N-(7-fluoro-1-naphthyl)-N'-(m-ethylphenyl)-N'-methylguanidine hydrochloride | 137160-21-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: N-(7-fluoro-1-naphthyl)-N'-(m-ethylphenyl)-N'-methylguanidine hydrochloride
• 英文别名: 1-(3-ethylphenyl)-2-(7-fluoronaphthalen-1-yl)-1-methylguanidine;hydrochloride
• CAS: 137160-21-5
• 化学式: C₂₀H₂₀FN₃*ClH
• 分子量: 357.858
• InChiKey: DTPKZERSDMIXEL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.05
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  41.6
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  N-(m-ethylphenyl)-N-methylcyanamide 、 7-fluoro-1-aminonaphthalene hydrochloride 在 sodium hydroxide 、 甲醇盐酸 、 silica gel 作用下， 以 二氯甲烷 为溶剂， 反应 2.5h， 以to give N-(7-fluoro-1-naphthyl)-N'-(m-ethylphenyl)-N'-methylguanidine hydrochloride (192 mg, 53%) as off-white crystals的产率得到N-(7-fluoro-1-naphthyl)-N'-(m-ethylphenyl)-N'-methylguanidine hydrochloride
  参考文献：
  名称：

  Tri-and tetra-substituted guanidines and their use as excitatory amino

  摘要：

  三取代和四取代的胍基化合物具有高结合亲和力，可与苯环哌啶（PCP）受体结合，并更倾向于低亲和力与大脑西格玛受体结合。这些胍基衍生物作为非竞争性抑制剂，通过阻断NMDA受体离子通道复合物的离子通道作用，从而抑制谷氨酸诱导的NMDA受体反应。这些化合物因此具有神经保护作用，并可用于治疗缺氧、低血糖、脑或脊髓缺血、脑或脊髓创伤以及癫痫、阿尔茨海默病、肌萎缩性侧索硬化、帕金森病、亨廷顿病、唐氏综合症、科萨科夫病和其他神经退行性疾病的治疗。

  公开号：

  US05767162A1

文献信息

• Tri- and tetra-substituted guanidines and their use as excitatory amino
  申请人：State of Oregon, acting by and through the Oregon State Board of Higher

  公开号：US05637622A1

  公开（公告）日：1997-06-10

  Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

  三取代和四取代的胍基化合物具有高结合亲和力，可与苯环环庚啡（PCP）受体结合，更好的是，它们对大脑σ受体的亲和力较低。这些胍基衍生物作为非竞争性抑制剂，通过作为NMDA受体离子通道复合物的通道阻滞剂，阻止谷氨酸诱导的NMDA受体反应。这些化合物因此具有神经保护活性，并可用于治疗低氧、低血糖、脑或脊髓缺血、脑或脊髓创伤引起的神经元丧失，并且对于治疗癫痫、阿尔茨海默病、肌萎缩性侧索硬化、帕金森病、亨廷顿病、唐氏综合症、科萨科夫病和其他神经退行性疾病也有用。
• Tri-and tetra-substituted guanidines and their use as excitatory amino
  申请人：State of Oregon, acting by and through the Oregon State Board of Higher

  公开号：US05767162A1

  公开（公告）日：1998-06-16

  Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

  三取代和四取代的胍基化合物具有高结合亲和力，可与苯环哌啶（PCP）受体结合，并更倾向于低亲和力与大脑西格玛受体结合。这些胍基衍生物作为非竞争性抑制剂，通过阻断NMDA受体离子通道复合物的离子通道作用，从而抑制谷氨酸诱导的NMDA受体反应。这些化合物因此具有神经保护作用，并可用于治疗缺氧、低血糖、脑或脊髓缺血、脑或脊髓创伤以及癫痫、阿尔茨海默病、肌萎缩性侧索硬化、帕金森病、亨廷顿病、唐氏综合症、科萨科夫病和其他神经退行性疾病的治疗。
• EP0517852A4
  申请人：——

  公开号：EP0517852A4

  公开（公告）日：1994-03-02
• TRI- AND TETRA-SUBSTITUTED GUANIDINES AND THEIR USE AS EXCITATORY AMINO ACID ANTAGONISTS
  申请人：STATE OF OREGON, acting by and through THE OREGON STATE BOARD OF HIGHER EDUCATION, acting for and on behalf of

  公开号：EP0517852A1

  公开（公告）日：1992-12-16
• US5262568A
  申请人：——

  公开号：US5262568A

  公开（公告）日：1993-11-16