Binding of methyltrienolone to glucocorticoid receptors in rat muscle cytosol

Androgen receptor measurements with [3H]-methyltrienolone [17 beta-hydroxy-17 alpha-methyl-estra-4,9,11-trien-3-one (R1881)] or [3H]testosterone in vastus lateralis muscle cytosol of intact male rats yielded similar numbers of binding sites. Gonadectomy significantly increased the androgen receptor...

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Bibliographic Details
Published inEndocrinology (Philadelphia) Vol. 109; no. 5; p. 1418
Main Authors Ho-Kim, M A, Tremblay, R R, Dubé, J Y
Format Journal Article
LanguageEnglish
Published United States 01.11.1981
Subjects
Adrenalectomy
Animals
Binding, Competitive
Castration
Cytosol - metabolism
Estrenes - metabolism
Kinetics
Male
Metribolone
Muscles - metabolism
Rats
Receptors, Glucocorticoid - metabolism
Receptors, Steroid - metabolism
Testosterone Congeners - metabolism
Triamcinolone Acetonide - metabolism
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Summary:Androgen receptor measurements with [3H]-methyltrienolone [17 beta-hydroxy-17 alpha-methyl-estra-4,9,11-trien-3-one (R1881)] or [3H]testosterone in vastus lateralis muscle cytosol of intact male rats yielded similar numbers of binding sites. Gonadectomy significantly increased the androgen receptor values, and both steroids gave similar results. The binding of [3H]-testosterone was not affected by adrenalectomy. In contrast, [3H]R1881 binding increased 2-fold after adrenalectomy. Competition experiments as well as sucrose density gradient analysis indicated that R1881, in addition to its binding of the androgen receptor, was also bound to glucocorticoid receptor. These results show that the synthetic androgen R1881 must be used with caution in tissues suspected to contain glucocorticoid receptors.
ISSN:0013-7227
DOI:10.1210/endo-109-5-1418