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首页> 外文期刊>Acta Pharmacologica Sinica >Imipramine blocks the transient outward potassium current in rat ventricular myocytes
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Imipramine blocks the transient outward potassium current in rat ventricular myocytes

机译：丙咪嗪阻断大鼠心室肌细胞的瞬时向外钾电流

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摘要

AIM: To examine the effects of imipramine on transient outward potassium current (I_to) in rat ventricular myocytes. METHODS: The patch- damp whole-cell recording techniques were used. RESULTS: Imipramine resulted in a concentration- dependent inhibition of I_to, with the IC_50 of 6.0 μmol·L~-1 and a concentration-dependent accelera- tion of I_to inactivation. The blocking showed no difference at different testing membrane potentials. Imipramine produced slight effects (about 3 and 4 mV, respectively) on steady-state activation and inactivation curves of I_to, and tended to prolong the recovery of I_to from inactivation (τ_control = 37±11 ms; τ_drug = 58±17 ms), but not significant (n=4, P>0.05). The inhibitory effect of imipramine on I_to was increased when the prepulses were prolonged progressively from 0 to 120 ms. (τ_control = 22±8 ms; τ_drug = 14±5 ms). CONCLUDIONS: Imipramine blocked I_to in concentration-dependent but voltage-independent manners, and with "open channel blocking" properties.
机译：目的：研究丙咪嗪对大鼠心室肌细胞瞬时外向钾电流（I_to）的影响。方法：使用贴片湿润全细胞记录技术。结果：丙咪嗪导致I_to的浓度依赖性抑制，IC_50为6.0μmol·L〜-1，且I_to失活的浓度依赖性加速。阻断在不同的测试膜电位下没有显示出差异。丙咪嗪对I_to的稳态激活和失活曲线产生轻微影响（分别约为3和4 mV），并倾向于延长I_to从失活的恢复时间（τ_control= 37±11 ms；τ_drug= 58±17 ms），但不显着（n = 4，P> 0.05）。当预脉冲从0 ms逐渐延长到120 ms时，丙咪嗪对I_to的抑制作用增强。 （τ_控制＝ 22±8ms；τ_药物＝ 14±5ms）。结论：丙咪嗪以浓度依赖性但与电压无关的方式阻断I_to，并具有“明渠阻断”特性。

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