Stimulation and inhibition of the sodium pump by cardioactive steroids in relation to their binding sites and their inotropic effect on guinea-pig isolated atria

Br J Pharmacol. 1979 Jun;66(2):175-84. doi: 10.1111/j.1476-5381.1979.tb13662.x.

Abstract

1 The actions of ouabain, ouabagenin and dihydroouabain on the contractility and on the ionic content have been investigated in left guinea-pig atria stimulated at 3.3 Hz. The specific binding of ouabain and its displacement by the other cardenolides have been determined. 2 The action of either ouabain or ouabagenin on Na and K content was qualitatively different according to the concentration employed. Low doses evoked a reduction of Nai whereas high doses produced an increase. Dihydroouabain evoked only a Nai gain. 3 The increase of KCl concentration from 2.7 to 12 mM decreased Nai in untreated atria and displaced ouabain dose-effect curves to the right. 4 ED50 values for the positive inotropic effect were lower than ED50 values for the inhibition of the pump and were not similarly affected by an increase in KCl concentration. 5 The specific binding of ouabain occurred at high and low affinity sites, related to Na pump stimulation and inhibition respectively. 6 The increase in KCl reduced the affinity of the two groups of sites for ouabain and increased the capacity of the high-affinity sites whereas the capacity of the other sites remained unchanged. 7 The results confirm the existence of two specific binding sites for ouabain in guinea-pig heart and suggest that the inhibition of the Na pump is not the only mechanism responsible for the positive inotropic effect of cardiac glycosides.

MeSH terms

  • Animals
  • Atrial Function
  • Biological Transport, Active / drug effects
  • Calcium / metabolism
  • Guinea Pigs
  • Heart / drug effects
  • Heart / physiology*
  • Magnesium / metabolism
  • Myocardial Contraction / drug effects*
  • Myocardium / metabolism*
  • Ouabain / analogs & derivatives*
  • Ouabain / metabolism
  • Ouabain / pharmacology*
  • Potassium / metabolism
  • Sodium / metabolism*

Substances

  • Ouabain
  • Sodium
  • Magnesium
  • Potassium
  • Calcium