[新合成的阿片受体配体与稳定表达于CHO细胞中的克隆μ阿片受体的结合特性]
[Binding characteristics of new synthesized opioid receptor ligands to cloned mu opioid receptors stably expressed in CHO cell].
作者信息
Hu Ping, Ye Cai-ying, Qiu Zhui-bai, Yang Hui-fen, Zhang De-chang
机构信息
Department of Pharmacology, Institute of Basic Medical Sciences, CAMS, PUMC, Beijing 100005, China.
出版信息
Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 2003 Feb;25(1):79-82.
OBJECTIVE
To determine the affinity of new opioid receptor ligands to cloned mu opioid receptors stably expressed in CHO cell.
METHODS
The binding characteristics of the opioid ligand [3H] diprenorphine (3H-dip) were studied by cellular biological techniques and radioligands binding in cloned mu opioid receptors stably expressed in CHO cells in saturation binding experiments, and were followed by competition binding experiments with a variety of new synthesized opioid receptor ligands.
RESULTS
The Kd and Bmax of [3H] diprenorphine bound to mu receptors were 1.06 nmol/L and 930 fmol/mg protein, respectively. Competition binding experiments revealed that ligand 3# and 12# displayed much higher affinity than DAMGO and Morphine for the cloned mu opioid receptor. However, the affinities of ligands 2#, 6#, 8# and 9# were lower than DAMGO and Morphine.
CONCLUSION
The present results suggest that the new ligands 3# and 12# have higher affinity to mu opioid receptors. However, ligands 2#, 6#, 8# and 9# have lower affinity to mu opioid receptors.
目的
确定新型阿片受体配体对稳定表达于CHO细胞中的克隆μ阿片受体的亲和力。
方法
采用细胞生物学技术和放射性配体结合法，在饱和结合实验中研究阿片配体[3H]二丙诺啡（3H - dip）与稳定表达于CHO细胞中的克隆μ阿片受体的结合特性，随后用多种新合成的阿片受体配体进行竞争结合实验。
结果
[3H]二丙诺啡与μ受体结合的Kd和Bmax分别为1.06 nmol/L和930 fmol/mg蛋白。竞争结合实验表明，配体3#和12#对克隆的μ阿片受体的亲和力远高于DAMGO和吗啡。然而，配体2#、6#、8#和9#的亲和力低于DAMGO和吗啡。
结论
目前的结果表明，新配体3#和12#对μ阿片受体具有更高的亲和力。然而，配体2#、6#、8#和9#对μ阿片受体的亲和力较低。
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