中文名 | 利凡斯的明 |
英文名 | Rivastigmine |
别名 | 卡巴拉汀 利斯的明 利凡斯的明 利伐斯的明 利瓦斯的明 卡巴拉汀杂质 N-乙基-N-甲基-氨基甲酸 3-((S)-1-(二甲氨基)乙基)苯酯 3-[(S)-1-(二甲氨基)乙基]苯酯 N-乙基-N-甲基-氨基甲酸 3-[(S)-1-(二甲氨基)乙基]苯酯 |
英文别名 | Revastigmine Rivastigmine RivastigiMine S-RivastigMine Rivastigmine base bis(sulfanylidene)ruthenium 3-[1-(dimethylamino)ethyl]phenyl ethyl(methyl)carbamate (S)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate 3-[(1S)-1-(dimethylamino)ethyl]phenyl ethyl(methyl)carbamate 3-((1S)-1-(Dimethylamino)ethyl)phenyl N-ethyl-N-methylcarbamate (S)-N-Ethyl-N-Methyl- 3-[1-(diMethylaMino)ethyl]- phenyl carbaMate Ethylmethylcarbamic acid 3-((1S)-1-(dimethylamino)ethyl)phenyl ester CarbaMic acid, N-ethyl-N-Methyl-, 3-[(1S)-1-(diMethylaMino)ethyl]phenyl ester |
CAS | 123441-03-2 |
EINECS | 602-936-0 |
化学式 | C14H22N2O2 |
分子量 | 250.34 |
InChI | InChI=1/C14H22N2O2/c1-6-16(5)14(17)18-13-9-7-8-12(10-13)11(2)15(3)4/h7-11H,6H2,1-5H3/t11-/m0/s1 |
密度 | 1.038±0.06 g/cm3(Predicted) |
沸点 | 316.2±34.0 °C(Predicted) |
比旋光度 | D20 -32.1° (c = 5 in ethanol) |
闪点 | 145℃ |
蒸汽压 | 0.000416mmHg at 25°C |
折射率 | 1.518 |
酸度系数 | pKa 8.99 (Uncertain) |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
敏感性 | Sensitive to light |
体外研究 | Rivastigmine (S-Rivastigmine; 1 µM; 24 hours) reduces LPS (2.5 µg/ml)-induced TNF-α and IL-6 by 50% and 46% combined with carbachol (10 µM), respectively and does not cause any significant reduction in pro-inflammatory cytokines . Rivastigmine (1 µM), carbachol (10 µM), or a combination of both drugs, does not have a cytotoxic effect on activated cells. |
体内研究 | Rivastigmine在其末梢性抑制作用中,对中枢神经系统具有选择性。它能减缓前脑损伤的大鼠中的记忆损伤。通过口服途径给药,药物吸收迅速。其生物利用度为0.355,蛋白质结合率低。其消除半衰期小于2小时,rivastigmine绕过肝代谢途径转变为其非活性代谢物。Rivastigmine还能以浓度依赖方式抑制AChE。 |
危险品运输编号 | UN 2810 6.1 / PGIII |
海关编号 | 2924296000 |
上游原料 | (R)-3-(1-hydroxyethyl)phenylethyl(methyl)carbamate |
参考资料 展开查看 | 1. [IF=1.965] Zhang Xiao-Zhong et al."Synthesis, in vitro assays, molecular docking, theoretical ADMET prediction, and evaluation of 4-methoxy-phenylthiazole-2-amine derivatives as acetylcholinesterase inhibitors."Med Chem Res. 2019 Oct;28(10):1683-1693 |
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