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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Changes of action potential and L-type calcium channel current of Sprague-Dawley rat ventricular myocytes by different amlodipine isomers.
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Changes of action potential and L-type calcium channel current of Sprague-Dawley rat ventricular myocytes by different amlodipine isomers.

机译：不同氨氯地平异构体对Sprague-Dawley大鼠心室肌细胞动作电位和L型钙通道电流的变化。

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摘要

To investigate the effects of S- and R-amlodipine (Aml) on action potential (AP) and L-type calcium channel current (ICa-L), the whole-cell patch-clamp technique was used on rat ventricular myocytes to record AP, ICa-L, peak currents, steady-state activation currents, steady-state inactivation currents, and recovery currents from inactivation with S-Aml and R-Aml at various concentrations. Increasing concentrations of S-Aml gradually shortened AP durations (APDs). At concentrations of 0.1, 0.5, 1, 5, and 10 micromol/L, S-Aml blocked 1.5% +/- 0.2%, 25.4% +/- 5.3%, 65.2% +/- 7.3%, 78.4% +/- 8.1%, and 94.2% +/- 5.0% of ICa-L, respectively (p < 0.05), and the half-inhibited concentration was 0.62 +/- 0.12 micromol/L. Current-voltage curves were shifted upward; steady-state activation and inactivation curves were shifted to the left. At these concentrations of S-Aml, the half-activation voltages were -16.01 +/- 1.65, -17.61 +/- 1.60, -20.17 +/- 1.46, -21.87 +/- 1.69, and -24.09 +/- 1.87 mV, respectively, and the slope factors were increased (p < 0.05). The half-inactivation voltages were -27.16 +/- 4.48, -28.69 +/- 4.52, -31.19 +/- 4.17, -32.63 +/- 4.34, and -35.16 +/- 4.46 mV, respectively, and the slope factors were increased (p < 0.05). The recovery times from inactivation of S-Aml were prolonged (p < 0.05). In contrast, R-Aml had no effect on AP and ICa-L (p > 0.05) at the concentrations tested. Thus, only S-Aml has calcium channel blockade activity, whereas R-Aml has none of the pharmacologic actions associated with calcium channel blockers.
机译：为了研究S-和R-氨氯地平（Aml）对动作电位（AP）和L型钙通道电流（ICa-L）的影响，将全细胞膜片钳技术用于大鼠心室肌细胞以记录AP ，ICa-L，峰值电流，稳态激活电流，稳态失活电流以及在不同浓度下用S-Aml和R-Aml失活的恢复电流。 S-Aml浓度的增加逐渐缩短了AP持续时间（APD）。在0.1、0.5、1、5和10 micromol / L的浓度下，S-Aml封闭1.5％+/- 0.2％，25.4％+/- 5.3％，65.2％+/- 7.3％，78.4％+/- ICa-L分别为8.1％和94.2％+/- 5.0％（p <0.05），半抑制浓度为0.62 +/- 0.12 micromol / L。电流-电压曲线向上移动;稳态激活和灭活曲线向左移动。在这些S-Aml浓度下，半激活电压为-16.01 +/- 1.65，-17.61 +/- 1.60，-20.17 +/- 1.46，-21.87 +/- 1.69和-24.09 +/- 1.87 mV ，并且斜率因子增加（p <0.05）。半灭活电压分别为-27.16 +/- 4.48，-28.69 +/- 4.52，-31.19 +/- 4.17，-32.63 +/- 4.34和-35.16 +/- 4.46 mV，斜率分别为增加（p <0.05）。 S-Aml失活的恢复时间延长（p <0.05）。相反，在测试浓度下，R-Aml对AP和ICa-L没有影响（p> 0.05）。因此，仅S-Aml具有钙通道阻滞活性，而R-Aml不具有与钙通道阻滞剂有关的药理作用。

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