2. Academic Validation
  3. N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors

N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors

  • Bioorg Med Chem Lett. 2007 Apr 1;17(7):2022-5. doi: 10.1016/j.bmcl.2007.01.020.
Paul V Fish 1,  M Jonathan Fray,  Alan Stobie,  Florian Wakenhut,  Gavin A Whitlock
Affiliations

Affiliation

  • 1 Sandwich Chemistry Department, Pfizer Global Research and Development, Sandwich Labs, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
PMID: 17267217 DOI: 10.1016/j.bmcl.2007.01.020
Abstract

A series of N-benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amine monoamine reuptake inhibitors are described. Selective dual 5-HT and NA reuptake inhibition was achieved, and analogues with weak CYP2D6 inhibition, good human in vitro metabolic stability and wide ligand selectivity, such as 12b, were identified.

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