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乙琥胺

乙琥胺用途

Ethosuximide 是一种广泛使用的抗癫痫药物,可改善多种神经退行性疾病模型的表型,且可阻断低电压激活的 T 型钙通道。

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乙琥胺名称

[ CAS 号 ]:
77-67-8

[ 中文名 ]:
乙琥胺

[ 英文名 ]:
Ethosuximide

[中文别名 ]:

[英文别名 ]:

(±)-Ethosuximide
2-Methyl-2-ethylsuccinimide
3-Ethyl-3-methylpyrrolidine-2,5-dione
2-Ethyl-2-methylsuccinimide
MFCD00072123
Ethymal
Zarontin
α-Ethyl-α-methylsuccinimide
Etosuximida
2,5-Pyrrolidinedione, 3-ethyl-3-methyl-

乙琥胺生物活性

[ 描述 ]:

Ethosuximide 是一种广泛使用的抗癫痫药物,可改善多种神经退行性疾病模型的表型,且可阻断低电压激活的 T 型钙通道。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

研究领域 >> 神经疾病

[ 靶点 ]

calcium channel[1]

[体外研究]

Ethosuximide在全身性失神经癫痫中的功效被认为是由于低压激活的T型钙通道的阻断。与载体对照相比,Ethosuximide处理的Tau转基因蠕虫中的总Tau水平没有降低。因此,Ethosuximide的拯救作用不是由于转基因抑制或毒性突变Tau蛋白的表达降低。相对于总Tau水平,可溶性和不溶性(RIPA可提取的)Tau的量的定量显示,与未处理的蠕虫相比,Ethosuximide处理的异常折叠的不溶性Tau和可溶性Tau的相应增加显着减少[1]。发现浓度为2μM或更多的Ethosuximide不仅比1μM浓度的Ethosuximide效果差,而且还诱导细胞毒性。 GABA染色免疫荧光图像显示,用Ethosuximide处理后,GABA阳性神经元的浓度分别为0.1和1μM时增加3倍和6.5倍。 BrdU染色显示Ethosuximide暴露2至3天后的细胞核增殖。低浓度Ethosuximide的核平均值为15.98±0.41,而Brdu染色后的高浓度为25.27±0.48。氯化锂[2]的这个数字是11.05±0.2。

[激酶实验]

将载体和Ethosuximide处理的Tau V337M蠕虫裂解并分离成可溶和不溶的级分。通过SDS-PAGE分离级分，并使用抗人Tau T46和抗肌动蛋白抗体进行蛋白质印迹。通过光密度测定法定量每个级分中Tau蛋白的丰度，并针对β-肌动蛋白进行标准化。裂解物中的总Tau水平表示为肌动蛋白标准化Tau相对于载体对照裂解物的百分比;顺序提取的级分中的Tau水平表示为肌动蛋白标准化的Tau相对于两种级分（可溶性+ RIPA）的总和的百分比[1]。

[细胞实验]

来自3日龄大鼠的前脑皮层的神经元干细胞用于该研究。通过取出碱性成纤维细胞生长因子（bFGF）使细胞分化，并以0.1μM和1μM的两种浓度暴露于Ethosuximide。在药物处理之前，用PBS冲洗细胞一次，并用含有不同浓度的Ethosuximide的新鲜的不含bFGF的DMEM / F12培养基替换培养基。每天用含有Ethosuximide的培养基进行培养基更换6天。然后，细胞被固定用于免疫细胞化学[2]。

[参考文献]

[1]. Chen X, et al. Ethosuximide ameliorates neurodegenerative disease phenotypes by modulating DAF-16/FOXO target gene expression. Mol Neurodegener. 2015 Sep 29;10:51.

[2]. Sondossi K, et al. Analysis of the antiepileptic, ethosuximide impacts on neurogenesis of rat forebrain stem cells. Fundam Clin Pharmacol. 2014 Oct;28(5):512-8.

