Azepines and Piperidines
with Dual Norepinephrine
Dopamine Uptake Inhibition and Antidepressant Activity

Anna Zacco (2004736); Bruce
T. Dembofsky (2004721); Carol Thompson (91831); Charles S. Elmore (2004724); Christopher A. Hurley (2004694); Christopher W. Becker (2004733); Clay W. Scott (1965760); David A. Nugiel (2004742); David Aharony (2004727); Dean G. Brown (1261668); Donald E. Pivonka (2004730); Donna Maier (2004715); Gary B. Steelman (2004709); Hazel
J. Hunt (2004703); Jian Yu (141239); JianWei Liu (2004712); Joseph McLaughlin (2004706); Karen Williams (771874); Lois A. Lazor (1845391); Michael W. Wood (2004718); Patricia Schroeder (647768); Peter R. Bernstein (2004739); Rebecca A. Urbanek (2004700); Scott R. Throner (1408840); Shuang Li (146392); Simon Sydserff (1845400); Stephanie Koch (2004697); Steven S. Wesolowski (1408843); Stuart Ward (2004688); Valerie Hoesch (2004691); Ye Wu (171928)

Azepines and Piperidines with Dual Norepinephrine Dopamine Uptake Inhibition and Antidepressant Activity

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, <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

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Last time updated on 16/03/2018