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  • Title: [Interaction of pregna-D'-pentaranes--pentacyclic derivatives of progesterone--with gestagen-binding sites of uterine cytosol].
    Author: Fanchenko ND, Kamernitskiĭ AV, Minina LS, Levina IS, Alekseeva ML.
    Journal: Biull Eksp Biol Med; 1988 Jun; 105(6):679-81. PubMed ID: 3390587.
    Abstract:
    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.
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