Literature DB >> 17196387

Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.

Georg Jaeschke1, Richard Porter, Bernd Büttelmann, Simona M Ceccarelli, Wolfgang Guba, Bernd Kuhn, Sabine Kolczewski, Jörg Huwyler, Vincent Mutel, Jens-Uwe Peters, Theresa Ballard, Eric Prinssen, Eric Vieira, Jürgen Wichmann, Will Spooren.   

Abstract

Optimization of affinity and microsomal stability led to identification of the potent, metabolically stable fenobam analog 4l. Robust in vivo efficacy of 4l was demonstrated in four different models of anxiety. Additionally, a ligand based pharmacophore alignment of fenobam and MPEP is proposed.

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Year:  2006        PMID: 17196387     DOI: 10.1016/j.bmcl.2006.12.033

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Attenuation of reinstatement of methamphetamine-, sucrose-, and food-seeking behavior in rats by fenobam, a metabotropic glutamate receptor 5 negative allosteric modulator.

Authors:  Lucas R Watterson; Peter R Kufahl; Natali E Nemirovsky; Kaveish Sewalia; Lauren E Hood; M Foster Olive
Journal:  Psychopharmacology (Berl)       Date:  2012-07-21       Impact factor: 4.530

2.  Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam().

Authors:  Moses G Gichinga; Jeremy P Olson; Elizabeth Butala; Hernán A Navarro; Brian P Gilmour; S Wayne Mascarella; F Ivy Carroll
Journal:  ACS Med Chem Lett       Date:  2011-10-05       Impact factor: 4.345

3.  Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships.

Authors:  Karen J Gregory; Meredith J Noetzel; Jerri M Rook; Paige N Vinson; Shaun R Stauffer; Alice L Rodriguez; Kyle A Emmitte; Ya Zhou; Aspen C Chun; Andrew S Felts; Brian A Chauder; Craig W Lindsley; Colleen M Niswender; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2012-08-03       Impact factor: 4.436

  3 in total

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