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  • Title: Luteolytic potency of PGD and PGF2 alpha derivatives.
    Author: Brambaifa N.
    Journal: Eur J Obstet Gynecol Reprod Biol; 1988 Apr; 27(4):319-25. PubMed ID: 3164283.
    Abstract:
    Competitive binding studies with PGD derivatives and PGF2 alpha analogues to the PGF2 alpha-receptor molecule as well as their abortifacient potency in pregnant rats have been studied. Radioligand binding studies were performed in membrane particles isolated from pseudopregnant rat ovaries, and in parallel studies luteolytic doses of these prostaglandins and analogues were administered to pregnant rats and the abortifacient potency was estimated. It was observed that substances which displayed high potency in receptor binding in vitro were also potent in terminating luteal function and inducing abortion. The structural requirements of PGF2 alpha and PGD derivatives for binding to the PGF2 alpha-receptor were established, thereby indicating the specificity and geometry of the PGF2 alpha-receptor. Natural prostaglandins are not used as abortifacients because they are rapidly inactivated. Exogenous prostaglandins, particularly prostaglandin E2 and prostaglandin F2 alpha, have been found to induce uterine contractions and cause regression of the corpus luteum. This study investigated competitive binding of prostaglandin F2 alpha and prostaglandin D derivatives in vitro and correlated the competitive binding with the ability of these prostaglandin derivatives to induce abortion in rats. 16-phenoxy-prostaglandin D derivatives were found to bind to the prostaglandin F2 alpha receptor as well as did prostaglandin F2 itself. Addition of an epoxide group at C15 and a phenoxy group at C16 did not reduce the binding affinity, but these chemical changes stabilized the molecule. The stabilized prostaglandin D derivative also exhibited a very high abortifacient activity when administered in luteolytic doses to pregnant female rats.
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