8-[4-[2-(1,2,3,4-tetrahydroisoquinolinyl)]butyl]-8-azaspiro[4,5]decane-7,9-dione: A new 5-HT1A receptor ligand with the same activity profile as buspirone

被引:38
作者
Mokrosz, JL [1 ]
DerenWesolek, A [1 ]
Tatarczynska, E [1 ]
Duszynska, B [1 ]
Bojarski, AJ [1 ]
Mokrosz, MJ [1 ]
ChojnackaWojcik, E [1 ]
机构
[1] POLISH ACAD SCI,INST PHARMACOL,DEPT NEW DRUGS,PL-31343 KRAKOW,POLAND
关键词
D O I
10.1021/jm950662c
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new analog of buspirone (1), i.e., 8-[4-[2-(1,2,3,4-tetrahydroisoquinolinyl)]butyl]8-azaspiro[4.5] decane-7,9-dione (6a), was synthesized. In was demonstrated that buspirone and its analog 6a were equipotent 5-HT1A ligands. Several behavioral models showed that 6a had essentially the same functional profile at 5-HT1A receptors as buspirone. The obtained results permit a conclusion that the basic nitrogen atom and terminal, bulky cycloimide moiety, but not the 2-pyrimidinyl group, of buspirone are directly involved in the formation of the bioactive complex with 5-HT1A receptors.
引用
收藏
页码:1125 / 1129
页数:5
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