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非甾体化合物与子宫孕酮受体的分子相互作用(第一部分)

Molecular interaction of nonsteroidal compounds with uterine progesterone receptor (Part I).

作者信息

Agnihotri A, Niwas S, Bhat B K, Kumar S, Seth M, Bhaduri A P, Srivastava A K, Kamboj V P

出版信息

Exp Clin Endocrinol. 1986 Dec;88(2):185-92. doi: 10.1055/s-0029-1210595.

Abstract

Progesterone-receptor binding affinity of some nonsteroidal molecules was assessed by competitive protein binding assay in rabbit as well as human uterine cytosol in vitro. Of 40 compounds belonging to 5 different series tested, 3-(p-anisoyl)-2-chloro-6, 7-dimethoxy-quinoline exhibited around 50% inhibition whereas 2-(p-anisoyl) naphthalene and 3-substituted phenyl-1-(3-(2-chloro-6, 7-dialkoxy) quinolinyl)prop-2-en-1-one showed around 20% inhibition in 3H-progesterone binding for rabbit and human uterine progesterone receptor.

摘要

通过竞争性蛋白结合试验,在体外对兔和人子宫胞质溶胶中一些非甾体分子的孕酮受体结合亲和力进行了评估。在所测试的属于5个不同系列的40种化合物中,3-(对茴香酰基)-2-氯-6,7-二甲氧基喹啉表现出约50%的抑制作用,而2-(对茴香酰基)萘和3-取代苯基-1-(3-(2-氯-6,7-二烷氧基)喹啉基)丙-2-烯-1-酮对兔和人子宫孕酮受体的3H-孕酮结合表现出约20%的抑制作用。

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