论文部分内容阅读
卡维地洛和维司力农是近年来受到瞩目的慢性充血性心力衰竭治疗药。电生理学研究表明这些药物可适度延长心室肌的动作电位时程(APD)而无明显的逆频度依存性,然而其产生这一作用的离子机制是不同的。卡维地洛可阻断L-型钙电流(I_(Ca)),一过性外向钾电流(I_(to))以及延迟整流钾电流(I_K),特别是其快速激活成份(I_(Kr))。维司力农是一个选择性的I_K阻滞剂,具有独特的药物-通道相互作用。根据维司力农对I_K的电位与时间依存性抑制作用,该药被认为在I_K(主要是I_(Kr))通道处于激活状态时与其结合,而在通道关闭时则发生解离。这些电生理学特性将为器质性心脏病患者理想的抗心律失常药的开发提供新的途径。
Carvedilol and Vernilidon are the therapeutic agents of chronic congestive heart failure that have drawn much attention in recent years. Electrophysiological studies have shown that these drugs can moderately prolong the action potential time-history (APD) of ventricular muscles without significant inverse frequency dependence, whereas the ionic mechanism that produces this effect is different. Carvedilol blocked L-type calcium current (I_ (Ca)), transient outward current (I_ (to)) and delayed rectifier potassium current (I_K), especially its rapid activation component )). Vernilone is a selective I_K blocker with unique drug-channel interactions. According to the potency and time-dependent inhibition of verapamil on I_K, the drug is thought to bind to I_K (mainly the I_ (Kr)) channel when activated and dissociate when the channel is closed. These electrophysiological properties will provide new avenues for the development of ideal anti-arrhythmic drugs in patients with structural heart disease.