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牵张激活离子通道阻滞剂钆也能阻断豚鼠离体心室肌细胞中的L型钙通道。

The stretch-activated ion channel blocker gadolinium also blocks L-type calcium channels in isolated ventricular myocytes of the guinea-pig.

作者信息

Lacampagne A, Gannier F, Argibay J, Garnier D, Le Guennec J Y

机构信息

Laboratoire de Physiologie des Cellules Cardiaques et Vasculaires, EP21 CNRS, Faculté des Sciences, Tours, France.

出版信息

Biochim Biophys Acta. 1994 Apr 20;1191(1):205-8. doi: 10.1016/0005-2736(94)90250-x.

Abstract

We show that gadolinium (Gd3+) is a potent calcium channel blocker in guinea-pig isolated ventricular myocytes. A dose-dependent inhibition of ICaL was found with an EC50 of 1.4 microM and a complete inhibition at 10 microM Gd3+. When compared with Cd2+, it appeared that the blockade of ICaL is a complex phenomenon probably involving more than one site of interaction (a Hill coefficient of 1.6 was found for Gd3+ vs. 1.0 for Cd2+). It is concluded that Gd3+ ions completely block ICaL at concentrations used to block stretch-activated channels (SAC), rendering its use as a specific SAC inhibitor problematic.

摘要

我们发现钆(Gd3+)是豚鼠离体心室肌细胞中一种有效的钙通道阻滞剂。发现对L型钙电流(ICaL)有剂量依赖性抑制,半数有效浓度(EC50)为1.4微摩尔,在10微摩尔Gd3+时完全抑制。与镉离子(Cd2+)相比,似乎对ICaL的阻断是一个复杂现象,可能涉及多个相互作用位点(Gd3+的希尔系数为1.6,而Cd2+为1.0)。得出的结论是,Gd3+离子在用于阻断牵张激活通道(SAC)的浓度下完全阻断ICaL,这使得将其用作特异性SAC抑制剂存在问题。

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