Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.
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.
Grasso
Silvana
S
Dipartimento Farmaco-Chimico, Università di Messina, viale Annunziata, 98168 Messina, Italy.
Micale
Nicola
N
Zappalà
Maria
M
Galli
Alessandro
A
Costagli
Chiara
C
Menniti
Frank S
FS
De Micheli
Carlo
C
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D001381:Azepines / Q000138:chemical synthesis* / Q000494:pharmacology*; D001569:Benzodiazepines; D001667:Binding, Competitive / Q000187:drug effects; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D051379:Mice; D008811:Mice, Inbred DBA; D011799:Quinazolines / Q000494:pharmacology; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D018009:Receptors, Glycine / Q000187:drug effects; D018092:Kainic Acid Receptors / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D001381:Azepines; D001569:Benzodiazepines; D018691:Excitatory Amino Acid Antagonists; D011799:Quinazolines; D018091:Receptors, AMPA; D018009:Receptors, Glycine; D018092:Kainic Acid Receptors; C418043:CP 526,427; C061950:GYKI 52466