Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2007, Vol. 18 ›› Issue (4): 223 doi: 10.1016/S1001-8042(07)60050-5


The preclinical pharmacological study of dopamine transporter imaging agent 18F-FP-β-CIT

LI Xiaomin1 CHEN Zhengping1* WANG Songpei1 TANG Jie1 LIN Yansong2 ZHU Zhaohui2 FANG Ping1   

  1. 1 Jiangsu Institute of Nuclear Medicine, Key Laboratory of Nuclear Medicine, Ministry of Health , Wuxi 214063, China;
    2 PET Center, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing 100730, China
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LI Xiaomin CHEN Zhengping WANG Songpei TANG Jie LIN Yansong ZHU Zhaohui FANG Ping. The preclinical pharmacological study of dopamine transporter imaging agent 18F-FP-β-CIT.Nuclear Science and Techniques, 2007, 18(4): 223     doi: 10.1016/S1001-8042(07)60050-5

Abstract: The paper is to study pharmacologic characteristics of 18F-FP-β-CIT (18F-N-(3-fluoropropyl)-2β- carbomethoxy- 3β- (4-iodophenyl)nortropane) as an imaging agent for dopamine transporter. The radiochemical purity of 18F-FP-β-CIT in aqueous solution was over 95% after standing at room temperature for 4h. Biodistribution displayed rapid uptake in rat brain (1.375 %ID/organ at 5min and 0.100 %ID/organ at 180 min) and the striatal uptake was 1.444, 0.731, 0.397, 0.230 and 0.146 %ID/g at 5, 30, 60, 120 and 180 min, respectively. The values of striatum/cerebellum, striatum /frontal cortex and striatum / hippocampus in rat’s brain at 30 min were 3.38, 2.17 and 2.40 respectively. The uptake in striatum can be blocked by β-CFT, suggesting that 18F-FP-β-CIT binds to DAT peculiarly. The compound was rapidly cleared from monkey’s blood. The striatal uptake was bilaterally decreased in the left-sided lesioned PD rats, compared with normal control. Brain PET imaging studies in normal monkey showed that 18F-FP-β-CIT was concentrated in striatum. The test of undue toxicity showed that the dose received by mice was 1250 times as by human, which indicates that 18F-FP-β-CIT is very safe. So 18F-FP-β-CIT is a promising PET imaging agent for DAT with safety and validity.

Key words: Parkinson’s disease, Dopamine transporter, Radionuclide imaging, 18F-FP-β-CIT, Biodistribution, Pharmacokinetics