The R(-)-enantiomer of efonidipine blocks T-type but not L-type calcium current in guinea pig ventricular myocardium

J Pharmacol Sci. 2004 Dec;96(4):499-501. doi: 10.1254/jphs.rcj04001x. Epub 2004 Dec 15.

Abstract

In guinea pig ventricular cardiomyocytes, the R(-)-enantiomer of efonidipine concentration-dependently blocked T-type Ca2+ current with 85% inhibition at 1 microM. In contrast, R(-)-efonidipine (1 microM) had no effect on the L-type Ca2+ current and Ca2+ transient in cardiomyocytes and contractile force in papillary muscles. Thus, R(-)-efonidipine is a highly selective blocker of the T-type Ca2+ current in native myocardia.

MeSH terms

  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, L-Type / drug effects*
  • Calcium Channels, T-Type / drug effects*
  • Dihydropyridines / pharmacology*
  • Guinea Pigs
  • Heart / drug effects*
  • Heart / physiology
  • Heart Ventricles
  • Nitrophenols / pharmacology*
  • Organophosphorus Compounds / pharmacology*
  • Stereoisomerism

Substances

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