氟卓林 | 70801-02-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯
• 中文名称: 氟卓林
• 英文名称: 8-fluoro-5-(4-fluorophenyl)-2-<4-(fluorophenyl)-4-hydroxy-butyl>-1,2,3,4-tetrahydro-γ-carboline
• 英文别名: flutroline；8-fluoro-5-(4-fluorophenyl)-2-<4-(4-fluorophenyl)-4-hydroxybutyl>-2,3,4,5-tetrahydro-1H-pyridio<4,3-b>indole；4-[8-fluoro-5-(4-fluoro-phenyl)-1,3,4,5-tetrahydro-pyrido[4,3-b]indol-2-yl]-1-(4-fluoro-phenyl)-butan-1-ol；4-[8-fluoro-5-(4-fluorophenyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-2-yl]-1-(4-fluorophenyl)butan-1-ol
• CAS: 70801-02-4
• 化学式: C₂₇H₂₅F₃N₂O
• 分子量: 450.504
• InChiKey: OYGDOCFZQVGFIP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  28.4
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  氟卓林 生成 8-fluoro-5-(4-fluorophenyl)-2-[(E)-4-(4-fluorophenyl)but-3-enyl]-3,4-dihydro-1H-pyrido[4,3-b]indole
  参考文献：
  名称：

  WELCH, W. M. ,, JR.

  摘要：

  DOI：
• 作为产物：
  描述：

  8-氟-1,3,4,5-四氢-2H-吡啶基-[4,3-b]吲哚-2-羧酸乙酯 在 氢氧化钾 、 lithium aluminium tetrahydride 、 水 、 sodium carbonate 、 N,N'-二环己基碳二亚胺 、 copper(I) bromide 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 反应 31.41h， 生成 氟卓林
  参考文献：
  名称：

  Neuroleptic activity in 5-aryltetrahydro-.gamma.-carbolines

  摘要：

  A series of 5-aryltetrahydro-gamma-carbolines was prepared by a novel N-arylation procedure and tested for neuroleptic activity in a rat antiamphetamine model. The systematic exploration of structural parameters leading to 8-fluoro-5-(4-fluorophenyl)-2-[4-hydroxy-4-(4-fluorophenyl)butyl]-2,3,5-tetrahydro-1H-pyrido[4,3-b]indole (CP-36,584, flutroline), a potent and long-acting neuroleptic compound, is described. These semirigid compounds provide a new, structurally distinct series with which to probe the conformational requirements for potent activity at the dopamine receptor.

  DOI：

  10.1021/jm00180a011

文献信息

• Co-administration of dopamine-receptor binding compounds
  申请人：Fernandes B. Prabhavathi

  公开号：US20070155720A1

  公开（公告）日：2007-07-05

  Methods for treating a patient having neurological, psychotic, and psychiatric disorders are described comprising the steps of administering to the patient an effective amount of a partial and/or full dopamine D 1 receptor agonist, and administering to the patient an effective amount of a dopamine D 2 receptor antagonist. Pharmaceutical compositions comprising a dopamine D 1 receptor agonist and a dopamine D 2 receptor antagonist are also described. The D 1 dopamine receptor agonist and the D 2 dopamine receptor antagonist can be administered to the patient in the same or in a different composition or compositions.

  描述了治疗患有神经、精神和精神障碍的患者的方法，包括向患者施用部分和/或全多巴胺D1受体激动剂的有效量，并向患者施用多巴胺D2受体拮抗剂的有效量。还描述了包含多巴胺D1受体激动剂和多巴胺D2受体拮抗剂的药物组合物。D1多巴胺受体激动剂和D2多巴胺受体拮抗剂可以以相同或不同的组合或组合物形式向患者施用。
• [EN] PRODRUG COMPOSITIONS AND METHODS OF TREATMENT<br/>[FR] COMPOSITIONS DE PROMÉDICAMENT ET PROCÉDÉS DE TRAITEMENT
  申请人：AQUESTIVE THERAPEUTICS INC

  公开号：WO2021087359A1

  公开（公告）日：2021-05-06

  Pharmaceutical compositions include a prodrug of epinephrine are described.

  药物组合物包括表述的肾上腺素前药。
• Multi-functional ionic liquid compositions for overcoming polymorphism and imparting improved properties for active pharmaceutical, biological, nutritional, and energetic ingredients
  申请人：Rogers D. Robin

  公开号：US20070093462A1

  公开（公告）日：2007-04-26

  Disclosed are ionic liquids and methods of preparing ionic liquid compositions of active pharmaceutical, biological, nutritional, and energetic ingredients. Also disclosed are methods of using the compositions described herein to overcome polymorphism, overcome solubility and delivery problems, to control release rates, add functionality, enhance efficacy (synergy), and improve ease of use and manufacture.

  揭示了离子液体及制备活性药物、生物、营养和能量成分的离子液体组合物的方法。还揭示了利用本文描述的组合物的方法，以克服多型性、克服溶解度和输送问题、控制释放速率、增加功能性、增强功效（协同作用）以及改善易用性和制造工艺。
• [EN] DREADD ACTUATORS<br/>[FR] ACTIONNEURS DREADD
  申请人：US HEALTH

  公开号：WO2019157083A1

  公开（公告）日：2019-08-15

  Disclosed is a compound of formula (I) in which R1, R2, and R3 are as described herein. Also provided are pharmaceutical compositions comprising the compound of formula (I) and methods of using the compound of formula (I), including a method of treating a disease or disorder and a method for effectuating a G-protein coupled receptor (GPCR)-mediated response in a subject.

  公开了一种化合物的化学式(I)，其中R1、R2和R3如本文所述。还提供了包含化合物的药物组合物的制剂(I)和使用化合物的方法(I)，包括治疗疾病或紊乱的方法以及在受试者中实现G蛋白偶联受体(GPCR)介导的反应的方法。
• COMPOSITIONS AND METHODS FOR TREATMENT OF VIRAL DISEASES
  申请人：Johansen Lisa M.

  公开号：US20100009970A1

  公开（公告）日：2010-01-14

  The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.

  本发明涉及用于治疗病毒性疾病的组合物、方法和试剂盒。在某些实施方式中，病毒性疾病是由单链RNA病毒、黄病毒科病毒或肝病毒引起的。在特定实施方式中，病毒性疾病是病毒性肝炎（例如甲型肝炎、乙型肝炎、丙型肝炎、丁型肝炎、戊型肝炎），药剂或药剂组合包括舍曲林、舍曲林类似物、UK-416244或UK-416244类似物。还包括用于鉴定可用于治疗病毒性疾病的新化合物的筛选方法。