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PF-03463275 is a centrally penetrant, orally available small molecule that acts as a selective and competitive inhibitor of glycine transporter 1 (GlyT1), also known as solute carrier family 6 member 9 (SLC6A9). By inhibiting GlyT1, it increases extracellular glycine levels in the synaptic cleft and is hypothesized to potentiate N-methyl-D-aspartate receptor (NMDAR) transmission through coagonist stimulation. This mechanism was investigated for its potential to treat cognitive impairments associated with schizophrenia. The drug demonstrated improvement in working memory accuracy in patients with schizophrenia but did not show significant benefit for cognitive impairment when combined with cognitive training compared to placebo. Clinical development reached phase II trials before being discontinued. The drug was developed by Pfizer[1][2][3][4][5][6][7].
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