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

@article{Stanton2009NeuroprotectionBA,
  title={Neuroprotection by a novel NMDAR functional glycine site partial agonist, GLYX-13},
  author={Patric K. Stanton and Pamela E. Potter and J Aguilar and Maria Decandia and Joseph r. Moskal},
  journal={NeuroReport},
  year={2009},
  volume={20},
  pages={1193-1197}
}
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… 
GLYX-13, a NMDA Receptor Glycine-Site Functional Partial Agonist, Attenuates Cerebral Ischemia Injury In Vivo and Vitro by Differential Modulations of NMDA Receptors Subunit Components at Different Post-Ischemia Stage in Mice
TLDR
In vitro oxygen-glucose deprivation stroke model, GLYX-13 blocked i-LTP and restored the ratio of NR2A/NR2B subunit composition and proposes the glycine site of NMDARs as a novel target for developing therapeutic strategies to store synaptic function in stroke.
Glycine-induced NMDA receptor internalization provides neuroprotection and preserves vasculature following ischemic stroke
TLDR
It is reported that following an ischemic event, in vivo, GINI also occurs and provides neuroprotection in the presence of a GlyT1 antagonist (GlyT1-A) and GlyT2-As preserve the vasculature in the peri-infarct area and could be a new target for the treatment of isChemic stroke.
GLYX-13, a NMDA Receptor Glycine-Site Functional Partial Agonist, Induces Antidepressant-Like Effects Without Ketamine-Like Side Effects
TLDR
It is shown that GLYX-13, a novel NMDAR glycine-site functional partial agonist, produces an antidepressant-like effect in the Porsolt, novelty induced hypophagia, and learned helplessness tests in rats without exhibiting substance abuse-related, gating, and sedative side effects of ketamine.
Commentary: GLYX-13 Ameliorates Schizophrenia-Like Phenotype Induced by MK-801 in Mice: Role of Hippocampal NR2B and DISC1
TLDR
The results suggest GLYX-13 as a candidate for schizophrenia treatment, and NR2B and DISC1 in the hippocampus may account for the molecular mechanisms of GLYx-13.
Modulation of the activity of N-methyl-d-aspartate receptors as a novel treatment option for depression: current clinical evidence and therapeutic potential of rapastinel (GLYX-13)
TLDR
Current clinical and animal studies regarding the therapeutic potential of rapastinel not only in MDD but also in other psychiatric disorders, such as obsessive–compulsive disorder and posttraumatic stress disorder are summarized and discussed.
A novel NMDA receptor glycine-site partial agonist, GLYX-13, has therapeutic potential for the treatment of autism
TLDR
It is shown that rats selectively bred for low rates of play-induced pro-social ultrasonic vocalizations (USVs) can be used to model certain core symptoms of autism and GLYX-13 shows promise for the treatment of autism.
Neuroprotective activity of creatylglycine ethyl ester fumarate.
  • O. Veselkina, V. Morozov, +5 authors T. Vlasov
  • Medicine
    Journal of stroke and cerebrovascular diseases : the official journal of National Stroke Association
  • 2015
TLDR
CrGEt holds a promise as a compound for treatment of ischemic brain disorders because it served as a substrate for creatine kinase and a partial agonist of N-methyl-D-aspartate receptors, which partly explains mechanism of its neuroprotective action.
Rapastinel alleviates the neurotoxic effect induced by NMDA receptor blockade in the early postnatal mouse brain
TLDR
A remarkable neuroprotective effect of rapastinel against apoptosis induced by the NMDAR antagonist MK-801 in comparison to that elicited by clozapine and the mGlu2/3 agonist LY354740 is found.
Positive emotional learning is regulated in the medial prefrontal cortex by GluN2B-containing NMDA receptors
TLDR
Modulation of GluN2B-containing NMDA receptors (NMDAR) in the medial prefrontal cortex (MPFC) is involved in positive emotional learning in rats by similar mechanisms as spatial/temporal learning in the hippocampus.
GLYX-13 Ameliorates Schizophrenia-Like Phenotype Induced by MK-801 in Mice : Role of Hippocampal NR 2 B and DISC 1
It is with great interest we have read the article "GLYX-13 Ameliorates Schizophrenia-Like Phenotype Induced by MK-801 in Mice: Role of Hippocampal NR2B and DISC1" (Zhou et al., 2018). Interestingly,
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