高等学校化学学报

高等学校化学学报 ›› 2001, Vol. 22 ›› Issue (7): 1157.

• 研究简报 • 上一篇    下一篇

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1, 吴宁1, 任维华1, 王锐1, 陈新滋2   

  1. 1. 兰州大学生命科学学院, 兰州 730000;
    2. 香港理工大学应用生物及化学科技系, 香港
  • 收稿日期:2000-06-27 出版日期:2001-07-24 发布日期:2001-07-24
  • 通讯作者: 王　锐(1963年出生),男,博士,教授,博士生导师,从事多肽生物化学与不对称合成研究.E-mail:wangrui@lzu.edu.cn E-mail:wangrui@lzu.edu.cn
  • 基金资助:

    国家自然科学基金(批准号:20072014);高等学校优秀青年教师教学科研奖励计划;甘肃省科技攻关项目基金(批准号:GS992-A43-087);甘肃省自然科学基金(批准号:ZS991-A23-056Y)

Synthesis and Action of Opiate Receptor Binding of Endomorphin-1 and Their Analogs

HUO Xiao-Feng1, WU Ning1, REN Wei-Hua1, WANG Rui1, Chen-Xin-Zi2   

  1. 1. School of Life Science, Lanzhou University, Lanzhou 730000, China;
    2. Department of Applied Biology and Chemical Technology, Hong Kong Polytechnic University, Hong Kong, China
  • Received:2000-06-27 Online:2001-07-24 Published:2001-07-24

PDF (PC)

被引次数

9

关键词: 内吗啡肽-1, 液相多肽合成, 阿片受体结合作用

Abstract: Endomorphin-1(EM-1) and its six analogs which were designed by rationally replacing the 2-/3-amino acid(Aa) of EM-1 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 μ opiate receptor(MOR) was  EM-1 >[ D-Ala2]EM-1 >[ D-Pro2]EM-1 > EM-1 >[ L-Tyr3]EM >[ L-Pro 3]EM >EM The sequence of their selectivity for MORis  EM-1 >[ D-Pro2]EM-1 =[ L-Tyr3]EM >[ D-Ala2]EM-1 =[ L-Pro3]EM >EM The results showed that, comparatively speaking, the 2-Aa was more closely related to the selectivity of EM-1 while the 3-Aa to their affinity, though the different replacement changed the AORBof EM-1 dissimilarly.

Key words: Endomorphin-1, Liquid phase peptides synthesis, Action of opiate receptor binding

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