Chinfloxacin hydrochloride inhibits HERG potassium channel at open state.
- Author:
Xiang-mei ZHANG
1
;
Zhong-hua ZHU
;
Xiao-li SUN
;
Jia GUO
;
Zhong-zhong ZHAO
;
Zhao ZHANG
Author Information
1. Jiangsu Key Laboratory for Molecular and Medical Biotechnology, Nanjing Normal University, Nanjing 210046, China.
- Publication Type:Journal Article
- MeSH:
Anti-Bacterial Agents;
administration & dosage;
chemistry;
pharmacology;
Aza Compounds;
pharmacology;
Dose-Response Relationship, Drug;
Ether-A-Go-Go Potassium Channels;
antagonists & inhibitors;
physiology;
Fluoroquinolones;
administration & dosage;
chemistry;
pharmacology;
HEK293 Cells;
Humans;
Inhibitory Concentration 50;
Kinetics;
Molecular Structure;
Patch-Clamp Techniques;
Potassium;
pharmacology;
Quinolines;
pharmacology;
Time Factors;
Transfection
- From:
Acta Pharmaceutica Sinica
2010;45(12):1491-1496
- CountryChina
- Language:Chinese
-
Abstract:
This study is designed to investigate the effects of chinfloxacin hydrochloride (CFX) on the kinetics of HERG K+ channel. Whole cell patch clamp technique was used to record HERG K+ currents from HEK293 cells transiently transfected with cgi-HERG-GFP plasmids and channel kinetics were assessed in the absence and presence of CFX and moxifloxacin hydrochloride (MOX). Results demonstrated that the open state of HERG K+ channel was inhibited by CFX in a concentration- and time-dependent manner, with an IC50 of 162.1 +/- 14.2 micromol x L(-1), two folds higher than its positive control MOX. But there were no significant effects on channel kinetics. In addition, the inhibitory effect of CFX on HERG was enhanced when cells were subjected to altered extracellular K+ concentration.
