Synthesis and evaluation of TSPO-targeting radioligand [18F]F-TFQC for PET neuroimaging in epileptic rats

Wenhui Fu; Qingyu Lin; Zhequan Fu; Tingting Yang; Dai Shi; Pengcheng Ma; Hongxing Su; Yunze Wang; Guobing Liu; Jing Ding; Hongcheng Shi; Dengfeng Cheng

Acta Pharmaceutica Sinica B (Feb 2025)

Synthesis and evaluation of TSPO-targeting radioligand [18F]F-TFQC for PET neuroimaging in epileptic rats

Wenhui Fu,
Qingyu Lin,
Zhequan Fu,
Tingting Yang,
Dai Shi,
Pengcheng Ma,
Hongxing Su,
Yunze Wang,
Guobing Liu,
Jing Ding,
Hongcheng Shi,
Dengfeng Cheng

Affiliations

Wenhui Fu: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China
Qingyu Lin: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China
Zhequan Fu: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China
Tingting Yang: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China
Dai Shi: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China
Pengcheng Ma: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China
Hongxing Su: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China
Yunze Wang: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China
Guobing Liu: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China
Jing Ding: Department of Neurology, Zhongshan Hospital, Fudan University, Shanghai 200032, China
Hongcheng Shi: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China; Corresponding authors.
Dengfeng Cheng: Department of Nuclear Medicine, Zhongshan Hospital, Fudan University, Shanghai 200032, China; Institute of Nuclear Medicine, Fudan University, Shanghai 200032, China; Shanghai Institute of Medical Imaging, Shanghai 200032, China; Corresponding authors.

Journal volume & issue: Vol. 15, no. 2
pp. 722 – 736

Abstract

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The translocator protein (TSPO) positron emission tomography (PET) can noninvasively detect neuroinflammation associated with epileptogenesis and epilepsy. This study explored the role of the TSPO-targeting radioligand [18F]F-TFQC, an m-trifluoromethyl ER176 analog, in the PET neuroimaging of epileptic rats. Initially, [18F]F-TFQC was synthesized with a radiochemical yield of 8%–10% (EOS), a radiochemical purity of over 99%, and a specific activity of 38.21 ± 1.73 MBq/nmol (EOS). After determining that [18F]F-TFQC exhibited good biochemical properties, [18F]F-TFQC PET neuroimaging was performed in epileptic rats at multiple time points in various stages of disease progression. PET imaging showed specific [18F]F-TFQC uptake in the right hippocampus (KA-injected site, i.e., epileptogenic zone), which was most pronounced at 1 week (T/NT 1.63 ± 0.21) and 1 month (T/NT 1.66 ± 0.20). The PET results were further validated using autoradiography and pathological analysis. Thus, [18F]F-TFQC can reflect the TSPO levels and localize the epileptogenic zone, thereby offering the potential for monitoring neuroinflammation and guiding anti-inflammatory treatment in patients with epilepsy.

Published in Acta Pharmaceutica Sinica B

ISSN: 2211-3835 (Print); 2211-3843 (Online)
Publisher: Elsevier
Country of publisher: Netherlands
LCC subjects: Medicine: Therapeutics. Pharmacology
Website: https://www.sciencedirect.com/journal/acta-pharmaceutica-sinica-b

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