168266-90-8
Chemical Structure
Vofopitant
Synonym(s): GR 205171
- CAS No.: 168266-90-8
- Formula:C21H23F3N6O
- Molecular Weight:432.44
IUPAC Name: (2S,3S)-N-(2-methoxy-5-(5-(trifluoromethyl)-1H-tetrazol-1-yl)benzyl)-2-phenylpiperidin-3-amine
InChIKey: XILNRORTJVDYRH-HKUYNNGSSA-N
SMILES: COC1=C(CN[C@@H]2[C@H](C3=CC=CC=C3)NCCC2)C=C(N4C(C(F)(F)F)=NN=N4)C=C1
Biological Activity: Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting[1][2][3][4][5][6].
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Vofopitant | 99.41% | Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting. | ||||||||||||||||||||
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rac-Vofopitant-d3 | rac-Vofopitant-d3 (rac-GR 205171-d3) is a racemic form of deuterated Vofopitant (HY-12142). Vofopitant (GR 205171A) is a blood-brain barrier-permeable NK1 receptor inhibitor with a pKi of 9.02 in mice. Vofopitant blocks vomiting-related responses and inhibits pseudoptyalism. Vofopitant exerts anxiolytic effects, regulates 5-HT receptor function and increases central 5-HT release. Vofopitant improves hyperarousal symptoms of post-traumatic stress disorder. Vofopitant can be used in research related to depression, anxiety, vomiting and postoperative nausea and vomiting. | |||||||||||||||||||||
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References
- [1]. Zocchi A, et al. Effects of antidepressant drugs and GR 205171, an neurokinin-1 (NK1) receptor antagonist, on the response in the forced swim test and on monoamine extracellular levels in the frontal cortex of the mouse. Neurosci Lett. 2003;345(2):73-76. [Content Brief]
- [2]. Furukawa N, et al. A neurokinin-1 receptor antagonist reduced hypersalivation and gastric contractility related to emesis in dogs. Am J Physiol. 1998;275(5):G1193-G1201. [Content Brief]
- [3]. Heldt SA, et al. 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;20(7):584-595. [Content Brief]
- [4]. Guiard BP, et al. Sustained pharmacological blockade of NK1 substance P receptors causes functional desensitization of dorsal raphe 5-HT 1A autoreceptors in mice. J Neurochem. 2005;95(6):1713-1723. [Content Brief]
- [5]. Mathew SJ, et al. A selective neurokinin-1 receptor antagonist in chronic PTSD: a randomized, double-blind, placebo-controlled, proof-of-concept trial. Eur Neuropsychopharmacol. 2011;21(3):221-229. [Content Brief]
- [6]. Meyer TA, et al. Neurokinin-1 receptor antagonists for the prevention of postoperative nausea and vomiting. Pharmacotherapy, 2023, 43(9): 922-934.
