213027-19-1
基本信息
1H-Imidazole, 5-[(1R,2R)-2-(5,5-dimethyl-1-hexyn-1-yl)cyclopropyl]-
物理化学性质
| 熔点 | 173-175 °C |
| 沸点 | 386.7±31.0 °C(Predicted) |
| 密度 | 1.03±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) | 14.18±0.10(Predicted) |
| 形态 | Solid |
| 颜色 | White to off-white |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P305+P351+P338 |
常见问题列表
pKi: 9.9 (Histamine H3 receptor)
Ki: 0.47 nM (Rat histamine H3 receptor)
Cipralisant (GT-2331) is a potent histamine H3 receptor antagonist with a pK i of 9.9 and a K i of 0.47 nM for rat histamine H3 receptor. Cipralisant acts as a full agonist at the recombinant rat histamine H3 receptor in vitro, and potently inhibits forskolin-induced cAMP accumulation with an EC 50 of 0.23 nM. Cipralisant increases the basal [ 35 S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC 50 , 5.6 nM).
Cipralisant (GT-2331) acts as an antagonist of histamine H3 receptor, and blocks R-α-methylhistamine (a histamine H3 receptor agonist)-induced water intake at 10 mg/kg via oral administration in rats.