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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.

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http://dx.doi.org/10.1016/0022-4731(85)90021-4DOI Listing

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