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内吗啡肽-1及其类似物的合成及与阿片受体结合作用

霍笑风;吴宁;任维华;王锐;陈新滋

  Endomorphin1(EM1) and its six analogs which were designed by rationally replacing the2/3amino acid(Aa) of EM1 were synthesized by using liquid phase peptides synthesis method to study their action of opiate receptor binding(AORB). The order of their affinity intensity for μopiate receptor(MOR)was EM1 >[DAla2]EM1 >[DPro2]EM1 >EM1 >[LTyr3]EM >[LPro3]EM >EMThe sequence of their selectivity for MOR is EM1 >[DPro2]EM1 =[LTyr3]EM >[DAla2]EM1 =[LPro3]EM >EMThe results showed that, comparatively speaking, the 2Aa was more closely related to the selectivity of EM1 while the 3Aa to their affinity, though the different replacement changed the AORB of EM1 dissimilarly.……   
[关键词]:内吗啡肽-1;液相多肽合成;阿片受体结合作用
[文献类型]:期刊
[文献出处]: 《高等学校化学学报2001年07期