Title of article
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists
Author/Authors
Bernd Büttelmann، نويسنده , , Jens-Uwe Peters، نويسنده , , Simona Ceccarelli، نويسنده , , Sabine Kolczewski، نويسنده , , Eric Vieira، نويسنده , , Eric P. Prinssen، نويسنده , , Will Spooren، نويسنده , , Franz Schuler، نويسنده , , J?rg Huwyler، نويسنده , , Richard H.P. Porter، نويسنده , , Georg Jaeschke، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
6
From page
1892
To page
1897
Abstract
Optimisation of affinity, chemical stability, metabolic stability and solubility led from a chemically labile HTS hit 1 to mGlu5 receptor antagonists (24–26) with high affinity for the allosteric MPEP binding site, improved microsomal metabolic stability and anxiolytic-like activity in vivo as assessed by the Vogel conflict drinking test.
Keywords
Metabotropic Glutamate Receptor , Anxiolysis , mGluR5 , Anxiolytic
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796686
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