DeFazio J, Lu J K, Vale W, Rivier J, Judd H L, Meldrum D R
Endocr Res. 1984;10(2):163-70. doi: 10.3109/07435808409035416.
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.
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。