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Ruthenium red as an effective blocker of calcium and sodium currents in guinea-pig isolated ventricular heart cells

机译:钌红是豚鼠离体心室心脏细胞中钙和钠电流的有效阻断剂

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class="enumerated" style="list-style-type:decimal">The effect of ruthenium red on calcium and sodium currents was studied in guinea-pig isolated ventricular heart cells with the whole cell patch-clamp technique.Ruthenium red very efficiently blocked the L-type calcium current in a dose-dependent manner. A significant block was observed for concentrations as low as 0.3 μM. Analysis of the dose-response curve with the logistic equation indicated an EC50 of 0.8 μM, a maximum inhibition of 85% reached at 5 μM, and a coefficient of 2.37.There was no shift in the voltage-dependence of the Ca current activation, nor in that of its steady-state inactivation determined with a 1 s prepulse. However, removal of Ca current inactivation at positive voltage was considerably reduced in the presence of concentrations of ruthenium red above 1 μM. A slowing of the time-course of inactivation of the Ca current was also observed.At 10 μM, a concentration generally used to block the sarcoplasmic Ca release channels or the mitochondrial Ca uptake, ruthenium red blocked 26.7±4.3% (n=8) of the sodium current, and slowed its inactivation time-course. No effect was observed on the voltage-dependence of the current activation or inactivation. The peak sodium current was also decreased at a 10 times lower concentration by 7.6±2.7% (n=3).Thus, at concentrations used to assess intracellular Ca movements, ruthenium red induced in heart cells a significant block of both Ca and Na channels.
机译:class =“ enumerated” style =“ list-style-type:decimal”> <!-list-behavior =枚举前缀-word = mark-type = decimal max-label-size = 0-> 用全细胞膜片钳技术研究了钌红对豚鼠离体心室心肌细胞钙和钠电流的影响。 钌红非常有效地阻断了一定剂量的L型钙电流依赖的方式。浓度低至0.3μm时,观察到明显的阻滞。用logistic方程分析剂量-反应曲线表明,EC50为0.8μM,5μM时最大抑制率为85%,系数为2.37。 Ca电流激活的依赖性,也不依赖于以1μs的预脉冲确定的稳态灭活。但是,当钌红浓度超过1μM时,正电压下Ca电流失活的去除率大大降低。 在10μM时,通常用于阻止肌浆Ca释放通道或线粒体Ca吸收的浓度,钌红则可以使Ca电流失活的时间变慢。 钠电流的4.3%(n = 8),并减缓了它的失活时间。没有观察到对电流激活或失活的电压依赖性的影响。钠电流峰值在浓度降低10倍时降低了7.6±2.7%(n = 3)。 因此,在用于评估细胞内Ca运动的浓度下,心脏细胞中诱导的钌红显着降低。钙和钠通道的阻滞。

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