Synthesis of C5-tetrazole derivatives of 2-amino-adipic acid displaying NMDA glutamate receptor antagonism |
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Authors: | Fatimazohra Lenda Nadine Crouzin M��lanie Cavalier Janique Guiramand Fabien Lant�� G��rard Barbanel Catherine Cohen-Solal Jean Martinez Farhate Guenoun Fr��d��ric Lamaty Michel Vignes |
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Affiliation: | 1. Institut des Biomol??cules Max Mousseron UMR 5247 CNRS-Universit??s Montpellier 1 et 2, Universit?? Montpellier 2, Pl. E. Bataillon, cc2400, 34095, Montpellier Cedex 5, France 2. Faculty of Sciences, University Moulay Ismail, B.P. 1201, Zitoune, Mekn??s, Morocco
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Abstract: | 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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