Potent and selective mGlu2 negative allosteric modulator (IC50 = 78 nM). Exhibits > 350-fold selectivity for mGlu2 over mGlu3. Also exhibits selectivity over other mGluRs and a panel of GPCRs, ion channels and transporters. CNS penetrant.
Bollinger et al (2017) Design and synthesis of mGlu2 NAMs with improved potency and CNS penetration based on a truncated picolinamide core. ACS Med.Chem.Lett. 8 919 PMID:28947937
















