5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition
| Autor: | Hans Allgeier, Yves Auberson, Serge Bischoff, Robert Moretti, Markus Schmutz, Kurt Lingenhoehl |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
medicine.medical_treatment
Clinical Biochemistry Pharmaceutical Science Pharmacology Binding Competitive Receptors N-Methyl-D-Aspartate Biochemistry Mice chemistry.chemical_compound Quinoxalines Drug Discovery Convulsion medicine Animals Humans Receptor Molecular Biology PEAQX Molecular Structure Chemistry Organic Chemistry Antagonist Glutamate receptor Electric Stimulation Anticonvulsant Agent Anticonvulsant Molecular Medicine NMDA receptor Anticonvulsants medicine.symptom |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 12:1099-1102 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(02)00074-4 |
| Popis: | NMDA antagonists derived from 5-phosphonomethyl-1,4-dihydroquinoxaline-2,3-dione (3a) are potent anticonvulsant agents, and display strong protective effects in the electroshock-induced convulsion assay in mice. Their preference for the human NMDAR 1A/2A over 1A/2B subunit composition was optimized, leading to (1RS,1'S)-PEAQX (9r), which shows a >100-fold selectivity. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect