Characterization of recombinant hERG K(+) channel inhibition by the active metabolite of amiodarone desethyl-amiodarone.

Unlabelled: The aim of this study was to determine the effects of desethyl-amiodarone (DEA), the major metabolite of the class III antiarrhythmic drug amiodarone, on human ether-à-go-go-related gene (hERG) encoded potassium channel current.

Materials And Methods: Whole-cell patch clamp recordings were made at 37 degrees C of ionic current (I(hERG)) carried by recombinant hERG channels expressed in HEK-293 cells.

Results: Desethyl-amiodarone inhibited I(hERG) with a half-maximal inhibitory concentration of approximately 158 nmol/L, compared with approximately 47 nmol/L for amiodarone.