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Article

Stereoselective block of the hERG potassium channel by the Class Ia antiarrhythmic drug disopyramide.

Cellular and molecular life sciences : CMLS - 28 Nov 2024

Zhang Yihong, El Harchi Aziza, James Andrew F, Oiki Shigetoshi, Dempsey Christopher E, Hancox Jules C

Abstract excerpt

Potassium channels encoded by human Ether-à-go-go-Related Gene (hERG) are inhibited by diverse cardiac and non-cardiac drugs. Disopyramide is a chiral Class Ia antiarrhythmic that inhibits hERG at clinical concentrations. This study evaluated effects of disopyramide enantiomers on hERG current (IhERG) from hERG expressing HEK 293 cells at 37 °C. S(+) and R(-) disopyramide inhibited wild-type (WT) IhERG with IC50...

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Identifiers

PMID: 39607488
DOI: 10.1007/s00018-024-05498-4
PMCID: PMC11604869

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