Literature DB >> 18954985

Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.

Linda M Bannwart1, David S Carter, Hai-Ying Cai, Jason C Choy, Robert Greenhouse, Saul Jaime-Figueroa, Pravin S Iyer, Clara J Lin, Eun Kyung Lee, Matthew C Lucas, Stephen M Lynch, Ann Marie Madera, Amy Moore, Kerem Ozboya, Lubica Raptova, Ralf Roetz, Ryan C Schoenfeld, Karin Ann Stein, Sandra Steiner, Marzia Villa, Robert J Weikert, Yansheng Zhai.   

Abstract

A series of 3,3-disubstituted pyrrolidine monoamine triple reuptake inhibitors were discovered. Analogues with low nanomolar potency, good human in vitro microsomal stability and in vitro permeability, and low drug-drug interaction potential are described. One example showed in vivo anti-depressant-like effects in the mouse tail suspension assay with a minimum effective dose of 30 mg/kg i.p.

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Year:  2008        PMID: 18954985     DOI: 10.1016/j.bmcl.2008.10.025

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Emerging targets for antidepressant therapies.

Authors:  Jeffrey J Rakofsky; Paul E Holtzheimer; Charles B Nemeroff
Journal:  Curr Opin Chem Biol       Date:  2009-06-06       Impact factor: 8.822

2.  Antidepressant potential of nitrogen-containing heterocyclic moieties: An updated review.

Authors:  Nadeem Siddiqui; Sandhya Bawa; Ruhi Ali; Obaid Afzal; M Jawaid Akhtar; Bishmillah Azad; Rajiv Kumar
Journal:  J Pharm Bioallied Sci       Date:  2011-04

3.  A perspective on multi-target drug discovery and design for complex diseases.

Authors:  Rona R Ramsay; Marija R Popovic-Nikolic; Katarina Nikolic; Elisa Uliassi; Maria Laura Bolognesi
Journal:  Clin Transl Med       Date:  2018-01-17
  3 in total

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