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米非司酮(mifepristone, Mifegyne,RU486)是第一个合成的抗孕激素,为炔诺酮衍生物,其C-17_α侧链可增加对受体的亲和力,而C-11_β环可产生拮抗活性。 受体的研究 由各种啮齿动物证明米非司酮为一种纯黄体酮拮抗剂。它与兔子宫黄体酮受体结合的亲和力要比黄体酮大5倍,而对人黄体酮受体的亲和力与黄体酮相似。它并不抑制体外卵细胞的生物合成。但在猕猴和人,当用绒促性素增加黄体酮而延长黄体期时,本药可终止黄体期。对小鼠、大鼠和猴均可终止妊娠。
Mifepristone (Mifegyne, RU486) is the first synthetic anti-progestin, a derivative of norethindrone, whose C-17-alpha side chain increases affinity for the receptor and C-11-beta ring produces antagonism active. Receptor Studies Mifepristone proved to be a pure progesterone antagonist by various rodents. It binds to the rabbit uterine progesterone receptor with a 5-fold greater affinity than progesterone, and has similar affinity to human progesterone receptors as progesterone. It does not inhibit in vitro egg cell biosynthesis. However, in macaques and humans, the drug may terminate the luteal phase when lengthening the luteal phase by using progesterone to increase progesterone. Pregnancy can be terminated in mice, rats and monkeys.