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新的^(99m)Tc标记σ受体肿瘤显像剂 被引量：1

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摘要 采用整体法设计合成了新的99mTc标记的配合物[N-[2-((2-oxo-2-(4-(3-phenylpropyl)piperazin-1-yl)ethyl)(2-mercaptoethyl)amino)acetyl]-2-aminoethanethiolato]technetium(Ⅴ)oxide(PPPE-MAMA′-99mTcO)([99mTc]-2)及其相应的铼配合物(PPPE-MAMA′-ReO)(Re-2).竞争结合实验表明Re-2对σ1和σ2受体有中等亲和力,Ki值分别为8.67±0.07和5.71±1.88μmol/L;荷MCF-7人乳癌裸鼠尾静脉注射[99mTc]-2后0.5h,4h,20h采集平面图像,20h时可以看到肿瘤部位有放射性浓集,共同注射[99mTc]-2和抑制剂氟哌啶醇(1mg/kg)后显像,20h时肿瘤部位无明显放射性浓集;体内生物分布结果显示,注射后24h肿瘤中的放射性摄取为0.14%±0.01%ID/g,肿瘤/肌肉比为6.02±0.87.上述结果表明:虽然用整体设计法对前体化合物的结构进行了较大修饰,但得到的99mTc-配合物([99mTc]-2)在肿瘤内仍有一定的浓集,与σ1和σ2受体仍保持一定的亲和力.在此配合物的基础上,对其进行进一步的结构修饰有可能得到对σ受体亲和力更高的肿瘤显像剂.
作者 樊彩云 贾红梅 Deuther-Conrad Winnie Brust Peter Steinbach Jrg 刘伯里
机构地区 北京师范大学化学系放射性药物教育部重点实验室 Institute of Interdisciplinary Isotope Research
出处 《中国科学（B辑）》 CSCD 北大核心 2005年第6期499-505,共7页 Science in China(Series B)
基金 国家自然科学基金资助项目(批准号:20471011)
关键词 肿瘤 σ受体 SPECT ^99MTC
分类号 TQ421.7 [化学工程]
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参考文献46

  • 1Quirion R,Bowen W D,Itzhak Y,et al.A proposal for the classification of sigma binding sites.Trends Pharmacol Sci,1992,13:85-86.
  • 2Su T P.Sigma receptors.Putative links between nervous,endocrine and immune systems.Eur J Biochem,1991,200:633-642.
  • 3Guitart X,Codony X,Monroy X.Sigma receptors:biology and therapeutic potential.Psychopharmacology,2004,174:301-319.
  • 4Vilner B J,John C S,Bowen W D.Sigma-1 and sigma-2 receptors are expressed in a wide variety of human and rodent tumor cell lines.Cancer Res,1995,55:408-413.
  • 5Mach R H,Smith C R,al-Nabulsi I,et al.σ2 receptors as potential biomarkers of proliferation in breast cancer.Cancer Res,1997,57:156-161.
  • 6Shiue C Y,Shiue G G,Zhang S X,et al.N-(N-benzylpi- peridin-4-yl)-2-[18F]fluorobenzamide:a potential ligand for PET imaging of σ receptors.Nucl Med Biol,1997,24:671-676.
  • 7Dence C S,John C S,Bowen W D,et al.Synthesis and evaluation of [18F] labeled benzamides:high affinity sigma receptor ligands for PET imaging.Nucl Med Biol,1997,24:333-340.
  • 8Shiue C Y,Shiue G G,Benard F,et al.N-(N-benzylpiperidin- 4-yl)-2-[18F]fluorobenzamide:A potential ligand for PET imaging of breast cancer.Nucl Med Biol,2000,27:763-767.
  • 9Rowland D J,Tu Z,Mach R H,et al.Investigation of a new sigma-2 receptor ligand for detection of breast cancer.J Labelled Cpd Radiopharm,2003,46:S6.
  • 10Everaert H,Flamen P,Franken P R,et al.Sigma receptor imaging by means of 123-IDAB scintigraphy; clinical application in melanoma and non-small cell lung cancer.Anticancer Res,1997,17:1577-1582.

二级参考文献2

共引文献2

同被引文献12

  • 1张秋艳,樊彩云,贾红梅.Sigma受体显像剂[J].化学进展,2007,19(5):713-721. 被引量：2
  • 2Vilner B J,John C S,Bowen W D.Sigma-1 and Sigma-2 Receptors are Expressed in a Wide Variety of Human and Rodent Tumor Cell Lines[J].Cancer Res,1995,55(2):408-413.
  • 3Bourrie B,Bribes E,Derocq J-M,et al.Sigma Receptor Ligands:Applications in Inflammation and Oncology[J].Curr Opi Invest Drugs,2004,5:1 158-1 163.
  • 4Quirion R,Bowen W D,Itzhak Y,et al.A Proposal for the Classification of Sigma Binding Sites[J].Trends Pharmacol Sci,1992,13:85-86.
  • 5Mach R H,Smith C R,Al-Nabulsi I,et al.σ2 Receptors as Potential Biomarkers of Proliferation in Breast Cancer[J].Cancer Res,1997,57:156-161.
  • 6Wheeler K T,Wang L-M,Wallen C A,et al.Sigma-2 Receptors as a Biomarker of Proliferation in Solid Tumours[J].Br J Cancer,2000,82(6):1 223-1 232.
  • 7Al-Nabulsi I,Mach R H,Wang L-M,et al.Effect of Ploidy,Recruitment,Environmental Factors,and Tamoxifen Treatment on the Expression of Sigma-2 Receptors in Proliferating and Quiescent Tumour Cells[J].Br J Cancer,1999,81(6):925-933.
  • 8Mach R H,Wheeler K T.Imaging the Proliferative Status of Tumor With PET[J].J Label Compd Radiopharm,2007,50:366-369.
  • 9Perregaard J,Ejner K,Sanchez C,et al.σ Ligands With Subnanomolar Affinity and Preference for the σ2 Binding Site.1,3-(ω-Aminoalky1)-1H-Indoles[J].J Med Chem,1995,38:1 998-2 008.
  • 10Bowen W D.Sigma Receptors:Recent Advances and New Clinical Potentials[J].Pharm Acta Helv,2000,74:211-218.

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中国科学（B辑）
2005年 第6期

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