title: 7,8-Methylenedioxy-4H-2,3-benzodiazepin-4-ones as novel AMPA receptor antagonists.
abstract: The synthesis and anticonvulsant activity of novel 7,8-methylenedioxy-4H-2,3-benzodiazepin-4-ones 3a-e, structurally-related to GYKI 52466 1, a well-known noncompetitive AMPA-receptor antagonist, are reported. The new compounds possess marked anticonvulsant properties and, in analogy to 1, antagonize seizures induced by AMPA. In addition, when compared to the model compound 1, compounds 3 show a longer-lasting anticonvulsant activity and a lower toxicity.
authors.affiliation: Istituto di Farmacologia, Facoltà di Medicina, Università di Messina, Italy.
authors.forename: A
authors.initials: A
authors.lastname: De Sarro
authors.forename: G
authors.initials: G
authors.lastname: De Sarro
authors.forename: R
authors.initials: R
authors.lastname: Gitto
authors.forename: S
authors.initials: S
authors.lastname: Grasso
authors.forename: N
authors.initials: N
authors.lastname: Micale
authors.forename: S
authors.initials: S
authors.lastname: Quartarone
authors.forename: M
authors.initials: M
authors.lastname: Zappalà
mesh_terms: D000161:Acoustic Stimulation; D000818:Animals; D014151:Anti-Anxiety Agents / Q000737:chemistry; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001569:Benzodiazepines; D001570:Benzodiazepinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007202:Indicators and Reagents; D051379:Mice; D008811:Mice, Inbred DBA; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy; D013329:Structure-Activity Relationship; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid / Q000633:toxicity
chemical_list: D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001570:Benzodiazepinones; D018691:Excitatory Amino Acid Antagonists; D007202:Indicators and Reagents; D018091:Receptors, AMPA; C061950:GYKI 52466; D001569:Benzodiazepines; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid