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新型III类抗心律失常制剂(AL-275)对实验性心肌及交感神经刺激的作用

[Effect of the novel III class anti-arrhythmia preparation (AL-275) in experimental myocardium and sympathetic stimulation].

作者信息

Kaverina N V, Lyskovtsev V V, Kishchuk E P

机构信息

Laboratory of Circulation System Pharmacology, Institute of Pharmacology, Russian Academy of Medical Sciences, Baltiiskaya ul. 8, Moscow, 125315 Russia.

出版信息

Eksp Klin Farmakol. 2001 Jan-Feb;64(1):33-7.

PMID:11544801
Abstract

AL-275, a new antiarrhythmic agent, exhibits the properties typical of the class III antiarrhythmogen: (i) prolongs the ventricular repolarization; (ii) inhibits the sinus node automatism; (iii) increases the effective refractory periods in atrium and ventricles; and (iv) does not modify AV and intraventricular conduction. AL-275 produces a pronounced antiarrhythmic and antifibrillatory action. The effect of AL-275 is independent of the heart rate, which is an advantage over the other class III agents. Both character and intensity of the electrophysiological and antiarrhythmic activity of AL-275 were fully retained upon the preliminary infusion of isoproterenol. Independence of the drug action of both the heart rate and the isoproterenol-induced changes in refractoriness are related to the ability of AL-275 to block a slow component (IKs) of the potassium current.

摘要

新型抗心律失常药物AL - 275具有Ⅲ类抗心律失常药物的典型特性:(i)延长心室复极;(ii)抑制窦房结自律性;(iii)增加心房和心室的有效不应期;(iv)不改变房室传导和室内传导。AL - 275具有显著的抗心律失常和抗纤颤作用。与其他Ⅲ类药物相比,AL - 275的作用不受心率影响,这是其优势所在。在预先输注异丙肾上腺素后,AL - 275的电生理和抗心律失常活性的特征及强度均得以完全保留。该药物作用不受心率及异丙肾上腺素诱导的不应期变化影响,这与AL - 275阻断钾电流慢成分(IKs)的能力有关。

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