T-type Ca2+ channel blockade prevents sudden death in mice with heart failure

Circulation. 2009 Sep 1;120(9):743-52. doi: 10.1161/CIRCULATIONAHA.109.857011. Epub 2009 Aug 17.

Abstract

Background: Pharmacological interventions for prevention of sudden arrhythmic death in patients with chronic heart failure remain limited. Accumulating evidence suggests increased ventricular expression of T-type Ca(2+) channels contributes to the progression of heart failure. The ability of T-type Ca(2+) channel blockade to prevent lethal arrhythmias associated with heart failure has never been tested, however.

Methods and results: We compared the effects of efonidipine and mibefradil, dual T- and L-type Ca(2+) channel blockers, with those of nitrendipine, a selective L-type Ca(2+) channel blocker, on survival and arrhythmogenicity in a cardiac-specific, dominant-negative form of neuron-restrictive silencer factor transgenic mice (dnNRSF-Tg), which is a useful mouse model of dilated cardiomyopathy leading to sudden death. Efonidipine, but not nitrendipine, substantially improved survival among dnNRSF-Tg mice. Arrhythmogenicity was dramatically reduced in dnNRSF-Tg mice treated with efonidipine or mibefradil. Efonidipine acted by reversing depolarization of the resting membrane potential otherwise seen in ventricular myocytes from dnNRSF-Tg mice and by correcting cardiac autonomic nervous system imbalance. Moreover, the R(-)-isomer of efonidipine, a recently identified, highly selective T-type Ca(2+) channel blocker, similarly improved survival among dnNRSF-Tg mice. Efonidipine also reduced the incidence of sudden death and arrhythmogenicity in mice with acute myocardial infarction.

Conclusions: T-type Ca(2+) channel blockade reduced arrhythmias in a mouse model of dilated cardiomyopathy by repolarizing the resting membrane potential and improving cardiac autonomic nervous system imbalance. T-type Ca(2+) channel blockade also prevented sudden death in mice with myocardial infarction. Our findings suggest T-type Ca(2+) channel blockade is a potentially useful approach to preventing sudden death in patients with heart failure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Arrhythmias, Cardiac / mortality
  • Arrhythmias, Cardiac / prevention & control
  • Autonomic Nervous System / drug effects
  • Autonomic Nervous System / physiology
  • Blood Pressure
  • Body Weight
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, L-Type / metabolism
  • Calcium Channels, T-Type / metabolism*
  • Cardiomyopathy, Dilated / drug therapy*
  • Cardiomyopathy, Dilated / mortality
  • Death, Sudden, Cardiac / prevention & control*
  • Dihydropyridines / pharmacology*
  • Disease Models, Animal
  • Female
  • Mibefradil / pharmacology
  • Mice
  • Mice, Inbred C57BL
  • Mice, Transgenic
  • Myocardial Infarction / drug therapy
  • Myocardial Infarction / mortality
  • Myocytes, Cardiac / physiology
  • Nitrendipine / pharmacology
  • Nitrophenols / pharmacology*
  • Organophosphorus Compounds / pharmacology
  • Patch-Clamp Techniques

Substances

  • Calcium Channel Blockers
  • Calcium Channels, L-Type
  • Calcium Channels, T-Type
  • Dihydropyridines
  • Nitrophenols
  • Organophosphorus Compounds
  • Mibefradil
  • efonidipine
  • Nitrendipine