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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