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Vestipitant

Summary

Vestipitant (INN)[1]: 98  is a drug developed by GlaxoSmithKline which acts as a selective antagonist for the NK1 receptor. It is under development as a potential antiemetic and anxiolytic drug,[2][3] and as a treatment for tinnitus[4] and insomnia.[5]

Vestipitant
Clinical data
ATC code
  • None
Identifiers
  • (2S)-N-{(1R)-1-[3,5-bis(trifluoromethyl)
    phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methylpiperazine-1-carboxamide
CAS Number
  • 334476-46-9 checkY
  • Mesylate: 334476-64-1 checkY
PubChem CID
  • 9832383
IUPHAR/BPS
  • 5757
ChemSpider
  • 8008111 ☒N
UNII
  • S052TOI9BI
  • Mesylate: OWR424W90Q checkY
KEGG
  • D06293 ☒N
ChEMBL
  • ChEMBL522987 ☒N
CompTox Dashboard (EPA)
  • DTXSID50187092 Edit this at Wikidata
Chemical and physical data
FormulaC23H21F10N3O
Molar mass545.425 g·mol−1
3D model (JSmol)
  • Interactive image
  • FC(F)(F)c1cc(F)ccc1C2CNCCN2C(=O)N(C)C(C)c3cc(C(F)(F)F)cc(c3)C(F)(F)F
  • InChI=1S/C23H24F7N3O/c1-13-8-18(24)4-5-19(13)20-12-31-6-7-33(20)21(34)32(3)14(2)15-9-16(22(25,26)27)11-17(10-15)23(28,29)30/h4-5,8-11,14,20,31H,6-7,12H2,1-3H3/t14-,20-/m1/s1 ☒N
  • Key:SBBYBXSFWOLDDG-JLTOFOAXSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

See also edit

References edit

  1. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 53" (PDF). World Health Organization. Retrieved 17 November 2016.
  2. ^ Reddy GK, Gralla RJ, Hesketh PJ (April 2006). "Novel neurokinin-1 antagonists as antiemetics for the treatment of chemotherapy-induced emesis". Supportive Cancer Therapy. 3 (3): 140–2. doi:10.3816/SCT.2006.n.011. PMID 18632487.
  3. ^ Brocco M, Dekeyne A, Mannoury la Cour C, Touzard M, Girardon S, Veiga S, et al. (October 2008). "Cellular and behavioural profile of the novel, selective neurokinin1 receptor antagonist, vestipitant: a comparison to other agents". European Neuropsychopharmacology. 18 (10): 729–50. doi:10.1016/j.euroneuro.2008.06.002. PMID 18657401. S2CID 8258896.
  4. ^ Clinical trial number NCT00394056 for "Vestipitant Or Vestipitant/Paroxetine Combination In Subjects With Tinnitus And Hearing Loss" at ClinicalTrials.gov
  5. ^ Ratti E, Carpenter DJ, Zamuner S, Fernandes S, Squassante L, Danker-Hopfe H, et al. (December 2013). "Efficacy of vestipitant, a neurokinin-1 receptor antagonist, in primary insomnia". Sleep. 36 (12): 1823–30. doi:10.5665/sleep.3208. PMC 3825431. PMID 24293756.