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154106-92-0

中文名稱 154106-92-0
英文名稱 RPR 104632
CAS 154106-92-0
分子式 C15H11BrCl2N2O4S
分子量 466.13
MOL 文件 154106-92-0.mol
154106-92-0 結(jié)構(gòu)式 154106-92-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T16797
英文別名
RPR 104632
2H-1,2,4-Benzothiadiazine-3-carboxylic acid, 2-[(3-bromophenyl)methyl]-6,8-dichloro-3,4-dihydro-, 1,1-dioxide

物理化學(xué)性質(zhì)

沸點658.6±65.0 °C(Predicted)
密度1.788±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)2.00±0.20(Predicted)

常見問題列表

生物活性
RPR104632 是一種特異性的 NMDA receptor 拮抗劑,具有神經(jīng)保護(hù)的作用。
體外研究

RPR104632 antagonizes the binding of [ 3 H]5,7-dichlorokynurenic acid to the rat cerebral cortex, with a K i of 4.9 nM. RPR104632 inhibits [ 3 H]N-[1-(2-thienyl)cyclohexyl]-3,4-piperidine ([ 3 H]TCP) binding in the presence of N-methyl-D-aspartate (NMDA) (IC 50 = 55 nM). RPR104632 inhibits the NMDA-evoked increase in guanosine 3',5'-cyclic monophosphate (cGMP) levels of neonatal rat cerebellar slices (IC 50 = 890 nM) in a non-competitive manner and markedly reduces NMDA-induced neurotoxicity in rat hippocampal slices and in cortical primary cell cultures. MK-801 (1 μM) completely protects the CA1 and CA3 pyramidal neurones against NMDA-induced toxicity, but these effects are not blocked by glycine. RPR104632 produces a significant and consistent neuroprotective effect towards all the NMDA-induced toxicity and has no effect when it is added alone at concentrations up to 10 μM. RPR104632 has neuroprotective potencies, with EC 50 of 4 μM.

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