Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists

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Abstract

A selected set of 1-aryl-7,8-methylenedioxy-2,3-benzodiazepin-4-ones and their analogues were evaluated for their ability to bind the competitive and noncompetitive sites of the AMPA receptors complex as well as to the glycine site of the NMDA receptors. The results put in evidence that most of the test compounds, despite a close structural similarity with GYKI 52466, possess a significantly different pharmacological profile.

A selected set of 1-aryl-7,8-methylenedioxy-2,3-benzodiazepin-4-ones and their analogues were evaluated for their ability to bind the competitive and noncompetitive sites of AMPA receptors as well as glycine/NMDA receptor site.

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Acknowledgements

This work was financially supported by the Ministero dell'Istruzione, dell'Università e della Ricerca (MIUR- COFIN2001), Rome, Italy. We thank Martin J. Pagnozzi, Mary A. Collins and John T. Lazzaro of Pfizer Inc. for excellent technical assistance.

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