The present invention provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced β-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.
本发明提供了具有减弱 D1R 脱敏作用的 D1 激动剂、相对于
多巴胺具有减弱的 β-
阿司匹林招募活性的 D1 激动剂、与 D1R 结合时与 D1R 的 Ser188 有明显相互作用但与 Ser202 的相互作用不明显的 D1 激动剂、与 D1R 结合时与 D1R 的 Asp103 的相互作用较弱且与 Ser198 的相互作用较弱的 D1 激动剂及其用途。