Synthesis and radiopharmacology of S-(2-18F-fluoroethyl)-L-methionine for tumor imaging / 药学学报

ABSTRACT

<p><b>AIM</b>To develop S-(2-18F-fluoroethyl)-L-methionine (18FEMET) as an amino acid positron emission tomography (PET) tracer for tumors, and to evaluate the value of 18FEMET in the differentiation of experimental tumor and experimental inflammation.</p><p><b>METHODS</b>18FEMET was prepared by nucleophilic fluorination reaction via a two-step procedure. Biodistribution of 18FEMET in normal mice, carcinoma-bearing mice and inflammatory mice, and 18FEMET PET imaging for carcinoma-bearing mice and inflammatory mice were performed compared with 2-[18F] fluoro-2-deoxy-D-glucose (FDG) and O-(2-[18F] fluoroethyl)-L-tyrosine (FET).</p><p><b>RESULTS</b>The overall radiochemical yield with no decay correction was 15%-25%, the whole synthesis time was about 70 min by manual operation, and the radiochemical purity was above 95%. High uptake and long retention of 18FEMET in pancreas, kidney, colon, liver and heart were observed. But low uptakes in brain and blood were found. Furthermore, high uptake of 18FEMET, FDG and FET in tumor, high uptake of FDG in inflammatory tissue, and almost no uptake of 18FEMET and FET in inflammatory tissue were also observed.</p><p><b>CONCLUSION</b>18FEMET is easy to prepare and can be used to differentiate between tumor and inflammatory tissue. It seems to be a potential amino acid tracer for tumors with PET imaging.</p>