Dopamine D3 receptor antagonists. 1. Synthesis and structure-activity relationships of 5, 6-dimethoxy-N-alkyl-and N-alkylaryl-substituted 2-aminoindans

SR Haadsma-Svensson, KA Cleek…

文献索引：Haadsma-Svensson; Cleek; Dinh; Duncan; Haber; Huff; Lajiness; Nichols; Smith; Svensson; Zaya; Carlsson; Lin Journal of Medicinal Chemistry, 2001 , vol. 44, # 26 p. 4716 - 4732

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被引用次数: 39

摘要

5, 6-Dimethoxy-2-(N-dipropyl)-aminoindan (3, PNU-99194A) was found to be a selective dopamine D3 receptor antagonist with potential antipsychotic properties in animal models. To investigate the effects of nitrogen substitution on structure-activity relationships, a series of 5, 6-dimethoxy-N-alkyl-and N-alkylaryl-substituted 2-aminoindans were synthesized and evaluated in vitro for binding affinity and metabolic stability. The results indicate that ...