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

Autor: Eun Kyung Lee, Ralf Roetz, Clara Jeou Jen Lin, Jason Choy, Amy Geraldine Moore, Sandra Steiner, Kerem Erol Ozboya, Yansheng Zhai, Robert James Weikert, Karin Ann Stein, David S. Carter, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Pravin Iyer, Hai-Ying Cai, Saul Jaime-Figueroa, Robert Greenhouse, Lubica Raptova, Ryan Craig Schoenfeld, Linda M. Bannwart, Marzia Villa
Rok vydání: 2008
Předmět:
Zdroj: Bioorganicmedicinal chemistry letters. 18(23)
ISSN: 1464-3405
Popis: 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.
Databáze: OpenAIRE