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乙胺碘呋酮和抗心律失常药物对豚鼠心房肌钠通道和钙通道的作用。

Effects of etafenone and antiarrhythmic drugs on Na and Ca channels of guinea pig atrial muscle.

作者信息

Hashimoto K, Satoh H, Imai S

出版信息

J Cardiovasc Pharmacol. 1979 Sep-Oct;1(5):561-70. doi: 10.1097/00005344-197909000-00008.

Abstract

Since Ca-mediated electrophysiological phenomena seem to be important in the generation of various arrhythmias, we quantitatively compared the effects of quinidine, disopyramide, procainamide, lidocaine, propranolol, and etafenone, a new coronary vasodilator with antiarrhythmic properties, on Na and Ca channels in normal and depolarized guinea pig atria. The maximum rate of rise of the normal action potential and the amplitude of the depolarized, Ca-mediated action potential were measured to examine the Na and Ca channel activity, respectively. In both preparations, the contractile force was determined concomitantly in order to establish the role of Ca influx in the inotropic effects of the drugs. All six drugs suppressed the Na channel, the effect being strongest with etafenone, followed in order by quinidine, propranolol, disopyramide, lidocaine, and procainamide. Only quinidine, disopyramide, and propranolol suppressed the Ca channel and only in concentrations higher than those required to block the Na channel. Etafenone and procainamide decreased Ca influx, while lidocaine had no effect on it. The negative inotropic effects of propranolol and disopyramide may be due to decreases in Ca influx, but the order drugs seem to have other mechanisms for their inotropic effects.

摘要

由于钙介导的电生理现象似乎在各种心律失常的发生中起重要作用,我们定量比较了奎尼丁、双异丙吡胺、普鲁卡因胺、利多卡因、普萘洛尔以及具有抗心律失常特性的新型冠状血管扩张剂乙胺碘呋酮对正常和去极化豚鼠心房钠通道和钙通道的影响。分别测量正常动作电位的最大上升速率和去极化的、钙介导的动作电位的幅度,以检测钠通道和钙通道活性。在两种制剂中,同时测定收缩力,以确定钙内流在药物变力作用中的作用。所有六种药物均抑制钠通道,其中乙胺碘呋酮的作用最强,其次依次为奎尼丁、普萘洛尔、双异丙吡胺、利多卡因和普鲁卡因胺。只有奎尼丁、双异丙吡胺和普萘洛尔抑制钙通道,且仅在高于阻断钠通道所需的浓度时才起作用。乙胺碘呋酮和普鲁卡因胺减少钙内流,而利多卡因对其无影响。普萘洛尔和双异丙吡胺的负性变力作用可能是由于钙内流减少,但其他药物似乎有其他变力作用机制。

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