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促性腺激素释放激素(GnRH)的(咪唑苄基)D-组氨酸6、去甘氨酸类似物对正常女性促性腺激素和雌二醇分泌的影响。

Effects of the (imBzl)D-His6, Des-Gly analog of GnRH on gonadotropin and estradiol secretion in normal women.

作者信息

DeFazio J, Lu J K, Vale W, Rivier J, Judd H L, Meldrum D R

出版信息

Endocr Res. 1984;10(2):163-70. doi: 10.3109/07435808409035416.

Abstract

The acute gonadotropin and estradiol responses following single subcutaneous injections of 10, 50, 100 and 200 micrograms of [(imBzl)]D-His6,Pro9-NEt]-GnRH were compared to those after 100 micrograms of [D-Trp6, Pro9-NEt]-GnRH. The gonadotropin responses after 50-100 micrograms of the D-His analog of GnRH were equivalent to those following 100 micrograms of the D-Trp analog. The ovarian E2 response, a reflection of the total cumulative secretion of gonadotropins, was similar at 100 micrograms of each analog. The estradiol response paralleled the increasing gonadotropin response accompanying the graded doses of the D-His analog, indicating the lack of a direct inhibitory action of this GnRH agonist on the ovary. Assessment of both gonadotropin and estradiol responses appears to be satisfactory for assessing relative potency among GnRH agonistic analogs.

摘要

将单次皮下注射10、50、100和200微克[(imBzl)]D-组氨酸6、脯氨酸9-乙酯]-GnRH后的急性促性腺激素和雌二醇反应与注射100微克[D-色氨酸6,脯氨酸9-乙酯]-GnRH后的反应进行比较。50-100微克GnRH的D-组氨酸类似物后的促性腺激素反应与100微克D-色氨酸类似物后的反应相当。每种类似物100微克时,反映促性腺激素总累积分泌的卵巢E2反应相似。雌二醇反应与随着D-组氨酸类似物剂量递增而增加的促性腺激素反应平行,表明该GnRH激动剂对卵巢缺乏直接抑制作用。评估促性腺激素和雌二醇反应对于评估GnRH激动剂类似物之间的相对效价似乎是令人满意的。

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