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Updated: Aug 15, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists
Maria Zappalà1, Alessia Pellicanò, Nicola Micale
1Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata 98168, Messina, Italy.
Abstract:
A series of 1-aryl-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-ones 2a-f, were synthesized and screened as anticonvulsant agents in DBA/2 mice against sound-induced seizures. The new compounds display anticonvulsant properties although the ED(50) values are higher than those of prototypes 1-aryl-3,5-dihydro-7,8-methylenedioxy-4H-2,3-benzodiazepin-4-ones (1) and GYKI 52466, well-known noncompetitive AMPA receptor antagonists. Functional tests were performed to evaluate the antagonistic activity at the AMPA and kainate receptors.
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