Re/^(99)Tc^m(CO)_3^+黄酮复合物的合成及其与Aβ斑块的结合特性  

Preparation of Re/^(99)Tc^m(CO)_3^+ Complexed Flavone and Its Characteristic Combined With β-amyloid Plaques

作　　者：杨洋[1] 刘永娟[1] 张华北[1] 

机构地区：[1]放射性药物教育部重点实验室北京师范大学化学学院,北京100875

出　　处：《同位素》2011年第3期158-165,共8页Journal of Isotopes

基　　金：国家自然基金(No.20671013);国家基础研究项目(No.2006CB500705)

摘　　要：为研制新型99Tcm(CO)3+标记的黄酮类Aβ显像剂,设计合成了同型Re/99Tcm(CO)3]+-黄酮类衍生物,用荧光法研究了Re(CO)3+-黄酮类衍生物在体外与Aβ斑块的结合特性,并初步观察了其在昆明小鼠体内的生物分布。结果表明,Re(CO)3+-黄酮类衍生物的亲和常数(Kd=5.43 nmol/L)比放射性碘标记的黄酮类衍生物高。正常小鼠的动物分布结果表明,2 min内脑初始摄取较高(0.46±0.23%ID/g),且清除较快(120 min时为0.13±0.04%ID/g)。以上结果表明,99Tcm(CO)3+-黄酮类衍生物有进一步研究的价值。In vivo PET and SPECT imaging of β-amyloid（Aβ） plagques in the brain may lead to early detection of Alzheimer＇s Disease（AD）,but the Aβ-detector labeled by 99Tcm fell behind.The purpose of this study was to develop novel 99Tcm（CO）3＋-labeled β-amyloid-detector based on the flavones.Isostructural Re/99Tcm（CO）3＋-flavones were designed and synthesized,and Re（CO）3＋-flavone were studied on its binding characteristic with β-amyloid plaques in vitro by fluorescence.The results showed that the binding affinity（Kd=5.43 nmol/L） of Re（CO）3＋-flavone was higher than flavone derivatives labeled by radioiodine.The biodistrubution of normal mice showed that 99Tcm（CO）3＋-flavone displayed moderate uptake（0.46±0.23%ID/g） at 2 min postinjection） in the brain and rapid clearance（0.13±0.04%ID/g） after 120 min injection.The above results demonstrated that 99Tcm（CO）3＋-flavone should be desirable as a potential SPECT imaging agent for β-amyloid aggregates.

关 键 词：99Tcm Aβ斑块 [Re/99Tcm(CO)3]+黄酮类衍生物 

分 类 号：R817[医药卫生—影像医学与核医学]