2-甲基血清素马来酸盐 | 78263-91-9

• 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: 2-甲基血清素马来酸盐
• 英文名称: 2-Methyl-5-hydroxytryptamine maleate
• 英文别名: 3-(2-aminoethyl)-2-methyl-1H-indol-5-ol;(Z)-but-2-enedioic acid
• CAS: 78263-91-9
• 化学式: C15H18N2O5
• 分子量: 306.31
• InChiKey: KFEAUMZKRNJEDU-BTJKTKAUSA-N

物化性质

• 熔点：
  186-187 °C
• 溶解度：
  H2O：可溶5mg/mL，澄清

计算性质

• 辛醇/水分配系数(LogP)：
  1.39
• 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

安全信息

• 海关编码：
  2933990090

制备方法与用途

生物活性

2-甲基-5-HT马来酸盐（2-甲基-5-羟色胺马来酸盐）是一种有效的选择性 5-HT3 受体激动剂，并显示出抗抑郁样作用。

靶点

5-HT₃受体

体内研究

2-甲基-5-HT马来酸盐 (2-甲基-5-羟色胺马来酸盐) 在腹腔注射 (i.p.) 下，剂量为 3 mg/kg，作用45分钟后，显著减少了不动时间（与对照组相比），显示出抗抑郁样效应。

动物模型	雄性 Sprague-Dawley 大鼠
剂量	3 mg/kg
给药方式	腹腔注射；45分钟
结果	显著减少不动时间，显示出抗抑郁样效应

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。
• 5-HT3 receptor agonists as neuroprotectors
  申请人：——

  公开号：US20040191312A1

  公开（公告）日：2004-09-30

  The invention discloses methods and compositions useful for treating and preventing neurodegenerative diseases. The methods and compositions utilize agonists for the 5-HT3 receptors. These molecules can be delivered alone or in combination with agents which treat or prevent neurodegenerative diseases such as those caused by ischemic stroke, Alzheimer's disease, diabetic peripheral neuropathy, multiple sclerosis, amyotrophic lateral sclerosis, traumatic brain injury, spinal cord injury, Huntington's disease or Parkinson's disease.

  本发明公开了用于治疗和预防神经退行性疾病的方法和组合物。这些方法和组合物利用 5-HT3 受体的激动剂。这些分子可以单独给药，也可以与治疗或预防神经退行性疾病的药物结合使用，如缺血性中风、阿尔茨海默病、糖尿病周围神经病变、多发性硬化症、肌萎缩性脊髓侧索硬化症、脑外伤、脊髓损伤、亨廷顿氏病或帕金森氏病引起的疾病。
• METHODS FOR TREATING NEUROLOGICAL DISORDERS OR DAMAGE
  申请人：Tyers Mike

  公开号：US20090076019A1

  公开（公告）日：2009-03-19

  A clonogenic neurosphere assay is described that carries out high throughput screens (HTS) to identify potent and/or selective modulators of proliferation, differentiation and/or renewal of neural precursor cells, neural progenitor cells and/or self-renewing and multipotent neural stem cells (NSCs). Compositions comprising the identified modulators and methods of using the modulators and compositions, in particular to treat neurological disorders (e.g. brain or CNS cancer) or damage are also disclosed.
• US5994392A
  申请人：——

  公开号：US5994392A

  公开（公告）日：1999-11-30