(-)-phenserine

• 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
• 英文名称: (-)-phenserine
• 英文别名: Pyrrolo[2,3-b]indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, 5-(N-phenylcarbamate), (3aS,8aR)-, (2R,3R)-2,3-dihydroxybutanedioate (1:1);Pyrrolo[2,3-b]indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, 5-(N-phenylcarbamate), (3aS,8aR)-, (2R,3R)-2,3-dihydroxybutanedioate (1:1)；[(8bS)-3,4,8b-trimethyl-2,3a-dihydro-1H-pyrrolo[2,3-b]indol-7-yl] N-phenylcarbamate
• 化学式: C₂₀H₂₃N₃O₂
• 分子量: 337.422
• InChiKey: PBHFNBQPZCRWQP-IJHRGXPZSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  44.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (-)-phenserine 在 palladium on activated charcoal 盐酸 、 氢气 作用下， 以 甲醇 为溶剂， 以99%的产率得到(3S)-3-[2'-(methylamino)ethyl]-1,3-dihydro-1,3-dimethyl-2H-indol-5-yl N-phenylcarbamate
  参考文献：
  名称：

  Pei, Xue-Feng; Yu, Qian-Sheng; Holloway, Harold W., Medicinal Chemistry Research, 1999, vol. 9, # 1, p. 50 - 60

  摘要：

  DOI：

文献信息

• Transdermal delivery system for treatment of cognitive disorders
  申请人：Bruinsma B. Gosse

  公开号：US20050266060A1

  公开（公告）日：2005-12-01

  An improved transdermal delivery composition is provided containing a low molecular weight fatty acid, and a long chain fatty acid or a long chain fatty acid lower alkyl ester, wherein the long chain is between about 1 to about 21 carbons long and preferably, contains at least one cis-olefinic bond. Preferred long chain components are oleic acid and ethyl oleate while the preferred low molecular weight fatty acid is propionic acid. The product may be used for treating a cognitive disorder by administering phenserine through a subject's skin.

  提供了一种改进的经皮递送组合物，其中包含低分子量脂肪酸和长链脂肪酸或长链脂肪酸低烷基酯，其中长链为约1至约21个碳长，且最好含有至少一个顺式烯烃键。首选的长链成分是油酸和乙酰油酸乙酯，而首选的低分子量脂肪酸是丙酸。该产品可通过给予芬西林经皮途径治疗认知障碍。
• Combinatorial therapy with an acetylcholinesterase inhibitor and (3aR) 1,3a,8 trimethyl 1,2,3,3a,8,8a hexahydropyrrolo[2,3 b]indol 5 yl phenylcarbamate
  申请人：Axonyx, Inc.

  公开号：EP1576955A1

  公开（公告）日：2005-09-21

  The present invention relates to an improved method of treating, reducing or delaying cognitive impairments associated with the β-amyloid peptide, either in combination with treatment by cholinomimetic replacement therapy or as a prophylactic treatment.

  本发明涉及一种治疗、减轻或延缓与β-淀粉样肽相关的认知障碍的改进方法，该方法可与胆碱能替代疗法结合使用，也可作为一种预防性治疗方法。
• Use of phenserine and a HMG CoA reductase inhibitor for delaying Alzheimer's disease progression
  申请人：Axonyx, Inc.

  公开号：EP1604686A1

  公开（公告）日：2005-12-14

  The present invention relates to compositions and methods of treating a cognitive disorder in a subject by administering an effective amount of a phenserine compound or a pharmaceutically acceptable salt thereof and an effective amount of a HMG CoA reductase inhibitor or a pharmaceutically acceptable salt thereof to a subject, thereby treating a cognitive disorder in the subject.

  本发明涉及治疗受试者认知障碍的组合物和方法，其方法是向受试者施用有效量的表皮生长因子化合物或其药学上可接受的盐和有效量的 HMG CoA 还原酶抑制剂或其药学上可接受的盐，从而治疗受试者的认知障碍。
• Combination therapy to improve brain function or promote neurogenesis for treating neurodegenerative conditions
  申请人：UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC.

  公开号：US10751340B2

  公开（公告）日：2020-08-25

  Disclosed herein are methods and materials for improving brain function and/or promoting neurogenesis m a patient suffering from impaired brain function. Specifically exemplified herein ls the co-administration of phenserine and NBI-18. A method of treating a neurodegenerative disease in a patient in need thereof, said method comprising co-administering to the patient phenserine, or pharmaceutically acceptable salt thereof, and NBI-18, or pharmaceutically acceptable salt thereof, in respective amounts and frequency such that they work together to improve brain function or induce neurogenesis in the patient.

  本文公开了用于改善脑功能和/或促进脑功能受损患者神经发生的方法和材料。在此具体举例说明的是联合给药芬丝林和 NBI-18。一种治疗有需要的患者的神经退行性疾病的方法，所述方法包括以各自的用量和频率向患者联合给药表皮生长因子或其药学上可接受的盐和NBI-18或其药学上可接受的盐，使它们共同作用以改善患者的脑功能或诱导神经发生。
• Combinatorial therapy with an acetylcholinesterase inhibitor and (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3,-b]indol-5-yl phenylcarbamate
  申请人：Bruinsma B. Gosse

  公开号：US20050182044A1

  公开（公告）日：2005-08-18

  The present invention relates to an improved method of treating, reducing or delaying cognitive impairments associated with the β-amyloid peptide, either in combination with treatment by cholinomimetic replacement therapy or as a prophylactic treatment.

  本发明涉及一种治疗、减轻或延缓与β-淀粉样肽相关的认知障碍的改进方法，该方法可以与胆碱能替代疗法相结合，也可以作为预防性治疗。