Kovács A D, Egyed A
Department of Biochemistry, EGIS Biological Laboratories, EGIS Pharmaceuticals Ltd., Budapest, Hungary.
Neurobiology (Bp). 1996;4(1-2):59-72.
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.
1-（4-氨基苯基）-4-甲基-7,8-亚甲基二氧基-5H-2,3-苯并二氮杂卓盐酸盐（GYKI 52466）是一种最近研发的非竞争性α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）/海人藻酸拮抗剂，在大鼠胚胎端脑细胞的成熟（体外培养17 - 20天）培养物中，其对喹啉酸（10或15微摩尔）和AMPA（20微摩尔）兴奋性毒性具有神经保护作用。GYKI 52466以剂量依赖性方式减弱喹啉酸（15微摩尔）或AMPA（20微摩尔）的神经毒性，其半数抑制浓度（IC50）分别为16微摩尔和10微摩尔。
