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ACS Med Chem Lett. 2012 Nov 12;4(1):46-51. doi: 10.1021/ml300262e. eCollection 2013 Jan 10.

Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.

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CNS Discovery Research, AstraZeneca Pharmaceuticals , 1800 Concord Pike, Wilmington, Delaware 19850-5437, United States.
Argenta , 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, CM19 5TR, United Kingdom.


Herein, we describe the discovery of inhibitors of norepinephrine (NET) and dopamine (DAT) transporters with reduced activity relative to serotonin transporters (SERT). Two compounds, 8b and 21a, 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.


antidepressant; dopamine; norepinephrine; uptake inhibitors

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