani MS, Bettica PU, Ratti EM, Charney DS. A selective neurokinin-1 receptor antagonist in chronic PTSD: a randomized, double-blind, placebo-controlled, proof-of-concept trial. Eur Neuropsychopharmacol. 2011 Mar;21(3):221-9. doi: 10.1016/j.euroneuro.2010.11.012 {{PMID|21194898}} 6 : Antiemetics|NK1 receptor antagonists|Amines|Phenol ethers|Tetrazoles|Trifluoromethyl compounds |
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