Vofopitant
Chemical compound
- none
- (2S,3S)-N-[(2-Methoxy-5-[5-(trifluoromethyl)tetrazol-1-yl]phenyl)methyl]-2-phenylpiperidin-3-amine
- 168266-90-8
- 6918331
- 5752
- 5293535
- K08BK043YS
- DTXSID10870099
- Interactive image
- 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 (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
- NK1 receptor antagonist
References
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- v
- t
- e
Neurokinin receptor modulators
- 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
- Agonists: Neurokinin A
- Antagonists: GR-159897
- Ibodutant
- Nepadutant
- Saredutant
- Agonists: Neurokinin B
- Senktide
- Antagonists: Elinzanetant
- Fezolinetant
- Osanetant
- Pavinetant
- SB-218,795
- SB-222,200
- Talnetant
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