Effects of fluoroquinolones on HERG currents

被引：96

作者：

Bischoff, U ^{[1
]}

Schmidt, C ^{[1
]}

Netzer, R ^{[1
]}

Pongs, O ^{[1
]}

机构：

[1] GENION Forsch Gesell, D-20149 Hamburg, Germany

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 2000年 / 406卷 / 03期

关键词：

HERG; QT-prolongation; fluoroquinolones; patch-clamp technique;

D O I：

10.1016/S0014-2999(00)00693-2

中图分类号：

R9 [药学];

学科分类号：

1007 [药学];

摘要：

We have investigated the effects of four fluoroquinolones on the human ether-a-go-go-related gene (HERG) mediated K+ currents to evaluate their potential to induce QT-prolongation. HERG currents were measured from stably transfected Chinese hamster ovary (CHO) cells by means of the patch-clamp technique. Bath application of sparfloxacin, moxifloxacin and grepafloxacin produced an inhibition of HERG outward currents at -40 mV with EC50 of 13.5 +/- 0.8, 41.2 +/- 2.0 and 37.5 +/- 3.3 mug/ml, respectively. Current inhibitions were reversible after washout of the compounds. By contrast, ciprofloxacin at concentrations of up to 100 mug/ml did not effect HERG outward currents. (C) 2000 Elsevier Science B.V. All rights reserved.

引用

收藏

页码：341 / 343

页数：3

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