Vofopitant 是一种有效的 NK1 receptor 拮抗剂，对人，大鼠和雪貂的 NK1 receptor 的 pKi 值分别为 10.6，9.5 和 9.8。
Vofopitant is potent tachykinin NK
1
receptor antagonist, with pK
i
s of 10.6, 9.5, and 9.8 for human, rat and ferret NK
1
receptor, respectively. Vofopitant less potently inhibits rat 5-HT1A, bovine 5-HT1D, rat 5-HT2A, rat Histamine H1, guinea-pig Histamine H2 and rat Ca
2+
channel, with pK
i
s of 6.3, 6.6, 6.5, 6.5, 6.6, and 5.6, respectively. Vofopitant shows negligible affinity at NK
2
and NK
3
, with pIC
50
of <5.0. 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.
Vofopitant (GR205171, 30 mg/kg, s.c.) increases the number of choices of the 25-s delayed reward in a T-maze. 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.