The direct actions of flecainide on the human cardiac ryanodine receptor: keeping open the debate on the mechanism of action of local anesthetics in CPVT.
نویسندگان
چکیده
منابع مشابه
The mechanism of flecainide action in CPVT does not involve a direct effect on RyR2.
RATIONALE Flecainide, a class 1c antiarrhythmic, has emerged as an effective therapy in preventing arrhythmias in patients with catecholaminergic polymorphic ventricular tachycardia (CPVT) refractory to β-adrenergic receptor blockade. It has been proposed that the clinical efficacy of flecainide in CPVT is because of the combined actions of direct blockade of ryanodine receptors (RyR2) and Na(+...
متن کاملMultiple modes of ryanodine receptor 2 inhibition by flecainide.
Catecholaminergic polymorphic ventricular tachycardia (CPVT) causes sudden cardiac death due to mutations in cardiac ryanodine receptors (RyR2), calsequestrin, or calmodulin. Flecainide, a class I antiarrhythmic drug, inhibits Na(+) and RyR2 channels and prevents CPVT. The purpose of this study is to identify inhibitory mechanisms of flecainide on RyR2. RyR2 were isolated from sheep heart, inco...
متن کاملMultiple Modes of Ryanodine Receptor 2 Inhibition by Flecainide s
Catecholaminergic polymorphic ventricular tachycardia (CPVT) causes sudden cardiac death due tomutations in cardiac ryanodine receptors (RyR2), calsequestrin, or calmodulin. Flecainide, a class I antiarrhythmic drug, inhibits Na and RyR2 channels and prevents CPVT. The purpose of this study is to identify inhibitory mechanisms of flecainide on RyR2. RyR2 were isolated from sheep heart, incorpor...
متن کاملChannel Activity of Cardiac Ryanodine Receptors (RyR2) Determines Potency and Efficacy of Flecainide and R-Propafenone against Arrhythmogenic Calcium Waves in Ventricular Cardiomyocytes
Flecainide blocks ryanodine receptor type 2 (RyR2) channels in the open state, suppresses arrhythmogenic Ca2+ waves and prevents catecholaminergic polymorphic ventricular tachycardia (CPVT) in mice and humans. We hypothesized that differences in RyR2 activity induced by CPVT mutations determines the potency of open-state RyR2 blockers like flecainide (FLEC) and R-propafenone (RPROP) against Ca2...
متن کاملMechanism of antiarrhythmic effects of flecainide in catecholaminergic polymorphic ventricular tachycardia.
Mechanism of Antiarrhythmic Effects of Flecainide in Catecholaminergic Polymorphic Ventricular Tachycardia To the Editor: We read with interest the recent article by Liu et al, in Circulation Research, on the mechanism underlying the antiarrhythmic effects of flecainide in catecholaminergic polymorphic ventricular tachycardia (CPVT).1 They conclude that Na channel block but not inhibition of th...
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ورودعنوان ژورنال:
- Circulation research
دوره 116 8 شماره
صفحات -
تاریخ انتشار 2015