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用-18标记的PET放射追踪剂用于成像巨细胞殖民地刺激因子1受体 (CSF1R)

Deepankar Das¹, Hyojin Cha¹, Ravi Naik¹

¹Department of Radiology and Radiological Science, Johns Hopkins Medical Institutions, Baltimore, MD, USA.

EJNMMI radiopharmacy and chemistry

|January 11, 2026

概括

研究人员开发了新的18F标记的正子发射断层扫描 (PET) 放射标志物,针对巨菌群刺激因子1受体 (CSF1R) 进行神经炎症成像. 该化合物[18F]3显示出有前途的大脑吸收和选择性,这表明它有可能用于临床翻译.

科学领域:

神经成像是一种神经成像.
放射化学放射化学是指辐射化学.
分子成像学分子成像学

背景情况:

定子发射断层扫描 (PET) 对于人类定量神经炎症成像至关重要.
巨菌群刺激因子1受体 (CSF1R) 是一个有前途的目标,因为它在激活的微质上表达.
目前没有合适的18F标记的CSF1R PET射线追踪器.

研究的目的:

合成和临床前评估用于成像CSF1R.新型18F标记PET放射追踪剂.
为了识别具有高亲和力,适合大脑透,并对CSF1R.具有选择性的辐射追踪器.

主要方法:

合成了一系列新的高亲和力CSF1R连体.
用18F进行放射性标记,并对5种得到的放射性标记物进行表征.
在体外测定,小鼠生物分布研究,的PET成像.

主要成果:

合成了5种被标记为18F的放射性追踪剂,其中[18F]3在小鼠中显示了最高的脑吸收率 (12.5%ID/g在5分钟内).
[18F]3在脂聚糖诱导的神经炎症模型中表明吸收增加 (97%的增加) 和的高脑吸收 (SUV=5.2).
在体内研究显示可逆动力学,适度的特异结合,和[18F]3的最小代谢,有利的剂量测量.

结论:

开发和评估了一系列新的CSF1R PET射线追踪器.
[18F]3对CSF1R和神经炎症具有有利的PET成像特性.
需要对非人类灵长类动物模型进行进一步评估,并将其转化为人类实验对象.

关键词:

在CSF1R中,CSF1R是最重要的.微质细胞中的微质细胞神经炎症是一种神经炎症.定子发射断层扫描 (PET) 是一种定子发射断层扫描.铁氨酸激酶酶的使用方法

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