ACS Medicinal Chemistry Letters p. 46 - 51 (2013)
Update date:2022-09-26
Topics:
Brown, Dean G.
Bernstein, Peter R.
Wu, Ye
Urbanek, Rebecca A.
Becker, Christopher W.
Throner, Scott R.
Dembofsky, Bruce T.
Steelman, Gary B.
Lazor, Lois A.
Scott, Clay W.
Wood, Michael W.
Wesolowski, Steven S.
Nugiel, David A.
Koch, Stephanie
Yu, Jian
Pivonka, Donald E.
Li, Shuang
Thompson, Carol
Zacco, Anna
Elmore, Charles S.
Schroeder, Patricia
Liu, Jianwei
Hurley, Christopher A.
Ward, Stuart
Hunt, Hazel J.
Williams, Karen
McLaughlin, Joseph
Hoesch, Valerie
Sydserff, Simon
Maier, Donna
Aharony, David
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.
Angelisun(Chongqing) Pharmaceutical Co., LTD.
Contact:+86-23-68030926-816
Address:D1-7 Tech & Entrepreneurs Park, Kecheng Road, Erlang Hi-Tech Areas, Chongqing, China
QINGDAO NEW FLOURISH INTERNATIOANAL TRADE CO., LTD.
Contact:+86 532 80861829
Address:No. 1, Yinchuan East Road, 266061, Qingdao, China
Zhejiang Sanmei Chemical Industry Co., Ltd
Contact:86-579-87633213
Address:Huchu Industrial Zone, Qingnian Rd., Wuyi County, Zhejiang Prov., China.
Jinan Trio PharmaTech Co., Ltd
Contact:86-531-88811783；+(0)13153010282
Address:2766 Yingxiu Road, Jinan High-Tech Zone, China
website:http://www.sagechem.com
Contact:+86-571-86818502
Address:Room C1301, New Youth Plaza, 8 Jia Shan Road, Hangzhou, China
Doi:10.1039/c4ob02602k
(2015)Doi:10.1021/jo302039n
(2012)Doi:10.1021/jm3016393
(2013)Doi:10.1016/j.catcom.2020.106249
(2021)Doi:10.1016/j.cclet.2012.11.007
(2012)Doi:10.1016/j.molstruc.2012.10.033
(2013)
