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氘和氟-18标记的谷氨酰胺——一种具有增强体内稳定性的正电子发射断层显像剂

Deuterium- and Fluorine-18-Labeled Glutaminea PET Imaging Agent with Enhanced In Vivo Stability.

作者信息

Akula Hari K, Hu Bao, Brunner Jaclyn, Li Kaixuan, Saleh Lemise, Vaska Paul, Qu Wenchao

机构信息

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

PET Research Core, Renaissance School of Medicine at Stony Brook University, Stony Brook, New York 11794, United States.

出版信息

ACS Omega. 2025 Jul 3;10(27):29741-29753. doi: 10.1021/acsomega.5c03771. eCollection 2025 Jul 15.

DOI:10.1021/acsomega.5c03771
PMID:40686998
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12268413/
Abstract

Deuterium and fluorine-18 dual-isotope-labeled fluoroglutamine, (2,4)-[4-F-3,3,4- ]-fluoroglutamine (4-[F]-FGln- ), was designed, synthesized, and biologically evaluated for its potential as a novel glutamine metabolic imaging agent with improved in vivo stability. The tetradeuterated homoserine intermediate was first synthesized via a six-step synthetic pathway, including a chiral HPLC separation process. Next, (2,4)-tosylate precursor was prepared following the reference-reported method, and 4-[F]-FGln- was successfully prepared using a semiautomated production process. After that, a head-to-head comparison of 4-[F]-FGln- with its parent compound 4-[F]-FGln including in vitro cell uptake and in vivo murine animal imaging studies illustrated that the new tracer 4-[F]-FGln- has a similar cell uptake manner and comparable tumor uptake and tumor-to-muscle ratio as 4-[F]-FGln, but moderately decreased radioactivity bone uptake at 120 min postinjection. Overall, the preliminary data from this research indicate the better in vivo stability of 4-[F]-FGln- compared with its counterpart 4-[F]-FGln, which warrants further investigation of this radiotracer as the new PET imaging agent with enhanced stability for probing the glutamine metabolism in vivo.

摘要

设计、合成了氘和氟 - 18双同位素标记的氟谷氨酰胺，即(2,4)-[4-F-3,3,4- ]-氟谷氨酰胺(4-[F]-FGln- )，并对其作为一种体内稳定性更高的新型谷氨酰胺代谢成像剂的潜力进行了生物学评估。首先通过包括手性高效液相色谱分离过程在内的六步合成途径合成了四氘代高丝氨酸中间体。接下来，按照参考文献报道的方法制备了(2,4)-甲苯磺酸酯前体，并使用半自动生产工艺成功制备了4-[F]-FGln- 。之后，对4-[F]-FGln- 与其母体化合物4-[F]-FGln进行了直接比较，包括体外细胞摄取和体内小鼠动物成像研究，结果表明新示踪剂4-[F]-FGln- 与4-[F]-FGln具有相似的细胞摄取方式、相当的肿瘤摄取和肿瘤与肌肉比值，但在注射后120分钟时放射性骨摄取略有降低。总体而言，本研究的初步数据表明4-[F]-FGln- 与其对应物4-[F]-FGln相比具有更好的体内稳定性，这使得该放射性示踪剂作为一种用于探测体内谷氨酰胺代谢的稳定性增强的新型正电子发射断层扫描(PET)成像剂值得进一步研究。

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