LUF7244 is a potent and selective voltage-gated potassium 11.1 (Kv11.1) channels negative allosteric modulator/activator that inhibits early afterdepolarizations in vitro. It decreases the affinity of Kv11.1 for cisapride, astemizole, dofetilide and sertindole. LUF7244 averts dofetilide‐induced torsades de pointes arrhythmias in dogs with chronic atrioventricular block. LUF7244 in combination with dofetilide rescues both congenital and acquired Kv11.1 trafficking defects and produces functional Kv11.1 current in trafficking defective G601S-Kv11.1 cells.
Potent and selective voltage-gated potassium 11.1 (Kv11.1) channels negative allosteric modulator/activator that inhibits early afterdepolarizations
Voltage-gated potassium 11.1 (Kv11.1) channels play a critical role in repolarization of cardiomyocytes during the cardiac action potential (AP). Drug-mediated Kv11.1 blockade results in AP prolongation, which poses an increased risk of sudden cardiac death. Many drugs, like pentamidine, interfere
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