but-2-enedioate;hydron;1-[10-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl]phenothiazin-2-yl]ethanone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻嗪类
• 英文名称: but-2-enedioate;hydron;1-[10-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propyl]phenothiazin-2-yl]ethanone
• 化学式: C31H37N3O10S
• 分子量: 643.7
• InChiKey: NUKVZKPNSKJGBK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.92
• 重原子数：
  45
• 可旋转键数：
  11
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  222
• 氢给体数：
  5
• 氢受体数：
  14

文献信息

• Novel Pharmaceutical Compositions for Treating Chronic Pain and Pain Associated with Neuropathy
  申请人：Singh Chandra U.

  公开号：US20130189354A1

  公开（公告）日：2013-07-25

  The present invention relates to compositions and methods for treating pain wherein the compositions comprise a combination of tramadol or a pharmaceutically acceptable salt thereof, magnesium or a pharmaceutically acceptable salt thereof; and gabapentin or pregabalin. The therapeutic combination can further contain capsaicin or an ester of capsaicin.

  本发明涉及用于治疗疼痛的组合物和方法，其中所述组合物包括曲马多或其药学上可接受的盐、镁或其药学上可接受的盐；以及加巴嘌醇或普瑞巴林。治疗组合物还可以包含辣椒素或辣椒素酯。
• PHARAMACEUTICAL COMPOSITIONS FOR TREATING CHRONIC PAIN AND PAIN ASSOCIATED WITH NEUROPATHY
  申请人：Singh Chandra Ulagaraj

  公开号：US20110039875A1

  公开（公告）日：2011-02-17

  The present invention provides methods and compositions for the treatment of neuropathic pain. In certain embodiments, compositions comprising an dextromethorphan (or other N-methyl-D-aspartate receptor antagonist), tramadol, and gabapentin can synergistically act to reduce pain in a human patient. Pharmaceutical compositions may also comprise a capsaicinoid, an esterified capsaicinoid, and/or a tricyclic antidepressant.

  本发明提供了治疗神经病痛的方法和组合物。在某些实施例中，含有右美沙芬（或其他N-甲基-D-天门冬氨酸受体拮抗剂）、曲马多和加巴喷丁的组合物可以协同作用于人类患者，以减轻疼痛。药物组合物也可以包括辣椒素类、酯化辣椒素类和/或三环抗抑郁剂。
• Inhibiting the development of tolerance to and/or dependence on an additive substance
  申请人：VIRGINIA COMMONWEALTH UNIVERSITY

  公开号：EP0608893A1

  公开（公告）日：1994-08-03

  Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA receptor activation, e.g., a ganglioside such as GM₁ or GT1b, a phenothiazine such as trifluoperazine or a naphthalenesulfonamide such as N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide, inhibit the development of tolerance to and/or dependence on addictive drugs, e.g., narcotic analgesics such as morphine, codeine, etc.

  阻断 N-甲基-D-天冬氨酸（NMDA）受体的无毒物质，如右美沙芬或右美沙芬等吗啡烷，或阻断 NMDA 受体激活的一种主要细胞内后果的物质，如神经节苷脂，如 GM₁或 GT1b，三氟拉嗪等吩噻嗪，或 N-(6-氨基己烷基)萘磺酰胺等、 神经节苷脂，如 GM₁或 GT1b；吩噻嗪，如三氟拉嗪；或萘磺酰胺，如 N-（6-氨基己基）-5-氯-1-萘磺酰胺；抑制对成瘾性药物，如吗啡、可待因等麻醉性镇痛药的耐受性和/或依赖性。
• Use of NMDA antagonists for the treatment of pain
  申请人：VIRGINIA COMMONWEALTH UNIVERSITY

  公开号：EP0615749A2

  公开（公告）日：1994-09-21

  A method of alleviating pain such as neuropathic pain or acute inflammatory pain is provided which comprises administering to a mammal that is either exhibiting pain or is about to be subjected to a pain-causing event a pain alleviating/pain suppressing amount of at least one nontoxic antagonist for the N-methyl-D-aspartate receptor, e.g., dextrorphan, or metabolic precursor of such antagonist, e.g., dextromethorphan, or at least one nontoxic substance that blocks a major intracellular consequence of N-methyl-D-aspartate receptor activation, e.g., a phenothiazine such as trifluoperazine.

  本发明提供了一种减轻疼痛（如神经性疼痛或急性炎症性疼痛）的方法，该方法包括向表现出疼痛或即将遭受致痛事件的哺乳动物施用至少一种N-甲基-D-天冬氨酸受体无毒拮抗剂（如右美沙芬）或这种拮抗剂的代谢前体（如右美沙芬）或至少一种阻断细胞内主要后果的无毒物质，以减轻疼痛/抑制疼痛、右美沙芬，或这种拮抗剂的代谢前体，如右美沙芬，或至少一种阻断 N-甲基-D-天冬氨酸受体激活的主要细胞内后果的无毒物质，如吩噻嗪，如三氟拉嗪。
• Pharmaceutical compositions for treating chronic pain and pain associated with neuropathy
  申请人：Singh Chandra Ulagaraj

  公开号：US10300031B2

  公开（公告）日：2019-05-28

  The present invention provides methods and compositions for the treatment of neuropathic pain. In certain embodiments, compositions comprising an dextromethorphan (or other N-methyl-D-aspartate receptor antagonist), tramadol, and gabapentin can synergistically act to reduce pain in a human patient. Pharmaceutical compositions may also comprise a capsaicinoid, an esterified capsaicinoid, and/or a tricyclic antidepressant.

  本发明提供了治疗神经性疼痛的方法和组合物。在某些实施方案中，由右美沙芬（或其他 N-甲基-D-天冬氨酸受体拮抗剂）、曲马多和加巴喷丁组成的组合物可以协同作用，减轻人类患者的疼痛。药物组合物还可包含辣椒素、酯化辣椒素和/或三环抗抑郁剂。