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Eur J Med Chem. 2003 Jul-Aug;38(7-8):661-70.

Antagonists and agonists at the glycine site of the NMDA receptor for therapeutic interventions.

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Department of Medicinal and Pharmaceutical Chemistry, Institute of Pharmacy, Johannes Gutenberg-University of Mainz, Staudinger Weg 5, 55099, Mainz, Germany.


For decades neuroreceptor research has focused on the development of NMDA glycine-site antagonists, after Johnson and Ascher found out in 1987 about the co-agonistic character of this achiral amino acid at the NMDA receptor. Contrary to the inhibitory glycine receptor (glycine(A)) the glycine binding site on the NMDA receptor (glycine(B)) is strychnine-insensitive. A great diversity of diseases showing a disturbed glutamate neurotransmission have been linked to the NMDA receptor. Glycine site antagonists have been investigated for acute diseases like stroke and head trauma as well as chronic ones like dementia and chronic pain.

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