Glutamate is essential for a proper synaptic communication in the central nervous system. Dysfunction of the glutamatergic excitatory neurotransmission seems to be implicated in psychiatric disorders. A growing body of evidence suggests that activation of the glutamatergic system, particularly N-methyl-D-aspartate (NMDA) receptor function, may represent a viable approach for the treatment of schizophrenia. The use of direct NMDA receptor agonists is limited due to the associated excitotoxicity, whereas the glycine modulatory site of the NMDA receptor has become an attractive target. The increase of the co-agonist glycine at the glycine modulatory site is one approach to enhance NMDA receptor function. Increased synaptic glycine levels can be achieved through inhibition of glycine reuptake from the synapse via glycine transporter type 1 (GlyT1). Several novel GlyT1 inhibitors have entered or are entering clinical studies the results of which will provide critical information about the validity of this approach to treat schizophrenia.

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