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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 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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

NK1R

Frequently Asked Questions

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