Inhibition of myocardial L- and T-type Ca2+ currents by efonidipine: possible mechanism for its chronotropic effect

Eur J Pharmacol. 1998 May 22;349(2-3):351-7. doi: 10.1016/s0014-2999(98)00204-0.

Abstract

Effects of efonidipine, a dihydropyridine phosphonate Ca2+ channel antagonist, on the guinea-pig heart were compared with those of nifedipine. In the sino-atrial node, 1 microM efonidipine produced increase in cycle length accompanied by prolongation of the phase 4 depolarization which was not prominent with 0.1 microM nifedipine. In ventricular myocytes, both efonidipine and nifedipine produced inhibition of the L-type Ca2+ current, nifedipine being tenfold more potent than efonidipine. Efonidipine also inhibited the T-type Ca2+ current at higher concentrations but nifedipine did not. Both Ca2+ channel antagonists had no or only a weak effect on K+ currents. In addition, 40 microM Ni2+, which selectively inhibited the T-type Ca2+ current, had no effect on myocardial Ca2+ transients and contractile force. In conclusion, efonidipine was shown to have inhibitory effects on both L- and T-type Ca2+ currents, which may contribute to its high negative chronotropic potency.

Publication types

  • Comparative Study

MeSH terms

  • Action Potentials / drug effects
  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels / drug effects*
  • Depression, Chemical
  • Dihydropyridines / pharmacology*
  • Female
  • Guinea Pigs
  • Heart / drug effects*
  • Heart / physiology
  • Heart Rate / drug effects*
  • Male
  • Myocardial Contraction / drug effects
  • Nifedipine / pharmacology
  • Nitrophenols*
  • Organophosphorus Compounds / pharmacology*
  • Patch-Clamp Techniques
  • Potassium Channels / drug effects
  • Sinoatrial Node / drug effects
  • Sinoatrial Node / physiology

Substances

  • Calcium Channel Blockers
  • Calcium Channels
  • Dihydropyridines
  • Nitrophenols
  • Organophosphorus Compounds
  • Potassium Channels
  • efonidipine
  • Nifedipine