Arylmethoxypyridines as novel, potent and orally active mGlu5 receptor antagonists

作者：Buttelmann B^*; Peters JU; Ceccarelli S; Kolczewski S; Vieira E; Prinssen EP; Spooren W; Schuler F; Huwyler J; Porter RHP; Jaeschke G

来源：Bioorganic & Medicinal Chemistry Letters, 2006, 16(7): 1892-1897.

DOI：10.1016/j.bmcl.2005.12.088

• mGluR5
• metabotropic glutamate receptor
• anxiolytic
• anxiolysis

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 M PEP binding site, improved microsomal metabolic stability and anxiolytic-like activity in vivo as assessed by the Vogel conflict drinking test.

• 出版日期2006-4-1