Abstract:
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.
Registro:
Documento: |
Artículo
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Título: | 21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat |
Autor: | Vicent, G.P.; Monteserín, M.C.; Veleiro, A.S.; Burton, G.; Lantos, C.P.; Galigniana, M.D. |
Filiación: | Departemento de Quim. Biol., Ciudad Universitaria, (1428) Buenos Aires, Argentina Departemento de Quim. Organ., Ciudad Universitaria, (1428) Buenos Aires, Argentina Fac. de Ciencias Exactas y Naturales, Universidad de Buenos Aires, PRHOM-Consejo Nac. Invest. Cie. y T., (1428) Buenos Aires, Argentina Department of Pharmacology, University of Michigan, Medical School, Ann Arbor, MI 48109-0632, United States Departemento de Quim. Biol., Ciudad Universitaria, Pabellón 2, 1428 Buenos Aires, Argentina
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Palabras clave: | 11beta,17beta dihydroxy 6 methyl 17alpha (1 propynyl)androsta 1,4,6 trien 3 one; 15beta,16beta methylenemexrenone; 21 hydroxy 6,19 oxidoprogesterone; aldosterone; corticosterone; dexamethasone; glucocorticoid antagonist; glucocorticoid receptor; mineralocorticoid receptor; progesterone; steroid; tyrosine aminotransferase; unclassified drug; animal tissue; article; controlled study; cytosol; dose response; drug conformation; drug receptor binding; enzyme induction; kidney cell; male; nonhuman; priority journal; rat; sodium retention |
Año: | 1997
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Volumen: | 52
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Número: | 4
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Página de inicio: | 749
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Página de fin: | 753
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DOI: |
http://dx.doi.org/10.1124/mol.52.4.749 |
Título revista: | Molecular Pharmacology
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Título revista abreviado: | MOL. PHARMACOL.
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ISSN: | 0026895X
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CODEN: | MOPMA
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CAS: | 11beta,17beta dihydroxy 6 methyl 17alpha (1 propynyl)androsta 1,4,6 trien 3 one, 74915-64-3; 15beta,16beta methylenemexrenone, 84542-26-7; aldosterone, 52-39-1, 6251-69-0; corticosterone, 50-22-6; dexamethasone, 50-02-2; progesterone, 57-83-0; tyrosine aminotransferase, 9014-55-5
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Registro: | https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v52_n4_p749_Vicent |
Referencias:
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Citas:
---------- APA ----------
Vicent, G.P., Monteserín, M.C., Veleiro, A.S., Burton, G., Lantos, C.P. & Galigniana, M.D.
(1997)
. 21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat. Molecular Pharmacology, 52(4), 749-753.
http://dx.doi.org/10.1124/mol.52.4.749---------- CHICAGO ----------
Vicent, G.P., Monteserín, M.C., Veleiro, A.S., Burton, G., Lantos, C.P., Galigniana, M.D.
"21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat"
. Molecular Pharmacology 52, no. 4
(1997) : 749-753.
http://dx.doi.org/10.1124/mol.52.4.749---------- MLA ----------
Vicent, G.P., Monteserín, M.C., Veleiro, A.S., Burton, G., Lantos, C.P., Galigniana, M.D.
"21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat"
. Molecular Pharmacology, vol. 52, no. 4, 1997, pp. 749-753.
http://dx.doi.org/10.1124/mol.52.4.749---------- VANCOUVER ----------
Vicent, G.P., Monteserín, M.C., Veleiro, A.S., Burton, G., Lantos, C.P., Galigniana, M.D. 21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat. MOL. PHARMACOL. 1997;52(4):749-753.
http://dx.doi.org/10.1124/mol.52.4.749