Title of article :
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
Author/Authors :
Michael D. Ennis، نويسنده , , Robert L. Hoffman، نويسنده , , Nabil B. Ghazal، نويسنده , , Rebecca M. Olson، نويسنده , , Christopher S. Knauer، نويسنده , , Chris L. Chio، نويسنده , , Deborah K. Hyslop، نويسنده , , Jeffery E. Campbell، نويسنده , , Lawrence W. Fitzgerald، نويسنده , , Nanette F. Nichols، نويسنده , , Kjell A. Svensson، نويسنده , , Robert B. McCall، نويسنده , , Christopher L. Haber، نويسنده , , Michelle L. Kagey، نويسنده , , Dac M. Dinh، نويسنده ,
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.
