Affinity of 18,19-dihydroxydeoxycorticosterone and 18-hydroxy-19-nor-deoxycorticosterone to aldosterone receptor and their mineralocorticoid activity.
Affinity of 18,19-dihydroxydeoxycorticosterone (18,19-diOH-DOC) and 18-hydroxy-19-nor-deoxycorticosterone (18-OH-19-nor-DOC) to aldosterone receptor and their mineralocorticoid activity were evaluated. 18,19-DiOH-DOC (1 X 10(-6) M) did not show appreciable binding to the receptor and its relative potency as a mineralocorticoid was estimated to be less than 1/8,000 of that of deoxycorticosterone (DOC). 18-OH-19-nor-DOC bound to the receptor with an affinity similar to that of 18-hydroxydeoxycorticosterone (18-OH-DOC) or spironolactone. Its sodium retaining activity was 0.04 times as great as that of DOC and similar to that of 18-OH-DOC.
D015070:18-Hydroxydesoxycorticosterone / Q000031:analogs & derivatives* / Q000494:pharmacology; D000315:Adrenalectomy; D000450:Aldosterone / Q000378:metabolism*; D000818:Animals; D001667:Binding, Competitive; D001681:Biological Assay; D003345:Corticosterone / Q000031:analogs & derivatives* / Q000494:pharmacology; D003600:Cytosol / Q000378:metabolism; D003900:Desoxycorticosterone / Q000031:analogs & derivatives*; D007668:Kidney / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011965:Receptors, Glucocorticoid / Q000187:drug effects / Q000378:metabolism*; D018161:Receptors, Mineralocorticoid; D011987:Receptors, Steroid / Q000378:metabolism*
D015070:18-Hydroxydesoxycorticosterone; D011965:Receptors, Glucocorticoid; D018161:Receptors, Mineralocorticoid; D011987:Receptors, Steroid; D003900:Desoxycorticosterone; D000450:Aldosterone; C036775:18,19-dihydroxydeoxycorticosterone; C042901:18-hydroxy-19-nordeoxycorticosterone; D003345:Corticosterone