Vofopitant

Last updated
Vofopitant
Vofopitant.svg
Clinical data
Other namesGR205171; GR-205171
Routes of
administration 		Oral
ATC code
  • none
Identifiers
  • (2S,3S)-N-[(2-Methoxy-5-[5-(trifluoromethyl)tetrazol-1-yl]phenyl)methyl]-2-phenylpiperidin-3-amine
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
Formula C21H23F3N6O
Molar mass 432.451 g·mol−1
3D model (JSmol)
  • COC1=C(C=C(C=C1)N2C(=NN=N2)C(F)(F)F)CN[C@H]3CCCN[C@H]3C4=CC=CC=C4
  • 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 (GR205171) 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 studied 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]

See also

References

  1. ↑ Gardner CJ, Armour DR, Beattie DT, Gale JD, Hawcock AB, Kilpatrick GJ, et al. (August 1996). "GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity". Regulatory Peptides. 65 (1): 45–53. doi:10.1016/0167-0115(96)00071-7. PMID   8876035. S2CID   8600542.
  2. ↑ Heldt SA, Davis M, Ratti E, Corsi M, Trist D, Ressler KJ (October 2009). "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". Behavioural Pharmacology. 20 (7): 584–95. doi:10.1097/FBP.0b013e32832ec594. PMC   2946835 . PMID   19675456.
  3. ↑ Furmark T, Appel L, Michelgård A, Wahlstedt K, Ahs F, Zancan S, et al. (July 2005). "Cerebral blood flow changes after treatment of social phobia with the neurokinin-1 antagonist GR205171, citalopram, or placebo". Biological Psychiatry. 58 (2): 132–42. doi:10.1016/j.biopsych.2005.03.029. PMID   16038684. S2CID   8252615.
  4. ↑ Mathew SJ, Vythilingam M, Murrough JW, Zarate CA, Feder A, Luckenbaugh DA, et al. (March 2011). "A selective neurokinin-1 receptor antagonist in chronic PTSD: a randomized, double-blind, placebo-controlled, proof-of-concept trial". European Neuropsychopharmacology. 21 (3): 221–9. doi:10.1016/j.euroneuro.2010.11.012. PMC   3478767 . PMID   21194898.
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