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 (2): 111

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Synthesis and labelling of epidepride

YANG Min, PEI Zhu-Guo, HU Ming-Yang, WANG Bo-Cheng, ZHOU Xing-Qin   

  1. State Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medixcine, Wuxi 214063
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YANG Min, PEI Zhu-Guo, HU Ming-Yang, WANG Bo-Cheng, ZHOU Xing-Qin. Synthesis and labelling of epidepride.Nuclear Science and Techniques, 2001, 12(2): 111

Abstract: S-[(1-ethyl -2-pyrrolidinyl )methyl}-5-iodo-2,3-dimethoxybenzamide (proposed generic name, epidepride) is a very potent dopamine D2 antagonist. It was synthesized by five steps from 3-methoxysalicylic acid. [131I ]epidepride was obtained in 97.3% radiochemical yields from the corresponding 5-(tributyltin) derivative using hydrogen peroxide as the oxidant. The aryltin precursor was prepared from non-labelled epidepride by palladium-catalyzed stannylation using bis(tri-n-butyltin) in triethylamine. [131I]cpidepride was stable under 4°C, and partition coefficient was 72.3 at pH 7.40. The biodistribution study in rats exihibited high localization in the striatum of the brain with the striatum/cerebellum ratio reaching 237/1 at 320 min postinjection. All these results suggest that [131I ]epidepride may be used widely as a useful dopamine D2 receptor imaging agent for SPECT.

Key words: [131I ]epidepride, Dopamine D2 antagonist, Synthesize, Aryltin precursor. Biodistribution, SPECT