21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat

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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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Detalles Bibliográficos
Autor principal: Vicent, G.P
Otros Autores: Monteserín, M.C, Veleiro, A.S, Burton, G., Lantos, C.P, Galigniana, M.D
Formato: Capítulo de libro
Lenguaje:Inglés
Publicado: American Society for Pharmacology and Experimental Therapy 1997
Materias:
ru 28362, Roussel Uclaf, France; zk 91587, New England Nuclear, United States
Acceso en línea:Registro en Scopus
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Registro en la Biblioteca Digital
Aporte de:Registro referencial: Solicitar el recurso aquí
Biblioteca Central Dr. Luis F. Leloir (FCEN) de Universidad de Buenos Aires
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024 7 |2 scopus  |a 2-s2.0-0030761842 
024 7 |2 cas  |a 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 
040 |a Scopus  |b spa  |c AR-BaUEN  |d AR-BaUEN 
030 |a MOPMA 
100 1 |a Vicent, G.P. 
245 1 0 |a 21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat 
260 |b American Society for Pharmacology and Experimental Therapy  |c 1997 
270 1 0 |m Vicent, G.P.; Departamento de Quimica Biologica, Ciudad Universitaria, Pabellon 2-1428 Buenos Aires, Argentina; email: gvicent@qb.fcen.uba.ar 
506 |2 openaire  |e Política editorial 
504 |a Hollemberg, S.M., Weinberger, C., Ong, E.S., Cereli, G., Oro, A., Lebo, R., Thompson, E.B., Evans, R.M., Primary structure and expression of a functional human glucocorticoid receptor cDNA (1985) Nature (Lond.), 318, pp. 635-641 
504 |a Forman, B.M., Evans, R.M., Nuclear hormone receptors activate direct, inverted, and everted repeats (1995) Ann. N. Y. Acad. Sci., 761, pp. 29-37 
504 |a Lantos, C.P., Burton, G., Roldán, A., Damasco, M.C., Aragonés, A., Structure-activity relationship in certain glucocorticoids and mineralocorticoids (1981) Physiopathology of Endocrine Diseases and Mechanisms of Hormone Action, pp. 477-494. , (R. J. Soto, A. de Nicola, and J. Blaquier, eds.). Alan R. Liss, New York 
504 |a Duax, W.L., Cody, V., Griffin, J.F., Rohrer, D.C., Weeks, C.M., Molecular conformation and protein binding affinity of progestins (1978) J. Toxicol. Environ. Health, 4, pp. 205-227 
504 |a Burton, G., Galigniana, M.D., De Lavallaz, S., Brachet-Cota, A.L., Sproviero, E.M., Ghini, A.A., Lantos, C.P., Damasco, M.C., Sodium-retaining activity of some natural and synthetic 21-deoxysteroids (1995) Mol. Pharmacol., 47, pp. 535-543 
504 |a Arriza, J., Weinberg, C., Cerelli, G., Glaser, T., Handelin, B., Housman, D., Evans, R., Cloning of human mineralocorticoid receptor complementary DNA: Structural and functional kinship with the glucocorticoid receptor (1987) Science (Washington D. C.), 237, pp. 268-275 
504 |a Teutsch, G., Nique, F., Lemoine, G., Bouchoux, F., Cérède, E., Gofflo, D., Philibert, D., General structure-activity correlations of antihormones (1995) Ann. N. Y. Acad. Sci., 761, pp. 5-28 
504 |a Grill, H.J., Nickisch, K., Schulze, P.E., Laurent, H., Elger, W., Heubner, A., Pollow, K., 3H-ZK91587: A new synthetic, highly specific ligand for mineralocorticoid receptor determination (1985) J. Steroid Biochem., 23 (SUPPL.), pp. 19S 
504 |a Sutanto, W., De Kloet, E.R., ZK91587: A novel synthetic antimineralocorticoid displays high affinity for corticosterone (Type I) receptors in the rat hippocampus (1988) Life Sci, 43, pp. 1537-1543 
504 |a Antiprogestins/antiglucocorticoids (1993) Endocrinology at Roussel-Udaf, p. 64 
504 |a Spitz, I.M., Bardin, C.W., Mefiprestone (RU486): A modulator of progestin and glucocorticoid action (1993) N. Engl. J. Med., 329, pp. 404-412 
504 |a Brachet-Cota, A.L., Burton, G., An improved preparation of 11,19-oxidopregn-4-ene-3,20-dione and 6,19-oxidopregnan-4-ene-3,11,20-trione (1990) Z. Naturforsch. Teil B Anorg. Chem. Org. Chem., 45, pp. 711-715 
504 |a Veleiro, A.S., Nevado, M.V., Monteserín, M.C., Burton, G., Syntheses of 21-hydroxy-11,19-oxidopregn-4-ene-3,20-dione and 21-hydroxy-6,19-oxidopregn-4-ene-3,20-dione (1995) Steroids, 60, pp. 268-271 
504 |a Galigniana, M.D., Vicent, G.P., Burton, G., Lantos, C.P., Features of the shuttle pair 11β-hydroxyprogesterone/11-ketoprogesterone (1997) Steroids, 62, pp. 358-364 
