Neuroprotection by a novel NMDAR functional glycine site partial agonist, GLYX-13.

Stanton PK, Potter PE, Aguilar J, Decandia M, Moskal JR
Neuroreport. 2009 20 (13): 1193-7

PMID: 19623090 · DOI:10.1097/WNR.0b013e32832f5130

GLYX-13 (threonine-proline-proline-threonine-amide) is an amidated di-pyrrolidine that acts as a functional partial agonist at the glycine site on N-methyl-D-aspartate glutamate receptors (NMDARs). GLYX-13 can both increase NMDAR conductance at NR2B-containing receptors, and reduce conductance of non-NR2B-containing receptors. Here, we report that GLYX-13 potently reduces delayed (24 h) death of CA1 pyramidal neurons produced by bilateral carotid occlusion in Mongolian gerbils, when administered up to 5 h post-ischemia. GLYX-13 also reduced delayed (24 h) neuronal death of CA1, CA3, and dentate gyrus principal neurons elicited by oxygen/glucose deprivation in in-vitro hippocampal organotypic slice cultures, when applied up to 2 h post-oxygen/glucose deprivation. The glycine site full agonist D-serine completely occluded neuroprotection, indicating that GLYX-13 acts by modulating activation of this site.

MeSH Terms (20)

Animals Brain Ischemia Carotid Artery Diseases Cell Death Cell Hypoxia Female Gerbillinae Glucose Hippocampus In Vitro Techniques Male Neurons Neuroprotective Agents Oligopeptides Rats Rats, Sprague-Dawley Receptors, N-Methyl-D-Aspartate Serine Stroke Time Factors

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