δ阿片受体研究新进展  

Recent progress on the study of δ poioid receptor

作　　者：金昔陆[1,2] 周德和[1,2] 池志强[1,2] 

机构地区：[1]上海医科大学药学院药理学教研室 [2]中国科学院上海药物研究所

出　　处：《中国药理学通报》1999年第1期1-4,共4页Chinese Pharmacological Bulletin

摘　　要：目的综述δ阿片受体研究进展。方法应用功能表达、受体结合、基因定位突变、构建嵌合受体等方法。结果和结论克隆出δ阿片受体，为３７２个氨基酸，属Ｇ蛋白耦联受体，存在７次跨膜结构。δ阿片受体中的天门冬氨酸９５（Ａｓｐ９５）残基和Ａｓｐ１２８残基处于受体结合位点的关键区域。δ阿片受体中的赖氨酸（Ｌｙｓ１０８）残基阻止ＤＡＭＧＯ与δ受体的结合；δ阿片受体的第３个细胞外环决定了δ受体激动剂对δ受体的选择性。δ受体第４跨膜域中的丝氨酸（Ｓｅｒ１７７）被突变可使经典拮抗剂呈现激动剂的性质。AIM To review the latest progress on the research of δ opioid receptor. METHODS Adopt some methods such as functional expression, receptor binding assay, site directed mutagenesis,chimera receptor.RESULTS and CONCLUTION Scientists have cloned δ opioid receptor and confirmed that δ opioid receptor sequences posses 372 amino acids with seven putative transmembrane domains and belong to the superfamily of G protein coupled receptors. The aspartate (Asp 95 and Asp 128 ) residue of δ opioid receptor lie in the critical area of the receptor binding site. The Lys 108 residue of δ opioid receptor prevents DAMGO from binding to δ opioid receptor. The third extracellular loop of δ opioid receptor determines the selectivity of δ opioid agonists. The mutation of a serine (Ser 177 ) in transmembrane 4 of δ opioid receptor confers full agonistic properties to classical antagonists.

关 键 词：阿片受体 δ阿片受体基因 受体结构 研究 功能 

分 类 号：R971.2[医药卫生—药品] R966[医药卫生—药学]