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^(188)Re直接法标记生长抑素类似物RC-160及其体内分布研究 被引量:4

Direct labeling of RC-160 with ^(188)Re and the biodistribution of ^(188)Re-RC-160 in mice
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摘要 目的 探讨188Re直接法标记生长抑素类似物RC 16 0的方法及观察其在小鼠体内的生物学分布。方法 酒石酸亚锡直接还原法进行RC 16 0的188Re标记 ,标记完成后加入抗坏血酸以防标记产物的再氧化。硅胶纸层析测定放化纯 ,并行小鼠体内分布实验。结果 188Re RC 16 0放化纯为 96 .2 % ,游离188Re为 0 .8% ,放射性胶体为 3.0 %。加抗坏血酸组在标记后 2 4h放化纯为 85 % ,对照组为 5 0 %。注射后 0 .5~ 1.0h血液中放射性下降了 87.2 % ,肾脏无明显浓集 ,标记物 2 4h内由消化系统排出体外。结论 188Re直接法标记RC 16 0放化纯高 ,方法简便 ,抗坏血酸的加入增加了标记物的稳定性。188Re RC 16 0在小鼠体内血液清除较快 ,经消化系统排除。 Objective To investigate labeling method of RC-160 with 188 Re and the biodistribution of 188 Re-RC-160 in mice. Methods RC-160 was labeled with 188 Re through stannous tartrate reduction at room temperature under nitrogen gas condition. Ascorbic acid was added to inhibit re-oxidation of 188 Re-RC-160. The radiochemical purity was tested with silicon paper chromatography. Its biodistribution in normal mice was analyzed. Results The radiochemical purity was 96.2%. Free 188 Re was less than 0.8%. Radioactive colloid was 3%. The radiochemical purity at 24 h after labeling was 85% in ascorbic acid group while 50% in control group. At 0.5~1.0 h after injection, radioactivity in blood decreased by 87.2%. No obvious accumulation of 188 Re-RC-160 in the kidney was observed. A great amount of radioactivity was detected in gastrointestinal system within 12~24 h. Conclusions The method is simple and easy to perform. The radiochemical purity is quite high. The stability of 188 Re-RC-160 is improved by adding ascorbic acid. Blood clearance of 188 Re-RC-160 in normal mice is quite fast. 188 Re-RC-160 is excreted through gastrointestinal tract.
出处 《中华核医学杂志》 CAS CSCD 北大核心 2002年第3期177-178,共2页 Chinese Journal of Nuclear Medicine
基金 国家自然科学基金资助项目 ( 39870 2 18) 全军医药卫生科研基金资助项目 ( 0 1MB12 0 )
关键词 ^188RE直接法 标记 生长抑素类似物 RC-160 体内 分布 研究 放射性同位素 同位素标记 药代动力学 Somatostatin Rhenium Radioisotopes Isotope labeling Pharmacokinetics
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参考文献4

  • 1Pollak MN,Schally AV.Mechanisms of antineoplastic action of somatostatin analogs[].Proceedings of the Society for Experimental Biology and Medicine.1998
  • 2Zamora PO,Marek MJ,Knapp FF Jr.Preparation of 188Re-RC-160 somatostatin analog: a peptide for local/regional radiotherapy[].Applied Radiation and Isotopes.1997
  • 3Zamora PO,Gulhke S,Bender H,et al.Experimental radiotherapy of receptor-positive human prostate adenocarcinoma with 188Re-RC-160, a directly-radiolabeled somatostatin analogue[].International Journal of Cancer.1996
  • 4Mishima M,Yano T,Jimbo H,et al.Inhibition of human endometrial cancer cell growth in vitro and in vivo by somatostatin analog RC-160[].American Journal of Obstetrics and Gynecology.1999

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