Alpha-甲基-5-羟色胺马来酸盐 | 97469-12-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 中文名称: Alpha-甲基-5-羟色胺马来酸盐
• 中文别名: Α-甲基-5-羟色胺马来酸盐
• 英文名称: 2-methyl-5-hydroxytryptamine maleate
• 英文别名: α-methyl-5-hydroxytryptamine maleate；alpha-Methyl-5-HT maleate；alpha-Methyl-5-hydroxytryptamine maleate；3-(2-aminopropyl)-1H-indol-5-ol;(Z)-but-2-enedioic acid
• CAS: 97469-12-0
• 化学式: C₄H₄O₄*C₁₁H₁₄N₂O
• 分子量: 306.318
• InChiKey: YQNHFSXRABPJLP-BTJKTKAUSA-N

物化性质

• 溶解度：
  H2O：>3mg/mL，澄清（加热）

计算性质

• 辛醇/水分配系数(LogP)：
  1.47
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  137
• 氢给体数：
  5
• 氢受体数：
  6

文献信息

• Dopamine analog amide
  申请人：——

  公开号：US20010056116A1

  公开（公告）日：2001-12-27

  The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

  该发明涉及使用脂肪酸载体和神经活性药物形成前药。该前药在胃和血液流动环境中稳定，并可通过口服递送。该前药容易穿过血脑屏障。一旦进入中枢神经系统，前药被水解成脂肪酸载体和药物以释放药物。在首选实施方式中，载体是4,7,10,13,16,19二十二碳六烯酸，药物是多巴胺。两者都是中枢神经系统的正常成分。药物和载体之间的共价键通常是酰胺键，这种键可以在胃的条件下存活。因此，前药可以被摄入，并且不会在胃中完全水解成载体分子和药物分子。
• Serotonergic compositions and methods for treatment of mild cognitive impairment
  申请人：——

  公开号：US20020173511A1

  公开（公告）日：2002-11-21

  A method of treating Mild Cognitive Impairment has been discovered. The treatment method comprises administering an effective amount of a serotonergic agent, including, but not limited to dexnorfenfluramine. The agent can be any serotonergic agonist, partial agonist, serotonin reuptake inhibitor, or combinations of these agents. The treatment method also encompasses combinations of serotonergic agents and non-steroidal anti-inflammatory agents. The treatment method may also delay the onset of Mild Cognitive Impairment, dementia, or both.

  现已发现一种治疗轻度认知障碍的方法。该治疗方法包括施用有效量的血清素能制剂，包括但不限于右诺芬氟拉明。该药物可以是任何血清素能激动剂、部分激动剂、血清素再摄取抑制剂或这些药物的组合。治疗方法还包括血清素能药物和非甾体抗炎药物的组合。治疗方法还可以延缓轻度认知功能障碍、痴呆或两者的发生。
• Compositions of a cyclooxygenase-2 selective inhibitor and a serotonin-modulating agent for the treatment of neoplasia
  申请人：Masferrer L. Jaime

  公开号：US20050085477A1

  公开（公告）日：2005-04-21

  The present invention provides compositions and methods for the treatment of neoplasia in a subject. More particularly, the invention provides a combination therapy for the treatment of a neoplasia comprising the administration to a subject of a serotonin modulating agent in combination with a cyclooxygenase-2 selective inhibitor.

  本发明提供了用于治疗受试者肿瘤的组合物和方法。更具体地说，本发明提供了一种治疗肿瘤的组合疗法，包括向受试者施用5-羟色胺调节剂与环氧化酶-2选择性抑制剂。
• Compositions of a cyclooxygenase-2 selective inhibitor and a serotonin-modulating agent for the treatment of central nervous system damage
  申请人：Stephenson T. Diane

  公开号：US20050080084A1

  公开（公告）日：2005-04-14

  The present invention provides compositions and methods for the treatment of central nervous system damage in a subject. More particularly, the invention provides a combination therapy for the treatment of a central nervous system ischemic condition or a central nervous system traumatic injury comprising the administration to a subject of a serotonin-modulating agent in combination with a cyclooxygenase-2 selective inhibitor.

  本发明提供了治疗受试者中枢神经系统损伤的组合物和方法。更具体地说，本发明提供了一种用于治疗中枢神经系统缺血性疾病或中枢神经系统创伤性损伤的组合疗法，该疗法包括向受试者施用血清素调节剂与环氧化酶-2 选择性抑制剂。
• COMPOSITIONS OF A CYCLOOXYGENASE-2 SELECTIVE INHIBITOR AND A SEROTONIN MODULATING AGENT FOR THE TREATMENT OF NEOPLASIA
  申请人：Pharmacia Corporation

  公开号：EP1660079A2

  公开（公告）日：2006-05-31