Herein, we report the discovery of a new, orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 (mGlu<sub>7</sub>) negative allosteric modulator (NAM) that achieves exposure in cerebral spinal fluid (CSF) 2.5× above the in vitro IC<sub>50</sub> at minimum effective doses (MEDs) of 3 mg/kg in preclinical anxiety models.