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 ›› 2001, Vol. 12 ›› Issue (4): 256

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Pharmacological studies of dopamine transporter imaging agent 125/131I -β- CIT

DING Shi-Yu1, ZHOU Xiang1, TANG Jun1, CITEN Zheng-Ping1, WANG Feng2, WU Chun-Ying1, LIN Yan-Song JI Shu-Ren1, LU Chun-Xiong1, FANG Ping1   

  1. 1 National Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medwine, Wusi 214063;
    2 1 Nuclear Medicine Department, The 2nd Hospital of Suzhow Universiiy, Suzhou 215004
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DING Shi-Yu, ZHOU Xiang, TANG Jun, CITEN Zheng-Ping, WANG Feng, WU Chun-Ying, LIN Yan-Song JI Shu-Ren, LU Chun-Xiong!, FANG Ping. Pharmacological studies of dopamine transporter imaging agent 125/131I -β- CIT.Nuclear Science and Techniques, 2001, 12(4): 256

Abstract: To prepare 125/131I-β- CIT (29-carbomthoxy-34- (4-iodophenyljtropane as an imaging agent for dopamine transporter (DAT), the labeling method from tail. utylstanny] precursor with peracetic acid has been reported in this article. The radio: chemical purity (RCP) of the labeled compound was aver 95% determined by HPLC and TLC. The stability, partition coefficicuts were also determined. ‘The pharuaco. logical studies of the imaging agent were performed in rats, mice, rabbits and notmal monkey. The ligand showed preferable uptake in brain (1.9%ID/organ i rats and 4.5%ID/organ in mice at 5min). The ratios of striatum/cerebellum, hippocani pus/cerebellum and cortex/cerebellum were 28.9. 3.97 and 4.75 at 6h in rats. aud 8.52, 2.99 and 3.06 at 6h in mice, respectively. In monkey brain imaging the ratios of striatumn/frontal cortex (ST/FC) and sti ccipital cortex (ST/OC) were 5.14 and 5.97 at 4h. respectively. All of above showed the high affinity of the igand uw DAT. The compound was primarily metabolized in liver becanse the hepatic nptake was much higher than other organs (75.4%1D/organ at 18h). The half-life of blood elimination was 5min. The dose received by mice was 2500 times as high as that re ceived by human in the test of undue toxicity, which evaluated the safety of the agent, All the results suggest that β- CIT can be used as a potential DAT imaging agent.

Key words: 125/131I-β-CIT, Labeling, Dopamine Transporter, Biodistribution, Parkinson's disease