论文部分内容阅读
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ＣＨＯＴ及野生型受体克隆ＣＨＯＷ．ＣＨＯＴ结合［３Ｈ］ｄｉｐｒｅｎｏｒｐｈｉｎｅ（Ｄｉｐ）及［３Ｈ］［ＤＡｌａ２，ＤＬｅｕ５］ｅｎｋｅｐｈａｌｉｎ（ＤＡＤＬＥ）的Ｋｄ值与ＣＨＯＷ一致，δ选择性激动剂对二者与［３Ｈ］Ｄｉｐ的结合均有很强的抑制作用，且Ｋｉ相似；而μ及κ选择性激动剂则对二者均无抑制作用．结论：δ阿片受体的Ｃ末端与受体结合配体的亲和力及选择性无关．
OBJECTIVE: To investigate the role of C-terminal δ opioid receptors in the affinity and selectivity of receptor-binding ligands. Methods: C - terminal truncated 31 amino acid residues and wild type δ opioid receptor were stably expressed in Chinese ovary cells (CHO cells). The binding characteristics of the expressed product and ligand were studied by receptor binding assay. Results: The expression of typical mutant receptor cloned CHO T and wild-type receptor clone CHO W. CHO-T binding [3H] diprenorphine (Dip) and [3H] [D Ala2, D Leu5] enkephalin (DADLE) Kd values consistent with CHO W, δ selective agonists on both and the [3H ] Dip all have a strong inhibitory effect, and the Ki is similar; and μ and κ selective agonists have no inhibitory effect on both. CONCLUSION: The C-terminal of δ-opioid receptor has no relation with the affinity and selectivity of receptor-binding ligand.