Atrial selectivity of ranolazine
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منابع مشابه
Mechanisms of atrial-selective block of Na⁺ channels by ranolazine: II. Insights from a mathematical model.
Block of Na(+) channel conductance by ranolazine displays marked atrial selectivity that is an order of magnitude higher that of other class I antiarrhythmic drugs. Here, we present a Markovian model of the Na(+) channel gating, which includes activation-inactivation coupling, aimed at elucidating the mechanisms underlying this potent atrial selectivity of ranolazine. The model incorporates exp...
متن کاملMechanisms of atrial-selective block of sodium channel by ranolazine
1 Mechanisms of atrial-selective block of sodium channel by ranolazine 2 I. Experimental analysis of the use-dependent block 3 4 Andrew C. Zygmunt,* Vladislav V. Nesterenko,* Sridharan Rajamani, Dan Hu, Hector 5 Barajas-Martinez, 1 Luiz Belardinelli, 2 Charles Antzelevitch 6 7 Masonic Medical Research Laboratory, Utica, NY and 2 Gilead Sciences, Inc., Palo Alto, CA 8 *V.V.N. and A.C.Z. contribu...
متن کاملAtrium-selective sodium channel block as a strategy for suppression of atrial fibrillation: differences in sodium channel inactivation between atria and ventricles and the role of ranolazine.
BACKGROUND The development of selective atrial antiarrhythmic agents is a current strategy for suppression of atrial fibrillation (AF). METHODS AND RESULTS Whole-cell patch clamp techniques were used to evaluate inactivation of peak sodium channel current (I(Na)) in myocytes isolated from canine atria and ventricles. The electrophysiological effects of therapeutic concentrations of ranolazine...
متن کاملMechanisms of atrial-selective block of Na⁺ channels by ranolazine: I. Experimental analysis of the use-dependent block.
Atrial-selective inhibition of cardiac Na(+) channel current (I(Na)) and I(Na)-dependent parameters has been shown to contribute to the safe and effective management of atrial fibrillation. The present study examined the basis for the atrial-selective actions of ranolazine. Whole cell I(Na) was recorded at 15°C in canine atrial and ventricular myocytes and in human embryonic kidney (HEK)-293 ce...
متن کاملNew Treatment Options for Late Na Current, Arrhythmias, and Diastolic Dysfunction
The late Na current is of pathophysiological importance for the heart. Ranolazine is an innovative anti-ischemic and antianginal agent that inhibits the late Na current, thereby reducing the Na-dependent Ca-overload, which improves diastolic tone and oxygen handling during myocardial ischemia. In addition, ranolazine seems to exert beneficial effects on diastolic cardiac function. Moreover, the...
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تاریخ انتشار 2011