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Article Dans Une Revue Amino Acids Année : 2011

Synthesis of C5-tetrazole derivatives of 2-amino-adipic acid displaying NMDA glutamate receptor antagonism.

Résumé

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.

Dates et versions

hal-00542138 , version 1 (01-12-2010)

Identifiants

Citer

Fatimazohra Lenda, Nadine Crouzin, Mélanie Cavalier, Janique Guiramand, Fabien Lanté, et al.. Synthesis of C5-tetrazole derivatives of 2-amino-adipic acid displaying NMDA glutamate receptor antagonism.. Amino Acids, 2011, 40 (3), pp.913-22. ⟨10.1007/s00726-010-0713-1⟩. ⟨hal-00542138⟩
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