| 中文名称 | 盐酸氯哌斯丁 |
| 英文名称 | Cloperastine hydrochloride |
| CAS号 | 14984-68-0 |
| 分子式 | C20H25Cl2NO |
| 分子量 | 366.32 |
| EINECS号 | 239-067-8 |
| 熔点 | 147.9° |
| 溶解度 | 可溶于DMSO(少许)、甲醇(少许) |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
| 默克索引编号 | 14,2395 |
| 危险品标志 | Xn |
| 危险类别码 | 22 |
| 安全说明 | 36 |
| WGK Germany | 3 |
| RTECS号 | TM6491500 |
| 海关编码 | 2933.39.9200 |
27 nM (K + currents)
Cloperastine inhibits the hERG K
+
currents in a concentrationdependent manner with an IC
50
value of 27 nM.
Among the antitussive agents, Cloperastine, which possesses antitussive and antiedemic activity, also relaxes the bronchial musculature. Cloperastine is a drug with a central antitussive effect, and is also endowed with an antihistaminic and papaverine-like activity similar to codeine but without its narcotic effects.
In the anesthetized guinea pigs, Cloperastine at a therapeutic dose of 1 mg/kg prolonged the QT interval and monophasic
action potential (MAP) duration without affecting PR interval or QRS width.
Cloperastine hydrochloride shows relatively low acute toxicity when administered by the intraperitoneal route in rats and mice, and shows minor toxicity by the oral route when administered as Cloperastine fendizoate, the LD
50
in rats and mice for the two administration routes exceeds 1000 and 2000 mg/kg, respectively.