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Inhibition of hERG K+ currents by antimalarial drugs in stably transfected HEK293 cells.

Abstract：

:Several antimalarial drugs are known to produce a QT interval prolongation via a blockade of the rapidly activating delayed rectifier K+ current (IKr), encoded by the human-ether-a-go-go-related gene (hERG). We investigated the influence of lumefantrine and its major metabolite desbutyl-lumefantrine, as well as halofantrine, chloroquine, and mefloquine, on wild type hERG K+ channels in stably transfected human embryonic kidney cells (HEK293) using the whole cell patch-clamp technique. All of the tested antimalarial drugs inhibited the hERG K+ channels in a concentration- and time-dependent manner. Only halofantrine blocked hERG tail currents voltage-dependently. The ranking of the half-maximal inhibitory concentrations (IC50) of the antimalarials was: halofantrine (0.04 microM)

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Traebert M,Dumotier B,Meister L,Hoffmann P,Dominguez-Estevez M,Suter W

doi

10.1016/j.ejphar.2003.11.003

keywords:

subject

Has Abstract

pub_date

2004-01-19 00:00:00

pages

41-8

issue

1

eissn

0014-2999

issn

1879-0712

pii

S0014299903026323

journal_volume

484

pub_type

杂志文章

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