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Vofopitant

CAS No. : 168266-90-8

MCE 站：Vofopitant

产品活性：Vofopitant 是一种有效的 NK₁ receptor 拮抗剂，对人，大鼠和雪貂的 NK₁ receptor 的 pK_i 值分别为 10.6，9.5 和 9.8。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Neurokinin Receptor

In Vitro: Vofopitant is potent tachykinin NK₁ receptor antagonist, with pK_is of 10.6, 9.5, and 9.8 for human, rat and ferret NK₁ receptor, 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 NK₂ and NK₃, with pIC₅₀ of <5.0. GR205171 (300 ?M) potentiates the effects of paroxetine on cortical [5-HT]ext, and inhibits paroxetine-induced increase in [5-HT]ext in the dorsal raphe nucleus.

In Vivo: 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.

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