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[1][2][3].

Product Specifications

CAS Number

[334476-46-9]

Product Name Alternative

GW597599

UNSPSC

12352005

Hazard Statement

H302

Target

Neurokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/vestipitant.html

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

Molecular Formula

C23H24F7N3O

Molecular Weight

491.44

Precautions

P264-P270-P330-P501

References & Citations

[1]Ratti E, et al. Efficacy of vestipitant, a neurokinin-1 receptor antagonist, in primary insomnia. Sleep. 2013 Dec 1;36 (12) :1823-30.|[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.|[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.