99TcmN(PNP)2+标记葡萄糖硫酮类衍生物混配配合物的研究

⁹⁹Tc^mN(PNP)²⁺标记葡萄糖硫酮类衍生物混配配合物的研究

摘要: 为研究新的⁹⁹Tc^mN核心标记的心肌和肿瘤显像药物，选用自行合成的二硫化碳-葡萄糖（硫酮类）衍生物L_n(L₁~L₅)制备一系列带有葡萄糖衍生物基团的新型⁹⁹Tc^m(DTC)(PNP)⁺类配合物，经TLC和HPLC检测，配合物的放射化学纯度均大于90%。小鼠生物分布实验表明，⁹⁹Tc^mN(PNP)L_n(L₁~L₅)系列配合物在正常小鼠体内初始的放射性摄取主要分布于心肌、肝、肺、肾等脏器，并且30 min内各脏器均可迅速清除。初步的荷EMT-6鼠生物分布实验显示，⁹⁹Tc^mN(PNP)L₂在肿瘤中放射性摄取不高，30 min时为（0.39±0.03）%ID/g，其它组织的放射性摄取与正常小鼠类似。

Abstract: A series of novel glucose-dithiocarbamate derivatives L_n(L₁-L₅) were selected to label with TcN²⁺ using bisphosphines (PNP) as coligands for the new myocardial and tumor imaging agents studies. The radiochemical purity of these complexes were above 90% according to the analysis results of HPLC and TLC. These complexes showed similar biodistribution characteristicswith a lower initial myocardial uptake and a rapid clearance from blood, muscle, liver and other tissues in normal mice. The low tumor accumulation of ⁹⁹Tc^mN(PNP)L₂ complexe appeared in mice xenografted with EMT-6 (0.39±0.03)%ID/g in 30 min after injection.