Nelson W L, Makielski J C
Cardiac Electrophysiology Laboratories, University of Chicago, Ill.
Circ Res. 1991 Apr;68(4):977-83. doi: 10.1161/01.res.68.4.977.
Heptanol blocks sodium current (INa) in nerve, but its effects on cardiac INa have not been well characterized. Block of INa by heptanol was studied in 16 internally perfused voltage-clamped cardiac Purkinje cells at reduced Na+ (45 mM outside, 0 mM inside). Heptanol block of peak sodium conductance was well described by a single-site binding curve with half block at 1.3 mM (20 degrees C) and showed no "use dependence." With 1.5 mM heptanol, block increased slightly by 0.7%/degrees C from 10 degrees C to 27 degrees C. With 3.0 mM heptanol, steady-state availability shifted by 9.4 +/- 1.3 mV (n = 6) in the hyperpolarizing direction, and steady-state activation shifted by 8.3 +/- 2.2 mV (n = 5) in the depolarizing direction, thus closing off the INa "window current." Heptanol also decreased the time to peak and accelerated the decay of INa. Similar results were found with octanol at lower concentrations. These alcohols have important effects on cardiac INa at concentrations used in studies for cellular uncoupling in heart.
庚醇可阻断神经中的钠电流(INa),但其对心脏INa的影响尚未得到充分研究。在16个内部灌注的电压钳制心脏浦肯野细胞中,于低钠(细胞外45 mM,细胞内0 mM)条件下研究了庚醇对INa的阻断作用。庚醇对钠电导峰值的阻断作用可用单点结合曲线很好地描述,半阻断浓度为1.3 mM(20摄氏度),且未表现出“使用依赖性”。使用1.5 mM庚醇时,从10摄氏度至27摄氏度,阻断作用随温度以0.7%/摄氏度的幅度略有增加。使用3.0 mM庚醇时,稳态可用性向超极化方向移动9.4±1.3 mV(n = 6),稳态激活向去极化方向移动8.3±2.2 mV(n = 5),从而关闭INa“窗口电流”。庚醇还缩短了钠电流峰值出现的时间并加速了其衰减。在较低浓度下,辛醇也得到了类似结果。在用于心脏细胞去偶联研究的浓度下,这些醇类对心脏INa具有重要影响。