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/99 Tcm (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 p-amy-loid-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 radioio-dine. 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 ag-gregates.
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