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1
Quantification of translocator protein (18 kDa) in the human brain with PET and a novel radioligand, (18)F-PBR06.使用正电子发射断层扫描(PET)和新型放射性配体(18)F - PBR06对人脑中转运体蛋白(18 kDa)进行定量分析。
J Nucl Med. 2009 Jul;50(7):1047-53. doi: 10.2967/jnumed.108.060186. Epub 2009 Jun 12.
2
Comparative evaluation of the translocator protein radioligands 11C-DPA-713, 18F-DPA-714, and 11C-PK11195 in a rat model of acute neuroinflammation.在大鼠急性神经炎症模型中对转运体蛋白放射性配体11C-DPA-713、18F-DPA-714和11C-PK11195的比较评估。
J Nucl Med. 2009 Mar;50(3):468-76. doi: 10.2967/jnumed.108.058669. Epub 2009 Feb 17.
3
Single-step high-yield radiosynthesis and evaluation of a sensitive 18F-labeled ligand for imaging brain peripheral benzodiazepine receptors with PET.用于正电子发射断层显像(PET)成像脑外周苯二氮䓬受体的一种灵敏的18F标记配体的单步高产率放射性合成及评估
J Med Chem. 2009 Feb 12;52(3):688-99. doi: 10.1021/jm8011855.
4
Nuclear imaging of neuroinflammation: a comprehensive review of [11C]PK11195 challengers.神经炎症的核成像:[11C]PK11195竞争剂的全面综述
Eur J Nucl Med Mol Imaging. 2008 Dec;35(12):2304-19. doi: 10.1007/s00259-008-0908-9. Epub 2008 Oct 1.
5
Synthesis of [11C]FEDAA1106 as a new PET imaging probe of peripheral benzodiazepine receptor expression.新型PET成像探针[11C]FEDAA1106的合成——用于外周苯二氮䓬受体表达研究
Eur J Med Chem. 2009 Jun;44(6):2748-53. doi: 10.1016/j.ejmech.2008.08.001. Epub 2008 Aug 13.
6
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7
Increased binding of peripheral benzodiazepine receptor in Alzheimer's disease measured by positron emission tomography with [11C]DAA1106.采用[11C]DAA1106正电子发射断层扫描技术测量阿尔茨海默病中外周苯二氮䓬受体结合增加。
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8
Kinetic analysis in healthy humans of a novel positron emission tomography radioligand to image the peripheral benzodiazepine receptor, a potential biomarker for inflammation.在健康人体中对一种新型正电子发射断层扫描放射性配体进行动力学分析,以成像外周苯二氮䓬受体,这是一种潜在的炎症生物标志物。
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9
Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo.两种用于体内成像脑外周苯二氮䓬受体的灵敏的11C标记芳氧基苯胺配体在猴体内的合成与评价
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10
Brain and whole-body imaging in nonhuman primates of [11C]PBR28, a promising PET radioligand for peripheral benzodiazepine receptors.用[11C]PBR28对非人灵长类动物进行脑和全身成像,[11C]PBR28是一种用于外周苯二氮䓬受体的有前景的正电子发射断层显像(PET)放射性配体。
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新型 PET 配体(18)F-PBR06 用于成像转位蛋白(18 kDa)的人体生物分布和辐射剂量学

Biodistribution and radiation dosimetry in humans of a new PET ligand, (18)F-PBR06, to image translocator protein (18 kDa).

机构信息

Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland 20892-2035, USA.

出版信息

J Nucl Med. 2010 Jan;51(1):145-9. doi: 10.2967/jnumed.109.068064. Epub 2009 Dec 15.

DOI:10.2967/jnumed.109.068064
PMID:20008980
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2997572/
Abstract

UNLABELLED

As a PET biomarker for inflammation, translocator protein (18 kDa) (TSPO) can be measured with an (18)F-labeled aryloxyanilide, (18)F-N-fluoroacetyl-N-(2,5-dimethoxybenzyl)-2-phenoxyaniline ((18)F-PBR06), in the human brain. The objective of this study was to estimate the radiation absorbed doses of (18)F-PBR06 based on biodistribution data in humans.

METHODS

After the injection of (18)F-PBR06, images were acquired from head to thigh in 7 healthy humans. Urine was collected at various time points. Radiation absorbed doses were estimated by the MIRD scheme.

RESULTS

Moderate to high levels of radioactivity were observed in organs with high densities of TSPO and in organs of metabolism and excretion. Bone had low levels of radioactivity. The effective dose was 18.5 muSv/MBq.

CONCLUSION

The effective dose of (18)F-PBR06, compared with other (18)F radioligands, was moderate. This radioligand had negligible defluorination, as indirectly assessed by bone radioactivity. Doses to the gallbladder wall and spleen may limit the amount of permissible injected radioactivity.

摘要

未加标签

作为炎症的 PET 生物标志物,转位蛋白(18 kDa)(TSPO)可以用(18)F 标记的芳氧基苯胺((18)F-N-氟乙酰基-N-(2,5-二甲氧基苄基)-2-苯氧基苯胺((18)F-PBR06)在人脑中进行测量。本研究的目的是根据人体的生物分布数据估算(18)F-PBR06 的吸收剂量。

方法

在 7 名健康人中注射(18)F-PBR06 后,从头部到大腿采集图像。在不同时间点收集尿液。通过 MIRD 方案估算辐射吸收剂量。

结果

在 TSPO 密度高的器官和代谢及排泄器官中观察到中等至高水平的放射性。骨骼放射性水平较低。有效剂量为 18.5 μSv/MBq。

结论

与其他(18)F 放射性配体相比,(18)F-PBR06 的有效剂量适中。这种放射性配体几乎没有脱氟作用,这可以通过骨骼放射性间接评估。胆囊壁和脾脏的剂量可能会限制允许注射的放射性物质的量。