Article
Molecular determinants of KCNQ1 channel block by a benzodiazepine.
Molecular pharmacology - 1 Jul 2003
Seebohm Guiscard, Chen Jun, Strutz Nathalie, Culberson Chris, Lerche Christian, Sanguinetti Michael C
Abstract excerpt
KCNQ1 channels underlie the slow delayed rectifier K+ current, mediate repolarization of cardiac action potentials, and are a potential therapeutic target for treatment of arrhythmia. (E)-(+)-N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(2,4-dichlorophenyl)-2-propenamide [L-735821 (L-7)] is a potent blocker of KCNQ1 channels. Here we describe the structural determinants of KCNQ1 that...
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