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

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

doi:10.1021/ml300262e

Ask about this paper

Answers are grounded in this paper and cite their sources.

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.

Discussion

No takes yet. Share an insight, caveat, or question.

Cite This Study

Brown et al. (2012) studied this question.

synapsesocial.com/papers/6a94e9afcd304312aafa581a https://doi.org/10.1021/ml300262e

View Full Paper

Ask AI

Bookmark

Share

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

Ask about this paper

Abstract

Discussion

Cite This Study

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

Ask about this paper

Abstract

Discussion

Cite This Study

Keep reading

Keep reading