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...
Guardado en:
| Autores principales: | , , , , , |
|---|---|
| Formato: | JOUR |
| Materias: | |
| Acceso en línea: | http://hdl.handle.net/20.500.12110/paper_0026895X_v52_n4_p749_Vicent |
| Aporte de: |
| id |
todo:paper_0026895X_v52_n4_p749_Vicent |
|---|---|
| record_format |
dspace |
| spelling |
todo:paper_0026895X_v52_n4_p749_Vicent2023-10-03T14:37:11Z 21-hydroxy-6,19-oxidoprogesterone: A novel synthetic steroid with specific antiglucocorticoid properties in the rat Vicent, G.P. Monteserín, M.C. Veleiro, A.S. Burton, G. Lantos, C.P. Galigniana, M.D. 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. JOUR info:eu-repo/semantics/openAccess http://creativecommons.org/licenses/by/2.5/ar 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, 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 |
| 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. |
| format |
JOUR |
| author |
Vicent, G.P. Monteserín, M.C. Veleiro, A.S. Burton, G. Lantos, C.P. Galigniana, M.D. |
| author_facet |
Vicent, G.P. Monteserín, M.C. Veleiro, A.S. Burton, G. Lantos, C.P. Galigniana, M.D. |
| author_sort |
Vicent, G.P. |
| 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 |
| url |
http://hdl.handle.net/20.500.12110/paper_0026895X_v52_n4_p749_Vicent |
| work_keys_str_mv |
AT vicentgp 21hydroxy619oxidoprogesteroneanovelsyntheticsteroidwithspecificantiglucocorticoidpropertiesintherat AT monteserinmc 21hydroxy619oxidoprogesteroneanovelsyntheticsteroidwithspecificantiglucocorticoidpropertiesintherat AT veleiroas 21hydroxy619oxidoprogesteroneanovelsyntheticsteroidwithspecificantiglucocorticoidpropertiesintherat AT burtong 21hydroxy619oxidoprogesteroneanovelsyntheticsteroidwithspecificantiglucocorticoidpropertiesintherat AT lantoscp 21hydroxy619oxidoprogesteroneanovelsyntheticsteroidwithspecificantiglucocorticoidpropertiesintherat AT galignianamd 21hydroxy619oxidoprogesteroneanovelsyntheticsteroidwithspecificantiglucocorticoidpropertiesintherat |
| _version_ |
1807320710832455680 |