Dissociation of E-4031 from the HERG channel caused by mutations of an amino acid results in greater block at high stimulation frequency

Abstract

The present results indicate that dissociation of a drug from the HERG channel results in greater block at high frequency. Although the mechanism by which the mutations cause the dissociation of E-4031 is uncertain, it is noteworthy that one methanesulfonanilide dissociates from the channel more easily than another.