168266-90-8
基本信息
Vofopitant
Vofopitant (GR 205171)
3-Piperidinamine, N-[[2-methoxy-5-[5-(trifluormethyl)-1H-tetrazol-1-yl]phenyl]methyl]-2-phenyl, (2S,3S)
3-Piperidinamine, N-[[2-methoxy-5-[5-(trifluormethyl)-1H-tetrazol-1-yl]phenyl]methyl]-2-phenyl, (2S-cis-)
物理化学性质
| 沸点 | 542.5±60.0 °C(Predicted) |
| 密度 | 1.39±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 9.13±0.10(Predicted) |
| CAS 数据库 | 168266-90-8 |
常见问题列表
pKi: 10.6 (Human NK 1 receptor), 9.5 (Rat NK 1 receptor), 9.8 (Ferret NK 1 receptor)
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.