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synthesis and Structure-Activity Relationships of 2,3-Benzodiazepines as AMPA Receptor Antagonists

[ Vol. 1 , Issue. 3 ]


M. Zappala, S. Grasso, N. Micale, S. Polimeni and C. De Micheli   Pages 243 - 253 ( 11 )


There is increasing evidence of the potential therapeutic utility of glutamate receptor antagonists in the treatment of several neurodegenerative disorders, including stroke and epilepsy. In the last few years noncompetitive AMPA receptor antagonists have received considerable attention due to their therapeutic potentiality. The discovery of GYKI 52466, the prototype of noncompetitive AMPA receptor antagonists endowed with anticonvulsant and neuroprotective properties, induced growing interest on 2,3-benzodiazepine derivatives. This review covers the chemistry and pharmacology of this important class of AMPA receptor antagonists.


2,3-Benzodiazepines, AMPA Receptor, glutamate receptor antagonists, neurodegenerative disorders, Stroke, Epilepsy, Anticonvulsant, Neuroprotective


Dipartimento Farmaco-Chimico, Universita di Messina, Viale Annunziata, 98168 Messina, Italy

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