N-[4-[2-(6-cyano-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]cyclohexyl]quinoline-4-carboxamide | 215803-78-4

• 物质功能分类: 生物化工 - 生化试剂 - 激动剂抑制剂
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: N-[4-[2-(6-cyano-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]cyclohexyl]quinoline-4-carboxamide
• CAS: 215803-78-4
• 化学式: C₂₈H₃₀N₄O
• 分子量: 438.6
• InChiKey: OLWRVVHPJFLNPW-UHFFFAOYSA-N

物化性质

• 沸点：
  679.3±55.0 °C(Predicted)
• 密度：
  1.23
• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  33
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  69
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• NOVEL DOPAMINE D3 RECEPTOR LIGANDS AND PREPARATION AND MEDICAL USES OF THE SAME
  申请人：INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY ACADEMY OF MILITARY MEDICAL SCIENCES

  公开号：US20140329831A1

  公开（公告）日：2014-11-06

  The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.

  本发明涉及一种新的哌嗪衍生物，其化学式为I，具有调节多巴胺D3受体的活性，其立体异构体，药学上可接受的盐或溶剂，以及包含该化合物的制药组合物，其制备过程以及在预防或治疗与中枢神经系统功能障碍相关的疾病，如帕金森病、精神分裂症、药物成瘾和复发，以及肾脏保护和免疫调节方面的用途，或作为研究D3R功能或与D3R功能障碍相关的疾病的工具。
• Method for in vivo detection of antipsychotic properties of dopamine D3 receptor ligands
  申请人：Institut National de la Santé et de la Recherche Médicale (INSERM)

  公开号：EP1462117A1

  公开（公告）日：2004-09-29

  The invention provides a method in vivo detecting anti-D3 receptor activity of dopamine D3 receptor ligands. The method of the invention makes use of a NMDA glutamate receptor antagonist to induce D3-mediated behavioral abnormalities and assess reversing effects of candidate ligands. The invention further relates to the use of a dopamine D3 receptor partial agonist or antagonist for the treatment of a substance-induced psychotic disorder or a dyskinesia associated with associated with dopamine agonist therapy.

  本发明提供了一种体内检测多巴胺 D3 受体配体抗 D3 受体活性的方法。本发明的方法利用 NMDA 谷氨酸受体拮抗剂诱导 D3 介导的行为异常，并评估候选配体的逆转效应。本发明进一步涉及使用多巴胺 D3 受体部分激动剂或拮抗剂治疗物质诱发的精神障碍或与多巴胺激动剂治疗相关的运动障碍。
• Essential tremor diagnostic and treatment
  申请人：INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)

  公开号：EP1591455A1

  公开（公告）日：2005-11-02

  The invention relates to an in vitro method for diagnosing essential tremor wherein a mutation of dopamine D3 receptor gene or protein is sought. The invention further relates to the use of a ligand having anti-dopamine D3 receptor activity for treatment of essential tremor.

  本发明涉及一种诊断本质性震颤的体外方法，其中寻找多巴胺 D3 受体基因或蛋白的突变。本发明还涉及一种具有抗多巴胺 D3 受体活性的配体用于治疗本质性震颤的用途。
• Compositions and methods for the treatment of neurodegenerative diseases
  申请人：Staunton Jane

  公开号：US20060270742A1

  公开（公告）日：2006-11-30

  The invention features compositions and methods for the treatment of neurodegenerative diseases.
• ESSENTIAL TREMOR DIAGNOSTIC AND TREATMENT
  申请人：Sokoloff Pierre

  公开号：US20090209551A1

  公开（公告）日：2009-08-20

  The invention relates to an in vitro method for diagnosing essential tremor wherein a mutation of dopamine D3 receptor gene or protein is sought. The invention further relates to the use of a ligand having anti-dopamine D3 receptor activity for treatment of essential tremor.