1 research outputs found
Azepines and Piperidines with Dual Norepinephrine Dopamine Uptake Inhibition and Antidepressant Activity
Herein, we describe the discovery
of inhibitors of norepinephrine
(NET) and dopamine (DAT) transporters with reduced activity relative
to serotonin transporters (SERT). Two compounds, <b>8b</b> and <b>21a</b>, along with nomifensine were tested in a rodent receptor
occupancy study and demonstrated dose-dependent displacement of radiolabeled
NET and DAT ligands. These compounds were efficacious in a rat forced
swim assay (model of depression) and also had activity in rat spontaneous
locomotion assay