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 ,
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
