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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Published in | Endocrinology (Philadelphia) Vol. 109; no. 5; p. 1418 |
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Main Authors | , , |
Format | Journal Article |
Language | English |
Published |
United States
01.11.1981
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Abstract | 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. |
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AbstractList | 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. |
Author | Ho-Kim, M A Tremblay, R R Dubé, J Y |
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Snippet | 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... |
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SubjectTerms | 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 |
Title | Binding of methyltrienolone to glucocorticoid receptors in rat muscle cytosol |
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