Title of article :
Synthesis and structure–activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT2A/2C receptor antagonists. Part 1
Author/Authors :
J. Ignacio Andrés، نويسنده , , Jes?s Alc?zar، نويسنده , , José M. Alonso-Meijide، نويسنده , , Adolfo D?az، نويسنده , , Javier Fernandez-Suarez، نويسنده , , M. Pilar Gil، نويسنده , , Laura Iturrino، نويسنده , , Encarna Matesanz، نويسنده , , Theo F. Meert، نويسنده , , Anton Megens، نويسنده , , Victor K. Sipido، نويسنده ,
Abstract :
The synthesis of a series of novel 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives as well as their 5-HT2A/2C and H1 receptor binding affinities are described. The in vivo activity as potential anxiolytics of the synthesised compounds was measured in a mCPP challenge test. One of the compounds, 2a, proved to be a potent 5-HT2A/2C receptor antagonist showing as well oral activity and therefore could be considered as a potential anxiolytic/antidepressant agent.
