摘要
目的:自动化合成5-羟色胺转运蛋白显像剂11 C-DASB并进行大鼠Micro PET/CT显像;方法:通过改变甲基化试剂、溶解前体溶剂及反应条件,得到优化的标记条件作为碳-11多功能合成模块的输入参数,进行自动化合成11 C-DASB,大鼠静脉注射11 C-DASB 45 min后进行显像;结果:采用11 C-CH3-Triflate作为甲基化试剂,通入新配制的含1mg去甲基DASB前体的500μL DMSO溶液内,80℃下加热2min,标准率为63.7%,大鼠显像表明,11 C-DASB特异性的浓聚于SERT富集区域;结论:经优化,11 C-DASB自动化合成可得到较高产率,大鼠显像表明,其特异性浓聚于SERT富集区域,有望作为5-羟色胺转运蛋白显像剂。
Objectives: Automatic synthesis of ^11C-DANB as a serotonin imaging agent was established and Micro PET/CT imaging with Wistar rat was performed. Methods: Optimization of 11C-DASB synthesis was established by modifying different n C-methylation agents, solvent and reaction conditions. Automated procedure for the synthesis of ^11C-DASB was established, and Micro PET/CT imaging was complied with Wistar rat. Results: The optimized ^11C-DASB synthesis was obtained. When ^11C-CH3-Triflate was used as methylation agent, 500 μL DMSO was used to dissolve 1 mg precursor, the reaction was carried out at 80 ℃ for 2 min, the radiochemical synthesis yield was 63.7%. Micro PET/CT studies in rat showed that the initial uptake of HC-DASB in the brain was high, especially in region of the highest density of SERT, such as colliculus and mid brain. Conclusion. The study should provide the basis for routine preparations of ^11C-DASB with high reliability, it may be useful for PET imaging of SERT binding sites in the brain.
出处
《同位素》
CAS
2015年第1期1-6,共6页
Journal of Isotopes
基金
国家自然科学基金资助(81371593)