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Aβ斑块显像剂11C-苯并呋喃衍生物的研究

11C labelled benzofuran derivatives as a new agent for β-amyloid imaging

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【作者】 张锦明郭喆田嘉禾王武尚刘伯里

【Author】 ZHANG Jin-ming GUO Zhe TIAN Jia-he Department of Nuclear Medicine,The PIA General Hospital,Beijing 100853,China

【机构】 解放军总医院核医学科西安西北核技术研究院北京师范大学化学系

【摘要】 目的合成新的11C 标记小分子苯并呋喃衍生物并研究其生物学性质。方法合成前体5-溴2-(4-胺基苯)苯并呋喃,用改良的11CH3I 法标记,生成5-溴-2-(4-N-11C-甲胺基苯)-苯并呋喃,以柱色层法测标记率。正常小鼠尾静脉注射5-溴-2-(4-N-11C-甲胺基苯)-苯并呋喃后不同时间处死,测每克组织百分注射剂量率(%ID/g)。结果改良11CH3I 法标记率为45%,放化纯大于95%。小鼠尾静脉注射药物后,放射性主要分布于肝和肾内,药物能迅速被脑摄取,2 min 达到3.2%ID/g,正常脑对其清除快于对碘的取代物,2与30 min 放射性摄取比值为1.34。结论 11C 标记小分子溴取代苯并呋喃衍生物,可作为β-淀粉样蛋白(Aβ)显像剂,其生物学性质明显优于碘的取代物。

【Abstract】 Objective Deposit of β-amyloid protein(Aβ)as senile plaque is one of the patho- physiologic features in Alzheimer’s disease.Several new derivatives of benzofuran were synthesized,11C la- belled,and tested as the potential imaging agents for targeting amyloid deposit.Methods 5-Br-2-(4-amin- ophenyl)benzofuran was synthesized and labelled by an improved method,in which the precursors were mixed with 11CH3I and dimethyl sulfoxide(DMSO)solution to get 5-Br-2-(4-N-11C-methylaminophenyl) benzofuran.The column method was employed to measure the labelling yields.The biodistribution of the product was studied in 9 normal mice.The characters of the precursor were confirmed by 1H NMR.Results The labelling yield was 45% with the author’s improved method used in the current study.The radiochemi- cal yield was over 95%.Most of the radioactivity was observed in liver and kidney after intravenous injec- tion.The peak uptake in normal mice brain(3.2 % ID/g)was noted at 2 rain post-injection with a washout faster for 5-Br-substituent than 5-I-substituent.The 2/30 rain ratio of cerebral uptake was 1.34.Conclu- sion The new derivative,11C labelled 5-Br-substituent,showed certain characteristics more favorable than literature reported 5-I-substituent as an Aβ imaging agent.

【基金】 国家自然科学基金(20471011)
  • 【文献出处】 中华核医学杂志 ,Chinese Journal of Nuclear Medicine , 编辑部邮箱 ,2007年01期
  • 【分类号】R817
  • 【被引频次】1
  • 【下载频次】8
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