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Product introduction
乙琥胺是一种二羰亚胺,是3位氢被一个甲基和一个乙基取代的吡咯烷-2,5-二酮。作为一种抗癫痫药,它用于治疗失神发作,也可用于肌阵挛性发作,但对强直-阵挛性发作无效。它具有抗衰老剂、T型钙通道阻滞剂和抗惊厥药的作用。它是一种二羰亚胺和吡咯烷酮。
Chinese name
乙琥胺, 电压门 T 型钙通道阻滞剂
English name
3-ethyl-3-methylpyrrolidine-2,5-dione
Chinese alias
2-乙基-2-甲基琥珀酰亚胺
English alias
ethosuximide | 77-67-8 | Zarontin | Ethosuxide | Etosuximida | Pyknolepsinum | 2-Ethyl-2-methylsuccinimide | Ethosuccimide | Ethosuccinimide | Atysmal | Suxilep | Suxinutin | Etosuximid | Mesentol | Pentinimid | Peptinimid | Petinimid | Petnidan | Succima
CAS number
77-67-8
molecular formula
C7H11NO2
molecular weight
141.17
Exact mass
10mM in DMSO
PSA
46.2
Logp
0.4
Safety
  • Treatment: 治疗应包括催吐(除非患者已经或可能迅速变得迟钝、昏迷或惊厥)或洗胃、活性炭、泻药和一般支持措施。血液透析可能对治疗乙琥胺过量有用。强制利尿和换血无效。(L1712) <<<169>> examined in male Fischer rats. Rats were fed a semipurified diet containing 0.4% ethoxyquin for 1 wk, gavaged with 250 ug of aflatoxin B1 per kg 5 times a wk during the next 2 wk, and finally restored to the control diet 1 wk after cessation of dosing. At 4 mo, focal areas of hepatocellular alteration were identified and quantitated by staining sections of liver for gamma-glutamyl transpeptidase. Treatment with ethoxyquin reduced by greater than 95% both area and volume of liver occupied by gamma-glutamyl transpeptidase-positive foci. Utilizing the same multiple dosing protocol, patterns of covalent modifications of DNA by aflatoxin B1 were dete...
  • Storage conditions: 乙琥胺胶囊应储存在密封容器中,温度低于30°C,最好在15-30°C之间。乙琥胺口服溶液应储存在密封、避光的容器中,温度低于30°C,最好在15-30°C之间;应避免冷冻。
  • Disposal method: SRP:在审查时,土地处理或填埋(卫生填埋)处置实践的标准正在重大修订中。在实施废物残渣(包括废物污泥)的土地处置之前,咨询环境监管机构以获取可接受的处置实践指导。
  • exposure pathway: 口服给药后的生物利用度为93%。
  • Harmful effect: * 一项研究表明,根据患者年龄,乙琥胺显著降低了拉莫三嗪的血清浓度。具体而言,接受乙琥胺治疗的儿童和青少年拉莫三嗪水平降低了37%,而成年人为14%。
  • Toxicity summary: 结合T型电压敏感性钙通道。电压敏感性钙通道(VSCC)介导钙离子进入可兴奋细胞,也参与多种钙依赖性过程,包括肌肉收缩、激素或神经递质释放、基因表达、细胞运动、细胞分裂和细胞死亡。异构体α-1G产生T型钙电流。T型钙通道属于"低电压激活(LVA)"组,可被米贝地尔强烈阻断。这类通道的一个特点是可在相当负的电位下开放,并且具有电压依赖性失活。T型通道在中枢神经细胞和心脏结细胞中起起搏功能,并在分泌细胞和血管平滑肌中支持钙信号传导...
