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首页> 外文期刊>Japanese Journal of Pharmacology >Modes of the Na Channel Blocking Action of Pilsicainide, a New Antiarrhythmic Agent, in Cardiac Cells
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Modes of the Na Channel Blocking Action of Pilsicainide, a New Antiarrhythmic Agent, in Cardiac Cells

机译：新型抗心律失常药物比西卡胺在心肌细胞中的钠通道阻断作用模式

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References(22) Cited-By(5) Using a whole cell clamp technique, the blockade of sodium currents (INa) by pilsicainide, a new antiarrhythmic agent, applied either intracellularly or extracellularly, was studied in single myocytes isolated from guinea pig right ventricle. Pilsicainide applied extracellularly inhibited the peak amplitude of INa in concentration (from 10-5 M to 10-4 M) and rate- (from 0.5 Hz to 3.0 Hz) dependent manners. The onset rate of the blockade in INa was almost constant, independent of frequency of stimulus, but higher at high concentration of pilsicainide. The time constant in the recovery phase from INa inactivation remained almost constant (65 to 75 msec) in the range of concentrations used. Similar results were obtained by intracellular application of 10-3 M pilsicainide. Pilsicainide applied intracellularly inhibited INa in a rate-dependent manner. The blocking potency of internally applied pilsicainide almost corresponded to that of external 10-5 M pilsicainide. The onset rate of INa inactivation (from 0.098/pulse to 0.130/pulse) and the recovery time constant (77 msec) was similar to those of external 10-5 M pilsicainide. These results suggest that pilsicainide, irrespective of intra- or extracellular application, shares a common binding site to block INa in cardiac myocytes.
机译：参考文献（22）被引用（5）使用全细胞钳技术，对从豚鼠右心室分离的单个心肌细胞中研究了新的抗心律不齐药物比尔西胺对细胞内或细胞外应用的钠电流（INa）的阻断作用。细胞外施用比西卡胺以浓度依赖性（从10-5 M到10-4 M）和速率依赖性（从0.5 Hz到3.0 Hz）抑制INa的峰幅度。 INa的阻滞发作率几乎恒定，与刺激频率无关，但在高浓度的比西卡尼中则更高。在所使用的浓度范围内，从INa失活的恢复阶段的时间常数几乎保持恒定（65到75毫秒）。通过细胞内施用10-3 M的pilsicainide获得了相似的结果。比西卡胺以速率依赖的方式在细胞内抑制INa。内部施用的比斯卡尼的封闭能力几乎与外部10-5 M的比斯卡尼的封闭能力相对应。 INa失活的发生率（从0.098 /脉冲到0.130 /脉冲）和恢复时间常数（77毫秒）与外部10-5 M pilsicainide相似。这些结果表明，无论在细胞内还是细胞外应用，比尔西胺都具有共同的结合位点来阻断心肌细胞中的INa。

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