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4-氨基喹啉、奎尼丁和利多卡因对蛙心房收缩纤维电生理效应的比较。

Comparison of the electrophysiological effects of 4-aminoquinoline, quinidine and lidocaine on frog atrial contractile fibres.

作者信息

Guerrero S, Zacharías J

出版信息

Gen Pharmacol. 1984;15(5):385-9. doi: 10.1016/0306-3623(84)90035-1.

DOI:10.1016/0306-3623(84)90035-1
PMID:6510673
Abstract

Standard microelectrode techniques were used to study the electrophysiological effects of 4-aminoquinoline (4-AQ), a 4-aminopyridine analogue, on frog atrial contractile fibres and the effects compared with those of quinidine and lidocaine. The effects of 4-AQ (250 and 500 microM) were: reduction of action potential amplitude, overshoot and maximum upstroke velocity (Vmax) and increase of action potential duration. These effects were reversible after washing. No change in membrane resting potential was observed with these drug concentrations. Quinidine (27 and 54 microM) caused no statistically significant changes of resting potential and overshoot but dose-dependently decreased Vmax. Action potential duration (APD) was shortened or unchanged at 60% repolarization, whereas at 90% repolarization APD was increased by the higher concentration of this drug. Quinidine (54 microM) also depressed action potential amplitude. Lidocaine (17 microM) induced a slight decrease of action potential amplitude and a marked reduction of Vmax as well as of APD without changing membrane resting potential or overshoot. Comparison of these results indicate that 4-AQ and quinidine share most electrophysiological effects such as depression of upstroke velocity, action potential total amplitude and repolarization rate at phase 3 of the transmembrane potential. Lidocaine and 4-AQ share only the capability of decreasing Vmax, whereas the effect upon repolarization was the opposite. Consequently, this study together with a previous one of our laboratory (Guerrero, 1982) suggest that 4-AQ is a drug having some quinidine-like properties.

摘要

采用标准微电极技术研究了4-氨基喹啉(4-AQ)(一种4-氨基吡啶类似物)对蛙心房收缩纤维的电生理效应,并将其与奎尼丁和利多卡因的效应进行比较。4-AQ(250和500微摩尔)的效应为:动作电位幅度、超射值和最大上升速度(Vmax)降低,动作电位时程延长。冲洗后这些效应可逆。这些药物浓度下未观察到膜静息电位的变化。奎尼丁(27和54微摩尔)对静息电位和超射值无统计学显著影响,但剂量依赖性地降低Vmax。在复极化60%时动作电位时程(APD)缩短或无变化,而在复极化90%时,该药物较高浓度可使APD延长。奎尼丁(54微摩尔)也降低动作电位幅度。利多卡因(17微摩尔)使动作电位幅度略有降低,Vmax以及APD显著降低,而膜静息电位或超射值无变化。这些结果比较表明,4-AQ和奎尼丁具有大多数电生理效应,如跨膜电位3期上升速度、动作电位总幅度和复极化速率降低。利多卡因和4-AQ仅具有降低Vmax的能力,而复极化效应相反。因此,本研究与我们实验室之前的一项研究(格雷罗,1982年)共同表明,4-AQ是一种具有某些奎尼丁样特性的药物。

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