Cloperastine disrupts hERG K+ currents in a concentration-dependent manner, displaying an IC50 value of 27±3 nM[1]. As an antitussive agent, cloperastine exhibits both antitussive and antiedemic activities and has the ability to relax bronchial musculature. It operates primarily through a central antitussive mechanism and has antihistaminic and papaverine-like activities, comparable to those of codeine but without the associated narcotic effects[2].
体内研究
In experiments with anesthetized guinea pigs, a therapeutic dose of cloperastine (1 mg/kg) was shown to prolong the QT interval and monophasic action potential (MAP) duration, though it did not affect the PR interval or QRS width[1].
Cloperastine hydrochloride, when administered intraperitoneally, has relatively low acute toxicity in rats and mice. Additionally, when given orally in the form of cloperastine fendizoate, it demonstrates minimal toxicity, with the LD50 values for rats and mice exceeding 1000 mg/kg and 2000 mg/kg, respectively[2].
体外研究
Cloperastine disrupts hERG K+ currents in a concentration-dependent manner, displaying an IC50 value of 27±3 nM[1].
As an antitussive agent, cloperastine exhibits both antitussive and antiedemic activities and has the ability to relax bronchial musculature. It operates primarily through a central antitussive mechanism and has antihistaminic and papaverine-like activities, comparable to those of codeine but without the associated narcotic effects[2].
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