[Modulation of the glucocorticoid receptor interaction with sodium ethazole].

P P Golikov, N Iu Nikolaeva

文献索引：Vopr. Med. Khim. 40(2) , 9-12, (1994)

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摘要

The effect of sodium sulfaethidole on Types II and III glucocorticoid receptors was studied in liver cytosol fraction obtained from female Wistar rats of 180-200 g body weight. Functions of Type II glucocorticoid receptors in liver cytosol were evaluated by triamcinolone 3H-acetonide and Type III glucocorticoid receptors by 3H-corticosterone. The Scatchard and Laynuiver-Berck analyses indicated that sodium sulfaethidole decreased the density of Type II glucocorticoid receptors and the complex association constant. A decrease in functions of Type II glucocorticoid receptors in the presence of the drug occurred by the competitive type. At the same time, sodium sulfaethidole increased greatly the function of Type III glucocorticoid receptors and an increase in the density of these receptors was realized noncompetitively. The decrease in the functions of Type II glucocorticoid receptors and increase in that of Type III receptors in the presence of sodium sulfaethidole suggest that the drug exhibits antiglucocorticoid properties.