[相关活性小分子]

乙琥胺物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
265.3±9.0 °C at 760 mmHg

[ 熔点 ]:
51ºC

[ 分子式 ]:
C₇H₁₁NO₂

[ 分子量 ]:
141.168

[ 闪点 ]:
123.8±18.9 °C

[ 精确质量 ]:
141.078979

[ PSA ]:
46.17000

[ LogP ]:
0.38

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
0.0±0.5 mmHg at 25°C

[ 折射率 ]:
1.451

[ 储存条件 ]:
Refrigerator

[ 水溶解性 ]:
ethanol: 100 mg/mL

乙琥胺MSDS

详细MSDS(安全技术说明书)

乙琥胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WN2800000

CHEMICAL NAME :: Succinimide, 2-ethyl-2-methyl-

CAS REGISTRY NUMBER :: 77-67-8

BEILSTEIN REFERENCE NO. :: 0117054

LAST UPDATED :: 199612

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C7-H11-N-O2

MOLECULAR WEIGHT :: 141.19

WISWESSER LINE NOTATION :: T5VMVTJ D2 D1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1530 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1325 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1810 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 780 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Behavioral - ataxia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 33300 ug/kg

SEX/DURATION :: female 6-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 66600 ug/kg

SEX/DURATION :: female 6-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 166 mg/kg

SEX/DURATION :: female 6-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - other developmental abnormalities

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2250 mg/kg

SEX/DURATION :: female 9-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 160 mg/kg

SEX/DURATION :: female 5-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3960 mg/kg

SEX/DURATION :: female 6-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

DOSE :: 962 mg/kg

SEX/DURATION :: female 8-10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - other developmental abnormalities

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 600 mg/kg

SEX/DURATION :: female 8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 2626 mg/kg

SEX/DURATION :: female 8-10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 48100 ug/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 18500 ug/kg

SEX/DURATION :: female 6-10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 185 mg/kg

SEX/DURATION :: female 6-10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Human Lymphocyte

DOSE/DURATION :: 30 mg/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 204,623,1988 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3882 No. of Facilities: 371 (estimated) No. of Industries: 4 No. of Occupations: 6 No. of Employees: 7032 (estimated) No. of Female Employees: 4379 (estimated)

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乙琥胺安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
WN2800000

[ 海关编码 ]:
2925190090

乙琥胺合成路线

详细合成路线

乙琥胺上下游产品

乙琥胺上游产品

乙琥胺下游产品

乙琥胺制备

由2-乙基-2-甲基丁二酸用氨水环合而得。将氨水（20%）加入2-乙基-2-甲基丁二酸，至pH为10以上。加热至200-220℃，反应20min。冷至50℃以下，加入氯仿。过滤，滤饼经氯仿洗涤后弃去合并洗、滤液，分取氯仿层。回收氯仿后减压蒸馏，收集150-160℃（2.13kPa）馏分，得乙琥胺。

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乙琥胺海关

[ 海关编码 ]: 2925190090

[ 中文概述 ]:
2925190090 其他酰亚胺及其衍生物盐. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2925190090 other imides and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

乙琥胺文献

Ethosuximide and phenytoin dose-dependently attenuate acute nonconvulsive seizures after traumatic brain injury in rats.

J. Neurotrauma 30(23) , 1973-82, (2013)

Acute seizures frequently occur following severe traumatic brain injury (TBI) and have been associated with poor patient prognosis. Silent or nonconvulsive seizures (NCS) manifest in the absence of mo...

How did phenobarbital's chemical structure affect the development of subsequent antiepileptic drugs (AEDs)?

Epilepsia 53 Suppl 8 , 3-11, (2012)

Phenobarbital has been in clinical use as an antiepileptic drug (AED) since 1912. The initial clinical success of phenobarbital and other barbiturates affected the design of subsequent AEDs (e.g., phe...

Histone deacetylase inhibitor valproic acid promotes the differentiation of human induced pluripotent stem cells into hepatocyte-like cells.

PLoS ONE 9(8) , e104010, (2014)

In this study, we aimed to elucidate the effects and mechanism of action of valproic acid on hepatic differentiation from human induced pluripotent stem cell-derived hepatic progenitor cells. Human in...

更多文献

乙琥胺

乙琥胺用途

乙琥胺名称

乙琥胺生物活性

乙琥胺物理化学性质

乙琥胺MSDS

详细MSDS(安全技术说明书)

乙琥胺毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

乙琥胺安全信息

乙琥胺合成路线

详细合成路线

乙琥胺上下游产品

乙琥胺上游产品

乙琥胺下游产品

乙琥胺制备

乙琥胺海关

乙琥胺文献

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