合成分子探针~(18)F-Fallypride并对帕金森病的Micro PET/CT显像分析  

Synthesis of a molecular probe 18F-Fallypride and analysis of its application in micro PET/CT imaging of Parkinson's disease

作　　者：刘晓杰 冯柳 陈夏彬 王宏智 LIU Xiaojie;FENG Liu;CHEN Xiabin;WANG Hongzhi(Department of Nuclear Medicine,The First Hospital of Jiaxing,Zhejiang Province,Jiaxing 314000,China;Jiangsu Huajing Institute of Molecular Imaging and Pharmaceutical Research Co.,Ltd.,Changshu 215500,China;Department of Rheumatology and Immunology,The First Hospital of Jiaxing,Zhejiang Province,Jiaxing 314000,China)

机构地区：[1]浙江省嘉兴市第一医院核医学科,浙江嘉兴314000 [2]江苏华景分子影像与药物研究院有限公司,江苏常熟215500 [3]浙江省嘉兴市第一医院风湿免疫科,浙江嘉兴314000

出　　处：《医学影像学杂志》2024年第7期123-127,共5页Journal of Medical Imaging

基　　金：浙江省嘉兴市科技计划项目(编号:2022AD30075);浙江省嘉兴市医学重点学科项目(编号:2023-ZC-016)。

摘　　要：目的 探讨利用(s)-(-)-N-(1-烯丙基吡咯烷-2-氨基甲基)-5-(3-^(18)F)-2,3-二甲氧基苯甲酰胺(^(18)F-Fallypride)探针与^(18)F-脱氧葡萄糖(fluorodeoxyglucose, FDG,^(18)F-FDG)探针,结合PET/CT成像技术,分析孤独感对老年帕金森病(PD)模型小鼠的影响。方法 采用自动化流程合成^(18)F-Fallypride,通过质量控制确保pH值6.0~7.0,且放射化学纯度超过95%。9只ICR品系小鼠按随机表法分为三组(PD模型组、单笼隔离组、群居饲养组),每组3只。PD模型组:通过7天腹腔注射1-甲基-4-苯基-1,2,3,6-四氢吡啶(1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine,MPTP)每天注射25 mg/kg。建立PD模型,该组作为阳性对照组,单笼隔离组:小鼠隔离独立饲养,群居饲养组:小鼠共同饲养于同一笼舍,该组作为阴性对照组。利用Micro PET/CT显像技术分别对小鼠注射^(18)F-Fallypride和^(18)F-FDG后进行PET扫描,并通过CT衰减校正进行图像重建。结果 通过自动化流程成功合成^(18)F-Fallypride,三批产率稳定在30.2%、30.1%、30.4%,放射化学纯度超过95%,满足质量控制标准。Micro PET/CT成像显示,^(18)F-Fallypride在小鼠纹状体具有特异性高摄取,其中群居饲养组小鼠纹状体摄取值为(8.58±2.11)%ID/g,显著高于PD模型组的(4.38±0.37)%ID/g,差异有统计学意义(P=0.027)和单笼隔离组的(4.56±0.11)%ID/g,差异有统计学意义(P=0.030)。^(18)F-FDG显像结果显示,PD模型组在多个脑区的摄取值均显著高于单笼隔离组和群居饲养组,差异有统计学意义(P<0.05),而单笼饲养组与PD模型组之间的脑区摄取值差异无统计学意义(P>0.05)。结论 与群居饲养组相比,单笼隔离组的脑部多巴胺D2受体活性降低,接近PD模型组的水平。然而,在脑区糖代谢方面,单笼隔离组与群居饲养组之间差异无统计学意义(P>0.05)。这一发现为深入分析帕金森病的潜在发病机制提供了实验数据和理论基础。Objective To explore the effect of loneliness on aging Parkinson's disease(PD)model mice by using ^(18)F-Fallypride probe and ^(18)F-FDG probe,combined with PET/CT imaging technology.Methods ^(18)F-Fallypride was synthesized by an automated process,with the pH value between 6.0 and 7.0 and the radiochemical purity over 95%.Nine ICR strain mice were randomly divided into three groups,i.e.,PD model group,single cage isolation group,and social feeding group,with three mice in each group.For PD model group,PD model was established by intraperitoneal injection of MPTP(25 mg/kg)for 7 days.For single cage isolation group,mice were isolated and independently fed.As for the social feeding group,mice were commonly fed in the same cage.By means of Micro PET/CT imaging technology,mice were injected with ^(18)F-Fallypride and ^(18)F-FDG for PET scanning,and the images were reconstructed by CT attenuation correction.Results In this study,^(18)F-Fallypride was success‐fully synthesized by an automated process,with three batches of yields stable at 30.2%,30.1%and 30.4%,and the radiochemi‐cal purity over 95%,meeting the quality control standards.Micro PET/CT imaging showed that ^(18)F-Fallypride had a specific high uptake in the mouse striatum,and the uptake value of the striatum in the social feeding group was(8.58±2.11)%ID/g,which was significantly higher than that in the PD model group(4.38±0.37%ID/g,P=0.027)and the single cage isolation group(4.56±0.11%ID/g,P=0.030).The results of ^(18)F-FDG imaging showed that the uptake values in multiple brain regions of PD model group were significantly higher than those of single cage isolation group and social group(P<0.05),whereas,there was no significant difference in the uptake values between single cage isolation group and normal control group(P>0.05).Conclusion Compared with the social group,the dopamine D2 receptor activity in the brain of mice in the single cage isolation group is de‐creased,which is close to the level of PD model group;however,no significant statistical

关 键 词：帕金森病 ~(18)F-二甲氧基苯甲酰胺 正电子发射断层显像 

分 类 号：R745.1[医药卫生—神经病学与精神病学] R817[医药卫生—临床医学]