新型脑突触密度核素分子探针^(18)F-SynVesT-1放射性标记、质量控制与显像分析  

Novel Brain Synaptic Density Nuclide Molecular Probe ^(18)F-SynVesT-1 Radiolabeling,Quality Control and Imaging Analysis

作　　者：胡政泉 向仕君 唐永祥[1] 陈登明[1] 胡硕[1,2] HU Zhengquan;XIANG Shijun;TANG Yongxiang;CHEN Dengming;HU Shuo(Department of Nuclear Medicine,XiangYa Hospital of Central South University,Changsha 410008,China;Key Laboratory of Biological Nano-technology of National Health Commission,Xiangya Hospital of Central South University,Changsha 410008,China)

机构地区：[1]中南大学湘雅医院核医学科(PET中心),长沙410008 [2]国家卫健委纳米生物技术重点实验室中南大学湘雅医院,长沙410008

出　　处：《同位素》2023年第4期373-379,共7页Journal of Isotopes

摘　　要：突触密度活体可视化评估与定量分析在神经和精神疾病的诊断、治疗监测和机制研究方面具有广阔的临床应用前景。突触前膜囊泡蛋白2A(synaptic vesicle protein 2A,SV2A)可反映突触密度情况并与神经元兴奋性改变、致痫网络形成和癫痫耐药密切相关。为可视化评估突触密度,本研究采用GE Tracerlab FXFN模块高效合成与标记特异性靶向SV2A新型PET核素分子探针^(18)F-SynVesT-1,通过理化性质、稳定性、比活度、细菌内毒素等检测技术进行质量控制,利用癫痫动物模型对^(18)F-SynVesT-1显像效果进行验证。结果显示,Tracerlab FXFN模块能实现^(18)F-SynVesT-1的高效合成,未校准放化产率为(11.4±2.6)%,且产品溶液满足临床及注射要求。本研究合成的^(18)F-SynVesT-1质控表现良好,可用于活体脑突触显像、突触密度定量评估及致痫灶异常检测分析。Neural synapses were the fundamental sites of interneuronal connections and the structural basis for information transmission in brain networks,and alterations in synapse density were closely related to a variety of nervous system disorders.Therefore,in vivo visual evaluation and quantitative measurement of synaptic density have broad clinical application prospects in the diagnosis,therapeutic monitoring,and potential mechanism research for neurological and psychiatric diseases.Previous research demonstrated that synaptic vesicle protein 2A(SV2A)located in neurons'presynaptic membrane of the brain gray matter could effectively reflect the synaptic density of the central nervous system,while also being closely related to neuronal excitatory changes,the epileptogenic network formation progress and epilepsy drug resistance.It was envisaged that novel nuclide molecular probes targeting SV2A will be developed and utilized to measure alterations in synaptic density in a variety of neurological and psychiatric disorders.This study intended to perform radioactive labeling and quality control for the first time on a high-specificity targeted synaptic density PET imaging agent,^(18)F-SynVesT-1.The GE Tracerlab FXFN module was used for agent automated agent synthesis while the physical and chemical properties,stability,specific activity,bacterial endotoxin,and other elements of the product solution were analyzed for agent quality control.And finally,the ^(18)F-SynVesT-1 PET imaging performance verification was verified using animal models of epilepsy.The results of this study showed that the GE TRACERLAB FXFN module could achieve an efficient synthesis of ^(18)F-SynVesT-1 with an uncalibrated yield of(11.4±2.6)%,and the product solution synthesized could meet the standard requirements of injection safety and routine clinical command for invasively disease evaluation.This study indicated that the objective product ^(18)F-SynVesT-1 synthesized had good quality control performance and that ^(18)F-SynVesT-1 PET/CT could be use

关 键 词：突触囊泡蛋白 ^(18)F-SynVesT-1 正电子发射型计算机断层扫描术 突触密度 癫痫 

分 类 号：TL923[核科学技术—核燃料循环与材料] R817[医药卫生—影像医学与核医学]