Abstract

Previous studies have demonstrated that 11-deoxycortisol (pregn-4-ene-17α,21-diol-3,20-dione) competes with glucocorticoids for binding to the glucocorticoid receptor and is a competitive antagonist of glucocorticoid action in vitro. 11-Deoxycortisol, however, has been reported to be ineffective as a glucocorticoid antagonist in vivo. The present study was undertaken to examine this discrepancy between the in vivo and in vitro antiglucocorticoid activities of 11-deoxycortisol. In adrenalectomized rats, 11-deoxycortisol antagonized dexamethasone (9a-fluoro-16a-methyl-pregna-l,4-diene-llβ-17α,21-triol-3,20-dione)-induced liver glycogen accumulation and growth suppression at plasma levels comparable to those at which antiglucocorticoid activity has been reported in vitro and was itself devoid of agonist activity. In intact rats, on the other hand, 11-deoxycortisol showed agonist activity in growth suppression and adrenal suppression assays, and failed to antagonize dexamethasone activity. Plasma cortisol, me...

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