A Novel Pet Tracer 18f-labeled Thiamine: Synthesis, Metabolic Kinetics, and Evaluation on Cerebral Thiamine Metabolism Status
Background:Someneuropsychological diseases are associated with abnormal thiamine metabolism, including Korsakoff-Wernicke syndrome and Alzheimer's disease. However, in vivo detection of brain thiamine metabolism status isstill unavailable and needs to be developed.Methods:A novel PET tracer 18F-labeled thiaminewasautomatically radio-synthesized via a two-step route. The main parameters of characterization were proved by high performance liquid chromatography (HPLC). Metabolic kinetics of
... kinetics of 18F-labeled thiamine and the status of cerebral thiamine uptakein mice and marmosets were studied by micro-positron emission tomography (PET)/computer tomography imaging. Also, in vivo stability, renal excretion rate, biodistribution, and the correlation between cerebral 18F-labeled thiamine retention and blood thiamine levels were investigated.Results: The 18F-labeled thiamine was stableboth in vitro and in vivoand manifested fast uptake and clearance in vivo. The biodistribution of 18F-labeled thiamine were consistent with previously reports on thiamine distribution in mice. The retention of cerebral 18F-labeled thiamine was higher in mice with thiamine deficiency than that in control mice, and negatively correlated with blood thiaminediphosphate levels in marmosets.Conclusion:The 18F-labeled thiamine met the requirements for ideal PET tracer to in vivoevaluate the status of cerebral thiamine metabolism. This study laid the foundation for further studies on the relevant diseases.