Effects of quinine and quinidine on the transient outward and on the L-type Ca2+ current in rat ventricular cardiomyocytes

被引:18
|
作者
Michel, D [1 ]
Wegener, JW [1 ]
Nawrath, H [1 ]
机构
[1] Univ Mainz, Inst Pharmakol, D-55101 Mainz, Germany
关键词
heart muscle; stereoselectivity; tertiary amines; pH value; binding sites; channel state;
D O I
10.1159/000064342
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effects of the enantiomers quinine and quinidine on the transient outward current (I-to) and on the L-type Ca2+ current (I-Ca) were investigated in rat ventricular cardiomyocytes using the patch-clamp technique. At a stimulation frequency of 2 Hz, both quinine depressed the magnitude of I-to and I-Ca; the half-maximal effects on Ito were achieved at 11 and 15 mumol/l, respectively, and those on I-Ca at 14 and 10 mumol/l, respectively. At 0.2 Hz, both drugs depressed the magnitude of I-to, but not that of I-Ca. A change in extracellular pH from 7.3 to 8.3 did not significantly influence the effects of the drugs (which are protonated to 98% at pH 7.3) on I-to or I-Ca. It is concluded that neither the different chemical structure nor the amount of protonation of quinine and quinidine controls their effects on I-to or I-Ca. Copyright (C) 2002 S. Karger AG, Basel.
引用
收藏
页码:187 / 192
页数:6
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