A Novel Pet Tracer 18f-labeled Thiamine: Synthesis, Metabolic Kinetics, and Evaluation on Cerebral Thiamine Metabolism Status [post]

Changpeng Wang, Siwei Zhang, Yuefei Zou, Hongzhao Ma, Donglang Jiang, Lei Sheng, Shaoming Sang, Lirong Jin, Yihui Guan, Yuan Gui, Zhihong Xu, Chunjiu Zhong
2020 unpublished
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
more » ... 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.
doi:10.21203/rs.3.rs-28109/v1 fatcat:l7q3gc3wazaonm5houf2ogvql4