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氟喹诺酮类药物对HERG电流的影响。

Effects of fluoroquinolones on HERG currents.

作者信息

Bischoff U, Schmidt C, Netzer R, Pongs O

机构信息

GENION Forschungsgesellschaft, Abteistrasse 57, 20149, Hamburg, Germany.

出版信息

Eur J Pharmacol. 2000 Oct 20;406(3):341-3. doi: 10.1016/s0014-2999(00)00693-2.

Abstract

We have investigated the effects of four fluoroquinolones on the human ether-à-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 EC(50) of 13.5+/-0.8, 41. 2+/-2.0 and 37.5+/-3.3 microg/ml, respectively. Current inhibitions were reversible after washout of the compounds. By contrast, ciprofloxacin at concentrations of up to 100 microg/ml did not effect HERG outward currents.

摘要

我们研究了四种氟喹诺酮类药物对人醚 - 去极化相关基因(HERG)介导的钾离子电流的影响,以评估它们诱发QT间期延长的可能性。通过膜片钳技术,从稳定转染的中国仓鼠卵巢(CHO)细胞中测量HERG电流。浴槽给药司帕沙星、莫西沙星和格帕沙星可抑制 - 40 mV时的HERG外向电流,其半数有效浓度(EC50)分别为13.5±0.8、41.2±2.0和37.5±3.3 μg/ml。洗脱化合物后,电流抑制作用可逆。相比之下,浓度高达100 μg/ml的环丙沙星对HERG外向电流无影响。

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