GZ-793A | 1356449-58-5

• 分子结构分类: 有机化合物 - 生物碱及其衍生物
• 英文名称: GZ-793A
• 英文别名: (2R)-3-[(2S,6R)-2,6-bis[2-(4-methoxyphenyl)ethyl]piperidin-1-yl]propane-1,2-diol
• CAS: 1356449-58-5
• 化学式: C₂₆H₃₇NO₄
• 分子量: 427.584
• InChiKey: ZUFHEOXKGIZZGE-TZRRMPRUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  31
• 可旋转键数：
  11
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  62.2
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  (2R,6S)-2,6-bis[2-(4-methoxyphenyl)ethyl]piperidine 、 (S)-缩水甘油 以 乙硫醇 为溶剂， 生成 GZ-793A
  参考文献：
  名称：

  Exploring the effect of N-substitution in nor-lobelane on the interaction with VMAT2: discovery of a potential clinical candidate for treatment of methamphetamine abuse

  摘要：

  我们合成了一系列 N-取代的洛贝兰类似物，并评估了它们在囊泡单胺转运体上的[3H]二氢四苄肼结合亲和力及其对囊泡[3H]多巴胺摄取的抑制作用。化合物 19a 含有一个 N-1,2(R)-二羟基丙基，已被确定为治疗甲基苯丙胺滥用的潜在临床候选药物。

  DOI：

  10.1039/c3md20374c

文献信息

• Use of selective serotonin 5-HT1A receptor agonists for treating side-effects of VMAT inhibitors
  申请人：Neurolixis

  公开号：US11191758B2

  公开（公告）日：2021-12-07

  The present invention relates to the reduction of the side-effects induced by tetrabenazine or other inhibitors of vesicular monoamine transporter (VMAT), in the treatment of central nervous system disorders such as Huntington's disease, L-DOPA-induced dyskinesias in Parkinson's disease, Tourette's syndrome or tardive dyskinesia. The invention comprises administering to a patient in need thereof an effective amount of activates selective serotonin 5-HT1A receptors agonist, whereby the side-effects of depression or Parkinsonism induced by tetrabenazine or other VMAT inhibitors are minimized.

  本发明涉及在治疗亨廷顿氏病、帕金森氏病中L-DOPA诱导的运动障碍、抽动秽语综合征或迟发性运动障碍等中枢神经系统疾病时，减少四苯嗪或其他囊泡单胺转运体（VMAT）抑制剂诱发的副作用。本发明包括向有需要的患者施用有效量的活化选择性5-羟色胺5-HT1A受体激动剂，从而最大限度地减少由四苯嗪或其他VMAT抑制剂诱发的抑郁症或帕金森病的副作用。
• USE OF SELECTIVE SEROTONIN 5-HT1A RECEPTOR AGONISTS FOR TREATING SIDE-EFFECTS OF VMAT INHIBITORS
  申请人：Neurolixis

  公开号：EP3664787B1

  公开（公告）日：2022-07-20
• Use Of Selective Serotonin 5-HT1A Receptor Agonists For Treating Side-Effects Of VMAT Inhibitors
  申请人：Neurolixis

  公开号：US20200155535A1

  公开（公告）日：2020-05-21

  The present invention relates to the reduction of the side-effects induced by tetrabenazine or other inhibitors of vesicular monoamine transporter (VMAT), in the treatment of central nervous system disorders such as Huntington's disease, L-DOPA-induced dyskinesias in Parkinson's disease, Tourette's syndrome or tardive dyskinesia. The invention comprises administering to a patient in need thereof an effective amount of activates selective serotonin 5-IIT 1A receptors agonist, whereby the side-effects of depression or Parkinsonism induced by tetrabenazine or other VMAT inhibitors are minimized
• Exploring the effect of N-substitution in nor-lobelane on the interaction with VMAT2: discovery of a potential clinical candidate for treatment of methamphetamine abuse
  作者：Guangrong Zheng、David B. Horton、Narsimha Reddy Penthala、Justin R. Nickell、John P. Culver、Agripina G. Deaciuc、Linda P. Dwoskin、Peter A. Crooks

  DOI：10.1039/c3md20374c

  日期：——

  A series of N-substituted lobelane analogues was synthesized and evaluated for their [3H]dihydrotetrabenazine binding affinity at the vesicular monoamine transporter and for their inhibition of vesicular [3H]dopamine uptake. Compound 19a, which contains an N-1,2(R)-dihydroxypropyl group, had been identified as a potential clinical candidate for the treatment of methamphetamine abuse.

  我们合成了一系列 N-取代的洛贝兰类似物，并评估了它们在囊泡单胺转运体上的[3H]二氢四苄肼结合亲和力及其对囊泡[3H]多巴胺摄取的抑制作用。化合物 19a 含有一个 N-1,2(R)-二羟基丙基，已被确定为治疗甲基苯丙胺滥用的潜在临床候选药物。