Vestipitant - Misplaced Pages

Chemical compound Pharmaceutical compound

Vestipitant
Clinical data

ATC code	None
Identifiers
IUPAC name (2S)-N-{(1R)-1-ethyl}-2-(4-fluoro-2-methylphenyl)-N-methylpiperazine-1-carboxamide
CAS Number	334476-46-9 Mesylate: 334476-64-1
PubChem CID	9832383
IUPHAR/BPS	5757
ChemSpider	8008111
UNII	S052TOI9BI Mesylate: OWR424W90Q
KEGG	D06293
ChEMBL	ChEMBL522987
CompTox Dashboard (EPA)	DTXSID50187092
Chemical and physical data
Formula	C₂₃H₂₁F₁₀N₃O
Molar mass	545.425 g·mol
3D model (JSmol)	Interactive image
SMILES FC(F)(F)c1cc(F)ccc1C2CNCCN2C(=O)N(C)C(C)c3cc(C(F)(F)F)cc(c3)C(F)(F)F
InChI 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 Key:SBBYBXSFWOLDDG-JLTOFOAXSA-N
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Vestipitant (INN) 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, and as a treatment for tinnitus and insomnia.

References

"International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 53" (PDF). World Health Organization. Retrieved 17 November 2016.
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.
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.
Clinical trial number NCT00394056 for "Vestipitant Or Vestipitant/Paroxetine Combination In Subjects With Tinnitus And Hearing Loss" at ClinicalTrials.gov
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.

v t e Antiemetics (A04)
5-HT₃ serotonin ion channel antagonists	Alosetron Azasetron Bemesetron Cilansetron Clozapine Dazopride Dolasetron Granisetron Lerisetron Mianserin Mirtazapine Olanzapine Ondansetron Palonosetron (+netupitant) Quetiapine Ramosetron Ricasetron Tropisetron Zatosetron
5-HT serotonin G-protein receptor antagonists	Clozapine Cyproheptadine Hydroxyzine Olanzapine Risperidone Ziprasidone
CB₁ agonists (cannabinoids)	Dronabinol Nabilone Tetrahydrocannabinol (cannabis)
D₂/D₃ antagonists	Chlorpromazine Haloperidol Hydroxyzine Metoclopramide Metopimazine Prochlorperazine Thiethylperazine Trimethobenzamide
H₁ antagonists (antihistamines)	Cyclizine Dimenhydrinate Diphenhydramine Hydroxyzine Meclizine Promethazine
mACh antagonists (anticholinergics)	Atropine Diphenhydramine Hydroxyzine (very mild) Hyoscyamine Scopolamine
NK₁ antagonists	Aprepitant Fosaprepitant Maropitant Netupitant Rolapitant
Others	Amisulpride Cerium oxalate Dexamethasone Lorazepam Midazolam Propofol

v t e Neurokinin receptor modulators
NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96345 CP-99994 CP-122721 Dapitant Elinzanetant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203040 GW-597599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant Vestipitant Vofopitant
NK₂	Agonists: Neurokinin A Antagonists: GR-159897 Ibodutant Nepadutant Saredutant
NK₃	Agonists: Neurokinin B Senktide Antagonists: Elinzanetant Fezolinetant Osanetant Pavinetant SB-218,795 SB-222,200 Talnetant

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