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尼普地洛(K-351)对犬心脏组织电生理特性的影响:与普萘洛尔和索他洛尔的比较。

Effects of nipradilol (K-351) on the electrophysiological properties of canine cardiac tissues: comparison with propranolol and sotalol.

作者信息

Nakaya H, Kimura S, Nakao Y, Kanno M

出版信息

Eur J Pharmacol. 1984 Sep 17;104(3-4):335-44. doi: 10.1016/0014-2999(84)90410-2.

DOI:10.1016/0014-2999(84)90410-2
PMID:6149947
Abstract

The electrophysiological effects of K-351 (0.3-300 microM), a new beta-adrenoceptor blocking drug, on canine Purkinje and ventricular muscle fibers were examined and compared with those of propranolol (0.3-30 microM) and sotalol (3-300 microM) using standard microelectrode techniques. K-351 and propranolol dose dependently reduced the maximum upstroke velocity of phase 0 and action potential amplitude in both cardiac tissues. Action potential durations (APD) of Purkinje fibers were shortened by both propranolol and K-351 but prolonged by sotalol. However, in ventricular muscle fibers K-351 and sotalol significantly prolonged APD and effective refractory periods which contrasted with the unchanged APD after propranolol. These results suggest that K-351 is a beta-blocking drug possessing a membrane stabilizing action (class I antiarrhythmic properties) and in ventricular muscles it can also exert an APD-prolonging effect (class III antiarrhythmic properties).

摘要

使用标准微电极技术,研究了新型β-肾上腺素受体阻断药物K-351(0.3 - 300微摩尔)对犬浦肯野纤维和心室肌纤维的电生理效应,并与普萘洛尔(0.3 - 30微摩尔)和索他洛尔(3 - 300微摩尔)进行了比较。K-351和普萘洛尔均剂量依赖性地降低了两种心脏组织中0期的最大上升速度和动作电位幅度。普萘洛尔和K-351均缩短了浦肯野纤维的动作电位持续时间(APD),但索他洛尔使其延长。然而,在心室肌纤维中,K-351和索他洛尔显著延长了APD和有效不应期,这与普萘洛尔作用后APD不变形成对比。这些结果表明,K-351是一种具有膜稳定作用(I类抗心律失常特性)的β阻断药物,在心室肌中它还可发挥延长APD的作用(III类抗心律失常特性)。

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1
Effects of nipradilol (K-351) on the electrophysiological properties of canine cardiac tissues: comparison with propranolol and sotalol.尼普地洛(K-351)对犬心脏组织电生理特性的影响:与普萘洛尔和索他洛尔的比较。
Eur J Pharmacol. 1984 Sep 17;104(3-4):335-44. doi: 10.1016/0014-2999(84)90410-2.
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引用本文的文献

1
Sotalol facilitates spontaneous ventricular defibrillation by enhancing intercellular coupling. An entirely new mechanism for its antiarrhythmic action.索他洛尔通过增强细胞间偶联促进自发性心室除颤。这是其抗心律失常作用的一种全新机制。
Heart Vessels. 1995;10(4):185-9. doi: 10.1007/BF01744984.
2
Sotalol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use.索他洛尔。对其药效学和药代动力学特性以及治疗用途的综述。
Drugs. 1987 Sep;34(3):311-49. doi: 10.2165/00003495-198734030-00002.
3
Effects of nipradilol on myocardial ischaemia produced by coronary stenosis in dogs.
尼普地洛对犬冠状动脉狭窄所致心肌缺血的影响。
Br J Pharmacol. 1987 Jun;91(2):411-9. doi: 10.1111/j.1476-5381.1987.tb10296.x.