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YM-90K is an AMPA receptor antagonist (Ki = 0.084 μM in a radioligand binding assay using rat brain membranes).1 It is selective for AMPA over kainate, NMDA-sensitive glutamate, and strychnine-insensitive glycine receptors (Kis = 2.2, >100, and 37 μM, respectively). Intrastriatal administration of YM-90K inhibits AMPA-induced decreases in choline acetyltransferase (ChAT) activity in rat striatum ex vivo in a dose-dependent manner. It inhibits audiogenic seizures in susceptible DBA/2 mice with a minimum effective dose of 3 mg/kg when administered intraperitoneally. Intravenous infusion of YM-90K (20 mg/kg per hour for 4 hours) reduces infarct size in a rat model of focal cerebral ischemia induced by thrombotic middle cerebral artery occlusion (MCAO) in rats.2
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2. Neuroprotective effect of a novel AMPA receptor antagonist, YM90K, in rat focal cerebral ischaemia. Brain Res. 773(1-2), 61-65 (1997).