Potential cardiotoxicity of compounds predicted based on the interaction of astemizole with the HERG (human ether-a-go-go-related gene) potassium channel

摘要

Assays and kits are provided for the screening of test compounds for their capability to induce cardiotoxicity in a subject. The assays and kits are based on the finding that the interaction of astemizole with the HERG (Human Ether-a-go-go-Related Gene) potassium channel can be exploited to predict cardiotoxicity of compounds during the development of new therapeutics and other agents. Figure 1 A shows the saturation binding of [3H]-astemizole to cell membrane preparations of HEK293 cells stably transfected with the HERG channel cDNA. TB represents Total Binding measured, NSB represents Non Specific Binding measured and SB represents Specific Binding measured.