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我们曾经报告,相对分子质量2 ku、5 ku直链甲氧基聚乙二醇(mP EG)修饰的脑啡肽(Tyr-Gly-Gly-Phe-Met,ENK)半衰期延长、清除率下降、镇痛药效增强[1]。在此基础上,本文对D-Ala替换ENK第2、5位氨基酸([D-Ala~2,D-Ala~5]-ENK,DADAE)、及其5 ku分子质量mP EG修饰双重结构改造的合成脑啡肽类似物进行了镇痛药效分析。
We have reported that the half-life of enkephalin (Tyr-Gly-Gly-Phe-Met, ENK) modified by 5 ku linear molecular weight polyethylene glycol (mPEG) Analgesic efficacy increased [1]. On this basis, the D-Ala double-stranded structure modification of amino acids 2 and 5 of ENK ([D-Ala ~ 2, D-Ala ~ 5] -ENK, DADAE) and its 5 ku molecular mass mP EG Analgesic efficacy analysis of synthetic enkephalin analogues.