| C—末端截短δ阿片受体的结合特征 |
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| 引用本文： | 王春河,周德和.C—末端截短δ阿片受体的结合特征[J].中国药理学报,1997,18(4):337-340. |
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| 作者姓名： | 王春河 周德和 |
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| 作者单位： | 中国科学院上海药物研究所 |
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| 摘 要： | 目的：研究δ阿片受体Ｃ－末端在受体结合配体的亲和力及选择性中的作用。方法：在中国苍鼠卵巢细胞（ＣＨＯ细胞）中分别稳定表达Ｃ末端截短３１个氨基酸残基及野生型δ阿片受体，用受体结合分析法研究了表达产物与配体的结合特征，结果：表达得到典型突变受体克隆ＣＨＯ－Ｔ及野生型受体克隆ＣＨＯ－Ｗ，ＣＨＯ－Ｔ结合（＾３Ｈ）ｄｉｐｒｅｎｏｒｐｈｉｎｅ（Ｄｉｐ）及（＾３Ｈ）（Ｄ－Ａｌａ＾２，Ｄ－Ｌｅｕ＾５）ｅｎｋｅｐｈ
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| 关 键 词： | δ阿片受体 阿片 脑啡肽 结合位点 C－末端 |
Binding properties of C-truncated delta opioid receptors. |
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| C H Wang,D H Zhou,J Chen,G E Li,G Pei,Z Q Chi.Binding properties of C-truncated delta opioid receptors.[J].Acta Pharmacologica Sinica,1997,18(4):337-340. |
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| Authors: | C H Wang D H Zhou J Chen G E Li G Pei Z Q Chi |
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| Institution: | Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China. |
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| Abstract: | AIM: To study the role of C-terminal delta opioid receptor involved in ligand binding affinity and selectivity. METHODS: The 31 amino acid residues of C-terminal truncated delta opioid receptors and the wild-type were expressed stably in Chinese hamster ovary (CHO) cells, respectively. Then the ligand binding properties of the products were studied by receptor binding assay. RESULTS: A typical mutated receptor clone CHO-T and a wild-type receptor clone CHO-W were obtained. The Kd values of 3H] diprenorphine (Dip) and 3H]leucine-2-alanine enkephalin (DADLE) bound to CHO-T were similar to CHO-W. Both the specific 3H]Dip bindings of CHO-T and CHO-W were strongly inhibited by delta selective agonists with similar Ki, but neither by mu nor kappa selective agonists. CONCLUSION: The C-terminal of the delta opioid receptor is not involved in the ligands binding affinity and selectivity. |
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