Antiglucocorticoid activity of androgens in rat thymus lymphocytes

Endocrinology
S Sasson, M Mayer

Abstract

The potent androgens testosterone and 5 alpha-dihydrotestosterone, but not the inactive androgens etiocholanolone and androsterone, display antiglucocorticoid activity in rat thymus-derived lymphocytes. At a concentration of 10(-5) M, the potent androgens markedly lower the in vitro cytolytic response of isolated thymic lymphocytes to 10(-8) M dexamethasone. AT 2.5 X 10(-5) M, these androgens completely prevent the inhibition produced by 5 X 10(-8) M dexamethasone on 2-deoxyglucose uptake and uridine uptake and incorporation in isolated thymic lymphocytes. In the cytosol fraction obtained from rat thymus homogenate, the active androgens competitively inhibit the binding of [3H]dexamethasone to glucocorticoid-specific receptors with Ki values of 1.2 X 10(-6) and 2.5 X 10(-6) M for testosterone and 5 alpha-dihydrotestosterone, respectively. Thymus-derived lymphocytes and nuclei isolated from these cells exhibit binding of [3H]dexamethasone. The bound dexamethasone is avidly displaced by an excess of nonradioactive dexamethasone as well as by nonradioactive testosterone or 5 alpha-dihydrotestosterone. In contrast to their antiglucocorticoid activity in vitro, these androgens fail to elicit antiglucocorticoid activity when administ...Continue Reading

Citations

Dec 1, 1981·Journal of Steroid Biochemistry·M Moguilewsky, R Deraedt
Mar 1, 1983·Journal of Steroid Biochemistry·G G RousseauJ P Schmit
Jan 1, 1983·Journal of Steroid Biochemistry·M MayerM Chaouat
Oct 1, 1988·Journal of Steroid Biochemistry·W L DuaxZ Wawrzak
Sep 1, 1990·The Journal of Steroid Biochemistry and Molecular Biology·C L MendenhallK Martin
Nov 1, 1995·Journal of Pineal Research·R J NelsonL J Kriegsfeld
Sep 1, 1989·The American Journal of the Medical Sciences·S KawaiG P Chrousos

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