Kv1.5 Open Channel Block by the Antiarrhythmic Drug Disopyramide: Molecular Determinants of Block
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منابع مشابه
Kv1.5 open channel block by the antiarrhythmic drug disopyramide: molecular determinants of block.
Kv1.5 is considered to be a potential molecular target for treatment of atrial fibrillation or flutter. Disopyramide is widely used in the treatment of atrial flutter and/or atrial fibrillation. 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 disop...
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The block of the transient outward K(+) current (I(to)) by disopyramide was studied in isolated rat right ventricular myocytes using whole cell patch-clamp techniques. Disopyramide at a concentration of 10 to 1000 microM reduced peak I(to) and accelerated the apparent rate of current inactivation. The onset of block was assessed using a double pulse protocol with steps from -70 to +50 mV. As th...
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BACKGROUND IKs, an important repolarizing current in heart, is an antiarrhythmic drug target and is markedly increased by activation of protein kinase A (PKA; eg, by beta-adrenergic stimulation). Because beta-adrenergic stimulation is a frequent trigger of arrhythmias, we hypothesized that PKA stimulation inhibits drug block. METHODS AND RESULTS CHO cells were transfected with KCNQ1 cDNA (enc...
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ژورنال
عنوان ژورنال: Journal of Pharmacological Sciences
سال: 2008
ISSN: 1347-8613,1347-8648
DOI: 10.1254/jphs.08084fp