Background: 1-H-1-(3-[18F]fluoro-2-hydroxypropyl)-2-nitroimidazole(18F-FMISO) is a specific molecular imaging probe for tumor hypoxia imaging

and its PET/CT imaging has an important clinical value for planning cancer radiotherapy target volume. Purpose: This study aimed to develop an improved

automated production of18F-FMISO and to perform Micro-PET/CT imaging of tumor hypoxia. Methods: Based on the labeling precursor NITTP and a simple "one-pot" method

an upgraded Explora GN module together with Explora LC was adopted to run radiofluorination(NITTP(10 mg)

MeCN(1.0 mL)

120oC

5.0 min)

hydrolysis(HCl(1.0 mol/L

1.0 mL)

130oC

8.0 min) and high performance liquid chromatography(HPLC) purification to produce18F-FMISO automatically. Moreover

Radio-HPLC and Radio-TLC were applied for the quality control

and Micro-PET/CT scanner for hypoxia imaging of SW1990 pancreatic tumor-bearing mice. Results: As results

18F-FMISO was obtained with the synthesis time for about 65 min

the radiochemical yield of(30 5.0)%(no decay corrected

n=20)

the radiochemical purity of above 99%

the specific activity of(2.04 0.17)×1011Bq· mol–1

plus with the enhanced chemical purity. Moreover

MicroPET/CT imaging showed that18F-FMISO presented whole-body distribution in SW1990 tumor-bearing mice

and the optimized time point for tumor hypoxia imaging was 3 h post injection with the uptake ratios of tumor-to-muscle of 3.00 0.08. Conclusion: In sum

we developed an improved

automated production of18F-FMISO with high performance liquid chromatography purification

high radiochemical yield

high specific activity and high reliability

and also verified its MicroPET/CT imaging of tumor hypoxia for providing experimental reference data.