三甲基-(10-三甲基铵基癸基)铵二溴化物 | 156-74-1

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 三甲基-(10-三甲基铵基癸基)铵二溴化物
• 中文别名: N,N,N,N',N',N'-六甲基-1,10-十烷双胺
• 英文名称: decamethonium
• 英文别名: TMA-10；1,10-Decamethylen-bis-trimethylammonium；Decamethylen-bis-(trimethylammonium)；Bis-(trimethylammonium)-decan；trimethyl-[10-(trimethylazaniumyl)decyl]azanium
• CAS: 156-74-1
• 化学式: C₁₆H₃₈N₂
• 分子量: 258.491
• InChiKey: MTCUAOILFDZKCO-UHFFFAOYSA-N

物化性质

• 物理描述：
  Solid
• 熔点：
  268-270 °C
• 溶解度：
  Substantial
• 稳定性/保质期：

  AQUEOUS SOLUTIONS ARE STABLE & MAY BE STERILIZED BY AUTOCLAVING. /DECAMETHONIUM BROMIDE/

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  18
• 可旋转键数：
  11
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  0

ADMET

代谢

...不被血浆胆碱酯酶水解，但由肾脏原样排出。

... IS NOT HYDROLYZED BY PLASMA CHOLINESTERASE BUT IS EXCRETED UNCHANGED BY KIDNEYS.

来源:Hazardous Substances Data Bank (HSDB)

代谢

没有在小动物中发现十羟二甲基胍的生物转化的证据。

NO EVIDENCE WAS FOUND FOR DECAMETHONIUM BIOTRANSFORMATION IN SMALL ANIMALS. ...

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

在人类中... 十甲季铵... 产生并维持具有去极化阻滞所有特征的神经肌肉阻滞... 这特别适用于它通过艾地芬尼，新斯的明和其他抗胆碱酯酶药物的对竞争性阻滞的拮抗作用而增强。

... IN MAN ... DECAMETHONIUM ... PRODUCE & MAINTAIN NEUROMUSCULAR BLOCKADE THAT HAS ALL CHARACTERISTICS OF DEPOLARIZING BLOCKADE ... THIS APPLIES IN PARTICULAR TO ITS INTENSIFICATION BY EDROPHONIUM, NEOSTIGMINE, & OTHER ANTI-CHOLINESTERASE AGENTS THAT ANTAGONIZE COMPETITIVE BLOCK.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

去极化肌肉松弛剂十甲季铵...已被证明与心得安（普萘洛尔）有相互作用...

DEPOLARIZING MUSCLE RELAXANTS DECAMETHONIUM...HAVE BEEN SHOWN TO INTERACT WITH PROPRANOLOL...

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

在洋地黄存在的情况下，尤其是如果出现钾流失，可能会发生心律失常，甚至心脏骤停。

IN PRESENCE OF DIGITALIS, ESP...IF K LOSS, CARDIAC ARRHYTHMIAS, & EVEN CARDIAC ARREST, MAY OCCUR.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 相互作用

去极化肌肉松弛剂十甲季铵...已在大鼠中显示与奎尼丁存在相互作用。

DEPOLARIZING MUSCLE RELAXANTS DECAMETHONIUM...HAVE BEEN SHOWN TO INTERACT WITH QUINIDINE IN ANIMALS.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

不同步使得十羟季铵的拮抗作用难以实现，因为一个阶段的拮抗剂可能是另一个阶段的协同剂。因此，人工呼吸是过量中毒的唯一可靠治疗方法。

...LACK OF SYNCHRONY MAKES ANTAGONISM OF DECAMETHONIUM DIFFICULT, SINCE ANTAGONISTS OF ONE PHASE ARE SYNERGISTS OF OTHER. THUS, ARTIFICIAL RESP IS ONLY RELIABLE TREATMENT OF OVERDOSE.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

• 吸收

迅速吸收。

Rapidly absorbed.

