内吗啡肽-1及其类似物的合成及与阿片受体结合作用  

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

作　　者：霍笑风[1] 吴宁[1] 任维华[1] 王锐[2] 陈新滋[2] 

机构地区：[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

出　　处：《高等学校化学学报》2001年第7期1157-1159,共3页Chemical Journal of Chinese Universities

基　　金：国家自然科学基金 (批准号 :2 0 0 72 0 14 );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 -A43-0 87);甘肃省自然科学基金 (批准号 :ZS991-A2 3-0 5 6 Y)

摘　　要：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 Ala 2]EM 1 >[ D Pro 2]EM 1 > EM 1 >[ L Tyr 3]EM >[ L Pro 3]EM >EM The sequence of their selectivity for MOR is  EM 1 >[ D Pro 2]EM 1 =[ L Tyr 3]EM >[ D Ala 2]EM 1 =[ L Pro 3]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 AORB of EM 1 dissimilarly.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 Ala 2]EM 1 >[ D Pro 2]EM 1 > EM 1 >[ L Tyr 3]EM >[ L Pro 3]EM >EM The sequence of their selectivity for MOR is  EM 1 >[ D Pro 2]EM 1 =[ L Tyr 3]EM >[ D Ala 2]EM 1 =[ L Pro 3]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 AORB of EM 1 dissimilarly.

关 键 词：内吗啡肽-1 液相多肽合成 阿片受体 结合作用 构象 亲和性 

分 类 号：R971.1[医药卫生—药品] TQ464.7[医药卫生—药学]