Vofopitant is potenttachykinin NK₁receptorantagonist, withpK_is of 10.6, 9.5, and 9.8 for human, rat and ferret NK₁receptor, respectively.

pKi: 10.6 (Human NK₁receptor), 9.5 (Rat NK₁receptor), 9.8 (Ferret NK₁receptor)^[1]

Vofopitant is potent tachykinin NK₁receptor antagonist, with pK_is of 10.6, 9.5, and 9.8 for human, rat and ferret NK₁receptor, respectively. Vofopitant less potently inhibits rat 5-HT1A, bovine 5-HT1D, rat 5-HT2A, rat Histamine H1, guinea-pig Histamine H2 and rat Ca²⁺channel, with pK_is of 6.3, 6.6, 6.5, 6.5, 6.6, and 5.6, respectively. Vofopitant shows negligible affinity at NK₂and NK₃, with pIC₅₀of<5.0^[1]. GR205171 (300 μM) potentiates the effects of paroxetine on cortical [5-HT]ext, and inhibits paroxetine-induced increase in [5-HT]ext in the dorsal raphe nucleus^[3].

Vofopitant (GR205171, 30 mg/kg, s.c.) increases the number of choices of the 25-s delayed reward in a T-maze^[2]. Vofopitant (GR205171, 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].

432.44

Solid

C₂₁H₂₃F₃N₆O

168266-90-8

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