504 |a Galigniana, M.D., Stability study on renal type I mineralocorticoid receptor (1996) Life Sci., 59, pp. 511-521 
504 |a Jordan, V.C., Dix, C.J., Effect of oestradiol benzoate, tamoxifen and monohydroxytamoxifen on immature rat uterine progesterone receptor synthesis and endometrial cell division (1979) J Steroid Biochem., 11, pp. 285-291 
504 |a Krisman, C., A method for the colorimetric estimation of glycogen with iodine (1962) Anal. Biochem., 4, pp. 17-23 
504 |a Fry, J., Jones, C., Webkin, P., Bridges, J., The enzymatic isolation of adult rat hepatocytes in a functional and viable state (1976) Anal. Biochem., 71, pp. 341-350 
504 |a Granner, D., Tomkins, G., Metabolism of amino acids and amines: Tyrosine amino-transferase (1975) Methods Enzymol., 17, pp. 633-637 
504 |a Gomez-Sanchez, C.E., Gomez-Sanchez, E.P., RU26988: A new tool for the study of the mineralocorticoid receptor (1983) Endocrinology, 113, pp. 1004-1009 
504 |a Funder, J.W., Glucocorticoid receptors (1992) J. Steroid Biochem. Mol. Biol., 43, pp. 389-394 
504 |a Galigniana, M.D., Vicent, G.P., Lantos, C.P., Burton, G., Ligand properties of 11,19-oxidoprogesterone: A preliminary report (1993) Ann. Assoc. Química Argentina, 81, pp. 333-340 
504 |a Krozowski, Z.S., Funder, J.F., Renal mineralocorticoid receptors and hippocampal corticosterone binding species have identical intrinsic steroid specificity (1983) Proc. Natl. Acad. Sci. USA, 80, pp. 6056-6060 
504 |a Kraujelis, K., Ulinskaite, A., Meilus, V., Transcortin in rat kidney: Subcellular distribution of transcortin-synthesizing polyribosomes (1991) J. Steroid Biochem. Mol. Biol., 38, pp. 43-47 
504 |a Jensen, E.V., Steroid hormone antagonists: An overview (1995) Ann. N. Y. Acad. Sci., 761, pp. 1-1 
504 |a Hendry, L.B., Chu, C.K., Rosser, M.L., Copland, J.A., Wood, J.C., Mahesh, V.B., Design of novel antiestrogens (1994) J. Steroid Biochem. Mol. Biol., 49, pp. 269-280 
520 3 |a 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.  |l eng 
593 |a Departemento de Quim. Biol., Ciudad Universitaria, (1428) Buenos Aires, Argentina 
593 |a Departemento de Quim. Organ., Ciudad Universitaria, (1428) Buenos Aires, Argentina 
593 |a Fac. de Ciencias Exactas y Naturales, Universidad de Buenos Aires, PRHOM-Consejo Nac. Invest. Cie. y T., (1428) Buenos Aires, Argentina 
593 |a Department of Pharmacology, University of Michigan, Medical School, Ann Arbor, MI 48109-0632, United States 
593 |a Departemento de Quim. Biol., Ciudad Universitaria, Pabellón 2, 1428 Buenos Aires, Argentina 
690 1 0 |a 11BETA,17BETA DIHYDROXY 6 METHYL 17ALPHA (1 PROPYNYL)ANDROSTA 1,4,6 TRIEN 3 ONE 
690 1 0 |a 15BETA,16BETA METHYLENEMEXRENONE 
690 1 0 |a 21 HYDROXY 6,19 OXIDOPROGESTERONE 
690 1 0 |a ALDOSTERONE 
690 1 0 |a CORTICOSTERONE 
690 1 0 |a DEXAMETHASONE 
690 1 0 |a GLUCOCORTICOID ANTAGONIST 
690 1 0 |a GLUCOCORTICOID RECEPTOR 
690 1 0 |a MINERALOCORTICOID RECEPTOR 
690 1 0 |a PROGESTERONE 
690 1 0 |a STEROID 
690 1 0 |a TYROSINE AMINOTRANSFERASE 
690 1 0 |a UNCLASSIFIED DRUG 
690 1 0 |a ANIMAL TISSUE 
690 1 0 |a ARTICLE 
690 1 0 |a CONTROLLED STUDY 
690 1 0 |a CYTOSOL 
690 1 0 |a DOSE RESPONSE 
690 1 0 |a DRUG CONFORMATION 
690 1 0 |a DRUG RECEPTOR BINDING 
690 1 0 |a ENZYME INDUCTION 
690 1 0 |a KIDNEY CELL 
690 1 0 |a MALE 
690 1 0 |a NONHUMAN 
690 1 0 |a PRIORITY JOURNAL 
690 1 0 |a RAT 
690 1 0 |a SODIUM RETENTION 
653 0 0 |a ru 28362, Roussel Uclaf, France; zk 91587, New England Nuclear, United States 
700 1 |a Monteserín, M.C. 
700 1 |a Veleiro, A.S. 
700 1 |a Burton, G. 
700 1 |a Lantos, C.P. 
700 1 |a Galigniana, M.D. 
773 0 |d American Society for Pharmacology and Experimental Therapy, 1997  |g v. 52  |h pp. 749-753  |k n. 4  |p MOL. PHARMACOL.  |x 0026895X  |t Molecular Pharmacology 
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856 4 0 |u https://doi.org/10.1124/mol.52.4.749  |y DOI 
856 4 0 |u https://hdl.handle.net/20.500.12110/paper_0026895X_v52_n4_p749_Vicent  |y Handle 
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962 |a info:eu-repo/semantics/article  |a info:ar-repo/semantics/artículo  |b info:eu-repo/semantics/publishedVersion 
999 |c 64126 

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