促黄体生成素释放激素（LH-RH）1位类似物的合成与生物活性

Synthesis and biological activity of position 1 analogs of LH-RH.

作者信息

Nikolics K, Coy D H, Vilchez-Martinez J A, Coy D J, Schally A V

出版信息

Int J Pept Protein Res. 1977 Jan;9(1):57-62. doi: 10.1111/j.1399-3011.1977.tb01837.x.

DOI:10.1111/j.1399-3011.1977.tb01837.x

PMID:320124

Abstract

(Formyl-sarcosine)1-LH-RH (I), (acetyl-sarcosine)1-LH-RH (II), (2-pyrrolidone-4-carboxylic acid)1-LH-RH (III), (N-methyl-2-pyrrolidone-4-carboxylic acid)1-LH-RH (IV, hydroxyproline1-LH-RH (V) and (cylcopentane-carboxylic acid)1-LH-RH (VI) were synthesized by solid phase methods on a benzhydrylamine resin support. Peptides I-IV were assayed for LH- and FSH-releasing activity over a 4-h period after subcutaneous infection into immature male rats in order to detect any prolongation ofactivity. The peptides were found to have the following integrated LH-releasing activities compared with LH-RH: I, 64%; II, 72%; III, 19%; IV, 58%. None of the peptides were found to be longer acting than LH-RH. Peptides V and VI were far less active, 0.001% and 1.4%, respectively.

摘要

（甲酰基 - 肌氨酸）1 - 促黄体激素释放激素（I）、（乙酰基 - 肌氨酸）1 - 促黄体激素释放激素（II）、（2 - 吡咯烷酮 - 4 - 羧酸）1 - 促黄体激素释放激素（III）、（N - 甲基 - 2 - 吡咯烷酮 - 4 - 羧酸）1 - 促黄体激素释放激素（IV）、羟脯氨酸1 - 促黄体激素释放激素（V）和（环戊烷 - 羧酸）1 - 促黄体激素释放激素（VI）通过在二苯甲基胺树脂载体上的固相方法合成。将肽I - IV皮下注射到未成熟雄性大鼠体内后，在4小时内测定其促黄体生成素和促卵泡生成素释放活性，以检测活性是否有任何延长。与促黄体激素释放激素相比，发现这些肽具有以下促黄体生成素释放综合活性：I为64%；II为72%；III为19%；IV为58%。未发现任何一种肽的作用时间比促黄体激素释放激素长。肽V和VI的活性远低于促黄体激素释放激素，分别为0.001%和1.4%。