The preclinical pharmacological study of dopamine transporter imaging agent <sup>18</sup>F-FP-β-CIT

Xiaomin LI; Zhengping CHEN; Songpei WANG; Jie TANG; Yansong LIN; Zhaohui ZHU; Ping FANG

doi:10.1016/S1001-8042(07)60050-5

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

RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE | Updated：2021-01-29

- The preclinical pharmacological study of dopamine transporter imaging agent ¹⁸F-FP-β-CIT
- Nuclear Science and Techniques Vol. 18, Issue 4, (2007)
- Affiliations：
  
  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
- Author bio：
  
  Correspondence author. E-mail: czp72@163.com
- Funds：
- DOI：10.1016/S1001-8042(07)60050-5
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Cite this article
Xiaomin LI, Zhengping CHEN, Songpei WANG, et al. The preclinical pharmacological study of dopamine transporter imaging agent ¹⁸F-FP-β-CIT. [J]. Nuclear Science and Techniques 18(4):223-226(2007)
DOI：

Xiaomin LI, Zhengping CHEN, Songpei WANG, et al. The preclinical pharmacological study of dopamine transporter imaging agent ¹⁸F-FP-β-CIT. [J]. Nuclear Science and Techniques 18(4):223-226(2007) DOI： 10.1016/S1001-8042(07)60050-5.

摘要

Abstract

The paper is to study pharmacologic characteristics of ,18,F-FP-β-CIT (,18,F-N-(3-fluoropropyl)-2β- carbomethoxy-3β- (4-iodophenyl)nortropane) as an imaging agent for dopamine transporter. The radiochemical purity of,18,F-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,18,F-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,18,F-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,18,F-FP-β-CIT is very safe. So,18,F-FP-β-CIT is a promising PET imaging agent for DAT with safety and validity.

关键词

Keywords

Parkinson's diseaseDopamine transporterRadionuclide imaging18F-FP-β-CITBiodistributionPharmacokinetics

references

Abi-Dargham A, Gandelsman M S, De Erausquin G A, et al. J Nucl Med, 1996, 37: 1129-1133.

Goodman M M, Keil R, Shoup T M, et al. J Nucl Med, 1997, 38: 119-126.

Yung B C K, Dannals R F, Kuhar M J, et al. J Nucl Med, 1993, 34: S197.

Kung H F, Kim H J, Kung M P, et al. Eur J Nucl Med, 1996, 23: 1527-1530.

Chalyl T, Dhawan V, Kazumata K, et al. Nucl Med Biol, 1996, 23: 999-1004.

Fang Ping, Chen Zhengping, Lin Yansong, et al. Isotopes (in Chinese), 2001, 14: 6-10.

Chen Zhengping, Wu Chunying, Zhang Zhengwei, et al. Chin J Nucl Med (in Chinese), 2003, 23: 241-243.

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National Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine

Nuclear Medicine Department, The 2nd Hospital of Suzhou University

Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine

The Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine

Huashan Hospital, Fudan University

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

DOI：10.1016/S1001-8042(07)60050-5

摘要

Abstract

关键词

Keywords

references

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