Weber T, Happ J, Krause U, Beyer J
Klin Wochenschr. 1978 Apr 1;56(7):363-4. doi: 10.1007/BF01477397.
Potent long acting anologs of GnRH are of great interest especially in view of treatment of hypothalamic hypogonadotropic hypogonadism and of cryptorchidism. To find necessary parenteral doses of such a substance immunoreactive serum LH and FSH were measured in 4 normal adult human males after s.c. injection of various doses of D-Leu6-des-Gly10-GnRH-EA. 5 microgram of the GnRH anlog were necessary to obtain increased serum gonadotropins over a period of at least 8 h. Comparable maximal levels were seen after i.v. bolus injection of 25 microgram natural GnRH a dose as used in diagnostic routine tests in 3 probands. Comparing the areas under the curves of LH secretion an over 15 times greater effectiveness of the analog was calculated.
促性腺激素释放激素(GnRH)的强效长效类似物备受关注,尤其是考虑到其在治疗下丘脑性低促性腺激素性腺功能减退症和隐睾症方面的应用。为了确定这种物质的必要皮下注射剂量,对4名正常成年男性皮下注射不同剂量的D-亮氨酸6-去甘氨酸10-GnRH-EA后,测定了免疫反应性血清促黄体生成素(LH)和促卵泡生成素(FSH)。至少8小时内,需要5微克的GnRH类似物才能使血清促性腺激素升高。在3名受试者中,静脉推注25微克天然GnRH(这是诊断常规测试中使用的剂量)后,观察到了类似的最大水平。比较LH分泌曲线下的面积,计算出该类似物的有效性超过15倍。