CAS NO: | 168266-90-8 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Vofopitant is potenttachykinin NK1receptorantagonist, withpKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1receptor, respectively. | ||||||||||||
IC50& Target | pKi: 10.6 (Human NK1receptor), 9.5 (Rat NK1receptor), 9.8 (Ferret NK1receptor)[1] | ||||||||||||
体外研究 (In Vitro) | Vofopitant is potent tachykinin NK1receptor antagonist, with pKis 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 pKis 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]. | ||||||||||||
体内研究 (In Vivo) | 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]. | ||||||||||||
Clinical Trial | |||||||||||||
分子量 | 432.44 | ||||||||||||
性状 | Solid | ||||||||||||
Formula | C21H23F3N6O | ||||||||||||
CAS 号 | 168266-90-8 | ||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||
储存方式 |
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