靶向大麻素2型受体PET探针18F-JR-1002在胰腺导管腺癌分子成像中的应用OA
Molecular imaging of pancreatic cancer with a cannabinoid type 2 receptor targeted PET probe
目的 开发一种靶向大麻素2型受体(CB2R)的新型PET探针(18F-JR-1002),用于胰腺导管腺癌(PDAC)的分子影像学诊断.方法 基于CB2R反向激动剂结构设计并合成18F-JR-1002,采用自动化合成仪(OnePlatform V3.1s)进行放射性标记,测定其放射化学产率、摩尔活度及体外稳定性.通过PANC-2-luc细胞构建小鼠原位PDAC模型,利用MicroPET/CT成像评估探针在肿瘤组织的摄取情况,并与正常小鼠对比分析.结果 18F-JR-1002的放射化学产率为34.7%±8.1%,摩尔活度达264.5±41.2 GBq/μmol,体外3 h内稳定性>95%.MicroPET成像显示,PDAC小鼠胰腺部位探针摄取量高于正常小鼠(P=3.34×10-9),该探针能特异性识别PDAC组织中高表达的CB2R.结论 本研究成功开发了一种高稳定性、高亲和力的CB2R靶向PET探针,可特异性识别PDAC,为早期诊断及疗效评估提供了新的分子影像工具.
Objective To develop a novel PET probe(18F-JR-1002)targeting the cannabinoid type 2 receptor(CB2R)for the molecular imaging diagnosis of pancreatic ductal adenocarcinoma(PDAC).Methods 18F-JR-1002 was designed and synthesized based on a CB2R inverse agonist structure.Radiolabeling was performed using an automated synthesizer(OnePlatform V3.1s),and its radiochemical yield,molar activity,and in vitro stability were determined.An orthotopic PDAC mouse model was established using PANC-2-luc cells.MicroPET/CT imaging was utilized to assess probe uptake in tumor tissues,which was compared with that in normal mice.Results The radiochemical yield of ¹⁸F-JR-1002 was 34.7%±8.1%,with a molar activity of 264.5±41.2 GBq/µmol.It demonstrated excellent in vitro stability(>95%over 3 h).MicroPET imaging revealed significantly higher probe uptake in the pancreatic region of PDAC mice compared to the normal group(P=3.34×10-9),indicating the probe's specific recognition of CB2R,which is highly expressed in PDAC tissues.Conclusion This study successfully developed a highly stable and affine CB2R-targeted PET probe that specifically identifies PDAC,providing a new molecular imaging tool for early diagnosis and treatment efficacy evaluation.
金灿;曹星海;陈俊威;谢玲华;毛迪龙;和庆钢
浙江大学化学工程与生物工程学院,浙江 杭州 310058浙江大学化学工程与生物工程学院,浙江 杭州 310058浙江大学化学工程与生物工程学院,浙江 杭州 310058浙江大学医学院附属第二医院脑科中心,浙江大学脑科学与脑医学学院,浙江 杭州 310009浙江大学化学工程与生物工程学院,浙江 杭州 310058浙江大学化学工程与生物工程学院,浙江 杭州 310058
大麻素2型受体正电子发射断层成像放射性示踪剂胰腺癌诊断
cannabinoid receptor type Ⅱpositron emission tomographyradioactive tracerpancreatic cancerdiagnosis
《分子影像学杂志》 2026 (2)
141-146,6
国家自然科学基金重大科研仪器研制项目(32027802)科技部重点研发计划课题(2021YFA1101702)浙江省"领雁"计划项目(2022C03071、2024C03100)Supported by the National Natural Science Foundation of China Major Research Instrument Development Project(32027802)
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