LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms). It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications. LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor. LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.