Three series of bitobic arylpiperazine-phenyl-hexahydropyrazinoquino- lines analogues were designed, synthesizedand evaluated as a novel class of selective ligands for the dopamine D3 receptor. Compounds 15a (K_i of 11.7 ± 1.8 and 373 nM at D3 and D2, respectively), 15c (K_i of 5.49 and 264 nM at D3 and D2, respectively), 15e (K_i of 14.9 and 325 nM at D3 and D2, respectively), 15i (K_i of 13.8 and 401 nM at D3 and D2, respectively) and 15l (K_i of 13.6 and 870 nM at D3 and D2, respectively) were found to demonstrate good binding affinity and selectivity, and especially compound 15c showeda similar binding affinity and selectivity compared with the contrast drug BP897.

设计，合成和评估了三个系列的疏水性芳基哌嗪-苯基-六氢吡嗪并喹啉-类似物，作为多巴胺D3受体的新型选择性配体。化合物15A（ķ_我的11.7±1.8和373 nM的分别在D3和D2，），15C（ķ_我的5.49和264 nM的分别在D3和D2，），15E（ķ_我的14.9和325 nM的在D3和D2 15i（分别在D3和D2处的K _i分别为13.8和401 nM）和15l（K _i分别在D3和D2处的13.6nM和870nM ）被证明表现出良好的结合亲和力和选择性，尤其是化合物15c与对比药物BP897相比显示出相似的结合亲和力和选择性。