Investigation of the relationship between opioid kappa receptor subtype and receptor dimerization

在构建kappa激动剂三维药效团模型的基础上，我们合成了结合模式为1、3、4的化合物，并评估了它们对阿片受体的结合亲和力和激动活性。这些化合物对kappa受体表现出选择性结合能力和拮抗活性，但结合强度和活性取决于其结构。化合物的结合模式未观察到影响用于功能分析的CellKey SystemTM检测到的阻抗模式。

On the basis of our 3D pharmacophore model of kappa agonists, compounds belonging to the binding mode 1, 3, or 4 were synthesized and their binding affinities and agonistic activities for the opioid receptors were evaluated. The test compounds showed selective binding abilities and agonistic activities for the kappa receptor although the strengths of bindings and activities depended on the structures. The binding modes of the compounds were not observed to affect the impedance patterns detected by CellKey SystemTM which was used in the functional assays.