Imaging DNA synthesis in vivo with 18F-FMAU and PET.

摘要: We imaged DNA synthesis in vivo with PET and 1 8 F-1-(2'-deoxy-2'-fluoro-β-D-arabinofuranosyl)thymine (FMAU), which is phosphorylated by thymidine kinases incorporated into DNA. Methods: produced F-FMAU injected the tracer 5 normal dogs studied them imaging or biodistribution for up to 2.5 h. The pharmacokinetics of FMAU blood urine were determined using high-performance liquid chromatography analysis. At end each study, selected tissues removed measure total activity retained these tissues. In addition, extracted acid precipitation, macromolecules can be precipitated determine radioactivity Results: Imaging tissue analysis showed increased lymph nodes, stomach, small intestine, bone marrow, mean standardized uptake values 1.4, 1.6, 2.3, 3.9, respectively, because varying degrees cell proliferation. contrast, was distributed tissue-to-muscle ratios approximately 1.0 nonproliferative organs such as lung, liver, kidneys. Analysis extracts precipitation demonstrated that 88% marrow 65% intestine precipitated. However, more than 90% nonproliferating heart lungs supernatant. Increased seen a high level kinase 2 gallbladder excretion. 95% present intact at studies. Conclusion: results selectively proliferating resistant degradation. These features indicate might an alternative C-thymidine tumors.