PDF(Pubmed)
Abstract：
OBJECTIVE: N-benzyl-N-methyl-2-[7, 8-dihydro-7-(2-[18F] fluoroethyl) -8-oxo-2-phenyl-9H-purin-9-yl] acetamide ([18F] FEDAC) is a novel positron emission tomography (PET) tracer that targets the translocator protein (TSPO; 18 kDa) in the mitochondrial outer membrane, which is known to be upregulated in various diseases such as malignant tumors, neurodegenerative diseases, and neuroinflammation. This study presents the first attempt to use [18F]FEDAC PET/CT and evaluate its biodistribution as well as the systemic radiation exposure to the radiotracer in humans.
METHODS: Seventeen whole-body [18F]FEDAC PET/CT (injected dose, 209.1 ± 6.2 MBq) scans with a dynamic scan of the upper abdomen were performed in seven participants. Volumes of interest were assigned to each organ, and a time-activity curve was created to evaluate the biodistribution of the radiotracer. The effective dose was calculated using IDAC-Dose 2.1.
RESULTS: Immediately after the intravenous injection, the radiotracer accumulated significantly in the liver and was subsequently excreted into the gastrointestinal tract through the biliary tract. It also showed high levels of accumulation in the kidneys, but showed minimal migration to the urinary bladder. Thus, the liver was the principal organ that eliminated [18F] FEDAC. Accumulation in the normal brain tissue was minimal. The effective dose estimated from biodistribution in humans was 19.47 ± 1.08 µSv/MBq, and was 3.60 mSV for 185 MBq dose.
CONCLUSIONS: [18F]FEDAC PET/CT provided adequate image quality at an acceptable effective dose with no adverse effects. Therefore, [18F]FEDAC may be useful in human TSPO-PET imaging.
METHODS: Seventeen whole-body [18F]FEDAC PET/CT (injected dose, 209.1 ± 6.2 MBq) scans with a dynamic scan of the upper abdomen were performed in seven participants. Volumes of interest were assigned to each organ, and a time-activity curve was created to evaluate the biodistribution of the radiotracer. The effective dose was calculated using IDAC-Dose 2.1.
RESULTS: Immediately after the intravenous injection, the radiotracer accumulated significantly in the liver and was subsequently excreted into the gastrointestinal tract through the biliary tract. It also showed high levels of accumulation in the kidneys, but showed minimal migration to the urinary bladder. Thus, the liver was the principal organ that eliminated [18F] FEDAC. Accumulation in the normal brain tissue was minimal. The effective dose estimated from biodistribution in humans was 19.47 ± 1.08 µSv/MBq, and was 3.60 mSV for 185 MBq dose.
CONCLUSIONS: [18F]FEDAC PET/CT provided adequate image quality at an acceptable effective dose with no adverse effects. Therefore, [18F]FEDAC may be useful in human TSPO-PET imaging.
摘要：
目的：N-苄基-N-甲基-2-[7，8-二氢-7-（2-[18F]氟乙基）-8-氧代-2-苯基-9H-嘌呤-9-基]乙酰胺（[18F]FEDAC）是一种新型的正电子发射断层扫描（PET）示踪剂，靶向线粒体外膜中的转运蛋白（TSPO；18kDa）已知在各种疾病如恶性肿瘤中上调，神经退行性疾病，和神经炎症。这项研究首次尝试使用[18F]FEDACPET/CT并评估其生物分布以及人体对放射性示踪剂的全身辐射暴露。
方法：十七个全身[18F]FEDACPET/CT（注射剂量，对7名参与者进行了209.1±6.2MBq）扫描和上腹部动态扫描。感兴趣的量被分配给每个器官，并创建时间-活动曲线以评估放射性示踪剂的生物分布。使用IDAC-剂量2.1计算有效剂量。
结果：静脉注射后立即，放射性示踪剂在肝脏中大量积累，随后通过胆道排泄到胃肠道中。它还显示出高水平的肾脏积累，但向膀胱的迁移很少.因此，肝脏是消除[18F]FEDAC的主要器官。正常脑组织中的积累很少。根据人体生物分布估计的有效剂量为19.47±1.08µSv/MBq，185MBq剂量为3.60mSV。
结论：[18F]FEDACPET/CT在可接受的有效剂量下提供了足够的图像质量，没有不良反应。因此,[18F]FEDAC可用于人TSPO-PET成像。
方法：十七个全身[18F]FEDACPET/CT（注射剂量，对7名参与者进行了209.1±6.2MBq）扫描和上腹部动态扫描。感兴趣的量被分配给每个器官，并创建时间-活动曲线以评估放射性示踪剂的生物分布。使用IDAC-剂量2.1计算有效剂量。
结果：静脉注射后立即，放射性示踪剂在肝脏中大量积累，随后通过胆道排泄到胃肠道中。它还显示出高水平的肾脏积累，但向膀胱的迁移很少.因此，肝脏是消除[18F]FEDAC的主要器官。正常脑组织中的积累很少。根据人体生物分布估计的有效剂量为19.47±1.08µSv/MBq，185MBq剂量为3.60mSV。
结论：[18F]FEDACPET/CT在可接受的有效剂量下提供了足够的图像质量，没有不良反应。因此,[18F]FEDAC可用于人TSPO-PET成像。
