Novel 4-substituted benzamides demonstrate potent, selective I(Ks) blockade and oral bioavailability, suggesting potential utility as antiarrhythmic agents.
Preclinical I(Ks) blockers should not yet alter arrhythmia management; leaves open selective channel blockade as a therapeutic hypothesis.
Multiple delayed rectifier potassium currents, including I(Ks), are responsible for the repolarization and termination of the cardiac action potential, and blockers of these currents may be useful as antiarrhythmic agents. Modification of compound 5 produced 19(S) that is the most potent I(Ks) blocker reported to date with >5000-fold selectivity over other cardiac ion channels. Further modification produced 24A with 23% oral bioavailability.
No takes yet. Share an insight, caveat, or question.
Lloyd et al. (2001) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: