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Cell. 2024 Aug 8;187(16):4176-4192.e17. doi: 10.1016/j.cell.2024.06.001. Epub 2024 Jul 2.
2
Synthetic F labeled biomolecules that are selective and promising for PET imaging: major advances and applications.用于正电子发射断层扫描（PET）成像具有选择性且前景广阔的合成F标记生物分子：主要进展与应用
RSC Med Chem. 2024 Apr 17;15(6):1899-1920. doi: 10.1039/d4md00033a. eCollection 2024 Jun 19.
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Radiosynthesis and Evaluation of a C-11 Radiotracer for Transient Receptor Potential Canonical 5 in the Brain.放射性合成与脑内瞬时受体电位经典型 5 放射性示踪剂的评价。
Mol Imaging Biol. 2023 Apr;25(2):334-342. doi: 10.1007/s11307-022-01760-y. Epub 2022 Aug 11.
4
Clinical validation of the novel HDAC6 radiotracer [F]EKZ-001 in the human brain.新型 HDAC6 放射性示踪剂 [F]EKZ-001 在人脑的临床验证。
Eur J Nucl Med Mol Imaging. 2021 Feb;48(2):596-611. doi: 10.1007/s00259-020-04891-y. Epub 2020 Jul 8.
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Ruthenium-Mediated F-Fluorination and Preclinical Evaluation of a New CB Receptor Imaging Agent [F]FPATPP.钌介导的 F-F 氟代反应和新型 CB 受体成像剂 [F]FPATPP 的临床前评估。
ACS Chem Neurosci. 2020 Jul 1;11(13):2009-2018. doi: 10.1021/acschemneuro.0c00313. Epub 2020 Jun 16.
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Translation of HDAC6 PET Imaging Using [F]EKZ-001-cGMP Production and Measurement of HDAC6 Target Occupancy in Nonhuman Primates.使用 [F]EKZ-001-cGMP 进行 HDAC6 PET 成像翻译及在非人灵长类动物中测量 HDAC6 靶标占有率。
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TRPC channels: Structure, function, regulation and recent advances in small molecular probes.TRPC 通道：结构、功能、调控及小分子探针的最新进展。
Pharmacol Ther. 2020 May;209:107497. doi: 10.1016/j.pharmthera.2020.107497. Epub 2020 Jan 28.
8
Development of a carbon-11 PET radiotracer for imaging TRPC5 in the brain.开发一种用于脑部 TRPC5 成像的碳-11 PET 放射性示踪剂。
Org Biomol Chem. 2019 Jun 5;17(22):5586-5594. doi: 10.1039/c9ob00893d.
9
Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.瞬时受体电位经典型通道调节剂（TRPC5）及相关疾病的研究进展
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两种用F-18进行放射化学合成有前景的瞬时受体电位香草酸亚型5（TRPC5）放射性配体的方法。

Two F-18 radiochemistry methods to synthesize a promising transient receptor potential canonical 5 (TRPC5) radioligand.

作者信息

Yu Yanbo, Jadhav Sandip B, Xing Zhimin, Jiang Hao, Qiu Lin, Huang Tianyu, Perlmutter Joel S, Li Zibo, Tu Zhude

机构信息

Department of Radiology, Washington University School of Medicine, St Louis, MO 63110, USA.

Department of Neurology and Neuroscience, Washington University School of Medicine, St Louis, MO 63110, USA.

出版信息

J Fluor Chem. 2024 Nov;280. doi: 10.1016/j.jfluchem.2024.110367. Epub 2024 Oct 22.

DOI:10.1016/j.jfluchem.2024.110367
PMID:40520526
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12161451/
Abstract

TRPC5 is a member of the mammalian transient receptor potential (TRP) channel superfamily and it has been implicated in various physiological and pathological mechanisms of neurological and psychiatric diseases. Fluorine-18 is one of the most widely used radionuclides for PET imaging due to its favorable chemical characteristics and nuclear-physical properties. Herein, we describe two complementary radiosynthetic approaches and preliminary evaluation for [F] as a novel and promising fluorine-18 labeled radiotracer for imaging TRPC5. The latter strategy employed a ruthenium-mediated radiofluorination method, facilitating the rapid synthesis of the desired radiotracer with substantial advantages in simplicity and efficiency.

摘要

TRPC5是哺乳动物瞬时受体电位（TRP）通道超家族的成员，它与神经和精神疾病的各种生理和病理机制有关。氟-18由于其良好的化学特性和核物理性质，是正电子发射断层扫描（PET）成像中使用最广泛的放射性核素之一。在此，我们描述了两种互补的放射性合成方法，并对[F]作为一种用于成像TRPC5的新型且有前景的氟-18标记放射性示踪剂进行了初步评估。后一种策略采用了钌介导的放射性氟化方法，有助于快速合成所需的放射性示踪剂，在简便性和效率方面具有显著优势。