Non-competitive inhibitors of metabotropic glutamate receptor 5 (mGluR5)

Based on a pharmacophore alignment on known non-competitive mGluR5 inhibitors applying 4SCan® technology, a new lead series was identified and further structurally investigated. Ki’s as low as around 100 nM were achieved.

Synthesis and SAR studies of non-competitive mGluR5 antagonists are described.Figure optionsDownload as PowerPoint slide