  • Regulatory information: 新西兰化学品状态清单: 乙琥胺: 没有单独批准,但可在适当的团体标准下使用
  • Health Effects: 可能引起潜在危险的皮疹,可能发展为史蒂文斯-约翰逊综合征,这是一种极其罕见但可能致命的皮肤疾病。
  • Hepatotoxicity: 可能性评分:E*(疑似但未证实为临床明显肝损伤的原因)。
  • Special Reports: 参考文献11篇,关于吸收、分布、排泄、胎盘转移和蛋白质结合。[CHANG T ET AL; 抗癫痫药物 417 (1972)]
  • Ambient water concentration: 虽然未找到有关乙琥胺的具体数据(SRC, 2007),但文献表明,一些来自人和兽医治疗的药物活性化合物在市政污水处理厂中不能完全去除,因此被排放到受纳水体中(1)。废水处理过程通常不是为了从废水中去除这些化合物而设计的(2)。选定的有机废物化合物可能降解成新的更持久的化合物,这些化合物可能被释放出来,替代或附加于母体化合物(2)。
  • Symptoms and Signs: 急性过量可能引起恶心、呕吐和中枢神经系统抑制,包括伴有呼吸抑制的昏迷。
  • FDA Requirements: 具有治疗等效性评估的批准药物产品清单确定了当前上市的销售处方药产品,包括乙琥胺,这些产品根据联邦食品、药品和化妆品法案第505节被FDA基于安全性和有效性批准。
  • Other safety information: 化学品评估:IMAP评估 - 2,5-吡咯烷二酮,3-乙基-3-甲基-:人类健康I级评估
  • non-human toxicity value: LD50 小鼠口服 1530 mg/kg
  • Milk Concentrations: 本研究共纳入10名接受乙琥胺(ES)治疗的癫痫母亲及其13名新生儿。...母乳中ES的浓度与母体血清相似(乳汁/血清:0.86 ± 0.08,n = 12),且哺乳婴儿的血清水平维持在15-40微克/毫升之间...
  • Hazard categories and classifications: 急性毒性 4 (95.7%)
  • Non-human toxic extract: /实验室动物:发育或生殖毒性/ 在妊娠第5-20天,给4-6周大的幼年大鼠在母体体重基础上每天10 mg/kg剂量的乙琥胺进行产前接触,以检查行为异常。4-5周龄幼鼠的钉扎行为显著比同龄对照组更频繁。然而,5-6周龄幼鼠的旷场行为基础活动和地西泮给药抑制的活动与对照组相比没有差异。阿扑吗啡(1 mg/kg, SC)诱导的刻板行为强度在5-6周龄幼鼠中显著高于对照组。这些结果表明产前接触乙琥胺可能导致中枢神经系统多巴胺能神经元的变化。
  • Antidote and first aid: /SRP:/ 高级治疗:对于意识不清、严重肺水肿或严重呼吸窘迫的患者,考虑经口或经鼻气管插管进行气道控制。使用气囊面罩装置进行正压通气技术可能有益。考虑对肺水肿进行药物治疗...。对于严重支气管痉挛,考虑给予β激动剂如沙丁胺醇...。监测心律并根据需要治疗心律失常...。开始静脉注射D5W /SRP: "保持通畅",最小流速/。如果出现低血容量迹象,使用0.9%生理盐水(NS)或乳酸盐林格氏液。对于伴有低血容量体征的低血压,谨慎给予液体。注意液体过载的迹象...。用地西泮或劳拉西泮治疗癫痫...。使用...
  • Carcinogen Classification: 对人类无致癌性迹象(未被IARC列出)。
  • Drug Induced Liver Injury: 参考文献:DOI:10.1016/j.drudis.2019.09.022
  • Effects During Pregnancy and Lactation: 截至修订日期,未找到相关已发表信息。
Related
upstream information
Manufacturing method:
丁酮 (CID:6569); 氰基乙酸乙酯 (CID:18504529); 乙琥胺 (CID:3291); 氰基乙酸乙酯 (CID:7764); 氢氰酸 (CID:768); 氨 (CID:222)
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Research chemical CAS 77-67-8 1ml

Yuanye Research chemical CAS 77-67-8 1ml, complete specifications; suitable for production, research, laboratory testing and inspection; digital one-stop procurement platform for scientific materials.

item number:T92091-1ml
Product model:1ml
level: 1ml
Lead Time:30days
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