| 词条 | PEAQX |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 429827414 | IUPAC_name = ({[(1S)-1-(4-bromophenyl)ethyl]amino}-(2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methyl)phosphonic acid | image = PEAQX.png | width = 240 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = | ATC_prefix = | ATC_suffix = | PubChem = 9868551 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 8044242 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | C=17 | H=17 | Br=1 | N=3 | O=5 | P=1 | molecular_weight = 454.211 g/mol | synonyms = PEAQX, NVP-AAM077 | smiles = C[C@@H](C1=CC=C(C=C1)Br)NC(C2=C3C(=CC=C2)N=C(C(=N3)O)O)P(=O)(O)O | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C17H17BrN3O5P/c1-9(10-5-7-11(18)8-6-10)19-17(27(24,25)26)12-3-2-4-13-14(12)21-16(23)15(22)20-13/h2-9,17,19H,1H3,(H,20,22)(H,21,23)(H2,24,25,26)/t9-,17?/m0/s1 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = XXZGNAZRWCBSBK-WFVOFKTRSA-N }}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] References1. ^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}} {{Ionotropic glutamate receptor modulators}}2. ^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 & Medicinal Chemistry Letters. 2002 Apr 8;12(7):1099-102. {{PMID|11909726}} 4 : NMDA receptor antagonists|Organobromides|Quinoxalines|Lactams |
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