Fanchenko N D, Kamernitskiĭ A V, Minina L S, Levina I S, Alekseeva M L
Biull Eksp Biol Med. 1988 Jun;105(6):679-81.
The interaction of promegestone (R-5020), progesterone (P) and its derivatives having and additional carbocyclic D' (pregna-D'-pentrans) with progestin-binding cytosol system of the uterus was studied in different species (rabbits, rats, guinea-pigs and men). A comparative analysis of the competitive binding data for the mentioned compounds has shown interspecies differences in ligand specificity. Two types of binding sites for 3H-D'-pentran (in contrast to R-5020 and P) have been detected in rabbit uterus cytosol, both in intact and estrogenized animals. However, in rabbits, estrogenization altered the values of the apparent equilibrium constants and binding capacities. At the same time, the interaction of pentran with progestin-binding sites in guinea-pig and human uterus cytosol is nonspecific. It is suggested that the features of the interaction of 3H-D'-pentran with its binding sites in rabbit uterus cytosol may be determined by an increase in hydrophobic bond.
在不同物种（兔、大鼠、豚鼠和人）中研究了孕美孕酮（R-5020）、孕酮（P）及其具有额外碳环D′（孕甾-D′-戊环）的衍生物与子宫孕激素结合胞浆系统的相互作用。对上述化合物竞争结合数据的比较分析显示了配体特异性的种间差异。在完整动物和雌激素处理的动物的兔子宫胞浆中均检测到了两种类型的3H-D′-戊环结合位点（与R-5020和P不同）。然而，在兔中，雌激素处理改变了表观平衡常数和结合容量的值。同时，戊环与豚鼠和人子宫胞浆中孕激素结合位点的相互作用是非特异性的。有人提出，3H-D′-戊环与其在兔子宫胞浆中结合位点相互作用的特征可能由疏水键的增加所决定。
