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:	Vicent, Guillermo Pablo, Veleiro, Adriana Silvia, Burton, Gerardo
Publicado:	1997
Materias:	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
Acceso en línea:	https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v52_n4_p749_Vicent http://hdl.handle.net/20.500.12110/paper_0026895X_v52_n4_p749_Vicent
Aporte de:	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires

id	paper:paper_0026895X_v52_n4_p749_Vicent
record_format	dspace
spelling	paper:paper_0026895X_v52_n4_p749_Vicent2023-06-08T14:53:55Z 21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat Vicent, Guillermo Pablo Veleiro, Adriana Silvia Burton, Gerardo 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 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. Fil:Vicent, G.P. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Veleiro, A.S. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. Fil:Burton, G. Universidad de Buenos Aires. Facultad de Ciencias Exactas y Naturales; Argentina. 1997 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v52_n4_p749_Vicent http://hdl.handle.net/20.500.12110/paper_0026895X_v52_n4_p749_Vicent
institution	Universidad de Buenos Aires
institution_str	I-28
repository_str	R-134
collection	Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA)
topic	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
spellingShingle	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 Vicent, Guillermo Pablo Veleiro, Adriana Silvia Burton, Gerardo 21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat
topic_facet	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
description	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.
author	Vicent, Guillermo Pablo Veleiro, Adriana Silvia Burton, Gerardo
author_facet	Vicent, Guillermo Pablo Veleiro, Adriana Silvia Burton, Gerardo
author_sort	Vicent, Guillermo Pablo
title	21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat
title_short	21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat
title_full	21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat
title_fullStr	21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat
title_full_unstemmed	21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat
title_sort	21-hydroxy-6,19-oxidoprogesterone: a novel synthetic steroid with specific antiglucocorticoid properties in the rat
publishDate	1997
url	https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_0026895X_v52_n4_p749_Vicent http://hdl.handle.net/20.500.12110/paper_0026895X_v52_n4_p749_Vicent
work_keys_str_mv	AT vicentguillermopablo 21hydroxy619oxidoprogesteroneanovelsyntheticsteroidwithspecificantiglucocorticoidpropertiesintherat AT veleiroadrianasilvia 21hydroxy619oxidoprogesteroneanovelsyntheticsteroidwithspecificantiglucocorticoidpropertiesintherat AT burtongerardo 21hydroxy619oxidoprogesteroneanovelsyntheticsteroidwithspecificantiglucocorticoidpropertiesintherat
_version_	1768543789285113856

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

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