Block of HERG k channel by classic histamine h(1) receptor antagonist chlorpheniramine.

ABSTRACT: Chlorpheniramine is a potent first-generation histamine H(1) receptor antagonist that can increase action potential duration and induce QT prolongation in several animal models. Since block of cardiac human ether-a-go-go-related gene (hERG) channels is one of leading causes of acquired long QT syndrome, we investigated the acute effects of chlorpheniramine on hERG channels to determine the electrophysiological basis for its proarrhythmic potential. We examined the effects of chlorpheniramine on the hERG channels expressed in Xenopus oocytes using two-microelectrode voltage-clamp techniques. Chlorpheniramine induced a concentration-dependent decrease of the current amplitude at the end of the voltage steps and hERG tail currents. The IC(50) of chlorpheniramine-dependent hERG block in Xenopu

SUBMITTER: Hong HK 

PROVIDER: S-EPMC2766741 | biostudies-literature | 2009 Jun

REPOSITORIES: biostudies-literature