Vofopitant is a potent antagonist of the tachykinin NK1 receptor (pKis: 10.6, 9.5, and 9.8 for the human, rat, and ferret NK1 receptor, respectively).

Vofopitant is potent antagonist of tachykinin NK1 receptor(pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively). Vofopitant shows negligible affinity at NK2 and NK3(pIC50 of<5.0)[1].In the dorsal raphe nucleus, GR205171 (300 μM) potentiates the effects of paroxetine on cortical [5-HT]ext, and inhibits paroxetine-induced increase in [5-HT]ext [3].

The number of choices of the 25-s delayed reward in a T-maze increased by Vofopitant (30 mg/kg, s.c.)[2]. Vofopitant (30 mg/kg, i.p.) increases the extracellular 5-HT levels in the frontal cortex of paroxetine-treated wild-type mice, rather than in wild-type mice and paroxetine-treated NK1 receptor knockout mice[3].

168266-90-8

C21H23F3N6O

432.44

GR 205171

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years