879222-14-7Relevant articles and documents
Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists
Buettelmann, Bernd,Peters, Jens-Uwe,Ceccarelli, Simona,Kolczewski, Sabine,Vieira, Eric,Prinssen, Eric P.,Spooren, Will,Schuler, Franz,Huwyler, Joerg,Porter, Richard H. P.,Jaeschke, Georg
, p. 1892 - 1897 (2007/10/03)
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.