Synthesis and evaluation of TSPO-targeting radioligand 18FF-TFQC for PET neuroimaging in epileptic rats.
- Author:
Wenhui FU
1
;
Qingyu LIN
1
;
Zhequan FU
1
;
Tingting YANG
1
;
Dai SHI
1
;
Pengcheng MA
1
;
Hongxing SU
1
;
Yunze WANG
1
;
Guobing LIU
1
;
Jing DING
2
;
Hongcheng SHI
1
;
Dengfeng CHENG
1
Author Information
- Publication Type:Journal Article
- Keywords: Epilepsy; Fluorine-18; Neuroimaging; PET; TSPO
- From: Acta Pharmaceutica Sinica B 2025;15(2):722-736
- CountryChina
- Language:English
- Abstract: 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.
