Cipralisant
| 中文名称 | Cipralisant |
|---|---|
| 中文同义词 | 化合物 T14970;化合物 CIPRALISANT |
| 英文名称 | Cipralisant |
| 英文同义词 | GT-2331;1H-Imidazole, 5-[(1R,2R)-2-(5,5-dimethyl-1-hexyn-1-yl)cyclopropyl]-;5-[2-(5,5-Dimethylhex-1-ynyl)cyclopropyl]-1H-imidazole;4-(2-(5,5-Dimethylhex-1-inyl)-cyclopropyl)imidazol |
| CAS号 | 213027-19-1 |
| 分子式 | C14H20N2 |
| 分子量 | 216.32 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 213027-19-1.mol |
| 结构式 |  |
Cipralisant 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 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 14.18±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
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.