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Dose-related target occupancy and effects on circuitry, behavior, and neuroplasticity of the glycine transporter-1 inhibitor, PF-03463275, in healthy and schizophrenia subjects

Biological Psychiatry Feb 01, 2018

D’Souza DC, et al. - Researchers here aimed at studying dose-related target occupancy and effects of the glycine transporter-1 inhibitor, PF-03463275, in healthy and schizophrenia subjects (SZS) to inform optimal dose selection for a clinical trial for cognitive impairments associated with schizophrenia (CIAS). Findings revealed linear dose-related Glycine transporter-1 (GlyT1) occupancy of PF-03463275. PF-03463275 enhanced neuroplasticity in SZs, while it did not show evidence of facilitating NMDA-R function in the ketamine assay. Collectively, the findings gave support for a clinical trial to test the ability of PF-03463275 to enhance CR towards addressing CIAS.
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