Myocardial and vascular effects of efonidipine in vitro as compared with nifedipine, verapamil and diltiazem

Gen Pharmacol. 1996 Apr;27(3):451-4. doi: 10.1016/0306-3623(95)02065-9.

Abstract

1. Effects of efonidipine on isolated myocardial and aortic preparations were compared with those of nifedipine, verapamil and diltiazem. 2. All drugs produced concentration-dependent negative chronotropic effects on isolated guinea-pig atrial preparations. The potency order was efonidipine > or = nifedipine > diltiazem > or = verapamil, EC30 values being 3.08 x 10(-8)M, 3.48 x 10(-8)M, 1.27 x 10(-7)M and 1.47 x 10(-7)M, respectively. 3. Nifedipine, verapamil and diltiazem produced concentration-dependent negative inotropic effects on isolated guinea-pig left atrial preparations. The potency order was nifedipine > verapamil > diltiazem, EC30 values being 4.94 x 10(-8)M, 1.49 x 10(-7)M and 8.03 x 10(-7)M, respectively. Efonidipine, even at 1 microM produced no inotropic effect: 10 microM efonidipine decreased the contractile force by about 20%. 4. All drugs concentration-dependently attenuated the KCl-induced contraction of isolated rat aortic ring preparation. The potency order was nifedipine > efonidipine > verapamil > diltiazem, EC30 values being 2.98 x 10(-9)M, 1.24 x 10(-8)M, 3.96 x 10(-8)M and 2.13 x 10(-7)M, respectively. 5. Thus, efonidipine was demonstrated to be a potent vasodilator with negative chronotropic but minimal negative inotropic activity, which may be of benefit in the treatment of cardiovascular disorders.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Aorta, Thoracic / drug effects
  • Calcium Channel Blockers / pharmacology*
  • Dihydropyridines / pharmacology*
  • Diltiazem / pharmacology
  • Female
  • Guinea Pigs
  • Heart / drug effects*
  • Heart Rate / drug effects
  • In Vitro Techniques
  • Male
  • Muscle Contraction / drug effects
  • Muscle, Smooth, Vascular / drug effects*
  • Myocardial Contraction / drug effects
  • Nifedipine / pharmacology
  • Nitrophenols*
  • Organophosphorus Compounds / pharmacology*
  • Potassium Chloride / antagonists & inhibitors
  • Potassium Chloride / pharmacology
  • Rats
  • Rats, Wistar
  • Verapamil / pharmacology

Substances

  • Calcium Channel Blockers
  • Dihydropyridines
  • Nitrophenols
  • Organophosphorus Compounds
  • efonidipine
  • Potassium Chloride
  • Verapamil
  • Diltiazem
  • Nifedipine