CP-802079 is a potent and selective glycine transporter type 1 (GlyT1) antagonist. Antagonists of GlyT1 increase levels of glycine in the synaptic cleft and, like direct glycine site agonists, they can augment NMDAR currents and NMDAR-mediated functions. CP-802,079 significantly increases the amplitude of the NMDAR currents and LTP.
