乏氧显像剂^(99)Tc^m-EtAO的制备和活性研究

PREPARATION AND EVALUATION OF ^(99)Tc^m-EtAO AS TUMOR HYPOXIA MARKER

为寻找结构简单、性能优良的乏氧显像剂 ,合成并用99Tcm 标记了 3 甲基 3 N (2 羟乙基 ) 2 丁酮肟 (EtAO) ,进行了体内外活性的研究 ,并与已知乏氧显像剂99Tcm Bn(AO) 2 比较。细胞实验结果表明 ,与99Tcm Bn(AO) 2 一样 ,99Tcm EtAO也具有亲乏氧性。荷瘤小鼠体内分布结果表明 ,99Tcm EtAO能选择性地滞留于肿瘤组织。作为一种潜在的乏氧显像剂 ,99Tcm

Seeking for hypoxia imaging agents with simple structure and good performance, 3 methyl 3 N (2 hydroxyethyl) 2 butanone oxime (EtAO) is synthesized and labeled with 99 Tc m. In vitro and in vivo evaluation of this complex as a tumor hypoxia marker is performed and the result is compared with that of 99 Tc m Bn(AO) 2, a putative hypoxic tracer. The cell experiments show that 99 Tc m EtAO has hypoxia affinity as well as 99 Tc m Bn(AO) 2. The biodistribution in tumor bearing mice indicates that 99 Tc m EtAO can concentrate selectively in tumor tissues. As a potential hypoxia imaging agent, 99 Tc m EtAO has the value for the further investigation.