期刊
AMINO ACIDS
卷 40, 期 3, 页码 913-922出版社
SPRINGER WIEN
DOI: 10.1007/s00726-010-0713-1
关键词
Glutamate; N-Methyl-D-Aspartate (NMDA); Synaptic transmission; Extrasynaptic receptors
资金
- French Ministry for Higher education and Research
- Centre National de la Recherche Scientifique (CNRS)
- Fondation pour la Recherche Medicale (FRM)
Five derivatives of 2-amino-adipic acid bearing a tetrazole-substituted in C5 position were synthesized. These compounds displayed selective antagonism towards N-methyl-d-aspartate (NMDA) receptors compared with AMPA receptors, and they were devoid of any neurotoxicity. Among these five analogues, one exhibited a higher affinity for synaptic NMDA responses than the other four. Therefore, C5 tetrazole-substituted of 2-amino-adipic acid represent an interesting series of new NMDA receptor antagonists. This approach may be considered as a new strategy to develop ligands specifically targeted to synaptic or extra-synaptic NMDA receptors.
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