Development of a radiolabeled uracil derivative as a potential PET tracer for angiogenesis imaging.

胸苷磷酸化酶（TP）的表达与血管生成和肿瘤侵袭密切相关。我们评估了^<11>C标记的5-溴-6-氧咪唑烷基甲基尿嘧啶具有TP抑制效力，作为一种新的靶向肿瘤中TP表达的PET放射性示踪剂。在A431荷瘤小鼠体内分布显示，注射后1小时，肿瘤/血液和肿瘤/肌肉活动摄取比分别为5和12。为了开发具有较长半衰期的新型PET示踪剂，我们进行了^<18> f标记尿嘧啶衍生物前体的合成。

The expression of thymidine phosphorylase (TP) is closely associated with angiogenesis and invasiveness of tumors. We evaluated ^<11>C labeled 5-bromo-6-oxoimidazolidinylmethyluracil having TP-inhibitory potency, as a new radiotracer for PET targeting TP expression in tumors. In vivo distribution of the radiotracer in A431 tumor bearing mice revealed tumor/blood and tumor/muscle activity uptake ratios of 5 and 12, respectively, at 1 h post-injection. To develop novel potential PET tracers having longer half-life, the synthesis of the precursor of ^<18>F-labeled uracil derivative was performed.