3-(乙酰氨基)丙烷磺酸钙 | 77337-73-6

• 物质功能分类: 生物化工 - 生化试剂 - 激动剂抑制剂
• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机磺酸及其衍生物
• 中文名称: 3-(乙酰氨基)丙烷磺酸钙
• 中文别名: 乙酰高牛磺酸钙；阿坎酸钙
• CAS: 77337-73-6
• 化学式: C5H11CaNO4S
• 分子量: 221.29
• InChiKey: FQYZCUOYXXIDPF-UHFFFAOYSA-N

物化性质

• 熔点：
  >300°C
• 溶解度：
  在水中的溶解度>5mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  -0.98
• 重原子数：
  12
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  91.8
• 氢给体数：
  2
• 氢受体数：
  4

安全信息

• 危险品标志：
  Xi
• 危险类别码：
  R36/37/38
• 海关编码：
  2924199090
• 安全说明：
  S26,S36,S36/37/39
• WGK Germany：
  3
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H315,H319,H335

制备方法与用途

生物活性

Acamprosate（N-乙酰半胱氨醇，钙盐）是一种合成化合物，其化学结构与氨基酸神经递质γ-氨基丁酸（GABA）及牛磺酸相似。

用途

Acamprosate 是一种 GABA 受体激动剂和谷氨酸系统调节剂。

文献信息

• Orally administrable galenic form comprising metformine and an absorption-promoting agent
  申请人：MERCK PATENT GmbH

  公开号：EP1410791A1

  公开（公告）日：2004-04-21

  The present invention relates to an orally administrable galenic form allowing improved absorption by the transmembrane or paracellular route in the gastrointestinal tract of active ingredients which are hydrophilic or ionizable in physiological media, comprising at least one such active ingredient, an absorption-promoting agent having an HLB greater than 8, the said absorption-promoting agent consisting of one or more lipid substances chosen from: polysorbates; ethers of polyoxyethylene and alkyl; esters of polyoxyethylene and fatty acids; fatty acids; fatty alcohols; bile acids and their salts with pharmaceutically acceptable cations; esters of C1-C6 alkanol with fatty acids; esters of polyol with fatty acids, the said polyol comprising from 2 to 6 hydroxyl functional groups; and polyglycolysed glycerides; in combination with one or more pharmaceutically acceptable excipients, the pharmaceutical forms comprising captopril being excluded.

  本发明涉及一种可口服的galenic形式，可改善胃肠道对在生理介质中亲水性或可离子化的活性成分的跨膜或细胞旁途径吸收，该形式包括至少一种此类活性成分、一种HLB大于8的吸收促进剂，所述吸收促进剂由一种或多种脂质物质组成，这些脂质物质选自聚山梨醇酯；聚氧乙烯和烷基的醚；聚氧乙烯和脂肪酸的酯；脂肪酸；脂肪醇；胆汁酸及其与药学上可接受的阳离子的盐；C1-C6 烷醇与脂肪酸的酯；多元醇与脂肪酸的酯，所述多元醇包括 2 至 6 个羟基官能团；以及聚乙二醇化甘油酯；与一种或多种药学上可接受的赋形剂结合使用，不包括含有卡托普利的药剂。
• Methods of treating posttraumatic stress disorder with acamprosate salts
  申请人：Synchroneuron, Inc.

  公开号：US10512621B2

  公开（公告）日：2019-12-24

  Embodiments disclosed herein generally relate to methods of treating posttraumatic stress disorder (PTSD) using acamprosate formulations and/or acamprosate formulations in combination with at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.

  本文公开的实施方案一般涉及使用阿坎酸制剂和/或阿坎酸制剂与至少一种其他药物（如神经安定剂（抗精神病药）和/或抗抑郁药）联合治疗创伤后应激障碍（PTSD）的方法。
• Methods of treating tardive dyskinesia and other movement disorders
  申请人：——

  公开号：US20020013366A1

  公开（公告）日：2002-01-31

  The present invention describes a novel treatment for movement disorders, including tardive dyskinesia, tic disorders, Tourette's syndrome, and blepharospasm, and other focal dystonias. The treatment of the present invention utilizes agents that simultaneously act as NMDA-type glutamate receptor antagonists and GABA-A receptor agonists. Preferably these two activities are characteristic of a single agent, for example acamprosate. Alternatively, separate agents having these activities can be combined and administered together. The invention also provides a third agent that acts as a non-competitive NMDA-receptor blocking agent or ion channel blocker that augments the effect of the primary treatment. A particularly preferred ion channel blocking agent is magnesium. Alternatively, magnesium can be administered alone for prevention and treatment of movement disorders.

  本发明描述了一种治疗运动障碍的新型疗法，包括迟发性运动障碍、抽搐症、图雷特综合征、眼睑痉挛和其他局灶性肌张力障碍。本发明的治疗方法利用了同时作为 NMDA 型谷氨酸受体拮抗剂和 GABA-A 受体激动剂的制剂。这两种活性最好是一种药剂的特性，例如阿坎酸。或者，也可以将具有这些活性的不同药剂组合在一起给药。本发明还提供了第三种药剂，作为非竞争性 NMDA 受体阻断剂或离子通道阻断剂，可增强主要治疗的效果。特别优选的离子通道阻断剂是镁。另外，也可以单独使用镁来预防和治疗运动障碍。
• Treatment of posttraumatic strees disorder, obsessive-compulsive disorder and related neuropsychiatric disorders
  申请人：——

  公开号：US20020119912A1

  公开（公告）日：2002-08-29

  The present invention describes a novel treatment for neuropsychiatric disorders, including anxiety disorders, mood disorders, psychotic disorders, somatoform disorders, and neuropsychiatric symptoms resulting from movement disorders. The treatment of the present invention utilizes any agent that simultaneously act as NMDA-type glutamate receptor antagonists and GABA-A receptor agonists. Preferably these two activities are characteristic of a single agent, for example acamprosate (calcium N-acetylhomotaurinate). Alternatively, separate agents having these activities can be combined as a compound or mixture and thereby administered together. The invention also provides for a third agent that acts as a non-competitive NMDA-receptor blocking agent or ion channel blocker, that augments the effect of the primary treatment. A particularly preferred ion channel blocking agent is magnesium.

  本发明描述了一种治疗神经精神障碍的新型疗法，包括焦虑症、情绪障碍、精神障碍、躯体形式障碍和运动障碍导致的神经精神症状。本发明的治疗方法利用任何同时作为 NMDA 型谷氨酸受体拮抗剂和 GABA-A 受体激动剂的制剂。这两种活性最好是同一种药剂的特性，例如阿坎酸（N-乙酰基高马尿酸钙）。或者，也可以将具有这些活性的不同药剂组合成化合物或混合物，从而一起给药。本发明还提供了作为非竞争性 NMDA 受体阻断剂或离子通道阻断剂的第三种药剂，可增强主要治疗的效果。特别优选的离子通道阻断剂是镁。
• ORALLY ADMINISTRABLE IMMEDIATE-RELEASE AND PROLONGED-RELEASE GALENIC FORM COMPRISING AN ABSORPTION-PROMOTING AGENT AND USE OF THIS ABSORPTION-PROMOTING AGENT
  申请人：MERCK PATENT GmbH

  公开号：EP1056445A1

  公开（公告）日：2000-12-06