Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2018 Impact factor 0.961

Nuclear Science and Techniques ›› 2003, Vol. 14 ›› Issue (1): 64

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

Preparation of an imaging agent for cerebral muscarinic acetylcholine receptor, (R,S) 131I-QNB

DING Shi-Yu1, LIN Yan-Song2, CHEN Zheng-Ping1, JI Shu-Ren1, LU Chun-Xiong1, ZHOU Xiang1, FANG Ping1, WU Chun-Ying1, WANG Bo-Cheng1, XIANG Jing-De1   

  1. 1State Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063;
    2Department of Nuclear Medicine, Peking Union Medical College Hospital, Beijing 100730
  • Supported by:
    Supported by the Foundation for Outstanding Young Members of Health Ministry in China(9925)
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DING Shi-Yu, LIN Yan-Song, CHEN Zheng-Ping, JI Shu-Ren, LU Chun-Xiong, ZHOU Xiang, FANG Ping, WU Chun-Ying, WANG Bo-Cheng, XIANG Jing-De. Preparation of an imaging agent for cerebral muscarinic acetylcholine receptor, (R,S) 131I-QNB.Nuclear Science and Techniques, 2003, 14(1): 64

Abstract: The method to synthesize a high affinity muscarinic receptor antagonist (R,S)I-QNB[(R)-(-)-1-azabicyclo [2,2,2]oct-3-yl-(S)-(+)-α-hydroxy-α-(4-[127I]iodophenyl)-α-phenyl acetate] from 4-nitrobenzophenone with improvement compared to literatures was reported in this article. IR, MS and 1HNMR characterized the final product. (R,S)131I-QNB was prepared using Cu(I) assisted iodine exchange labeling, and showed by TLC that the radiolabeling yield(RLY) was over 80%, and radiochemical purity(RCP) was over 95%. Stability of the labeled compound was also determined. It was found that (R,S)131I-QNB dried by nitrogen blowing can stay at 4-10℃ for a week without change of RCP.

Key words: (R,S)I-QNB, Preparation, 131I labeling, Cerebral muscarinic acetylcholine receptors