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

IF 1.7 4区化学 Q3 CHEMISTRY, INORGANIC & NUCLEAR

Journal of Fluorine Chemistry Pub Date : 2024-10-22 DOI:10.1016/j.jfluchem.2024.110367

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

引用次数: 0

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 in vivo evaluation for [¹⁸F]TZ78141 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.

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用两种 F-18 放射化学方法合成有前景的瞬态受体电位 5 (TRPC5) 放射配体

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 具有良好的化学特性和核物理特性，是 PET 成像最广泛使用的放射性核素之一。在此，我们介绍了两种互补的放射合成方法，并对[18F]TZ78141进行了初步的体内评估，它是一种新型的、有前途的氟-18标记放射性示踪剂，可用于TRPC5成像。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很大的优势。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Fluorine Chemistry 化学-无机化学与核化学

CiteScore

3.80

自引率

10.50%

发文量

审稿时长

33 days

期刊介绍： The Journal of Fluorine Chemistry contains reviews, original papers and short communications. The journal covers all aspects of pure and applied research on the chemistry as well as on the applications of fluorine, and of compounds or materials where fluorine exercises significant effects. This can include all chemistry research areas (inorganic, organic, organometallic, macromolecular and physical chemistry) but also includes papers on biological/biochemical related aspects of Fluorine chemistry as well as medicinal, agrochemical and pharmacological research. The Journal of Fluorine Chemistry also publishes environmental and industrial papers dealing with aspects of Fluorine chemistry on energy and material sciences. Preparative and physico-chemical investigations as well as theoretical, structural and mechanistic aspects are covered. The Journal, however, does not accept work of purely routine nature. For reviews and special issues on particular topics of fluorine chemistry or from selected symposia, please contact the Regional Editors for further details.