皮质醇的17α-和/或21-酯以及17α,21-二酯对大鼠胸腺细胞糖皮质激素受体的相对亲和力。

Relative affinity of 17 alpha- and/or 21-esters and 17 alpha, 21-diesters of cortisol for a glucocorticoid receptor from rat thymocytes.

作者信息

Solo A J, Tramposch K M, Szeto D W, Suto M J

出版信息

J Med Chem. 1982 Jun;25(6):747-9. doi: 10.1021/jm00348a027.

Abstract

The affinity, relative to cortisol (1), of 17 alpha- and 21-esters and 17 alpha,21-diesters of cortisol for the glucocorticoid receptor of rat thymus cytosol was determined by a competitive binding assay which used [3H]dexamethasone. Esterification of the 21-hydroxy group of cortisol caused a loss of relative affinity to 0.046 for acetate and 0.32 for valerate. Esterification of the 17 alpha-hydroxy group resulted in an increase in relative affinity to 1.14 for acetate, 12.4 for butyrate, and 11.5 for valerate. Diesters had relative affinities which reflected both trends. Thus, the 21-acetate, 21-propionate, 21-butyrate, and 21-valerate of cortisol 17-acetate had relative affinities of 0.036, 0.093, 0.152, and 0.272. The 21-acetate, 21-propionate, and 21-butyrate of cortisol 17-valerate had relative affinities of 0.76, 1.17, and 1.33.

摘要

采用竞争结合分析法，以[3H]地塞米松为标记物，测定了皮质醇的17α-酯、21-酯及17α,21-二酯相对于皮质醇（1）对大鼠胸腺细胞溶质糖皮质激素受体的亲和力。皮质醇21-羟基的酯化导致其相对亲和力降低，醋酸酯为0.046，戊酸酯为0.32。17α-羟基的酯化则使相对亲和力增加，醋酸酯为1.14，丁酸酯为12.4，戊酸酯为11.5。二酯的相对亲和力反映了这两种趋势。因此，皮质醇17-醋酸酯的21-醋酸酯、21-丙酸酯、21-丁酸酯和21-戊酸酯的相对亲和力分别为0.036、0.093、0.152和0.272。皮质醇17-戊酸酯的21-醋酸酯、21-丙酸酯和21-丁酸酯的相对亲和力分别为0.76、1.17和1.33。