PEAQX: Difference between revisions
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'''PEAQX''' is a competitive [[antagonist (pharmacology)|antagonist]] at the [[NMDA receptor]]. |
'''PEAQX''' is a competitive [[antagonist (pharmacology)|antagonist]] at the [[NMDA receptor]]. Although originally described as 100-fold selective for GluN1/GluN2A receptors vs. GluN1/GluN2B receptors, more detailed studies<ref>Frizelle PA, Chen PE, Wyllie DJ 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'' 2006 Sep;70(3):1022-32. PMID 16778008</ref> 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.<ref>Auberson YP, Allgeier H, Bischoff S, Lingenhoehl K, Moretti R, Schmutz M. 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition. ''Bioorganic and Medicinal Chemistry Letters''. 2002 Apr 8;12(7):1099-102. PMID 11909726</ref> |
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Revision as of 03:56, 19 May 2011
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| Clinical data | |
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| Other names | PEAQX |
| Identifiers | |
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| Chemical and physical data | |
| Formula | C17H17BrN3O5P |
| Molar mass | 454.211 g/mol g·mol−1 |
| 3D model (JSmol) | |
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| (verify) | |
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
- ^ Frizelle PA, Chen PE, Wyllie DJ 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 2006 Sep;70(3):1022-32. PMID 16778008
- ^ Auberson YP, Allgeier H, Bischoff S, Lingenhoehl K, Moretti R, Schmutz M. 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition. Bioorganic and Medicinal Chemistry Letters. 2002 Apr 8;12(7):1099-102. PMID 11909726