11C-多奈哌齐的自动化合成与显像初步研究OA

A radiotracer,11C-donepezil(11C-DNP)was synthesized by a fully automatic method,and its biodistribution characteristics were assessed in normal Kunming mice.Dynamic Micro PET/CT imaging was performed in normal Sprague-Dawley(SD)rats to generate time-activity curves,and the PET/CT study was conducted in heart failure model pigs.The radiotracer 11C-DNP was synthesized using the Triflate-11CH3 method.The crude product was purified by semi-preparative high-performance liquid chromatography(HPLC).Radiochemical purity and specific activity of the final product were assessed using radio-HPLC analysis.Pharmacokinetic characteristics were determined using a combination of biodistribution studies and dynamic micro-PET/CT imaging experiments.The feasibility of using 11C-DNP for cardiac parasympathetic nerve imaging was validated in heart failure model pigs using PET/CT.An automated synthesis process was established using a carbon multifunctional synthesis module,achieving a total synthesis time of approximately 40 minutes,a radiochemical yield of(13.90±2.50)%,radiochemical purity>99%,and a specific activity of(48.88±4.20)GBq/mmol.Biodistribution experiments conducted in normal Kunming mice demonstrated rapid uptake in the heart and lungs,with the highest heart-to-lung ratio(approximately 1.61:1)observed at 10 minutes post-injection.Dynamic Micro PET/CT imaging in normal Sprague-Dawley(SD)rats revealed significant radiotracer accumulation in tissues rich in acetylcholinesterase nerve fibers.Time-activity curves of major organs indicated that the tracer was primarily metabolized via the hepatobiliary and urinary systems.PET/CT imaging in heart failure model pigs identified multiple regions of sparse or deficient radiotracer uptake within the left ventricle.The automated synthesis of 11C-DNP was successfully achieved,characterized by high radiochemical yield and specific activity.Pharmacokinetic analysis confirmed its rapid metabolism in tissues enriched with acetylcholinesterase nerve fibers.PET/CT imaging in heart failure model pigs accurately reflected the extent of cardiac nerve damage.