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氚标记胆红素的研制及应用

Investigation on 3H-labelled bilirubin for Study of blood-brain barrier

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【作者】 曹蓉珍董墨张雨龙周瑞菊

【Author】 Cao Rongzhen; Dong Mo; Zhang Yulong; Zhou Ruiju(Shanghai Institute of Nuclear Research,Academia Sinica, Shanghai 201800 )

【机构】 中国科学院上海原子核研究所

【摘要】 由胆绿素经钠硼氚还原生成氚标记胆红素,而胆绿素是由胆红素经DDQ脱氢氧化形成,钠硼氚是在镍催化及高温下由销硼氢与氚气交换得到。氚标记胆红素比活度为306TBq/mol,放化纯度经高效液相色谱及纸层析鉴定均大于95%,用氚标记胆红素进行开放血脑屏障的动物实验获得了满意的结果。

【Abstract】 ynthesis of 3H-labelled bilirubin is described.3H-bilirubin is prepared by the reduction of biliverdin using sodium boro-[3H]-hydride in methanol solvent.But biliverdin is synthesized through dehydrogenation of bilirubin with 2, 3-dichloro-5,6-dicyanobenzoquinone(DDQ)in dimethyl sulphoxide and sodium boro-[3H]-hydride is produced by exchange of sodium boro-hydride with tritium gas using nickel catalyst at high temperature.The specific activity of obtained 3H-bilirubin is 306GBq/mmol,while the radiochemical purity is over 95% by HPLC and paper chromatography.The permeatied profile of 3H-labelled bilirubin in rat brain has been satisfyingly obtained in animal experiments.

【基金】 上海市科委基金
  • 【分类号】TL923
  • 【被引频次】1
  • 【下载频次】39
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