Bischoff U, Schmidt C, Netzer R, Pongs O
GENION Forschungsgesellschaft, Abteistrasse 57, 20149, Hamburg, Germany.
Eur J Pharmacol. 2000 Oct 20;406(3):341-3. doi: 10.1016/s0014-2999(00)00693-2.
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.
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。
