Blockade of HERG Human K+ Channels by the Antidepressant Drug Paroxetine
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概要
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The effects of paroxetine, a selective serotonin reuptake inhibitor, on human ether-a-go-go-related gene (HERG) channels were investigated using the whole-cell patch-clamp technique. The HERG channels were stably expressed in human embryonic kidney cells. Paroxetine inhibited the peak tail currents of the HERG channel in a concentration-dependent manner, with an IC50 value of 0.45 µM and a Hill coefficient of 0.85. These effects were reversible after wash-out of the drug. The paroxetine-induced inhibition of the HERG channels was voltage-dependent. There was a steep increase in inhibition over the voltage range of the channel opening. Also, a shallow voltage-dependent inhibition was detected over the voltage range in which the channels were fully activated. The fractional electrical distance was estimated to be 0.11. Paroxetine induced a leftward shift in the voltage-dependence of the steady-state activation of the HERG channels. Before and after application of the 1 µM paroxetine, the half-maximum activation was −14.21 mV and −27.04 mV, respectively, with no shift in the slope value. The HERG channel block was not use-dependent. The characteristics of the block were dependent on open and inactivated channel states rather than closed state. Paroxetine had no effect on activation and deactivation kinetics, steady-state inactivation. These results suggest that paroxetine blocks the HERG channels by binding to these channels in the open and inactivated states.
著者
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Choe Han
Department Of Physiology And Research Institute For Biomacromolecules University Of Ulsan College Of
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Choi Bok
Department Of Pharmacology Chonbuk National University Medical School
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Hahn Sang
Department Of Physics Chung-ang University
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Lee Seung
Department Of Anesthesiology And Pain Medicine Dong-a University Hospital
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Sung Min
Department Of Computer Science And Engineering College Of Information And Communication Korea University
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Lee Hyang
Department of Pharmacology, Institute for Medical Sciences, Chonbuk National University Medical School
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SUNG Min
Department of Pharmacology, Institute for Medical Sciences, Chonbuk National University Medical School
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Chu Daehyun
Department of Physiology, Bio-Medical Institute of Technology, University of Ulsan College of Medicine
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Jo Su-Hyun
Department of Physiology, Institute of Bioscience and Biotechnology, BK21 plus Graduate Program, Kangwon National University College of Medicine
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