Happ J, Depper M, Weber T, Hartmann U, Kollmann F, Beyer J
Endokrinologie. 1979 Apr;74(1):33-41.
Potent long acting analogs of GnRH are of great interest especially in view of pernasal (p.n.) treatmen of hypogonadism of hypothalamic origin and of cryptorchidism. To find the necessary p.n. dosage of such a substance, serum LH and FSH were measured in 6 normal adult human males after p.n. application of various doses of D Leu6-des-Gly10-GnRH ethylamide. 50 microgram of the GnRH analog were necessary to obtain increased serum gonadotropins over a period of at least 8 hours. By repeated p.n. application of 200 microgram of synthetic GnRH every 2 hours in 6 normal adult males a considerable increase of serum gonadotropins could be demonstrated as well. Pernasal application of 200 microgram GnRH repeated at an interval of 1 hour in 3 cryptorchid boys produced a distinct increase of the serum gonadotropins. The intraindividual comparison of 200 microgram GnRH and 20 microgram of the GnRH analog in one boy showed equivalent net increases of the gonadotropins. With the analog the gonadotropin increase lasted for about 6 hours.
促性腺激素释放激素(GnRH)的强效长效类似物备受关注,特别是考虑到经鼻(p.n.)治疗下丘脑源性性腺功能减退和隐睾症。为了确定这种物质的必要经鼻剂量,在6名正常成年男性经鼻应用不同剂量的D-亮氨酸6-去甘氨酸10-GnRH乙酰胺后,测量了血清促黄体生成素(LH)和促卵泡生成素(FSH)。至少8小时内,需要50微克的GnRH类似物才能使血清促性腺激素增加。在6名正常成年男性中,每2小时重复经鼻应用200微克合成GnRH,也可使血清促性腺激素显著增加。在3名隐睾症男孩中,每1小时重复经鼻应用200微克GnRH,可使血清促性腺激素明显增加。在一名男孩中对200微克GnRH和20微克GnRH类似物进行个体内比较,结果显示促性腺激素的净增加量相当。使用类似物时,促性腺激素增加持续约6小时。