【摘要】 目的研究新合成的阿片受体配基对稳定表达于CHO细胞的μ阿片受体的结合特性。方法采用细胞生物学和放射性配基结合的方法,以能稳定表达μ阿片受体的CHO细胞为模型,检测阿片受体配基犤3H犦diprenorphine(3H-dip)与μ阿片受体的饱和性结合特征及一系列新合成阿片配基的竞争性结合特征。结果(3H-dip)结合μ阿片受体的平衡解离常数Kd值为1.06nmol/L;受体最大容量Bmax为930fmol/mg蛋白。竞争性结合实验表明3#和12#配基对μ阿片受体的亲和力高于DAMGO和吗啡。2#、6#、8#和9#配基对μ受体的亲和力低于DAMGO和吗啡。结论新配基3#和12#对μ亚型的阿片受体有良好的亲和力。2#、6#、8#和9#配基对μ受体的亲和力较低。更多还原

【Abstract】 Objective To determine the affinity of new opioid receptor ligands to clonedμopioid receptors stably expressed in CHO cell.Methods The binding characteristics of the opioid liganddiprenorphine ( 3 H-dip)were studied by cellular biological techniques and radioligands binding in clonedμopioid 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 diprenorphine bound toμreceptors were1.06nmol/L and930fmol/mg protein,respectively.Competition binding experiments revealed that ligand3 # and12 # displayed much higher affinity than DAMGO and Morphine for the clonedμopioid receptor.However,the affinities of ligands2 # ,6 # ,8 # and9 # were lower than DAMGO and Morphine.Conclusion The present results suggest that the new ligands3 # and12 # have higher affinity toμopioid receptors.However,ligands2 # ,6 # ,8 # and9 # have lower affinity toμopioid receptors.更多还原