一种新型前列腺素F 2α衍生物（ZK 71 677）与假孕大鼠卵巢的结合。

Binding of a novel prostaglandin F 2 alpha-derivative (ZK 71 677) to pseudopregnant rat ovaries.

作者信息

Brambaifa N

出版信息

J Recept Res. 1986;6(3-4):195-207. doi: 10.3109/10799898609074810.

Abstract

Prostaglandin (PG)F 2 alpha is believed to regulate the life span of the corpus luteum and this physiologically induced change could be related to the binding properties of PGF 2 alpha in the corpus luteum. Corpora lutea formation was therefore stimulated in juvenile rats with PMSG and HCG. In membrane particles obtained after differential centrifugation, radioligand binding studies were performed with PGF 2 alpha and a novel PGF 2 alpha-derivative (ZK 71 677) on day 7 after HCG administration. Evaluation of the binding parameters revealed a competitive interaction between PGF 2 alpha and ZK 71 677 for the PGF 2 alpha-receptor molecule. When other prostaglandin analogues were used to establish biological potency, the data obtained from receptor binding analysis compared well with the abortifacient potency of these compounds in pregnant rats. The results provide further evidence for the nature and specificity of the PGF 2 alpha-receptor molecule.

摘要

前列腺素（PG）F 2α被认为可调节黄体的寿命，这种生理诱导的变化可能与PGF 2α在黄体中的结合特性有关。因此，用孕马血清促性腺激素（PMSG）和人绒毛膜促性腺激素（HCG）刺激幼年大鼠形成黄体。在HCG给药后第7天，对差速离心后获得的膜颗粒进行了PGF 2α和一种新型PGF 2α衍生物（ZK 71 677）的放射性配体结合研究。结合参数评估显示，PGF 2α和ZK 71 677对PGF 2α受体分子存在竞争性相互作用。当使用其他前列腺素类似物确定生物活性时，受体结合分析获得的数据与这些化合物在妊娠大鼠中的堕胎效力相当。这些结果为PGF 2α受体分子的性质和特异性提供了进一步的证据。