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CH-200的抗心律失常及电生理效应

Antiarrhythmic and electrophysiological effects of CH-200.

作者信息

Hashimoto K, Tsukada T, Matsuda H, Imai S

出版信息

Eur J Pharmacol. 1977 Sep 15;45(2):185-94. doi: 10.1016/0014-2999(77)90088-7.

DOI:10.1016/0014-2999(77)90088-7
PMID:902689
Abstract

A new antiarrhythmic drug CH-200, 5-phenacyl-thieno[3,2-c]yridinium, was compared with procainamide and lidocaine in a two-stage coronary ligation arrhythmia model for its efficacy and electrophysiological properties. CH-200 suppressed arrhythmia in beagle dogs more effectively than did procainamide and lidocaine. The antiarrhythmic effects of CH-200 and procainamide developed slowly and lasted longer than those of lidocaine. Electrophysiological studies with CH-200 showed that it decreased max dV/dt of the action potential. This effect was dependent on the heart rate: the higher the rate, the stronger the effect. CH-200, procainamide and lidocaine prolonged the effective refractory period and this effect seemed to be responsible for suppressing the arrhythmia after coronary ligation. CH-200 and procainamide increased the frequency of ventricular pacemaker activity, while lidocaine decreased it. These effects appear to be unimportant for the antiarrhythmic effects.

摘要

一种新型抗心律失常药物CH - 200(5 - 苯甲酰噻吩并[3,2 - c]吡啶鎓),在两阶段冠状动脉结扎心律失常模型中,就其疗效和电生理特性与普鲁卡因胺和利多卡因进行了比较。CH - 200比普鲁卡因胺和利多卡因更有效地抑制了比格犬的心律失常。CH - 200和普鲁卡因胺的抗心律失常作用起效缓慢,持续时间比利多卡因更长。对CH - 200的电生理研究表明,它降低了动作电位的最大dV/dt。这种作用取决于心率:心率越高,作用越强。CH - 200、普鲁卡因胺和利多卡因延长了有效不应期,这种作用似乎是冠状动脉结扎后抑制心律失常的原因。CH - 200和普鲁卡因胺增加了心室起搏活动的频率,而利多卡因则降低了该频率。这些作用对于抗心律失常作用似乎并不重要。

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