Chemistry:PEAQX

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Short description: Chemical compound
PEAQX
PEAQX.svg
Clinical data
Other namesPEAQX, NVP-AAM077
Identifiers
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC17H17BrN3O5P
Molar mass454.217 g·mol−1
3D model (JSmol)
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PEAQX is a competitive antagonist at the NMDA receptor. Although originally described as 100-fold selective for GluN1/GluN2A receptors vs. GluN1/GluN2B receptors, more detailed studies[1] of the Ki of PEAQX revealed it only shows a 5 fold difference in affinity for GluN1/GluN2A vs. GluN1/GluN2B receptors. It is also a potent anticonvulsant in animal tests.[2]

References

  1. "Equilibrium constants for (R)-[(S)-1-(4-bromo-phenyl)-ethylamino]-(2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-methyl]-phosphonic acid (NVP-AAM077) acting at recombinant NR1/NR2A and NR1/NR2B N-methyl-D-aspartate receptors: Implications for studies of synaptic transmission". Molecular Pharmacology 70 (3): 1022–32. September 2006. doi:10.1124/mol.106.024042. PMID 16778008. 
  2. "5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition". Bioorganic & Medicinal Chemistry Letters 12 (7): 1099–102. April 2002. doi:10.1016/s0960-894x(02)00074-4. PMID 11909726.