同位素2026，Vol.39Issue(2)：132-139,8.DOI:10.7538/tws.2025.youxian.074
11C-多奈哌齐的自动化合成与显像初步研究
Automatic Synthesis and Preliminary Imaging Study of 11C-Donepezil
摘要
Abstract
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.关键词
11C-多奈哌齐/心脏副交感神经系统/心肌受体/PET/CT显像Key words
11C-DNP/cardiac parasympathetic nervous system/myocardial receptor/PET/CT imaging分类
能源科技引用本文复制引用
单崇玮,王慧,谷婧,邬心爱,王文睿,何玉林..11C-多奈哌齐的自动化合成与显像初步研究[J].同位素,2026,39(2):132-139,8.基金项目
国家自然科学基金项目(82060323) （82060323）
内蒙古医科大学重点项目(YKD2025ZD001) （YKD2025ZD001）
内蒙古医学科学院公立医院科研联合基金科技项目(2025GLLH0166) （2025GLLH0166）
