Progesterone derivatives that bind to the digitalis receptor.
Examination of mammalian steroid hormones, their metabolites and semi-synthetic analogs in a radioreceptor binding assay for cardiac glycosides led to the identification of active derivatives of hydroxyprogesterone. The active compounds are potent inhibitors of purified sodium, potassium-ATPase and of the sodium pump in isolated tissues. Metabolism of progesterone offers a mechanism for the generation of endogenous substances that resemble, both structurally and biologically, the digitalis cardioactive steroids.
D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D004070:Digitalis / Q000378:metabolism*; D009928:Organ Specificity; D010946:Plants, Medicinal; D010947:Plants, Toxic; D011374:Progesterone / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology*; D011956:Receptors, Cell Surface / Q000378:metabolism; D011955:Receptors, Drug / Q000378:metabolism*; D000254:Sodium-Potassium-Exchanging ATPase; D013329:Structure-Activity Relationship
D011956:Receptors, Cell Surface; D011955:Receptors, Drug; C027082:digitalis receptor; D011374:Progesterone; D000254:Sodium-Potassium-Exchanging ATPase