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

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

  • Bioorg Med Chem Lett. 2008 Dec 1;18(23):6062-6. doi: 10.1016/j.bmcl.2008.10.025.
Linda M Bannwart 1,  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
Affiliations

Affiliation

  • 1 Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA.
PMID: 18954985 DOI: 10.1016/j.bmcl.2008.10.025
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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