| Identification | Back Directory | [Name]
VESTIPITANT | [CAS]
334476-46-9 | [Synonyms]
VESTIPITANT
(2S)-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-N-methylpiperazine-1-carboxamide
1-Piperazinecarboxamide, N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-N-methyl-, (2S)- | [Molecular Formula]
C23H24F7N3O | [MDL Number]
MFCD09833223 | [MOL File]
334476-46-9.mol | [Molecular Weight]
491.45 |
| Hazard Information | Back Directory | [Uses]
Vestipitant (GW597599) is a neurokinin-1 receptor antagonist (pKi: 9.4, hNK1) with hypnotic effects and the ability to suppress primary insomnia. Vestipitant can effectively block substance P-mediated extracellular regulated kinase phosphorylation and relieve anxiety and possible depression induced by the agonist GR73632 (HY-P1192) in gerbils. Vestipitant can also improve functional dyspnea, anxiety, insomnia, irritable bowel disease, gastroesophageal reflux disease, tinnitus and antiemetic effects[1][2][3]. | [IC 50]
hNK1: 9.4 (pKi) | [References]
[1] Ratti E, et al. Efficacy of vestipitant, a neurokinin-1 receptor antagonist, in primary insomnia. Sleep. 2013 Dec 1;36(12):1823-30. DOI:10.5665/sleep.3208
[2] Kranke P, et al. Comparison of vestipitant with ondansetron for the treatment of breakthrough postoperative nausea and vomiting after failed prophylaxis with ondansetron. Br J Anaesth. 2015 Mar;114(3):423-9. DOI:10.1093/bja/aeu376
[3] Brocco M, et al. Cellular and behavioural profile of the novel, selective neurokinin1 receptor antagonist, vestipitant: a comparison to other agents. Eur Neuropsychopharmacol. 2008 Oct;18(10):729-50. DOI:10.1016/j.euroneuro.2008.06.002 |
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