334476-46-9
Chemical Structure
Vestipitant
Synonym(s): GW597599
- CAS No.: 334476-46-9
- Formula:C23H24F7N3O
- Molecular Weight:491.44
IUPAC Name: (S)-N-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethyl)-2-(4-fluoro-2-methylphenyl)-N-methylpiperazine-1-carboxamide
InChIKey: SBBYBXSFWOLDDG-JLTOFOAXSA-N
SMILES: C[C@H](C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)N(C)C(N2[C@@H](C3=C(C=C(C=C3)F)C)CNCC2)=O
Biological Activity: 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].
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Vestipitant | 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. | |||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
