Vofopitant

Vofopitant
	File:Vofopitant.svg
Systematic (IUPAC) name
	(2S,3S)-N-[(2-methoxy-5-[5-(trifluoromethyl)tetrazol-1-yl]phenyl)methyl]-2-phenylpiperidin-3-amine
Clinical data
Routes of; administration	Oral
Identifiers
CAS Number	168266-90-8
ATC code	none
PubChem	CID: 6918331
IUPHAR/BPS	5752
ChemSpider	5293535
Chemical data
Formula	C21H23F3N6O
Molecular mass	432.442 g/mol
	SMILES COC1=C(C=C(C=C1)N2C(=NN=N2)C(F)(F)F)CN[C@H]3CCCN[C@H]3C4=CC=CC=C4 ;
	InChI InChI=1S/C21H23F3N6O/c1-31-18-10-9-16(30-20(21(22,23)24)27-28-29-30)12-15(18)13-26-17-8-5-11-25-19(17)14-6-3-2-4-7-14/h2-4,6-7,9-10,12,17,19,25-26H,5,8,11,13H2,1H3/t17-,19-/m0/s1 ; Key:XILNRORTJVDYRH-HKUYNNGSSA-N ;

Vofopitant (GR-205,171) is a drug which acts as an NK₁ receptor antagonist. It has antiemetic effects as with other NK₁ antagonists,^[1] and also shows anxiolytic actions in animals.^[2] It was trialled for applications such as the treatment of social phobia and post-traumatic stress disorder, but did not prove sufficiently effective to be marketed.^[3]^[4]

References

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↑ Gardner CJ, Armour DR, Beattie DT, Gale JD, Hawcock AB, Kilpatrick GJ, Twissell DJ, Ward P. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53. PMID 8876035
↑ Heldt SA, Davis M, Ratti E, Corsi M, Trist D, Ressler KJ. Anxiolytic-like effects of the neurokinin 1 receptor antagonist GR-205171 in the elevated plus maze and contextual fear-potentiated startle model of anxiety in gerbils. Behav Pharmacol. 2009 Oct;20(7):584-95. doi: 10.1097/FBP.0b013e32832ec594 PMID 19675456
↑ Furmark T, Appel L, Michelgård A, Wahlstedt K, Ahs F, Zancan S, Jacobsson E, Flyckt K, Grohp M, Bergström M, Pich EM, Nilsson LG, Bani M, Långström B, Fredrikson M. Cerebral blood flow changes after treatment of social phobia with the neurokinin-1 antagonist GR205171, citalopram, or placebo. Biol Psychiatry. 2005 Jul 15;58(2):132-42. PMID 16038684
↑ Mathew SJ, Vythilingam M, Murrough JW, Zarate CA Jr, Feder A, Luckenbaugh DA, Kinkead B, Parides MK, Trist DG, Bani MS, Bettica PU, Ratti EM, Charney DS. A selective neurokinin-1 receptor antagonist in chronic PTSD: a randomized, double-blind, placebo-controlled, proof-of-concept trial. Eur Neuropsychopharmacol. 2011 Mar;21(3):221-9. doi: 10.1016/j.euroneuro.2010.11.012 PMID 21194898