Wiegelmann W, Solbach H G, Kley H K, Nieschlag E, Rudorff K H, Krüskemper H L
Horm Res. 1976;7(1):1-10. doi: 10.1159/000178702.
The effect of a new analogue of the gonadotrophin-releasing hormone LH-RH, D-Ser(TBU)6-EA10-LH-RH, on the secretion of LH, FSH, as well as testosterone, oestradiol, HGH, prolactin, TSH, and cortisol was studied in normal men. The same subjects were injected intravenously in 4-day intervals with 1.0, 2.5, 5.0, and 10.0 mug of this substance. A significant LH but no FSH release was seen after doses of 1.0 and 2.5 mug LH-RH analogue, while after 5.0 and 10.0 mug dose-dependent increases of LH and imposed elevations of FSH were observed. Peak levels of LH were reached after 30 min, those of FSH after intravenous injection after 120 min. LH and FSH remained elevated for 8-10 h. LH peak levels after 5 mug of LH-RH analogue were comparable to those seen after injection of 100 mug of the decapeptide LH-RH. Following the release of LH and FSH after doses of 5.0 and 10.0 mug LH-RH analogue, there was a late stimulating effect in testosterone and oestradiol secretion. HGH, TSH, prolactin, and cortisol were not influenced by the LH-RH analogue.
在正常男性中研究了促性腺激素释放激素LH-RH的一种新类似物D-Ser(TBU)6-EA10-LH-RH对促黄体生成素(LH)、促卵泡生成素(FSH)以及睾酮、雌二醇、生长激素(HGH)、催乳素、促甲状腺激素(TSH)和皮质醇分泌的影响。以4天的间隔给同一批受试者静脉注射1.0、2.5、5.0和10.0微克的这种物质。注射1.0和2.5微克LH-RH类似物后可见LH显著释放,但FSH无释放,而注射5.0和10.0微克后观察到LH呈剂量依赖性增加且FSH也升高。LH在30分钟后达到峰值水平,FSH在静脉注射后120分钟达到峰值水平。LH和FSH升高持续8 - 10小时。注射5微克LH-RH类似物后的LH峰值水平与注射100微克十肽LH-RH后所见的峰值水平相当。在注射5.0和10.0微克LH-RH类似物后LH和FSH释放后,对睾酮和雌二醇分泌有后期刺激作用。HGH、TSH、催乳素和皮质醇不受LH-RH类似物影响。