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

Preparation of an imaging agent for cerebral muscarinic acetylcholine receptor, (R,S) 131 I-QNB 1 first-author 2 1 1 1 1 1 1 1 1 State Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063; State Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063; Department of Nuclear Medicine, Peking Union Medical College Hospital, Beijing 100730 Department of Nuclear Medicine, Peking Union Medical College Hospital, Beijing 100730 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 1 HNMR characterized the final product. (R,S) 131 I-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) 131 I-QNB dried by nitrogen blowing can stay at 4-10℃ for a week without change of RCP. (R,S)I-QNB Preparation 131 I labeling Cerebral muscarinic acetylcholine receptors References Holman B L , Gibson R E , Hill T C et al . JAMA , 1985 , 254 ( 21 ): 3063 - 3066 JAMA Weinberger D R , Gibson R , Coppola R et al . Arch Neurol , 1991 , 48 : 169 - 176 Arch Neurol Weinberger D R , Jones D , Reba R C et al . J Neuropsychiatr Clin Neurosci , 1992 , 4 ( 3 ): 239 - 248 J Neuropsychiatr Clin Neurosci Eckelman W C , Grissom M , Conklin J et al . J Pharm Sci , 1984 , 74 : 529 - 534 J Pharm Sci Kiesewetter D O , Paik C H , Flippen-Anderson J L et al . J Label Compd Radiopharm , 1996 , 37 : 686 - 688 J Label Compd Radiopharm Zeeberg B R , Boulay S F , Gitler M S et al . Appl Radiat Isot , 1997 , 48 ( 4 ): 463 - 467 Appl Radiat Isot Eckelman W C , Reba R C , Rzeszotarski W J et al . Science , 1984 , 223 : 291 - 293 Science Gibson R E , Moody T , Schneidau T A et al . Life Sci , 1992 , 50 : 629 - 637 Life Sci Kiesewetter D O , Silverton J V , Eckelman W C . J Med Chem , 1995 , 38 : 1711 - 1719 J Med Chem Lee J , Paik C H , Kiesewetter D O et al . Nucl Med Biol , 1995 , 22 ( 6 ): 773 - 781 Nucl Med Biol Rzeszotarski W J , Eckelman W C , Francis B E et al . J Med Chem , 1984 , 27 : 156 - 159 J Med Chem Cohen V I , Rzeszotarski W J , Gibson R E et al . J Pharm Sci , 1989 , 78 ( 10 ): 833 - 836 J Pharm Sci Owens J , Murray T , McCulloch J et al . J Label Compo Radiopharmaceuticals , 1991 , 31 ( 1 ): 45 - 60 J Label Compo Radiopharmaceuticals Lee K S , He X S , Weinberger D R . US 5569447 Wu C Y , Ji S R , Lu C X . Nucl Sci Tech , 2000 , 11 ( 4 ): 240 - 246 Nucl Sci Tech R817,O615.2,Q51 Supported by the Foundation for Outstanding Young Members of Health Ministry in China (9925) 2002-03-18 2003-02-01 2021-01-19 2003 Nuclear Science and Techniques 01 14