R(-)-去甲阿朴吗啡氢溴酸盐 | 478-76-2

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 阿朴菲
• 中文名称: R(-)-去甲阿朴吗啡氢溴酸盐
• 中文别名: 6-庚炔醇
• 英文名称: Norapomorphine
• 英文别名: (6aR)-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol
• CAS: 478-76-2
• 化学式: C₁₆H₁₅NO₂
• 分子量: 253.29
• InChiKey: MHPQCGZBAVXCGA-GFCCVEGCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  19
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  52.5
• 氢给体数：
  3
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  R(-)-去甲阿朴吗啡氢溴酸盐 、 [11C]methyl iodide 、 N,N-二甲基甲酰胺 生成 R-[N-methyl-11C]norapomorphine hydrobromide
  参考文献：
  名称：

  LANGSTROEM, B.;ANTONI, G.;HALLDIN, C.;MALMBORG, P.;NAGREN, K.;RIMLAND, A.+, J. LABELLED COMPOUNDS AND RADIOPHARM., 1984, 21, N 11-12, 1200-1202

  摘要：

  DOI：

文献信息

• APOMORPHINE INHIBITORS OF AMYLOID-BETA (ABETA) FIBRIL FORMATION AND THEIR USE IN AMYLOIDOSIS BASED DISEASE
  申请人：Lashuel A. Hilal

  公开号：US20080096909A1

  公开（公告）日：2008-04-24

  Described is a new class of small molecule inhibitors of amyloid β protein (Aβ) aggregation, based on apomorphine. These molecules target the nucleation phase of Aβ self-assembly and interfere effectively with aggregation of Aβ 1-40 into amyloid fibrils in vitro as determined by transmission electron microscopy, Thioflavin T (ThT) fluorescence, and velocity sedimentation. Structure-activity studies using apomorphine analogues demonstrate that 10,11-dihydroxy substitutions of the D ring are preferred for the inhibitory effectiveness of these aporphines, and that methylation of these hydroxyl groups reduces their inhibitory potency. The ability of these small molecules to inhibit Aβ amyloid fibril formation appears to be linked to their ability to undergo auto-oxidation in solution, implicating an auto-oxidation product as the active Aβ inhibitor. Sedimentation velocity and electron microscopy studies demonstrate that apomorphine and analogues facilitate oligomerization of Aβ into short nonfibrillar soluble assemblies, but inhibit Aβ fibrillization.
• US7517853B2
  申请人：——

  公开号：US7517853B2

  公开（公告）日：2009-04-14
• US8822442B2
  申请人：——

  公开号：US8822442B2

  公开（公告）日：2014-09-02
• LANGSTROEM, B.;ANTONI, G.;HALLDIN, C.;MALMBORG, P.;NAGREN, K.;RIMLAND, A.+, J. LABELLED COMPOUNDS AND RADIOPHARM., 1984, 21, N 11-12, 1200-1202
  作者：LANGSTROEM, B.、ANTONI, G.、HALLDIN, C.、MALMBORG, P.、NAGREN, K.、RIMLAND, A.+

  DOI：——

  日期：——