Blockade of HERG channels expressed in Xenopus oocytes by the histamine receptor antagonists terfenadine and astemizole

被引：190

作者：

Suessbrich, H ^{[1
]}

Waldegger, S ^{[1
]}

Lang, F ^{[1
]}

Busch, AE ^{[1
]}

机构：

[1] UNIV TUBINGEN,INST PHYSIOL 1,D-72076 TUBINGEN,GERMANY

来源：

FEBS LETTERS | 1996年 / 385卷 / 1-2期

关键词：

histamine receptor antagonist; HERG; K+ channel; torsades de pointes;

D O I：

10.1016/0014-5793(96)00355-9

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：

The widely used histamine receptor antagonists terfenadine and astemizole were shown to prolong the QT interval in electrocardiographic recordings in cases of overdose or inappropriate co-medications, indicating a possible interaction with cardiac K+ channels. Here, terfenadine and astemizole both inhibited the human ether-a-go-go related gene (HERG) encoded channels expressed in Xenopus oocytes at nanomolar concentrations in a use- and voltage-dependent fashion. In contrast, inhibition of other delayed rectifier (Kv1.1 and I-sK) or inward rectifier K+ channels (IRK1) was much, weaker and occurred only at high micromolar concentrations. These results suggest that blockade of HERG channels by terfenadine and astemizole might contribute to the cardiac side effects of these compounds.

引用

页码：77 / 80

页数：4

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