Bay K8644对心脏细胞中钙通道电流的电压依赖性调节
Voltage-dependent modulation of Ca channel current in heart cells by Bay K8644.
作者信息
Sanguinetti M C, Krafte D S, Kass R S
出版信息
J Gen Physiol. 1986 Sep;88(3):369-92. doi: 10.1085/jgp.88.3.369.
Abstract
We have investigated the voltage-dependent effects of the dihydropyridine Bay K8644 on Ca channel currents in calf Purkinje fibers and enzymatically dispersed rat ventricular myocytes. Bay K8644 increases the apparent rate of inactivation of these currents, measured during depolarizing voltage pulses, and shifts both channel activation and inactivation in the hyperpolarizing direction. Consequently, currents measured after hyperpolarizing conditioning pulses are larger in the presence of drug compared with control conditions, but are smaller than control if they are measured after positive conditioning pulses. Most of our experimental observations on macroscopic currents can be explained by a single drug-induced change in one rate constant of a simple kinetic model. The rate constant change is consistent with results obtained by others with single channel recordings.
摘要
我们研究了二氢吡啶类药物Bay K8644对小牛浦肯野纤维和酶分散的大鼠心室肌细胞钙通道电流的电压依赖性作用。Bay K8644增加了在去极化电压脉冲期间测量的这些电流的表观失活速率，并使通道激活和失活都向超极化方向移动。因此，与对照条件相比，在超极化预处理脉冲后测量的电流在药物存在时更大，但如果在正预处理脉冲后测量则比对照小。我们对宏观电流的大多数实验观察结果可以用简单动力学模型的一个速率常数的单一药物诱导变化来解释。速率常数的变化与其他人通过单通道记录获得的结果一致。
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Nisoldipine: a new, more selective calcium current blocker in cardiac Purkinje fibers.尼索地平：一种新型、对心脏浦肯野纤维更具选择性的钙电流阻滞剂。
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