Ca2+ channel sensitivity towards the blocker isradipine is affected by alternative splicing of the human α1C subunit gene

被引：59

作者：

Zühlke, RD ^{[1
]}

Bouron, A ^{[1
]}

Soldatov, NM ^{[1
]}

Reuter, H ^{[1
]}

机构：

[1] Univ Bern, Dept Pharmacol, CH-3010 Bern, Switzerland

来源：

FEBS LETTERS | 1998年 / 427卷 / 02期

关键词：

Ca2+ channel; splice variant; channel blocker; dihydropyridine; Xenopus oocyte;

D O I：

10.1016/S0014-5793(98)00425-6

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

L-type Ca2+ channels are important targets for drugs, such as dihydropyridines (DHPs), in the treatment of cardiovascular diseases. Channel expression is regulated by alternative splicing, It has been suggested that in the cardiovascular system tissue-specific expression of different L-type Ca2+ channel splice variants may underlie the observed differences in sensitivities to channel block by DHPs. We investigated the sensitivity of Ca2+ channel splice variants derived from the hunlan alpha(1C) gene to the DHP isradipine, Among seven alpha(1C) channels we observed up to IO-fold differences in IC50 values for isradipine, as well as changes in the voltage dependence of DHP action. (C) 1998 Federation of European Biochemical Societies.

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页码：220 / 224

页数：5

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