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[^(1...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[^(18)F]F-TFQC,an m-trifluoromethyl ER176 analog,in the PET neuroimaging of epileptic rats.Initially,[^(18)F]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[^(18)F]F-TFQC exhibited good biochemical properties,[^(18)F]F-TFQC PET neuroimaging was performed in epileptic rats at multiple time points in various stages of disease progression.PET imaging showed specific[^(18)F]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,[^(18)F]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.展开更多
基金supported by the National Natural Science Foundation of China(No.82172002 and 82272058,China)Shanghai Municipal Science and Technology Committee of Shanghai Outstanding Academic Leaders Plan(No.21XD1423500,China)National Key Research and Development Program of China(No.2022YFC2406901).
文摘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[^(18)F]F-TFQC,an m-trifluoromethyl ER176 analog,in the PET neuroimaging of epileptic rats.Initially,[^(18)F]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[^(18)F]F-TFQC exhibited good biochemical properties,[^(18)F]F-TFQC PET neuroimaging was performed in epileptic rats at multiple time points in various stages of disease progression.PET imaging showed specific[^(18)F]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,[^(18)F]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.
