3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu 5: Identification of easily prepared tool compounds with CNS exposure in rats

Andrew S. Felts, Stacey R. Lindsley, Jeffrey P. Lamb, Alice L. Rodriguez, Usha N. Menon, Satyawan Jadhav, Carrie K. Jones, P. Jeffrey Conn, Craig W. Lindsley, Kyle Allen Emmitte

Research output: Contribution to journalArticle

18 Scopus citations

Abstract

Development of SAR in a 3-cyano-5-fluoro-N-arylbenzamide series of non-competitive antagonists of mGlu 5 using a functional cell-based assay is described in this Letter. Further characterization of selected potent compounds in in vitro assays designed to measure their metabolic stability and protein binding is also presented. Subsequent evaluation of two new compounds in pharmacokinetic studies using intraperitoneal dosing in rats demonstrated good exposure in both plasma and brain samples.

Original languageEnglish
Pages (from-to)4390-4394
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number15
DOIs
StatePublished - 1 Aug 2010

Keywords

  • Addiction
  • Allosteric modulator
  • CNS
  • Fragile X syndrome
  • GERD
  • GPCR
  • PD-LID
  • mGlu5

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