Effect of 6-dehydro-DOCA and 6-dehydro-9 alpha-fluorocortisol acetate on the excretion of sodium and potassium in the rat.
Deoxycorticosterone acetate (DOCA) and 9 alpha-fluorocortisol acetate (9 alpha-F-Cac) can be modified by the introduction of a double bond at carbons 6 and 7 (6-dehydro-derivatives). Such a modification markedly changes the effect of the steroids on urinary excretion of Na+ and K+. Since 6-7 reduction of DOCA and 9 alpha-F-Cac substantially reduces affinity for Type II receptors but not Type I receptors, 6-dehydro-derivatives will thus bind preferentially to receptors influencing the retention of sodium (the "mineralocorticoid" or Type I receptor), and compete with mineralocorticoids for such receptors. We interpret the increase in both natriuresis and kaliuresis when mineralocorticoids and their dehydro-derivatives are administered together as evidence for a Type II receptor mediation of these ion fluxes.
D000450:Aldosterone / Q000494:pharmacology; D000818:Animals; D003900:Desoxycorticosterone / Q000031:analogs & derivatives* / Q000494:pharmacology; D003907:Dexamethasone / Q000378:metabolism; D005438:Fludrocortisone / Q000031:analogs & derivatives* / Q000494:pharmacology; D009318:Natriuresis / Q000187:drug effects*; D011188:Potassium / Q000652:urine*; D051381:Rats; D011965:Receptors, Glucocorticoid / Q000502:physiology; D013329:Structure-Activity Relationship; D014316:Tritium
D011965:Receptors, Glucocorticoid; D014316:Tritium; C047108:6-dehydrodeoxycorticosterone acetate; D003900:Desoxycorticosterone; D000450:Aldosterone; C047109:6-dehydrofluorocortisol acetate; D003907:Dexamethasone; D011188:Potassium; D005438:Fludrocortisone; C034635:fludrocortisone acetate