Synthesis and dopaminergic activity of heterocyclic analogues of 5,6-dihydroxy-2-aminotetralins
作者:Joan Bosch、Tomàs Roca、Carles G. Pérez、Stefania Montanari
DOI:10.1016/s0960-894x(00)00049-4
日期:2000.3
of 5,6-dihydroxy-2-aminotetralins (6) were synthesized and their in vitro dopaminergic activity was compared to that of (-)-DP-5,6-ADTN and the novel potent agonist Z12571. The results show that changing the cathecol ring for a heterocycle decreases the D1-like activity of the target molecules 6. However, the D2-like activity of tetrahydroquinoline (6j) was comparable to that of (-)-DP-5,6-ADTN.
合成了5,6-二羟基-2-氨基四氢萘的杂环类似物(6),并将其体外多巴胺能活性与(-)-DP-5,6-ADTN和新型强效激动剂Z12571进行了比较。结果表明,改变杂环的导管环会降低目标分子6的D1样活性。但是,四氢喹啉(6j)的D2样活性与(-)-DP-5,6-相当。 ADTN。