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The Antidepressant Drug Fluoxetine Is an Inhibitor of Human Ether-A-Go-Go-Related Gene (HERG) Potassium Channels

The Journal of Pharmacology and Experimental Therapeutics, 2002
Fluoxetine is a commonly prescribed antidepressant compound. Its action is primarily attributed to selective inhibition of the reuptake of serotonin (5-hydroxytryptamine) in the central nervous system. Although this group of antidepressant drugs is generally believed to cause fewer proarrhythmic side effects compared with tricyclic antidepressants ...
Bernd Gut   +3 more
openaire   +2 more sources

Molecular Determinants of Cocaine Block of Human Ether-á-go-go-Related Gene Potassium Channels

The Journal of Pharmacology and Experimental Therapeutics, 2006
The use of cocaine causes cardiac arrhythmias and sudden death. Blockade of the cardiac potassium channel human ether-á-go-go-related gene (hERG) has been implicated as a mechanism for the proarrhythmic action of cocaine. hERG encodes the pore-forming subunits of the rapidly activating delayed rectifier K(+) channel (I(Kr)), which is important for ...
Jun Guo, Hongying Gang, Shetuan Zhang
openaire   +3 more sources

Halide Ion Effects on HumanEther-à-go-goRelated Gene Potassium Channel Properties

ASSAY and Drug Development Technologies, 2013
The human Ether-à-go-go related gene (hERG) potassium channel has been widely used to counter screen potential pharmaceuticals as a biomarker to predict clinical QT prolongation. Thus, higher throughput assays of hERG are valuable for early in vitro screening of drug candidates to minimize failure in later-stage drug development due to this potentially
Joseph J. Salata   +5 more
openaire   +3 more sources

Development of a high-throughput electrophysiological assay for the human ether-à-go-go related potassium channel hERG

Journal of Pharmacological and Toxicological Methods, 2013
Drug-induced prolongation of the QT interval via block of the hERG potassium channel is a major cause of attrition in drug development. The advent of automated electrophysiology systems has enabled the detection of hERG block earlier in drug discovery.
Brian Donovan   +4 more
openaire   +3 more sources

Blockade of Human Cardiac Potassium Channel Human Ether-a-go-go-Related Gene (HERG) by Macrolide Antibiotics

The Journal of Pharmacology and Experimental Therapeutics, 2002
Several macrolides have been reported to cause QT prolongation and ventricular arrhythmias such as torsades de pointes. To clarify the underlying ionic mechanisms, we examined the effects of six macrolides on the human ether-a-go-go-related gene (HERG)-encoded potassium current stably expressed in human embryonic kidney-293 cells.
Jing Lin   +4 more
openaire   +3 more sources

Self‐Assembled Artificial Ion‐Channels toward Natural Selection of Functions

Angewandte Chemie - International Edition, 2021
Li-bo Huang, Zhanhu Sun, Mihail Barboiu
exaly  

Angstrom-scale ion channels towards single-ion selectivity

Chemical Society Reviews, 2022
Huacheng Zhang, Xingya Li, Jue Hou
exaly  

Artificial channels for confined mass transport at the sub-nanometre scale

Nature Reviews Materials, 2021
Gongping Liu, Jie Shen, Wanqin Jin
exaly  

Water in Nanopores and Biological Channels: A Molecular Simulation Perspective

Chemical Reviews, 2020
Charlotte I Lynch   +2 more
exaly  

Voltage-gated potassium channels as therapeutic targets

Nature Reviews Drug Discovery, 2009
Heike Wulff, Neil A Castle, Luis A Pardo
exaly  

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