D-cycloserine (DCS), (4R)-4-amino-1,2-oxazolidin-3-one, is a partial agonist at the strychnine-insensitive
glycine modulatory site associated with the N-methyl-D-aspartate (NMDA) receptor complex. DCS is also a less efficient ligand of
NMDA receptor function than endogenous full agonists, such as glycine and D-serine.
At high doses, DCS acts as an antagonist by displacing more efficacious endogenous
agonists, but at moderate doses, DCS facilitates glutamatergic neurotransmission via
the NMDA receptor. Recent meta-analysis shows that glycine, D-serine, and sarcosine
(N-methylglycine), an endogenous glycine transporter-1 inhibitor, are more effective
than DCS in improving the overall psychopathology in patients with schizophrenia receiving
antipsychotic drugs (
1
). This suggests a relatively narrow therapeutic window for DCS, most likely due to
its partial agonist properties.To read this article in full you will need to make a payment
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Article info
Publication history
Published online: August 09, 2012
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© 2013 Society of Biological Psychiatry. Published by Elsevier Inc. All rights reserved.