Effects of dihydropyridine calcium channel modulators in the heart: pharmacological and radioligand binding correlations

Biochem Biophys Res Commun. 1984 Nov 30;125(1):387-94. doi: 10.1016/s0006-291x(84)80380-0.

Abstract

Bay k 8644 produced a concentration-dependent positive inotropic effect followed by a negative inotropic effect in isolated and intact cardiac preparations. Nimodipine in low concentrations produced slight positive inotropy and in higher concentrations, the usual negative inotropic action. Radioligand binding experiments revealed equilibrium dissociation constants that, taken together with the pharmacological data, suggest that dihydropyridines bind to receptor subtypes and have varying intrinsic activities.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
  • Animals
  • Binding Sites
  • Calcium / pharmacology
  • Calcium Channel Blockers / pharmacology*
  • Depression, Chemical
  • Dogs
  • Dose-Response Relationship, Drug
  • Myocardial Contraction / drug effects*
  • Myocardium / metabolism
  • Nicotinic Acids / pharmacology
  • Nifedipine / analogs & derivatives*
  • Nifedipine / metabolism
  • Nifedipine / pharmacology
  • Nimodipine
  • Nitrendipine
  • Rats
  • Stimulation, Chemical

Substances

  • Calcium Channel Blockers
  • Nicotinic Acids
  • Nimodipine
  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
  • Nitrendipine
  • Nifedipine
  • Calcium