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Cloperastine fendizoate

CAS No. : 85187-37-7

MCE 站：Cloperastine fendizoate

产品活性：Cloperastine fendizoate 抑制 hERG K⁺ 电流，IC₅₀ 为 27 nM，这种作用具有浓度依赖性。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

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.

In Vivo: In the anesthetized guinea pigs, Cloperastine at a therapeutic dose of 1 mg/kg prolonged the QT interval and monophasicaction 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 LD₅₀ in rats and mice for the two administration routes exceeds 1000 and 2000 mg/kg, respectively.

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