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• W1589702965 startingPage "643" @default.
• W1589702965 abstract "Abstract: The administration of certain fluoroquinolone antibacterials has recently been linked to QT interval prolongation, raising the clinical concerns over the cardiotoxicity of these agents. In this study, the effects of a novel fluoroquinolone, antofloxacin hydrochloride (AX) on human-ether-à-go-go-related gene (HERG) encoding potassium channels and the biophysical mechanisms of drug action were performed with whole-cell patch-clamp technique in transiently transfected HEK293 cells. The administration of AX caused voltage- and time-dependent inhibition of HERG K+ current (IHERG/MiRP1) in a concentration-dependent manner but did not markedly modify the properties of channel kinetics, including activation, inactivation, deactivation and recovery from inactivation as well. In comparison with sparfloxacin (SPX), levofloxacin lactate (LVFX), the potency of AX to inhibit HERG tail currents was the least one, with an IC50 value of 460.37 μM. By contrast, SPX was the most potent compound, displaying an IC50 value of 2.69 μM whereas LVFX showed modest potency, with an IC50 value of 43.86 μM, respectively. Taken together, our data suggest that AX only causes a minor reduction of IHERG/MiRP1 at the estimated free plasma level." @default.
• W1589702965 created "2016-06-24" @default.
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• W1589702965 date "2010-03-25" @default.
• W1589702965 modified "2023-10-07" @default.
• W1589702965 title "The Action of a Novel Fluoroquinolone Antibiotic Agent Antofloxacin Hydrochloride on Human-Ether-à-go-go-Related Gene Potassium Channel" @default.
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• W1589702965 doi "https://doi.org/10.1111/j.1742-7843.2010.00550.x" @default.
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