Cloperastine fendizoate inhibits the hERG K currents in a concentration-dependent manner with an IC 50 value of 27 nM.
性状
Solid
IC50 & Target[1][2]
27 nM (K currents)
体外研究(In Vitro)
Cloperastine inhibits the hERG K currents in a concentrationdependent manner with IC50 value of 27±3 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Takahara A, et al. Effects of the antitussive drug cloperastine on ventricular repolarization in halothane-anesthetized guinea pigs. J Pharmacol Sci. 2012;120(3):165-75.[2]. Catania MA, et al. Pharmacological and clinical overview of cloperastine in treatment of cough. Ther Clin Risk Manag. 2011;7:83-92.
溶解度数据
In Vitro: DMSO : 10 mg/mL (15.43 mM; Need ultrasonic)配制储备液