Positron Emission Tomography (PET) Imaging of Metabotropic Glutamate Receptor Subtype 2 (mGlu2) Based on a Negative Allosteric Modulator Radioligand

Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator

“…In addition to a number of publications from other institutions on their efforts − toward identifying selective mGluR2 inhibitors, our company recently published an approach to identification of selective mGluR2 NAMs, which led to the discovery of a 4-arylquinoline-2-carboxamide series. A high throughput screen identified compound 1 (Figure ); initial SAR studies demonstrated that C2-carboxamide was required for potency, the C4 vector preferred lipophilic groups, and C7 tolerated polar groups.…”