Description
A potent, selective, brain permeable, orally available glycine transporter-1 (GlyT1) inhibitor with IC50 of 92nM (rat GlyT1), 50-fold selectivity over GlyT2; shows minimal affinity for many other receptors except for u-opioid receptors (IC50=1.83uM); inhibits ex vivo [ (3)H]-glycine uptake in mouse cortical homogenate, improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimer's disease. Schizophrenia Phase 1 Discontinued