Clemizole hydrochloride blocks cardiac potassium currents stably expressed in HEK 293 cells.

ABSTRACT:

Background and purpose

Clemizole, a histamine H₁ receptor antagonist has a potential therapeutic effect on hepatitis C infection and also potently inhibits TRPC5 ion channels. The aim of the present study was to investigate whether clemizole blocks cardiac K⁺ currents and thus affects cardiac repolarization.

Experimental approach

Whole-cell patch techniques was used to examine the effects of clemizole on hERG channel current, I_Ks and K_v 1.5 channel current in HEK 293 cell expression systems as well as on ventricular action potentials of guinea pig hearts. Isolated hearts from guinea pigs were used to determine the effect on the ECG.

Key results

Clemizole decreased hERG current by blocking both open and closed states of the c

SUBMITTER: Jie LJ 

PROVIDER: S-EPMC5241390 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature