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

RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE

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

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

Nuclear Science and Techniques

Vol.14, No.1

pp.64-68

Published in print 01 Feb 2003

CLC：R817,O615.2,Q51

20100

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.

(R,S)I-QNBPreparation131I labelingCerebral muscarinic acetylcholine receptors

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