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乳和-18标记的胺是一种具有增强体内稳定性的PET成像剂

Hari K Akula^1,2, Bao Hu^1,2, Jaclyn Brunner^3,4

¹Department of Psychiatry and Behavioral Health, Renaissance School of Medicine at Stony Brook University, Stony Brook, New York 11794, United States.

|July 21, 2025

概括

一种新的双同位素标记为质胺, (2S,4R) - [4-18F-3,3,4-d3]-质胺 (4-[18F]-FGln-d3),在体内改善了对胺代谢成像的稳定性. 这种新型的放射追踪剂与其原始化合物相比,提供了可比的瘤吸收率和减少的骨吸收率.

科学领域:

核医学就是核医学.
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:

谷氨胺代谢在各种生理和病理过程中至关重要,包括癌症.
目前用于谷氨胺代谢的成像剂可能在体内稳定性的局限性.
需要开发具有增强稳定性的新型放射性追踪剂,以进行准确的体内评估.

研究的目的:

设计,合成和评估一种新型的和-18双同位素标记为黄胺, (2S,4R) - [4-18F-3,3,4-d3]-黄胺 (4-[18F]-FGln-d3).
评估4-[18F]-FGln-d3作为一种具有改善体内稳定性的谷氨酸代谢成像剂的潜力.
为了比较4-[18F]-FGln-d3与其母化合物4-[18F]-FGln.d3的性能,

主要方法:

通过六个步骤的途径合成一个四基化荷马塞林中间体,包括性HPLC.
制备一个 (2S,4S) -托西拉酸前体.
半自动生产4-[18F]-FGln-d3和随后的体外细胞吸收和体内小鼠成像研究.

主要成果:

成功合成并制备了4-[18F]-FGln-d3.
4-[18F]-FGln-d3表现出与4-[18F]-FGln.d3相似的细胞吸收和可比的瘤吸收和瘤与肌肉的比率.
一个值得注意的发现是,注射后120分钟4-[18F]-FGln-d3的放射性骨吸收量适度降低.

结论:

初步数据表明,与4-[18F]-FGln.d3相比,4-[18F]-FGln.d3在体内稳定性得到改善.
改进的稳定性要求进一步调查4-[18F]-FGln-d3作为PET成像剂.
这种新型的放射追踪器有望在体内以更高的稳定性探测谷氨胺代谢.

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