共 36 条
Synthesis of C5-tetrazole derivatives of 2-amino-adipic acid displaying NMDA glutamate receptor antagonism
被引:10
作者:

Lenda, Fatimazohra
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Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France
Univ Moulay Ismail, Fac Sci, Zitoune, Meknes, Morocco Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France

Crouzin, Nadine
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Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France

Cavalier, Melanie
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Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France

Guiramand, Janique
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Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France

Lante, Fabien
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Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France

Barbanel, Gerard
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Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France

Cohen-Solal, Catherine
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Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France

Martinez, Jean
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Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France

Guenoun, Farhate
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Univ Moulay Ismail, Fac Sci, Zitoune, Meknes, Morocco Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France

Lamaty, Frederic
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机构:
Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France

Vignes, Michel
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机构:
Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France
机构:
[1] Univ Montpellier I, Inst Biomol Max Mousseron, CNRS, UMR 5247, F-34095 Montpellier 5, France
[2] Univ Moulay Ismail, Fac Sci, Zitoune, Meknes, Morocco
来源:
关键词:
Glutamate;
N-Methyl-D-Aspartate (NMDA);
Synaptic transmission;
Extrasynaptic receptors;
EXCITATORY AMINO-ACID;
HIPPOCAMPAL CULTURES;
ALZHEIMERS-DISEASE;
LOW-AFFINITY;
CELL-DEATH;
NEURONS;
MEMANTINE;
AGONIST;
PHARMACOLOGY;
MECHANISM;
D O I:
10.1007/s00726-010-0713-1
中图分类号:
Q5 [生物化学];
Q7 [分子生物学];
学科分类号:
071010 ;
081704 ;
摘要:
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.
引用
收藏
页码:913 / 922
页数:10
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Ferreira, MCJ
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Récasens, M
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