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阿普林定对兔窦房结细胞所致心动过缓的研究。

Studies on the bradycardia induced by aprindine in rabbit sinoatrial node cells.

作者信息

Kotake H, Igawa O, Miyamoto J, Hasegawa J, Furuse T, Mashiba H

出版信息

Pharmacology. 1986;33(1):14-20. doi: 10.1159/000138194.

Abstract

The effects of aprindine (1 X 10(-7) to 4 X 10(-6) M) were examined on membrane potential and current of rabbit sinoatrial node by means of conventional microelectrode and double microelectrode voltage clamp methods. Aprindine decreased, in a dose-dependent manner, the spontaneously firing frequency, the maximum rate of depolarization and the action potential amplitude, and prolonged the action potential duration at half-amplitude. The slope of the diastolic depolarization was also reduced by the drug. In the voltage clamp experiment, aprindine reduced the slow inward current (Isi), the time-dependent potassium current (Ik) and the hyperpolarization activated current (Ih). The recovery time constant of Isi was prolonged by aprindine, while the kinetics of Ik was not altered. It is indicated that aprindine does not have an effect on a specific conductance or a single current system, but that the drug exerts an inhibitory effect on the electrical activity of sinoatrial node.

摘要

采用传统微电极和双微电极电压钳方法,研究了阿普林定(1×10⁻⁷至4×10⁻⁶M)对兔窦房结膜电位和电流的影响。阿普林定以剂量依赖性方式降低自发放电频率、最大去极化速率和动作电位幅度,并延长动作电位半幅持续时间。该药还降低了舒张期去极化斜率。在电压钳实验中,阿普林定降低了慢内向电流(Isi)、时间依赖性钾电流(Ik)和超极化激活电流(Ih)。阿普林定延长了Isi的恢复时间常数,而Ik的动力学未改变。结果表明,阿普林定对特定电导率或单一电流系统无影响,但对窦房结的电活动有抑制作用。

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