FAUC 73

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: FAUC 73
• 英文别名: (4-ethynylcyclohex-3-enyl)dipropylamine；FAU C73；(4-Ethynyl-3-cyclohexenyl)dipropylamine；4-ethynyl-N,N-dipropylcyclohex-3-en-1-amine
• 化学式: C₁₄H₂₃N
• 分子量: 205.343
• InChiKey: IOUKEEFTYOZOKJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  15
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  trifluoromethanesulfonic acid 4-dipropylaminocyclohex-1-enyl ester 在 copper(l) iodide 、 四(三苯基膦)钯 、 二甲基十二/十四烷基叔胺 、 四丁基氟化铵 作用下， 以 四氢呋喃 为溶剂， 反应 0.75h， 生成 FAUC 73
  参考文献：
  名称：

  Conjugated Enynes as Nonaromatic Catechol Bioisosteres:  Synthesis, Binding Experiments, and Computational Studies of Novel Dopamine Receptor Agonists Recognizing Preferentially the D₃ Subtype

  摘要：

  To evaluate nonaromatic catechol bioisosteres, the conformationally restrained enynes 1 and enediynes 2 were synthesized via palladium-catalyzed coupling as the key reaction step. Subsequent receptor binding studies at the dopamine receptor subtypes D-1, D-2 long, D-2 short, D-3, and D-4 showed highly interesting binding profiles for the enynes la and 1b when compared to dopamine. At the guanine nucleotide-sensitive high-affinity binding site of the Da receptor, the target compound 1b (K-i = 5.2 nM) was 10-fold more potent than dopamine but less potent at the D-2 and D-4 subtypes. In contrast to dopamine the agonists la and Ib showed strong selectivity for the receptors of the D-2 family (D-2-D-4) As far as We know, this study represents the first report on nonaromatic dopamine agonists. Comparison of molecular electrostatic potentials, derived from semiempirical molecular orbital calculations, and lipophilicity maps was performed.

  DOI：

  10.1021/jm991098z

文献信息

• Novel D3 Dopamine Receptor Agonists to Treat Dyskinesia in Parkinson's Disease
  申请人：College of Medicine Philadelphia Health & Education Corporation d/b/a Drexel University

  公开号：US20140228355A1

  公开（公告）日：2014-08-14

  The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.

  本发明提供了一种方法，用于抑制、抑制或预防帕金森病患者的左旋多巴诱发的运动障碍，包括向患者给予至少一种本发明化合物的药物组合物。本发明还提供了一种方法，用于抑制、抑制或预防帕金森病患者的病情，包括向患者给予至少一种本发明化合物的药物组合物。
• D3 dopamine receptor agonists to treat dyskinesia in Parkinson's disease
  申请人：DREXEL UNIVERSITY

  公开号：US10543180B2

  公开（公告）日：2020-01-28

  The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.

  本发明提供了一种抑制、抑制或预防帕金森病患者左旋多巴诱发的运动障碍的方法，包括向患者施用包含至少一种本发明化合物的药物组合物的步骤。本发明进一步提供了一种抑制、抑制或预防患者帕金森病的方法，包括向患者施用包含至少一种本发明化合物的药物组合物的步骤。
• NOVEL D3 DOPAMINE RECEPTOR AGONISTS TO TREAT DYSKINESIA IN PARKINSON'S DISEASE
  申请人：Philadelphia Health and Education Corporation

  公开号：EP2603215A2

  公开（公告）日：2013-06-19
• US9289400B2
  申请人：——

  公开号：US9289400B2

  公开（公告）日：2016-03-22
• US9675565B2
  申请人：——

  公开号：US9675565B2

  公开（公告）日：2017-06-13