四种促黄体生成激素释放激素类似物的体内抑制活性。

Inhibitory activity of four analogs of luteinizing hormone-releasing hormone in vivo.

作者信息

Ferland L, Labrie F, Coy D H, Coy E J, Schally A V

出版信息

Fertil Steril. 1975 Sep;26(9):889-93. doi: 10.1016/s0015-0282(16)41353-1.

Abstract

Four analogs of luteinizing hormone-releasing hormone (LH-RH), [des-His2,D-Ala6]-LH-RH, [des-His2,D-Ala6, des-Gly-NH2(10)1-LH-RH ethylamide, [des-His2,D-Leu6]-LH-RH, and [D-Phe2,D-Leu6]-LH-RH, at 300-fold molar ratios (analog/LH-RH) led to an almost complete inhibition of LH response to LH-RH in anesthetized 4-day cycling rats on the afternoon of proestrus. At a 75-fold molar ratio, [des-His2,D-Ala6]-LH-RH still inhibited the LH-RH-induced LH release by 50%. The ethylamide substitution at the COOH terminus of [des-His2,D-Ala6]-LH-RH did not significantly improve the inhibitory activity of the molecule.

摘要

四种促黄体生成激素释放激素（LH-RH）类似物，即[去组氨酸2，D-丙氨酸6]-LH-RH、[去组氨酸2，D-丙氨酸6，去甘氨酰胺（10）1]-LH-RH乙酰胺、[去组氨酸2，D-亮氨酸6]-LH-RH和[D-苯丙氨酸2，D-亮氨酸6]-LH-RH，以300倍摩尔比（类似物/LH-RH）在动情前期下午对麻醉的4日龄周期大鼠，几乎完全抑制了LH对LH-RH的反应。在75倍摩尔比时，[去组氨酸2，D-丙氨酸6]-LH-RH仍能抑制LH-RH诱导的LH释放达50%。[去组氨酸2，D-丙氨酸6]-LH-RH羧基末端的乙酰胺取代并未显著提高该分子的抑制活性。