来源:DrugBank

吸收、分配和排泄

四价铵神经肌肉阻滞剂从胃肠道吸收非常差且不规则。/神经肌肉阻滞剂/

QUATERNARY AMMONIUM NEUROMUSCULAR BLOCKING AGENTS ARE VERY POORLY & IRREGULARLY ABSORBED FROM THE GI TRACT. /NEUROMUSCULAR BLOCKING AGENTS/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

瘫痪发作大约需要2分钟，作用持续时间通常约为15分钟；血浆半衰期大约为0.5-1小时。消除主要是通过肾小球过滤和肾小管分泌的结合...

ONSET OF PARALYSIS IS ABOUT 2 MIN, & DURATION OF ACTION IS USUALLY ABOUT 15 MIN; PLASMA T/2 IS APPROX 0.5-1 HR. ELIMINATION IS MAINLY BY COMBINATION OF GLOMERULAR FILTRATION & TUBULAR SECRETION...

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

(14)C在肌肉注射[(14)C]癸甲铵后的分布...通过全身放射自显影在小鼠中进行比较。肝脏对(14)C的摄取速率和程度与尿液排泄速率成反比。 ...(14)C在软骨中迅速积累...在给药后也摄取于肌肉组织中...

DISTRIBUTION OF (14)C AFTER IP ADMIN OF [(14)C]DECAMETHONIUM...IN MICE WERE COMPARED BY WHOLE BODY AUTORADIOGRAM. RATE & EXTENT OF HEPATIC UPTAKE OF (14)C WERE INVERSELY PROPORTIONAL TO RATE OF URINARY EXCRETION. ...(14)C WAS RAPIDLY ACCUM IN CARTILAGE...ALSO TAKEN UP IN MUSCULAR TISSUES AFTER DOSING...

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

没有在小动物中发现十羟二甲基胍的生物转化证据。在兔子中，80%的静脉注射药物在24小时内以原药形式迅速通过尿液排出，胆汁和肺排出途径未被利用。血脑屏障和胎盘保护防止药物转移进入大脑和胎儿。

NO EVIDENCE WAS FOUND FOR DECAMETHONIUM BIOTRANSFORMATION IN SMALL ANIMALS. IN RABBITS, 80% OF IV INJECTION WAS EXCRETED RAPIDLY IN 24 HR URINE AS UNCHANGED DRUG, & BILIARY & PULMONARY ELIMINATIVE ROUTES WERE NOT UTILIZED. BLOOD-BRAIN BARRIER & PLACENTA PROTECT AGAINST TRANSFER...INTO BRAIN & FETUS.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 海关编码：
  2923900090

反应信息

• 作为反应物：
  描述：

  碘代硫代乙酰胆碱 、 5,5'-二硫双(2-硝基苯甲酸) 、 1,4-dithio-D,L-threitol 、 1,2,3,4-Tetrahydroacridin-10-ium-9-amine;chloride;hydrate 、 4-(5-{4-[Dimethyl(prop-2-enyl)ammonio]phenyl}-3-oxopentyl)-N,N-dimethyl-N-prop-2-enylbenzenaminium 、 三甲基-(10-三甲基铵基癸基)铵二溴化物 、 乙基-(3-羟基苯基)-二甲基氯化铵 、 m-(N,N,N-trimethylammonio)trifluoromethylacetophenone 、 (-)-huperzine A 生成 6-丙烯酰-2-二甲氨基萘
  参考文献：
  名称：

  Ligand sensing fluorescent acetylcholinesterase for detection of organophosphate activity

  摘要：

  本发明涉及制备标记AChE和标记AChE抑制剂结合物组合物的方法以及用于检测有毒物质如有机磷、杀虫剂和其他神经毒剂积累的方法。本发明还涉及在各种领域中使用标记AChE和标记AChE抑制剂结合物组合物的方法，包括检测生物样本中的有毒物质，食品和水分析领域，环境监测领域和工业领域。

  公开号：

  US08642273B2

文献信息

• 7,11-Methanocycloocta[b]quinoline derivative as highly functionalizable acetylcholinesterase inhibitors
  申请人：Universite de Rouen

  公开号：EP2377853A1

  公开（公告）日：2011-10-19

  The present invention concerns new highly functionalizable Huprine derivatives of formula I: a method for preparing such compounds and their use for treating neurological diseases in which the level of acetylcholine is affected such as Alzheimer's disease; their use for affinity chromatography as well as their use as enantioselective catalyst.

