[(1R,15S,17S)-17-ethyl-3,13-diazapentacyclo[13.3.1.02,10.04,9.013,18]nonadeca-2(10),4(9),5,7-tetraen-7-yl]methanol

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 依波格型生物碱
• 英文名称: [(1R,15S,17S)-17-ethyl-3,13-diazapentacyclo[13.3.1.02,10.04,9.013,18]nonadeca-2(10),4(9),5,7-tetraen-7-yl]methanol
• 化学式: C₂₀H₂₆N₂O
• 分子量: 310.4
• InChiKey: ZKRUBMGTGMPTIC-OCKILCDSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  23
• 可旋转键数：
  2
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  39.3
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• METHODS AND COMPOSITIONS FOR REDUCING TOLERANCE TO OPIOID ANALGESICS
  申请人：DemeRx, Inc.

  公开号：US20150258108A1

  公开（公告）日：2015-09-17

  A method for modulating tolerance to an opioid analgesic in a patient undergoing opioid analgesic therapy, the method comprising interrupting or administering concurrently with said opioid analgesic therapy an amount of noribogaine, noribogaine derivative, or pharmaceutically acceptable salt and/or solvate thereof that provides a therapeutic serum concentration of noribogaine. In some embodiments, the therapeutic average serum concentration is 50 ng/mL to 180 ng/mL, said concentration being sufficient to re-sensitize the patient to the opioid as an analgesic while maintaining a QT interval of less than about 500 ms during said treatment.

  一种用于调节接受阿片类镇痛治疗的患者对阿片类镇痛剂的耐受性的方法，该方法包括在阿片类镇痛治疗期间中断或同时给予一定量的诺利波甲胺、诺利波甲胺衍生物或其药学上可接受的盐和/或溶剂，以提供治疗性血清浓度的诺利波甲胺。在某些实施例中，治疗性平均血清浓度为50ng/mL至180ng/mL，该浓度足以使患者对阿片类镇痛剂重新敏感作为镇痛剂，同时在治疗期间维持QT间期小于约500ms。
• N-SUBSTITUTED NORIBOGAINE PRODRUGS
  申请人：DemeRx, Inc.

  公开号：US20140315891A1

  公开（公告）日：2014-10-23

  This invention relates generally to prodrugs of noribogaine. This invention also relates to pharmaceutical compositions comprising the prodrugs of noribogaine as well as method of treating pain, addiction and/or stress using such compounds and/or pharmaceutical compositions.
• METHOD FOR NORIBOGAINE TREATMENT IN PATIENTS ON METHADONE
  申请人：DemeRx, Inc.

  公开号：US20150045350A1

  公开（公告）日：2015-02-12

  A short treatment with noribogaine shows promise for treating drug dependency. Many opioid addicts are treated with methadone. Giving noribogaine to mammal concurrently being administered methadone surprisingly exacerbates methadone's negative side-effects, and increases the risk of death. Therefore, prior to noribogaine treatment, a patient on methadone therapy undergoes a period of methadone abstinence to wash out the methadone. Surprisingly, noribogaine does not react negatively to morphine. According to the invention, methadone regimen is replaced with morphine prior to noribogaine treatment.
• METHODS FOR ACUTE AND LONG-TERM TREATMENT OF DRUG ADDICTION
  申请人：DemeRx, Inc.

  公开号：US20150231147A1

  公开（公告）日：2015-08-20

  This invention is directed to a method of treating opioid or opioid-like drug addiction, including acute and post-acute withdrawal symptoms, comprising treating an addicted patient with noribogaine at a dosage that provides an average serum concentration of about 50 ng/mL to about 180 ng/mL under conditions where the QT interval prolongation does not exceed about 50 milliseconds.
• USE OF NORIBOGAINE FOR THE TREATMENT OF PAIN
  申请人：DemeRX, Inc.

  公开号：US20150258104A1

  公开（公告）日：2015-09-17

  This invention is directed to methods of treating pain in patients comprising treating patients with noribogaine at a dosage that provides an average serum concentration of 50 ng/mL to 180 ng/mL, including under conditions where the QT interval prolongation does not exceed about 50 milliseconds.