The novel late Na⁺ current inhibitor, GS-6615 (eleclazine) and its anti-arrhythmic effects in rabbit isolated heart preparations.

ABSTRACT:

Background and purpose

Enhanced late Na⁺ current (late I_Na ) in the myocardium is pro-arrhythmic. Inhibition of this current is a promising strategy to stabilize ventricular repolarization and suppress arrhythmias. Here, we describe GS-6615, a selective inhibitor of late I_Na , already in clinical development for the treatment of long QT syndrome 3 (LQT3).

Experimental approach

The effects of GS-6615 to inhibit late I_Na , versus other ion currents to shorten the ventricular action potential duration (APD), monophasic APD (MAPD) and QT interval, and decrease to the incidence of ventricular arrhythmias was determined in rabbit cardiac preparations. To mimic the electrical phenotype of LQT3, late I_Na was increased using the

SUBMITTER: Rajamani S 

PROVIDER: S-EPMC5056228 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature