130798-51-5

NMDA receptors are neuroreceptors that have binding sites for glycine or D-serine as well as L-glutamate. MDL 29951 is an antagonist of NMDA receptors with high affinity for the glycine binding site (K_i = 140 nM). It is functional both in vitro and in vivo. MDL 29951 blocks NMDA receptor-dependent convulsions in audiogenic seizure-susceptible DBA/2J mice. It is used to evaluate the role of the glycine site of the NMDA receptor in neurological signaling. MDL 29951 is also an agonist of the G protein-coupled receptor GPR17 (EC₅₀ values range from 7 nM to 6 μM, depending on the assay). GPR17 is thought to be involved in oligodendrocyte differentiation and myelin formation/repair.

MDL 29951 is an allosteric inhibitor of the enzyme fructose 1,6-bisphosphatase.

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1) Hennen?et al. (2013),?Decoding Signaling and Function of the Orphan Protein-Coupled Receptor GPR17 with a small molecule agonist; Sci. Signal.,?6?ra93 2) Salituro?et al. (1992)?3-(2-Carboxyindol-3-yl)propionic Acid-Based Antagonists of the N-Methyl-D-aspartic Acid Receptor Associated Glycine Binding Site; J. Med. Chem.,?35?1791