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Binding of glucocorticoid antagonists to androgen and glucocorticoid hormone receptors in rat skeletal muscle.
J Steroid Biochem. 1986 Feb; 24(2):481-7.JS

Abstract

The binding of ten steroids possessing antiglucocorticoid activity has been studied in rat skeletal muscle cytosol. The affinity of these steroids for both the androgen and the glucocorticoid receptors was determined by competition with radioactive R1881 (methyltrienolone, metribolone) and dexamethasone, respectively. The antiglucocorticoid activity of these compounds was assessed in rat hepatoma (HTC) cells by measuring their inhibitory effect on the glucocorticoid-induced tyrosine aminotransferase activity. This led to identification of five novel in vitro glucocorticoid antagonists. All the steroids tested bound to both the glucocorticoid and the androgen receptors in muscle. Four steroids had an affinity for the glucocorticoid receptor higher than for the androgen receptor. The assumption is made that the steroids tested also behave as antagonists when binding to the glucocorticoid receptor in muscle and behave as agonists when binding to the androgen receptor. On this basis, the data allow one to compute a potential anticatabolic (PAG) and a potential anabolic (PAA) index for each compound. These indices might be of predictive value to determine whether these steroids exert their anabolic action in muscle through the glucocorticoid receptor or through the androgen receptor. The data also make it unlikely that satellite cells are a preferential target for anabolic steroids in muscle.

Authors

No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

3486322

Citation

Danhaive, P A., and G G. Rousseau. "Binding of Glucocorticoid Antagonists to Androgen and Glucocorticoid Hormone Receptors in Rat Skeletal Muscle." Journal of Steroid Biochemistry, vol. 24, no. 2, 1986, pp. 481-7.
Danhaive PA, Rousseau GG. Binding of glucocorticoid antagonists to androgen and glucocorticoid hormone receptors in rat skeletal muscle. J Steroid Biochem. 1986;24(2):481-7.
Danhaive, P. A., & Rousseau, G. G. (1986). Binding of glucocorticoid antagonists to androgen and glucocorticoid hormone receptors in rat skeletal muscle. Journal of Steroid Biochemistry, 24(2), 481-7.
Danhaive PA, Rousseau GG. Binding of Glucocorticoid Antagonists to Androgen and Glucocorticoid Hormone Receptors in Rat Skeletal Muscle. J Steroid Biochem. 1986;24(2):481-7. PubMed PMID: 3486322.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Binding of glucocorticoid antagonists to androgen and glucocorticoid hormone receptors in rat skeletal muscle. AU - Danhaive,P A, AU - Rousseau,G G, PY - 1986/2/1/pubmed PY - 1986/2/1/medline PY - 1986/2/1/entrez SP - 481 EP - 7 JF - Journal of steroid biochemistry JO - J Steroid Biochem VL - 24 IS - 2 N2 - The binding of ten steroids possessing antiglucocorticoid activity has been studied in rat skeletal muscle cytosol. The affinity of these steroids for both the androgen and the glucocorticoid receptors was determined by competition with radioactive R1881 (methyltrienolone, metribolone) and dexamethasone, respectively. The antiglucocorticoid activity of these compounds was assessed in rat hepatoma (HTC) cells by measuring their inhibitory effect on the glucocorticoid-induced tyrosine aminotransferase activity. This led to identification of five novel in vitro glucocorticoid antagonists. All the steroids tested bound to both the glucocorticoid and the androgen receptors in muscle. Four steroids had an affinity for the glucocorticoid receptor higher than for the androgen receptor. The assumption is made that the steroids tested also behave as antagonists when binding to the glucocorticoid receptor in muscle and behave as agonists when binding to the androgen receptor. On this basis, the data allow one to compute a potential anticatabolic (PAG) and a potential anabolic (PAA) index for each compound. These indices might be of predictive value to determine whether these steroids exert their anabolic action in muscle through the glucocorticoid receptor or through the androgen receptor. The data also make it unlikely that satellite cells are a preferential target for anabolic steroids in muscle. SN - 0022-4731 UR - https://www.unboundmedicine.com/medline/citation/3486322/Binding_of_glucocorticoid_antagonists_to_androgen_and_glucocorticoid_hormone_receptors_in_rat_skeletal_muscle_ L2 - https://medlineplus.gov/steroids.html DB - PRIME DP - Unbound Medicine ER -