Azepines and Piperidines with Dual Norepinephrine Dopamine Uptake Inhibition and Antidepressant Activity
ACS Medicinal Chemistry Letters2012Vol. 4(1), pp. 46–51
Citations Over Time
Dean G. Brown, Peter R Bernstein, Ye Wu, Rebecca A. Urbanek, Christopher W. Becker, Scott Throner, Bruce T. Dembofsky, Gary B. Steelman, Lois Ann Lazor, Clay W. Scott, Michael W. Wood, Steven S. Wesolowski, David A. Nugiel, Stephanie C. Koch, Jian Yu, Donald E. Pivonka, Shuang Li, Carol Thompson, Anna Zacco, Charles S. Elmore, Patricia Schroeder, Jianwei Liu, Christopher A. Hurley, Stuart I. Ward, Hazel Hunt, Karen Williams, Joseph K. McLaughlin, Valerie Hoesch, S G Sydserff, Donna L. Maier, David Aharony
Abstract
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.
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