~(99)Tc~mN-HL91的制备及其生物分布
Synthesis and Biodistribution of ~(99)Tc~mN-HL91 Complex
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摘要: 以丁二酰二酰肼(SDH)为N3-离子供给体,SnCl2·2H2O为还原剂,室温下制备99TcmN2+ 中间体,并于100 ℃水浴中与HL91配体进行交换反应,制得99TcmN HL91 配合物,标记率大于 90%;室温下放置 6 h,99TcmN HL91标记率仍大于90%;其脂水分配系数 lg P为-1.026±0.019,水溶性较99 Tcm HL91(lg P为-0.859±0.009)强;正常小鼠体内生物分布显示,99TcmN HL91 在血液、肝脏中的清除较99 Tcm HL91 快;由于99TcmN核的引入,使得99TcmN HL91配合物在乏氧选择性和生物体内代谢方面不同于99 Tcm HL91,前者在荷瘤小鼠体内没有明显的肿瘤摄取。Abstract: The complex ~(99)Tc~mN-HL91 is synthesized through ligand exchange reaction. The ~(2+) (intermediate) is prepared with succinic dihydrazide (SDH) as a donor of nitride nitrogen atom (N~(3-)) in the presence of stannous chloride dihydrate a reductant at room temperature. Then HL91 is added to the \~(2+) intermediate and react at 100 ℃. The labeling efficiency of the product is over 90% measured by thin layer chromatography(TLC). The lg P of ~(99)Tc~mN-HL91(-1.026±0.019) indicates it is a hydrophilic complex. It is stable over 6 h at room temperature. The biodistribution results in mice indicate that it has quick blood and liver cleanness than ~(99)Tc-HL91. It differs from ~(99)Tc~m-HL91 in the hypoxic selectivity and biologic metabolism. ~(99)Tc~mN-HL91 has no significant uptake in hypoxia tumors in tumor-bearing mice.