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

AJ Solo, KM Tramposch, DW Szeto…

Index: Solo; Tramposch; Szeto; Suto Journal of Medicinal Chemistry, 1982 , vol. 25, # 6 p. 747 - 749

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Citation Number: 11

Abstract

The affinity, relative to cortisol (l), of 17a-and 21-esters and 17a, 2l-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. Esterfication of the l7a- hydroxy group resulted in an increase in relative affinity to 1.14 for acetate, 12.4 for ...