Protection against non-NMDA receptor-mediated excitotoxicity by GYKI 52466 in mature telencephalic cultures of the rat.
The neuroprotective effect of 1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine hydrochloride (GYKI 52466), a recently developed non-competitive alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA)/kainate antagonist was demonstrated against quisqualate (10 or 15 microM) and AMPA (20 microM) excitotoxicity in mature (17-20 days in vitro) cultures of rat embryonic telencephalic cells. GYKI 52466 attenuated quisqualate (15 microM) or AMPA (20 microM) neurotoxicity in a dose-dependent manner with IC50 of 16 microM and 10 microM, respectively.
Kovács
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Department of Biochemistry, EGIS Biological Laboratories, EGIS Pharmaceuticals Ltd., Budapest, Hungary.
Egyed
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D000818:Animals; D014151:Anti-Anxiety Agents; D001569:Benzodiazepines / Q000494:pharmacology*; D002478:Cells, Cultured; D004622:Embryo, Mammalian; D018691:Excitatory Amino Acid Antagonists / Q000494:pharmacology*; D009474:Neurons / Q000166:cytology* / Q000187:drug effects / Q000473:pathology; D009498:Neurotoxins / Q000633:toxicity*; D016318:Quisqualic Acid / Q000633:toxicity*; D051381:Rats; D017207:Rats, Sprague-Dawley; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors; D018092:Kainic Acid Receptors / Q000037:antagonists & inhibitors; D013687:Telencephalon / Q000166:cytology*; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid / Q000633:toxicity*
D014151:Anti-Anxiety Agents; D001569:Benzodiazepines; D018691:Excitatory Amino Acid Antagonists; D009498:Neurotoxins; D016318:Quisqualic Acid; D018091:Receptors, AMPA; D018092:Kainic Acid Receptors; D018350:alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; C061950:GYKI 52466