Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588015 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
A series of 3-(phenoxy-phenyl-methyl)-pyrrolidine analogues were discovered to be potent and balanced norepinephrine (NE) and serotonin (5-hydroxytryptamine, 5-HT) reuptake inhibitors. Several of these compounds were identified to have suitable in vitro pharmacokinetic properties for an orally dosed and CNS-targeted drug. Compound 39b, in particular, was identified as a potent NET and SERT reuptake inhibitor (NSRI) with minimal off-target activity and demonstrated robust efficacy in the spinal nerve ligation model of pain behavior.
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Authors
Lori Jean Van Orden, Priscilla M. Van Dyke, D. Roland Saito, Timothy J. Church, Ray Chang, Jacqueline A.M. Smith, William J. Martin, Sarah Jaw-Tsai, Eric L. Stangeland,