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MDL-29951 is an experimental small molecule that acts as a potent and selective antagonist at the glycine site of the N-methyl-D-aspartate (NMDA) receptor, with a Ki of approximately 0.14 μM for [3H]glycine binding in vitro and in vivo[2][3][5]. It displays over 2000-fold selectivity for the glycine binding site relative to glutamate recognition sites on NMDA receptors[5]. In addition to its NMDA receptor antagonism, MDL‑29951 functions as an agonist at G protein-coupled receptor GPR17 and inhibits fructose‑1,6‑bisphosphatase (FBPase), with varying potency across species[7][5]. The compound has demonstrated neuromodulatory, anticonvulsant, and antinociceptive activities in preclinical models. It has been investigated primarily for research purposes related to neuroprotection and myelin repair (e.g., multiple sclerosis), but it is not approved for clinical use[7][9].
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