期刊文献+
任意字段
题名或关键词
题名
关键词
文摘
作者
第一作者
机构
刊名
分类号
参考文献
作者简介
基金资助
栏目信息

[^(125)I]TZDM的制备

Preparation of [^(125)I]TZDM
下载PDF
导出
摘要 优良的Aβ显像剂必须对Aβ斑块有较高的亲和性,而体外竞争结合实验是筛选Aβ斑块显像剂的有效方法,实验中需要使用放射性配基[125I]TZDM。以对溴苯胺为起始原料,经过四步反应合成了[125I]TZDM的前体化合物Bu3Sn-TZDM,并通过125I进行标记制备了[125I]TZDM,标记率为62.5%。粗产物通过HPLC分离后,获得放射化学纯度大于97%的[125I]TZDM,实际产率为25%。 An excellent Aβ vitro competition binding imaging agent must have high assay is an effective method affinity for Aβ plaques. The in for determining the affinity of unlabelled imaging agents for Aβ plaques. [125Ⅰ]TZDM was often used as a radioactive ligand in the assay. In this paper, Bu3 Sn-TZDM, a precursor compound of [125Ⅰ]TZDM, was synthesized by four steps from 4-bromo-aniline. After the precursor compound was labeled with [125Ⅰ], crude [125Ⅰ]TZDM was obtained. The labelling yield is 62.5%. [125Ⅰ]TZDM is separated with HPLC and has more than 97% radiochemical purity. The actual yield is 25%.
作者 王武尚 张锦明 刘伯里
机构地区 西北核技术研究所 北京师范大学化学学院 解放军总医院核医学科
出处 《核化学与放射化学》 CAS CSCD 北大核心 2010年第1期57-60,共4页 Journal of Nuclear and Radiochemistry
基金 国家自然科学基金资助项目(No.30640042)
关键词 阿尔茨海默病 [125I]TZDM Aβ斑块 Aβ显像剂 Alzheimer＇s disease [125Ⅰ]TZDM Aβ plaques Aβ imaging agent
分类号 O614.712 [理学—无机化学]
  • 相关文献

参考文献13

  • 1王武尚,张锦明,刘伯里.AD脑Aβ放射性显像剂的研究进展[J].同位素,2004,17(4):232-240. 被引量：8
  • 2Engler H, Blomqvist G, Bergstrom M, et al. First Human Study With a Benzothiazole Amyloid-Imaging Agent in Alzheimer's Disease and Control Subjects[J]. Neurobiol Aging, 2002, 23(1):S429.
  • 3Patoine B. Advances in Alzheimer's Diagnostic Tools Expected to Speed Drug Trials [J]. Brain Work, 2002, 12(5): 1-2.
  • 4Schmitt F A, Davis D G, Wekstein D R, et al. "Preclinical" AD Revisited: Neuropathology of Cognitively Normal Older Adults[J]. Neurology, 2000, 55: 370-376.
  • 5Klunk W E, Engler H, Nordberg A, et al. Imaging Brain Amyloid in Alzheimer's Disease With Pittsburgh Compound-B[J]. Ann Neurol, 2004, 55:306-319.
  • 6Kung M P, Zhuang Z P, Hou C, et al. Characterization of Radioiodinated Ligand Binding to Amyloid Beta Plaques[J]. J Mol Neurosci, 2003, 20: 249- 254.
  • 7Zhuang Z P, Kung M P, Hou C, et al. Radioiodinated Styrylbenzenes and Thioflavins as Probes for Amyloid Aggregates[J]. J Med Chem, 2001, 44(12): 1 905-1 914.
  • 8Ono M, Wilsonc A, Nobregac J, et al. ^11C-Labeled Stilbene Derivatives as All-Aggregate-Specific PET Imaging Agents for Alzheimer's Disease[J].Nucl Med Biol, 2003, 30: 565-571.
  • 9Zhuang Z P, Kung M P, Hou C, et al, IBOX(2-(4 '-Dimethylaminophenyl)-6-Iodobenzoxazole) : A Ligand for Imaging Amyloid Plaques in the Brain[J]. Nucl Med Biol, 2001, 28: 887-894.
  • 10Ono M, Kung M P, Hou C, et al. Benzofuran Derivatives as Aβ-Aggregate-Specific Imaging Agents for Alzheimer's Disease[J]. Nucl Med Biol, 2002, 29: 633-642.

二级参考文献48

  • 1Wang Y, Klunk WE, Huang GF, et al. Development of 123I-labelled Agents for Amyloid Imaging[J]. J Labelled Cpd Radiopharm, 2003, 46: S173.
  • 2Vanderghinste D, Eeckhoudt MV, Cleynhens J, et al. Synthesis and Preliminary Evaluation of 99mTc-BAT-thioflavine T Derivatives for in Vivo Visualization of Amyloid β[A]. Nicolini M, Mazzi U. Technetium, Rhenium and Other Metals in Chemistry and Nuclear Medicine[C]. Italy: SGE, 2002. 463～465.
  • 3Pelecanou M, Pirmettis I, Patsis G, et al. Tricarbonyl Complexes of Re and Tc With a Bifunctional Tridentate NNO Ligand Carrying the 2-Phenyl-Benzothiazole Moiety[J]. J Labelled Cpd Radiopharm, 2003, 46: S25.
  • 4Zhuang ZP, Kung MP, Hou C, et al. IBOX(2-(4′-dimethylaminophenyl)-6-iodobenzoxazole): a Ligand for Imaging Amyloid Plaques in the Brain[J]. Nucl Med Biol, 2001, 28: 887～894.
  • 5Ono M, Kung MP, Hou C, et al. Benzofuran Derivatives as Aβ-aggregate-specific Imaging Agents for Alzheimer's Disease[J]. Nucl Med Biol, 2002, 29: 633～642.
  • 6Kung MP, Hou C, Zhuang ZP, et al. IMPY: an Improved Thioflavin-T Derivative for in Vivo Labeling of β-Amyloid Plaques[J]. Brain Res, 2002, 956: 202～210.
  • 7Cai L, Chin FT, Pike VW, et al. Evaluation of 18F-labeled IMPY Derivatives as PET Radioligands for β-Amyloid in Alzheimer's Disease[J]. J Labelled Cpd Radiopharm, 2003, 46: S166.
  • 8Zhuang ZP, Kung MP, Wilson A, et al. Structure-activity Relationship of Imidazo[1,2-a]pyridines as Ligands for Detecting β-Amyloid Plaques in the Brain[J]. J Med Chem, 2003, 46: 237～243.
  • 9Agdeppa ED, Kepe V, Liu J, et al. Binding C-haracteristics of Radiofluorinated 6-dialkylamino-2-naphthylethylidene Derivatives as Positron Emission Tomography Imaging Probes for β-amyloid Plaques in Alzheimer's Disease[J]. J Neurosci, 2001, 21: RC189: 1～5.
  • 10Lee CW, Kung MP, Hou C, et al. Dimethylam-ino-fluorenes: Ligands for Detecting β-amyloid Plaques in the Brain[J]. Nucl Med Biol, 2003, 30: 573～580.

共引文献7

核化学与放射化学
2010年 第1期

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部