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首页> 外文期刊>Pharmacology: International Journal of Experimental and Clinical Pharmacology >Y-27632, a Rho-Associated Protein Kinase Inhibitor, Inhibits Voltage-Dependent K plus Channels in Rabbit Coronary Arterial Smooth Muscle Cells
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Y-27632, a Rho-Associated Protein Kinase Inhibitor, Inhibits Voltage-Dependent K plus Channels in Rabbit Coronary Arterial Smooth Muscle Cells

机译:Y-27632,Rho相关的蛋白激酶抑制剂,抑制兔冠状动脉平滑肌细胞中的电压依赖性钾离子通道

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We examined the effects of the Rho-associated protein kinase (ROCK) inhibitor Y-27632 on voltage-dependent K+ (Kv) channels in rabbit coronary arterial smooth muscle cells using the whole-cell patch clamp technique. Y-27632 reduced the amplitude of the Kv current in a concentration-dependent manner, with an IC50 of 0.87 +/- 0.06 mu mol/l and a Hill coefficient of 1.48 +/- 0.06. Y-27632 did not affect the steady-state activation or inactivation curves, suggesting that the drug does not affect the voltage sensitivity of Kv channels. Another ROCK inhibitor, H-1152, did not affect the Kv current and had no significant effect on the Y-27632-induced inhibition of Kv channels, indicating that the inhibitory effect of Y-27632 on the Kv current is independent of ROCK signaling. From these results, we conclude that Y-27632 inhibits the Kv channel current in a dose-dependent and ROCK signaling-independent manner. (C) 2016 S. Karger AG, Basel
机译:我们使用全细胞膜片钳技术检查了Rho相关蛋白激酶(ROCK)抑制剂Y-27632对兔冠状动脉平滑肌细胞中电压依赖性K +(Kv)通道的影响。 Y-27632以浓度依赖的方式降低Kv电流的幅度,IC50为0.87 +/- 0.06μmol / l,希尔系数为1.48 +/- 0.06。 Y-27632不会影响稳态激活或失活曲线,这表明该药物不会影响Kv通道的电压敏感性。另一种ROCK抑制剂H-1152不会影响Kv电流,并且对Y-27632诱导的Kv通道抑制没有显着影响,表明Y-27632对Kv电流的抑制作用与ROCK信号无关。从这些结果,我们得出结论,Y-27632以剂量依赖和ROCK信号独立的方式抑制Kv通道电流。 (C)2016 S.Karger AG,巴塞尔

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