Vofopitant
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]
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| Other names | GR205171; GR-205171 |
| Routes of administration | Oral |
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| Formula | C21H23F3N6O |
| Molar mass | 432.451 g·mol−1 |
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See also
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.
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