3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸
中文名称 | 3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸 |
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中文同义词 | 3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸;化合物 T16032 |
英文名称 | (Z)-2-CARBOXY-4,6-DICHLOROINDOLE-3-(2'-PHENYL-2'-CARBOXY)-ENE |
英文同义词 | MDL-105212;MDL 105,519;3-[(1E)-2-Carboxy-2-phenylethenyl]-4,6-dichloro-1H-indole-2-carboxylic acid;(Z)-2-CARBOXY-4,6-DICHLOROINDOLE-3-(2'-PHENYL-2'-CARBOXY)-ENE;MDL 105,519 >=98% (HPLC), solid;1H-Indole-2-carboxylic acid, 3-[(1E)-2-carboxy-2-phenylethenyl]-4,6-dichloro- |
CAS号 | 161230-88-2 |
分子式 | C18H11Cl2NO4 |
分子量 | 376.19 |
EINECS号 | |
相关类别 | |
Mol文件 | Mol File |
结构式 |
3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸 性质
沸点 | 601.3±55.0 °C(Predicted) |
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密度 | 1.594±0.06 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | 在DMSO中的溶解度为5 毫克/毫升 |
酸度系数(pKa) | 3.20±0.19(Predicted) |
形态 | 固体 |
颜色 | 白色 |
MDL 105519 is a potent and selective ligand for the glycine recognition site that completely inhibit the binding of [ 3 H]glycine to rat brain membranes with a K i value of 10.9 nM. MDL 105519 is approximately 10,000-fold selective for the glycine recognition site relative to the other receptor types investigated. MDL 105519 inhibits NMDA-dependent responses, such as elevations of [ 3 H]TCP binding in brain membranes, cyclic GMP accumulation in brain slices, and alterations in cytosolic Ca 2+ and Na + -Ca 2+ currents in cultured neurons. Inhibition is non-competitive with respect to NMDA and could be nullified with D-serine.
MDL 105519 is an NMDA receptor antagonist in vivo . Intravenously administration of MDL 105519 prevents harmaline-stimulated increases in cerebellar cyclic GMP content, providing biochemical evidence of NMDA receptor antagonism in vivo . This antagonism is associated with anticonvulsant activity in genetically based, chemically induced, and electrically mediated seizure models. Anxiolytic activity is observed in the rat separation-induced vocalization model, but muscle-relaxant activity is apparent at lower doses. Higher doses impair rotorod performance, but are without effect on mesolimbic dopamine turnover or prepulse inhibition of the startle reflex.
安全信息
WGK Germany | 3 |
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提供商 | 语言 |
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英文
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-15085 | 3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸 MDL 105519 | 161230-88-2 | 5mg | 1000元 |
2024/04/30 | HY-15085 | 3-[(1E)-2-羧基-2-苯乙烯基]-4,6-二氯-1H-吲哚-2-羧酸 MDL 105519 | 161230-88-2 | 10mM * 1mLin DMSO | 1100元 |