规格: | 98% |
分子量: | 309.7 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Background:
YM-90K is an AMPA receptor antagonist (Ki= 0.084 μM in a radioligand binding assay using rat brain membranes).1It 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 striatumex vivoin 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
1.Ohmori, J., Sakamoto, S., Kubota, H., et al.6-(1H-Imidazol-1-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione hydrochloride (YM90K) and related compounds: Structure-activity relationships for the AMPA-type non-NMDA receptorJ. Med. Chem.37(4)467-475(1994) 2.Umemura, K., Shimakura, A., and Nakashima, M.Neuroprotective effect of a novel AMPA receptor antagonist, YM90K, in rat focal cerebral ischaemiaBrain Res.773(1-2)61-65(1997)