Novel 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives displaying combined norepinephrine reuptake inhibition and 5-HT2A/2C receptor antagonism

A novel series of cis-fused 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives modified at position C-11 was prepared and evaluated for its potential antidepressant/anxiolytic properties. In vitro affinities for the norepinephrine transporter and for 5-HT2A and 5-HT2C receptors, as well as the ED50 values obtained in some in vivo assays predictive for antidepressant and anxiolytic potential are reported.

Graphical abstractA novel series of cis-fused tetrahydrofuran derivatives modified at position C-11 was prepared and evaluated for its potential antidepressant/anxiolytic properties. In vitro affinities for the norepinephrine transporter and for 5-HT2A and 5-HT2C receptors, as well as the ED50 values obtained in some in vivo assays predictive for antidepressant and anxiolytic potential are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide