학술논문
2,3,4,5-Tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT2C agonists
Document Type
Article
Author
Source
Subject
*TRANQUILIZING drugs
*PSYCHIATRIC drugs
*
Language
ISSN
0960-894X
Abstract
The design and synthesis of the novel 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,7-a]indole 5 is described. This azepinoindole has excellent affinity for 5-HT2C (Ki 4.8 nM) and modest selectivity over 5-HT2A (∼4-fold). Several N- and C11-substituted analogues of 5 were prepared, as were a number of biaryl indoline derivatives. The anxiolytic potential for the azepinoindole template 5 is demonstrated by activity in a mouse shock–aggression assay. [Copyright &y& Elsevier]