Cortes-Prieto J, Garcia-Garcia M D, Arencibia-Rocha J, Oriol-Bosch A, Ayuso-Gutiérrez J L, Coy D H, Schally A V
Int J Fertil. 1978;23(3):224-8.
A long-acting analog of LH-RH, D-Ala6-desGly10-LH-RH propylamide (D-Ala6-LH-RH PA) was administered intramuscularly in a dose of 250 micrograms to 11 women with amenorrhea in whom the determinations of urinary steroid secretion, progesterone challenge, clomiphene, HMG, and LH-RH tests had been performed previously. Blood samples were taken twice before the injection and at 0.5, 1, 2, 4, 8, 12, 24, 26, 28, 30, and 32 h. No visible side effects were observed. Plasma levels of LH and FSH were determined by radioimmunoassays and expressed in mIU/2nd-IRP HMG/ml. The analog caused a great elevation in plasma LH and FSH levels. The maximal absolute increment for LH was between 3.93 and 115.89 mIU/ml, and the maximal increment in percentage was between 220 and 4,300. The time of the LH peak varied between 0.5 and 12 h. For FSH, the maximal absolute increment was between 6.45 and 50.92 mIU/ml and the maximal increment in percentage was between 63 and 1,442. The peak of FSH occurred in most cases at 4 to 8 h.
给11名闭经女性肌肉注射250微克长效促黄体生成素释放激素类似物D-丙氨酸6-去甘氨酸10-促黄体生成素释放激素丙酰胺(D-Ala6-LH-RH PA),这些女性之前已进行过尿甾体分泌测定、黄体酮激发试验、克罗米芬试验、人绝经期促性腺激素试验以及促黄体生成素释放激素试验。在注射前及注射后0.5、1、2、4、8、12、24、26、28、30和32小时采集血样两次。未观察到明显副作用。通过放射免疫分析法测定血浆促黄体生成素(LH)和促卵泡生成素(FSH)水平,并以mIU/第二国际参考品人绝经期促性腺激素/毫升表示。该类似物导致血浆LH和FSH水平大幅升高。LH的最大绝对增量在3.93至115.89 mIU/毫升之间,最大百分比增量在220至4300之间。LH峰值出现时间在0.5至12小时之间。对于FSH,最大绝对增量在6.45至50.92 mIU/毫升之间,最大百分比增量在63至1442之间。大多数情况下,FSH峰值出现在4至8小时。