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154164-30-4

中文名稱(chēng) 1,4-二氫-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮單鹽酸鹽
英文名稱(chēng) YM90Khydrochloride
CAS 154164-30-4
分子式 C11H7N5O4.HCl
MOL 文件 154164-30-4.mol
154164-30-4 結(jié)構(gòu)式 154164-30-4 結(jié)構(gòu)式

基本信息

中文別名
1,4-二氫-6-(1H-咪唑-1-基)-7-硝基-2,3-喹啉二酮單鹽酸鹽
1,4-二氫-6-(1H-咪唑-1-基)-7-硝基-2,3-喹喔啉二酮單鹽酸鹽
英文別名
CS-885
YM 90K
YM-90K HCL
YM90Khydrochloride
6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-
6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione
1,4-Dihydro-6-(1H-imidazol-1-yl)-7-nitro-2,3-quinoxalinedionehydrochloride
1,4-Dihydro-6-(1H-imidazol-1-yl)-7-nitro-2,3-quinoxalinedione monohydrochloride
2,3-Quinoxalinedione,1,4-dihydro-6-(1H-imidazol-1-yl)-7-nitro-,monohydrochloride
2,3-Quinoxalinedione,1,4-dihydro-6-(1H-imidazol-1-yl)-7-nitro-, hydrochloride (1:1)

物理化學(xué)性質(zhì)

儲(chǔ)存條件Desiccate at RT
溶解度Soluble to 10 mM in DMSO with gentle warming
形態(tài)粉末

常見(jiàn)問(wèn)題列表

生物活性
YM90K 是一種有效的選擇性的 AMPA 受體拮抗劑,Ki 為 84 nM。YM90K 抑制海藻酸酯 (Ki 為 2.2 μM) 和 NMDA (Ki 為 37 μM) 受體的效力較低,并具有神經(jīng)保護(hù)作用。
靶點(diǎn)

Ki: 84 nM (AMPA receptor), 2.2 μM (Kainate receptor) and 37 μM (NMDA receptor)

體外研究

YM90K co-injected with AMPA or kainate into the rat striatum protect cholinergic neurons against AMPA- or kainate-induced neurotoxicity.

體內(nèi)研究

YM90K shows potent suppressive activity against audiogenic seizure in DBA/2 mice; ED 50 values of YM90K against tonic seizure is 2.54 mg/kg (i.p.). The duration of the anticonvulsant effects of YM90K is 30 min.
In a global ischemia model, YM90K (15 mg/kg i.p.) significantly prevents the delayed neuronal death in the hippocampal CA1 region in Mongolian gerbils when administered 1 h after 5-min ischemia. The therapeutic time window for the neuroprotective effect of YM90K (30 mg/kg i.p.) is 6 h.
In a focal ischemia model, YM90K (30 mg/kg i.v. bolus+10 mg/kg/h for 4 h) reduces the volume of ischemic damage in the cerebral cortex in F344 rats.

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