2126040-21-7
2126040-21-7 結(jié)構(gòu)式
基本信息
2-(3-氯-4-氟苯基)-N-(1-環(huán)己基-3-甲基-1H-吡唑-5-基)乙酰胺
Benzeneacetamide, 3-chloro-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)-4-fluoro-
物理化學(xué)性質(zhì)
常見問題列表
EC50: 165 nM (GIRK 1/2); 720 nM (GIRK1/4 )
VU0810464 (0, 0.1, 0.3, 1, 3, 10, 30 μM) produces a concentration‐dependent response curves of currents in SAN and HPC cells, in addition, VU0810464 is 9‐fold higher potency for Kir3 channel activation in neurons as compared to SAN cells.
VU0810464 (intraperitoneal?injection; 30 mg/kg, 10 mg/kg; 30mg/kg; pre-treated 30 mins) produces a dose-dependent reduction of SIH response in Male C57BL/6J mice. To test if VU0810464 plays it role through Kir3 channel activation, VU0810464 (10 mg/kg) suppresses the SIH response in wild‐ type mice, but has no impact on Kcnj3 ?/? mice. VU0810464 (intraperitoneal?injection?; 30 mg/kg; 15, 30, 45, or 60 min post‐injection) displays a favourable distribution to the brain (K p,uu = 0.83), has a improvement over ML297 (K p,uu = 0.32). Clearance of VU0810464 is rapid,brain and plasma half-lives is 20 min in a PK study.
| Animal Model: | Male C57BL/6J mice, Kcnj3 ?/? siblings female and male C57BL/6J mice |
| Dosage: | 10 mg/kg; 30mg/kg |
| Administration: | Intraperitoneal?injection |
| Result: | Reduced stress‐induced hyperthermia (SIH), a physiological test of anxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1) ?/? mice. |