  这项发明涉及公式I的新型高度功能化的Huprine衍生物：一种制备这类化合物的方法，以及它们用于治疗神经系统疾病（如阿尔茨海默病）中乙酰胆碱水平受影响的用途；它们用于亲和层析以及作为对映选择性催化剂的用途。
• [EN] BIS-CATIONIC COMPOUNDS AND USE THEREOF<br/>[FR] COMPOSES BIS-CATIONIQUES ET UTILISATION ASSOCIEE
  申请人：UNIV SYDNEY

  公开号：WO2005047230A1

  公开（公告）日：2005-05-26

  The present invention relates to bis-cationic compounds comprising quaternary ammonium groups and/or quaternary phosphonium groups. The invention also relates to the use of bis-cationic compounds as Phospholipase B inhibitors and the use of bis­ cationic compounds for the treatment or prevention of microbial infection.

  本发明涉及含有季铵基团和/或四元磷基团的双阳离子化合物。该发明还涉及将双阳离子化合物用作磷脂酶B抑制剂以及将双阳离子化合物用于治疗或预防微生物感染。
• Physical, chemical, and isotopic (atomic) labels
  申请人：Pearl Technology Holdings, LLC.

  公开号：US20040258617A1

  公开（公告）日：2004-12-23

  Chemical or isotopic labels are added to, e.g., a potentially lethal drug formulation, to generate a unique chemical fingerprint. Combinations of chemical additives are mixed with the drug to aid in their isolation and identification, especially when such drugs are used for illicit purposes. When stable isotopes are incorporated into lethal drugs, the labeling process conveys a very unique internal chemical signature and greatly aids in the identification of the parent drug in body fluids and tissues. When heath-care providers become aware that certain drugs can now be easily tracked and identified in a victim, individuals may be reluctant to utilize these agents for ill purposes.

  化学或同位素标记被添加到例如潜在致命的药物配方中，以生成独特的化学指纹。化学添加剂的组合与药物混合在一起，以帮助其隔离和识别，尤其是当这些药物被用于非法目的时。当稳定同位素被纳入致命药物中时，标记过程传达了非常独特的内部化学签名，并极大地帮助在体液和组织中识别母药。当医疗保健提供者意识到某些药物现在可以轻松跟踪和识别受害者时，个人可能会不愿意将这些药物用于不良目的。
• [EN] PROTEIN DEGRADERS AND USES THEREOF<br/>[FR] AGENTS DE DÉGRADATION DES PROTÉINES ET UTILISATIONS DE CES DERNIERS
  申请人：KYMERA THERAPEUTICS INC

  公开号：WO2019060742A1

  公开（公告）日：2019-03-28

  The present invention provides compounds, compositions thereof, and methods of using the same for the targeted degradation of proteins, and the treatment of target protein-mediated disorders.

  本发明提供了化合物、其组合物以及使用这些化合物的方法，用于靶向降解蛋白质，以及治疗靶蛋白介导的疾病。
• [EN] 7,11-METHANOCYCLOOCTA [B] QUINOLINE DERIVATIVE AS HIGHLY FUNCTIONALIZABLE ACETYLCHOLINESTERASE INHIBITORS<br/>[FR] DÉRIVÉ DE 7,11-METHANOCYCLOOCTA [B] QUINOLINE UTILISÉ COMME INHIBITEURS DE L'ACÉTYLCHOLINESTÉRASE POUVANT ÊTRE HAUTEMENT FONCTIONNALISÉS
  申请人：UNIV ROUEN

  公开号：WO2011124712A1

  公开（公告）日：2011-10-13

  The present invention concerns new highly functionalizable Huprine derivatives of formula I: a method for preparing such compounds and their use for treating neurological diseases in which the level of acetylcholine is affected such as Alzheimer's disease.

  本发明涉及公式I的新的高度可功能化的Huprine衍生物，以及制备这类化合物的方法，以及它们在治疗神经系统疾病中的应用，如阿尔茨海默病，其中乙酰胆碱水平受到影响。

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