Literature DB >> 22523618

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

Moses G Gichinga1, Jeremy P Olson, Elizabeth Butala, Hernán A Navarro, Brian P Gilmour, S Wayne Mascarella, F Ivy Carroll.   

Abstract

In an effort to discover potent and selective metabotropic glutamate receptor subtype 5 (mGluR5) antagonists, 15 tetrahydropyrimidinone analogues of 1-(3-chlorophenyl)-3-(1-methyl-4-oxo-4,5-dihydro-1H-imidazol-2-yl)-urea (fenobam) were synthesized. These compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro efficacy assay. The IC(50) value for 1-(3-chlorophenyl)-3-(1-methyl-4-oxo-1,4,5,6-tetrahydropyridine)urea (4g) was essentially identical to that of fenobam.

Entities:  

Year:  2011        PMID： 22523618      PMCID： PMC3328804          DOI： 10.1021/ml200162f

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  16 in total

1.  Reinforcing and locomotor stimulant effects of cocaine are absent in mGluR5 null mutant mice.

Authors:  C Chiamulera; M P Epping-Jordan; A Zocchi; C Marcon; C Cottiny; S Tacconi; M Corsi; F Orzi; F Conquet
Journal:  Nat Neurosci       Date:  2001-09       Impact factor: 24.884

2.  Synthesis and receptor assay of aromatic-ethynyl-aromatic derivatives with potent mGluR5 antagonist activity.

Authors:  David Alagille; Ronald M Baldwin; Bryan L Roth; Jarda T Wroblewski; Ewa Grajkowska; Gilles D Tamagnan
Journal:  Bioorg Med Chem       Date:  2005-01-03       Impact factor: 3.641

3.  Cyclohexenyl- and dehydropiperidinyl-alkynyl pyridines as potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.

Authors:  Peter C Chua; Johnny Y Nagasawa; Leo S Bleicher; Benito Munoz; Edwin J Schweiger; Lida Tehrani; Jeffrey J Anderson; Merryl Cramer; Janice Chung; Mitchell D Green; Chris D King; Grace Reyes-Manalo; Nicholas D P Cosford
Journal:  Bioorg Med Chem Lett       Date:  2005-10-15       Impact factor: 2.823

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

Authors:  Georg Jaeschke; 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
Journal:  Bioorg Med Chem Lett       Date:  2006-12-15       Impact factor: 2.823

5.  Metabotropic glutamate 5 receptor antagonism is associated with antidepressant-like effects in mice.

Authors:  Xia Li; Anne B Need; Melvyn Baez; Jeffrey M Witkin
Journal:  J Pharmacol Exp Ther       Date:  2006-06-27       Impact factor: 4.030

6.  Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.

Authors:  Richard H P Porter; Georg Jaeschke; Will Spooren; Theresa M Ballard; Bernd Büttelmann; Sabine Kolczewski; Jens-Uwe Peters; Eric Prinssen; Jürgen Wichmann; Eric Vieira; Andreas Mühlemann; Silvia Gatti; Vincent Mutel; Pari Malherbe
Journal:  J Pharmacol Exp Ther       Date:  2005-07-22       Impact factor: 4.030

Review 7.  Therapeutic implications of the mGluR theory of fragile X mental retardation.

Authors:  M F Bear
Journal:  Genes Brain Behav       Date:  2005-08       Impact factor: 3.449

8.  Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.

Authors:  Simona M Ceccarelli; Georg Jaeschke; Bernd Buettelmann; Jörg Huwyler; Sabine Kolczewski; Jens-Uwe Peters; Eric Prinssen; Richard Porter; Will Spooren; Eric Vieira
Journal:  Bioorg Med Chem Lett       Date:  2006-12-15       Impact factor: 2.823

9.  Potential anxiolytic- and antidepressant-like effects of MPEP, a potent, selective and systemically active mGlu5 receptor antagonist.

Authors:  E Tatarczyńska; A Klodzińska; E Chojnacka-Wójcik; A Palucha; F Gasparini; R Kuhn; A Pilc
Journal:  Br J Pharmacol       Date:  2001-04       Impact factor: 8.739

10.  Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.

Authors:  Yasuyoshi Iso; Ewa Grajkowska; Jarda T Wroblewski; Jared Davis; Nicholas E Goeders; Kenneth M Johnson; Subramaniam Sanker; Bryan L Roth; Werner Tueckmantel; Alan P Kozikowski
Journal:  J Med Chem       Date:  2006-02-09       Impact factor: 7.446
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  1 in total

1.  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
  1 in total

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