TY - JOUR T1 - 21-Hydroxy-6,19-oxidoprogesterone: A Novel Synthetic Steroid with Specific Antiglucocorticoid Properties in the Rat JF - Molecular Pharmacology JO - Mol Pharmacol SP - 749 LP - 753 DO - 10.1124/mol.52.4.749 VL - 52 IS - 4 AU - G. P. Vicent AU - M. C. Monteserín AU - A. S. Veleiro AU - G. Burton AU - C. P. Lantos AU - M. D. Galigniana Y1 - 1997/10/01 UR - http://molpharm.aspetjournals.org/content/52/4/749.abstract N2 - In the rat, the conformationally highly bent steroid 21-hydroxy-6,19-oxidoprogesterone efficiently displaces [3H]corticosterone from thymus-glucocorticoid receptors and blocks type II receptors in kidney cytosols but competes with neither [3H]aldosterone 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 corticosterone or dexamethasone, 2.5 μm21OH-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. ER -