Study on the reaction kinetics of ⁹⁹Tc^m-labeled BIDP

Study on the reaction kinetics of 99 Tc m -labeled BIDP 1 first-author 1 1 corresp Corresponding author. E-mail address: shineng914@yahoo.com.cn Corresponding author. E-mail address: shineng914@yahoo.com.cn shineng914@yahoo.com.cn 1 1 Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China A novel zoledronic acid derivative, 1-hydroxy-2-(2-butyl-1H-imidazole-1-yl)-ethylidene-1,1- diphosphonic acid (BIDP), was synthesized and labeled with 99 Tc m . The detailed kinetic study on the labeling reaction between BIDP and 99 Tc m was carried out. The results indicated that the reaction rate constants k were 0.0258, 0.0268, 0.0305, 0.0323, 0.0351 and 0.0384 min -1 at 0°C, 5°C, 10°C, 15°C, 20°C and 25°C, respectively. From the Arrhenius equation k = A· e – E a/( RT ) , the activation energy E a of the labeling reaction was calculated to be 10.45 kJ/mol. And the correlation between k and temperature (T) was also deduced as ln k =–1258.8×(1/ T )+0.9531. In addition, it was found that in order to get a high radiolabeling yield (RLY) ( > 90%), the reaction temperature must be up to 12°C. 99 Tc m -BIDP Labeling reaction kinetics Reaction rate constant k Reaction activation energy E a Radiolabeling yield (RLY) References EI-Mabhouh A A , Mercer J R . Eur J Nucl Med Mol Imaging , 2008 , 35 : 1240 - 1248 . Eur J Nucl Med Mol Imaging Green J R . J Org Chem , 2005 , 690 : 2439 - 2448 . J Org Chem Ross J R , Saunders Y , Edmonds P M , et al . Health Technol Asses , 2004 , 4 : 1 - 16 . Health Technol Asses Ogawa K , Mukai T , Arano Y , et al . Nucl Med Biol , 2006 , 33 : 513 - 520 . Nucl Med Biol Garcia E , Schibli R , Schubiger P A . Nucl Sci Tech , 2007 , 18 : 88 - 100 . Nucl Sci Tech Shalaby-Rana E , Majd M . J Nucl Med , 2001 , 42 : 878 - 883 . J Nucl Med Widler L , Jaeggi K A , Glatt M , et al . J Med Chem , 2002 , 45 : 3721 - 3738 . J Med Chem Wang H Y , Luo S N , Xie M H , et al . Nucl Tech , 2006 , 29 : 438 - 441 . Nucl Tech Asikoglu A , Durak F G . Appl Radiat Isot , 2009 , 67 : 1616 - 1621 . Appl Radiat Isot Luo S N , Wang H Y , Xie M H , et al . Chin J Nucl Med , 2005 , 25 : 341 - 344 . Chin J Nucl Med Guo X H , Luo S N , Wang H Y , et al . Nucl Sci Tech , 2006 , 17 : 285 - 288 . Nucl Sci Tech Yan X H , Luo S N , Niu G S , et al . Nucl Sci Tech , 2008 , 19 : 165 - 168 . Nucl Sci Tech Niu G S , Luo S N , Yan X H , et al . Nucl Tech , 2008 , 31 : 698 - 701 . Nucl Tech Chen C Q , Luo S N , Lin J G , et al . Nucl Sci Tech , 2009 , 20 : 302 - 306 . Nucl Sci Tech Lin J G , Luo S N , Chen C Q , et al . Appl Radiat Isot , 2010 , 68 : 1616 - 1622 . Appl Radiat Isot Kung H F , Liu B L , Pan S R . Appl Radiat Isot , 1989 , 40 : 677 - 681 . Appl Radiat Isot Wei Y , Wang X B , Liu B L , et al . Nucl Tech , 1990 , 13 : 445 - 448 . Nucl Tech Luo S N , Xie M H , Fang P , et al . Nucl Tech , 1992 , 15 : 296 - 299 . Nucl Tech Liu S , Edwards D S , Harris A R , et al . Appl Radiat Isot , 1997 , 48 : 1103 - 1111 . Appl Radiat Isot EI-Mabhouh A A , Angelov C A , Cavell R , et al . Nucl Med Biol , 2006 , 33 : 715 - 722 . Nucl Med Biol Zhu J Q , Wu C Y , Lu C X . Nucl Sci Tech , 2003 , 14 : 135 - 137 . Nucl Sci Tech DjokićD D , JankovićD L , NikolićN S . Bioorgan Med Chem , 2008 , 16 : 4457 - 4465 . Bioorgan Med Chem 10.13538/j.1001-8042/nst.22.174-177 Supported by National Natural Science Foundation of China (Nos. 20801024 and 21001055) , Natural Science Foundation of Jiangsu Province (No.BK2009077) , Science Foundation of Health Department of Jiangsu Province (No.H200963) 2010-11-23 2011-06-20 2021-01-19 2011 Nuclear Science and Techniques 03 22