Article
State dependent dissociation of HERG channel inhibitors.
British journal of pharmacology - 1 Aug 2007
Stork D, Timin E N, Berjukow S, Huber C, Hohaus A, Auer M, Hering S
Abstract excerpt
BACKGROUND AND PURPOSE: Inhibition of HERG channels prolongs the ventricular action potential and the QT interval with the risk of torsade de pointes arrhythmias and sudden cardiac death. Many drugs induce greater inhibition of HERG channels when the cell membrane is depolarized frequently. The dependence of inhibition on the pulsing rate may yield different IC(50) values at different frequencies and thus affect...
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