van Ginneken A C, Bouman L N, Jongsma H J, Duivenvoorden J J, Opthof T, Giles W R
Department of Physiology, Academic Medical Centre, Amsterdam, The Netherlands.
Eur Heart J. 1987 Dec;8 Suppl L:25-33. doi: 10.1093/eurheartj/8.suppl_l.25.
Three different bradycardic agents, alinidine, AQ-A39 and UL-FS49 increase the intrinsic cycle length of the isolated SA node preparation of the rabbit. This increase is mainly caused by a decrease in rate of diastolic depolarization. One of these agents, alinidine, was used to study the underlying ionic mechanism of the decrease in the diastolic depolarization rate in isolated cells and small cell clusters of the rabbit SA node. In these preparations alinidine slowed down the rate of spontaneous activity at higher concentrations (80 microM). At lower concentrations (10 microM) the decrease in rate of spontaneous activity was variable, but injection of a hyperpolarizing current slowed the spontaneous rate more in the presence of alinidine, indicating an increase in membrane resistance. In voltage clamp experiments we found that the main effect of alinidine was a block of the hyperpolarization activated current if. The block was potential dependent and was maximal in the potential range in which diastolic depolarization occurs. These results are discussed in relation to previous findings of others.
三种不同的心动过缓药物,阿利尼定、AQ - A39和UL - FS49可增加兔离体窦房结标本的固有周期长度。这种增加主要是由舒张期去极化速率降低引起的。其中一种药物阿利尼定被用于研究兔窦房结离体细胞和小细胞簇舒张期去极化速率降低的潜在离子机制。在这些标本中,阿利尼定在较高浓度(80微摩尔)时减慢了自发活动速率。在较低浓度(10微摩尔)时,自发活动速率的降低是可变的,但在阿利尼定存在的情况下,注入超极化电流会使自发速率减慢得更多,这表明膜电阻增加。在电压钳实验中,我们发现阿利尼定的主要作用是阻断超极化激活电流If。这种阻断是电压依赖性的,并且在发生舒张期去极化的电位范围内最大。将结合其他人先前的研究结果对这些结果进行讨论。