Potent and selective glycine transporter 1 (GlyT1) inhibitor (IC50
values are 15.8 and > 30 000 nM at GlyT1 and GlyT2 respectively). Induces a dose-dependent elevation in CSF levels of glycine, and enhances acetylcholine and dopamine release in the striatum and prefrontal cortex respectively. Produces profound locomotor and respiratory impairments at higher doses.
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Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs cortical brain areas.
Perry et al.