Pregnanes That Bind To The Digitalis Receptor

Abstract

Steroid binding domains of Na, K-ATPase and the nuclear hormone receptors share amino acid sequence homologies. In a ouabain radioligand assay, the potencies of series of planar or bent steroid moieties suggest that the domain in Na,K-ATPase can accommodate compounds with a planar configuration. The A/B -cis, C/D-cis steroid configuration in the cardenolides, in conjunction with appropriate substituents at the 3 and 17 positions, may represent a fortuitous “fit” for the exogenous compounds. It remains to be determined if the putative physiological digitalis-like substance is a member of a hormonal steroid family, an endogenous ouabain-like compound or both

Key Words:

• progesterone
• pregnanes
• sodium-potassium ATPase
• endogenous digitalis
• cardiac glycosides
• steroids