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

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• 作者：Xiaomin LI ; Zhengping CHEN ; Songpei WANG ; Jie TANG ; Yansong LIN ; Zhaohui ZHU ; Ping FANG
• 关键词：Parkinson's disease ; Dopamine transporter ; Radionuclide imaging ; ¹⁸F-FP-β ; -CIT ; Biodistribution ; Pharmacokinetics
  CLC numbers ; 0628.5⁺1 ; R962 ; R742.5 ; R817
• 刊名：Nuclear Science and Techniques
• 出版年：2007
• 出版时间：August 2007
• 年：2007
• 卷：18
• 期：4
• 页码：223-226
• 全文大小：736 K

文摘

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 5 min 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-FPβ-CIT is very safe. So ¹⁸F-FP-β-CIT is a promising PET imaging agent for DAT with safety and validity.