21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat
In the rat, the conformationally highly befit steroid 21-hydroxy-6,19- oxidoprogesterone efficiently displaces [3H]corticostetone from thymus- glucocorticoid receptors and blocks type II receptors in kidney cytosols but competes with neither [3H]aldosterona for kidney-mineralocorticoid receptors nor...
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| Autores principales: | , , , , , |
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| Formato: | JOUR |
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| Acceso en línea: | http://hdl.handle.net/20.500.12110/paper_0026895X_v52_n4_p749_Vicent |
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| Sumario: | In the rat, the conformationally highly befit steroid 21-hydroxy-6,19- oxidoprogesterone efficiently displaces [3H]corticostetone from thymus- glucocorticoid receptors and blocks type II receptors in kidney cytosols but competes with neither [3H]aldosterona for kidney-mineralocorticoid receptors nor [3H]progesterone for uterus-progesterone receptors. It evokes Na+ retention only at very high doses (~100 μg/100 g of rat weight) and is unable to induce tyrosine aminotransferase or to increase glycogen deposits in rat liver. When coincubated with corticostarone or dexamethasone, 2.5 μM 21OH-6OP inhibits 80% of tyrosine, aminotransferase induction. It may therefore be used experimentally as an antiglucocorticoid virtually lacking mineralocorticoid or glucocorticoid properties as well as affinity for mineralocorticoid or progesterone receptors. |
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