Title : Kv1.5 open channel block by the antiarrhythmic drug disopyramide: molecular determinants of block.

Pub. Date : 2008 Sep

PMID : 18818480






4 Functional Relationships(s)
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1 Kv1.5 open channel block by the antiarrhythmic drug disopyramide: molecular determinants of block. Disopyramide potassium voltage-gated channel subfamily A member 5 Homo sapiens
2 The present study was undertaken to characterize the effects of disopyramide on currents mediated by Kv1.5 channels and to determine the putative binding site involved in the inhibitory effects of disopyramide. Disopyramide potassium voltage-gated channel subfamily A member 5 Homo sapiens
3 Disopyramide acting from the cytoplasmic side of the membrane produced blocking effects on Kv1.5 that exhibited several features typical of an open channel blocker. Disopyramide potassium voltage-gated channel subfamily A member 5 Homo sapiens
4 Ala-scanning mutagenesis of the Kv1.5 pore domain combined with macroscopic current analysis suggested that disopyramide interacted only with the Val512 residue that faces to the central cavity of the channel. Disopyramide potassium voltage-gated channel subfamily A member 5 Homo sapiens