Casper R F, Sheehan K L, Yen S S
J Clin Endocrinol Metab. 1980 Jan;50(1):179-81. doi: 10.1210/jcem-50-1-179.
After the sc administration of 1, 10, and 50 micrograms of the LRF agonist [D-Trp6,Pro9,NEt]LRF, dose-dependent increments in circulating levels of LH, FSH, and estradiol were observed which were 2- to 3-fold greater in the late than in the early follicular phase. The 10-microgram dose of LFR agonist appears to induce a maximal acute gonadotropin-estradiol response. Both 10- and 50-microgram doses of the agonist elicited gonadotropin increments which were several times greater than that seen during the midcycle surge. The only difference between the two doses was the more sustained action on gonadotropin release of the latter. It is estimated that this superactive LRF agonist is approximately 140 times more potent than the decapeptide LRF. These observations provide information useful in the application of this LRF agonist for clinical studies.
皮下注射1、10和50微克促黄体激素释放因子（LRF）激动剂[D-色氨酸6，脯氨酸9，N-乙基]LRF后，观察到促黄体生成素（LH）、促卵泡激素（FSH）和雌二醇循环水平呈剂量依赖性增加，在卵泡晚期增加幅度比卵泡早期大2至3倍。10微克剂量的LRF激动剂似乎能诱导最大的急性促性腺激素-雌二醇反应。10微克和50微克剂量的激动剂均引起促性腺激素增加，比月经周期中期高峰时的增加幅度大几倍。这两种剂量之间的唯一差异是后者对促性腺激素释放的作用更持久。据估计，这种超活性LRF激动剂的效力比十肽LRF约强140倍。这些观察结果为将这种LRF激动剂应用于临床研究提供了有用信息。
