Identificador persistente para citar o vincular este elemento:
http://hdl.handle.net/10553/48425
Título: | Identification of a specific binding site for the anabolic steroid stanozolol in male rat liver microsomes | Autores/as: | Boada, LD Fernández, Leandro Zumbado, Manuel Luzardo, Octavio P. Chirino, Ricardo Díaz-Chico, Bonifacio N. |
Clasificación UNESCO: | 32 Ciencias médicas 3209 Farmacología |
Palabras clave: | H-3 Dexamethasone Binding Glucocorticoid-Binding Estrogen-Receptors Nuclear Envelopes Androgen Receptor, et al. |
Fecha de publicación: | 1996 | Publicación seriada: | Journal of Pharmacology and Experimental Therapeutics | Resumen: | Male rat liver microsomes contain a [H-3]dexamethasone binding site, capable of binding glucocorticoids and progesterone. We have shown previously that the 17 alpha-alkylated androgen, stanozolol, can inhibit the [H-3]dexamethasone binding to microsomes through a negative allosteric mechanism, which gives rise to the possibility of its interaction with a different binding site. In this study, the existence of a single-saturating binding site, capable of binding the radioactive steroid with a maximum number of the specific binding site of 49 +/- 2 pmol/mg of protein and a K-d of 37 +/- 1.3 nM was demonstrated by using [H-3]stanozolol. In competition experiments, only stanozolol and danazol were able to compete with [H-3]stanozolol for its binding to microsomes, among more than 60 steroids and other compounds tested. The binding of [H-3]stanozolol was depressed after protease treatment of the microsomes, or after the administration of cycloheximide to adult male rats for 24 hr, which suggest its proteic nature. The [H-3]stanozolol binding site was detected in many tissues of the rat, with the highest concentrations being found in the liver. It was detected from birth,increasing afterward in concentration and reaching a peak at 2 to 3 months of age. This is the first experimental verification of the existence in liver microsomes of a specific binding site for some 17 alpha-alkylated androgens, such as stanozolol and danazol, different from the androgen receptor or the [H-3]dexamethasone binding site. | URI: | http://hdl.handle.net/10553/48425 | ISSN: | 0022-3565 | Fuente: | Journal Of Pharmacology And Experimental Therapeutics[ISSN 0022-3565],v. 279 (3), p. 1123-1129 |
Colección: | Artículos |
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