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F-标记二氢甲噻嗪:用于成像完整大脑中活性氧的正电子发射断层扫描放射性示踪剂。

F-Labeled dihydromethidine: positron emission tomography radiotracer for imaging of reactive oxygen species in intact brain.

机构信息

School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.

Central Research Laboratory, Hamamatsu Photonics K. K., 5000 Hirakuchi, Hamakita-Ku, Hamamatsu, Shizuoka 434-8601, Japan.

出版信息

Org Biomol Chem. 2020 Apr 1;18(13):2387-2391. doi: 10.1039/d0ob00126k.

Abstract

Dihydromethidine (DHM) labeled with 18F at the para position of the peripheral benzene ring was designed as a positron emission tomography (PET) radiotracer for non-invasive imaging of reactive oxygen species (ROS). This compound readily crosses the blood-brain barrier and is oxidized by ROS, and the oxidation product is retained intracellularly. PET imaging of ROS-producing rat brain microinfused with sodium nitroprusside identified specific brain regions with high ROS concentrations. This tracer should be useful for studies of the pathophysiological roles of ROS, and in the diagnosis of neurodegenerative diseases.

摘要

二氢甲基多巴胺(DHM)在苯环的对位用 18F 标记,被设计为一种正电子发射断层扫描(PET)放射性示踪剂,用于非侵入性成像活性氧(ROS)。该化合物很容易穿过血脑屏障并被 ROS 氧化,氧化产物被保留在细胞内。用硝普酸钠微灌注产生 ROS 的大鼠脑进行 PET 成像,确定了具有高 ROS 浓度的特定脑区。这种示踪剂应该对研究 ROS 的病理生理作用以及神经退行性疾病的诊断有用。

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