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

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

  • Bioorg Med Chem Lett. 2010 Aug 1;20(15):4390-4. doi: 10.1016/j.bmcl.2010.06.064.
Andrew S Felts 1,  Stacey R Lindsley,  Jeffrey P Lamb,  Alice L Rodriguez,  Usha N Menon,  Satyawan Jadhav,  Carrie K Jones,  P Jeffrey Conn,  Craig W Lindsley,  Kyle A Emmitte
Affiliations

Affiliation

  • 1 Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
PMID: 20598884 DOI: 10.1016/j.bmcl.2010.06.064
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.

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