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 ›› 2006, Vol. 17 ›› Issue (1): 43 doi: 10.1016/S1001-8042(06)60010-9

• RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICIN • Previous Articles     Next Articles

Synthesis, radiolabeling and animal studies of [131I]MPPI: A 5-HT1A imaging agent

SUN Bai-Shan1, 2 LU Chun-Xiong1 ZOU Mei-Fen1 JIANG Quan-Fu1 WANG Song-Pei1 LI Xiao-Min1 CHEN Zheng-Ping1 ZHU Jun-Qing1 WU Chun-Ying1, 2   

  1. 1 Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China
    2 School of Biotechnology, The Key Laboratory of Biotechnology, Ministry of Education, Southern Yangtze University, Wuxi 214036, China
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SUN Bai-Shan LU Chun-Xiong ZOU Mei-Fen JIANG Quan-Fu WANG Song-Pei LI Xiao-Min CHEN Zheng-Ping ZHU Jun-Qing WU Chun-Ying. Synthesis, radiolabeling and animal studies of [131I]MPPI: A 5-HT1A imaging agent.Nuclear Science and Techniques, 2006, 17(1): 43     doi: 10.1016/S1001-8042(06)60010-9
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Abstract: The synthesis and biological evaluation of serotonin (5-HT1A) imaging agent [131I]- 4-iodo-N-{2-[4-(2-methoxyphenyl)-piperazin-1-yl]-ethyl}-N-pridin-2-yl-benzamide ([131I]MPPI ) are reported. The chemical structure of aimed compound and intermediates were confirmed by IR, 1 HNMR, and MS. Radiochemical purity was above 99% determined by TLC. Biodistribution of [131I]MPPI in rats displayed high uptake in hippocampus and low uptake in cerebellum. The ratio of the uptake of [131I]MPPI in hippocampus to that in cerebellum was 2.90 at 30 min post injection. The radioactivity in thyroid was 0.069 and 0.128% ID/g organ at 5 min and 120 min, respectively, and it was increased with time, which suggests that in vivo deiodination may be the major route of metabolism. Ex vivo autoradiography of brain section displayed significant decrease of radioactivity in hippocampus when pretreated with 8-OH-DPAT, a selective 5HT1A agonist, compared with control. These findings strongly suggested that 131I-MPPI could be used as an in vivo marker for studies of pharmacology of the 5-HT1A receptor system in animals.The synthesis and biological evaluation of serotonin (5-HT1A) imaging agent [131I]- 4-iodo-N-{2-[4-(2-methoxyphenyl)-piperazin-1-yl]-ethyl}-N-pridin-2-yl-benzamide ([131I]MPPI ) are reported. The chemical structure of aimed compound and intermediates were confirmed by IR, 1 HNMR, and MS. Radiochemical purity was above 99% determined by TLC. Biodistribution of [131I]MPPI in rats displayed high uptake in hippocampus and low uptake in cerebellum. The ratio of the uptake of [131I]MPPI in hippocampus to that in cerebellum was 2.90 at 30 min post injection. The radioactivity in thyroid was 0.069 and 0.128% ID/g organ at 5 min and 120 min, respectively, and it was increased with time, which suggests that in vivo deiodination may be the major route of metabolism. Ex vivo autoradiography of brain section displayed significant decrease of radioactivity in hippocampus when pretreated with 8-OH-DPAT, a selective 5HT1A agonist, compared with control. These findings strongly suggested that 131I-MPPI could be used as an in vivo marker for studies of pharmacology of the 5-HT1A receptor system in animals.