[The problem of the cellular receptor for cardiac glycosides (author's transl)]

Abstract

This review concerns the Na+, K+ -ATPase as well as the Na+, K+ -pump in the intact membrane and the highly specific inhibition of this transport system by cardiac glycosides. The interaction between glycoside and enzyme and the regulation of the kinetics of glycoside binding by ATP, K+, Na+, Mg2+ and Ca2+ are described. Emphasis is placed on the significance of the Na+, K+ -pump as the pharmacological receptor for cardiac glycosides. The problem encountered and progress made in attempting to correlate the inotropic action of cardiac glycosides with the binding of these drugs to the heart muscle and with the inhibition of the Na+, K+ -pump are reported. Recent results concerning increases of the intracellular Na+ concentration which are obtained by a partial inhibition of the Na+, K+ -pump and which are followed by an elevation of the intracellular Ca2+ -activity are reviewed. The discovery of a digitalis-like endogenous activity corresponds to the high specificity of the receptor for cardiac glycosides.