title: New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists.
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.
authors.affiliation: Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata 98168, Messina, Italy.
authors.forename: Maria
authors.initials: M
authors.lastname: Zappalà
authors.forename: Alessia
authors.initials: A
authors.lastname: Pellicanò
authors.forename: Nicola
authors.initials: N
authors.lastname: Micale
authors.forename: Frank S
authors.initials: FS
authors.lastname: Menniti
authors.forename: Guido
authors.initials: G
authors.lastname: Ferreri
authors.forename: Giovambattista
authors.initials: G
authors.lastname: De Sarro
authors.forename: Silvana
authors.initials: S
authors.lastname: Grasso
authors.forename: Carlo
authors.initials: C
authors.lastname: De Micheli
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology; D001569:Benzodiazepines / Q000494:pharmacology*; D001667:Binding, Competitive; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008811:Mice, Inbred DBA; D008956:Models, Chemical; D011485:Protein Binding; D051381:Rats; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D018092:Kainic Acid Receptors / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D001569:Benzodiazepines; D018091:Receptors, AMPA; D018092:Kainic Acid Receptors; C061950:GYKI 52466