Asch R H, Balmaceda J P, Eddy C A, Siler-Khodr T, Coy D H, Schally A V
Fertil Steril. 1981 Sep;36(3):388-91. doi: 10.1016/s0015-0282(16)45742-0.
Regularly cycling rhesus monkeys were bilaterally oophorectomized for study of postcastration rise of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). The animals were divided in two groups, control animals, which received vehicle, and experimental animals, which received intramuscularly 1 mg of a potent luteinizing hormone-releasing hormone (LHRH) inhibitory analog ([N-Ac-D-Trp1-3,D-p-Cl-phe2,D-Phe6,D-Ala10]-LH-RH) from the day of castration for 10 days. The controls showed significant elevations of FSH and LH 3 to 4 days after castration, but in the experimental animals the rise in gonadotropins was blocked until the LHRH antagonist administration was discontinued. The dynamics of gonadotropin elevation after the discontinuation of [N-Ac-D-Trp1-3,D-p-Cl-phe2,D-Phe6,D-Ala10]-LH-RH administration were similar to those observed in control animals after castration. The availability of a compound that selectively inhibits FSH and LH secretion in primates opens a new approach to contraception and for the treatment of conditions in which gonadotropin inhibition is desired.
为研究去势后促卵泡激素(FSH)和促黄体生成素(LH)的升高情况,对定期骑行的恒河猴进行双侧卵巢切除。将动物分为两组,一组为接受赋形剂的对照动物,另一组为从去势当天起连续10天肌肉注射1毫克强效促黄体生成素释放激素(LHRH)抑制类似物([N-乙酰-D-色氨酸1-3,D-对氯苯丙氨酸2,D-苯丙氨酸6,D-丙氨酸10]-LH-RH)的实验动物。对照组在去势后3至4天FSH和LH显著升高,但在实验动物中,促性腺激素的升高被阻断,直到停止给予LHRH拮抗剂。停止给予[N-乙酰-D-色氨酸1-3,D-对氯苯丙氨酸2,D-苯丙氨酸6,D-丙氨酸10]-LH-RH后促性腺激素升高的动态变化与去势后对照动物中观察到的相似。一种能选择性抑制灵长类动物FSH和LH分泌的化合物的出现,为避孕以及治疗需要抑制促性腺激素的病症开辟了一条新途径。