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

Neuroreport. 2009 Aug 26;20(13):1193-7. doi: 10.1097/WNR.0b013e32832f5130.

Abstract

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Brain Ischemia / drug therapy
  • Carotid Artery Diseases / drug therapy
  • Cell Death / drug effects
  • Cell Hypoxia / drug effects
  • Female
  • Gerbillinae
  • Glucose / deficiency
  • Hippocampus / drug effects*
  • Hippocampus / physiology
  • In Vitro Techniques
  • Male
  • Neurons / drug effects*
  • Neurons / physiology
  • Neuroprotective Agents / pharmacology*
  • Oligopeptides / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, N-Methyl-D-Aspartate / agonists*
  • Receptors, N-Methyl-D-Aspartate / metabolism
  • Serine / metabolism
  • Stroke / drug therapy
  • Time Factors

Substances

  • NR2B NMDA receptor
  • Neuroprotective Agents
  • Oligopeptides
  • Receptors, N-Methyl-D-Aspartate
  • Serine
  • GLYX-13 peptide
  • Glucose