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卵巢孕酮对多种动物的早期妊娠起着必不可少的作用,切断孕酮的来源将终止其妊娠。通过诱导功能性的溶黄体作用或用抗体使循环中的孕酮失效都可能中断妊娠。阻断孕酮功能的目的,理论上可以通过阻断它结合于其子宫受体来达到。曾有报道,一种药物R-2323,在人体其作用是可疑的,月经过期后给药它似乎不起流产作用,月经中期给药,它作为假想的孕酮拮抗剂而起抗着床作用,也可能由于它抑制垂体促性腺激素的分泌而起抗排卵作用。本文介绍了寻找孕酮竞争性拮抗剂的方案。如图所示,第一个程序受体结合能力并不是结论性的,因这种结合既表征激动剂又表征拮抗剂。因而有一定结合亲和力的化合物要继以孕激素活性和抗孕激素活性的生物学试验,即对家兔子宫内膜转化的抑制或刺激作用,对去势大鼠孕酮维持妊娠的抑制作用,对大鼠和金地鼠着床后的妊娠终止作用。
Ovarian progesterone plays an essential role in the early pregnancy of many animals and cutting off the source of progesterone will stop its pregnancy. Pregnancy may be interrupted by inducing a functional dissolution of the corpus luteum or by failure of the circulating progesterone with antibodies. The purpose of blocking progesterone function can in theory be achieved by blocking it from binding to its uterine receptor. It has been reported that a drug R-2323, whose action is suspicious in the human body, appears to be refractory to abortion after menstruation, menstrual metaphase, and serves as an anti-implantation effect as a hypothetical progesterone antagonist , May also be due to its inhibition of pituitary gonadotropin secretion and anti-ovulation. This article describes the search for competitive progesterone antagonist program. As shown, the first receptor’s ability to bind to the receptor is not conclusive, as the binding characterizes both the agonist and the antagonist. Thus there is a certain combination of affinity compounds to be followed by progesterone activity and anti-progesterone activity of the biological test, that is, the inhibition of rabbit endometrial transformation or stimulation of the role of ovariectomized rats progesterone maintenance pregnancy inhibition, Termination of pregnancy after implantation in rats and golden hamsters.