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The treatment of schizophrenia has long been dominated by aminergic receptor antagonist-based therapeutics largely founded on the dopamine hypothesis of schizophrenia. More recently the glutamatergic theory has come to the fore which may potentially address some of the deficiencies of current therapies. While there are many approaches to manipulating the glutamatergic system, the most advanced approach is to increase synaptic concentrations of the NMDA receptor co-agonist glycine via inhibition of the glycine transporter 1 (GlyT-1).