5-Aminomethylquinoxaline-2,3-diones. Part I: A novel class of AMPA receptor antagonists.
A series of 5-aminomethylquinoxaline-2,3-diones have been identified as potent and selective AMPA antagonists. Some of these compounds are also active at the glycine-binding site of the NMDA receptors. A number of these novel, water-soluble quinoxaline-2,3-dione derivatives display protective effects in the electroshock-induced convulsion model in mice.
Auberson
Y P
YP
Novartis Pharma AG, Basel, Switzerland. yves.auberson@pharma.novartis.com
Bischoff
S
S
Moretti
R
R
Schmutz
M
M
Veenstra
S J
SJ
D000818:Animals; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D011810:Quinoxalines / Q000737:chemistry / Q000494:pharmacology*; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*; D012640:Seizures / Q000517:prevention & control
D018691:Excitatory Amino Acid Antagonists; D011810:Quinoxalines; D018091:Receptors, AMPA