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抗孕激素甾体RMI 12,936及相关化合物对大鼠抗生育作用的进一步研究。

Further investigation of the antifertility effects in the rat of the antiprogestational steroid, RMI 12,936, and related compounds.

作者信息

Kendle K E

出版信息

J Reprod Fertil. 1978 Mar;52(2):373-7. doi: 10.1530/jrf.0.0520373.

Abstract

The antifertility activities of RMI 12,936 and 7alpha-methyltestosterone may be reversed by progesterone implants in ovariectomized, but not in intact, rats on Day 8 of pregnancy. The presence of the ovary for 48 h after administration of RMI 12,936 is necessary for irreversible antifertility activity to be developed, and it is concluded that this activity is due to a metabolite other than 7alpha-methyltestosterone. 7alpha-Methylandrostenedione was significantly less potent than RMI 12,936 in antifertility tests, while the uterotrophic activity of RMI 12,936 was not inhibited by aromatization inhibitors, suggesting that the active metabolite is not produced by dehydrogenation or aromatization of 7alpha-methyltestosterone.

摘要

在妊娠第8天,对于卵巢切除的大鼠,孕酮植入物可逆转RMI 12,936和7α-甲基睾酮的抗生育活性,但对于未切除卵巢的大鼠则不能。给予RMI 12,936后48小时内卵巢的存在是产生不可逆抗生育活性所必需的,并且得出结论,这种活性是由7α-甲基睾酮以外的一种代谢物引起的。在抗生育试验中,7α-甲基雄烯二酮的效力明显低于RMI 12,936,而RMI 12,936的子宫营养活性不受芳香化抑制剂的抑制,这表明活性代谢物不是由7α-甲基睾酮的脱氢或芳香化产生的。

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