Preparation and preliminary biological evaluation of ⁹⁹Tc^m-TADP as bone imaging agent

Preparation and preliminary biological evaluation of 99 Tc m -TADP as bone imaging agent 1 2 first-author 2 1 corresp Corresponding author. E-mail: shineng914@yahoo.com.cn Corresponding author. E-mail: shineng914@yahoo.com.cn shineng914@yahoo.com.cn 1 2 2 2 2 1 School of Chemical and Material Engineering, Southern Yangtze University, Wuxi 214122, China School of Chemical and Material Engineering, Southern Yangtze University, Wuxi 214122, China Key Laboratory of Nuclear Medicine (Jiangsu Institute of Nuclear Medicine), Ministry of Health, Wuxi 214063, China Key Laboratory of Nuclear Medicine (Jiangsu Institute of Nuclear Medicine), Ministry of Health, Wuxi 214063, China TADP, 2-(1H-1,2,4-triazol-1-yl)-1-hydroxyethane-1,1-diphosphonic acid, was synthesized by three step reactions from the raw material 1H-1,2,4-triazole. 99 Tc m -TADP was prepared with 5 mg TADP at pH 7.0 by joining 99 Tc m O 4 - with SnCl 2 ·2H 2 O in aqueous solution for 10 min at room temperature. Both labeling yield and radiochemical purity of 99 Tc m -TADP were more than 95%. The biodistribution in rats and bone scan in rabbits were also studied. The uptake of organ was expressed as %ID/g. The results showed that the bone uptake is up to 17.17%ID/g which is the maximum of bone uptake at 30 min after injection of 99 Tc m -TADP in rats, bone-to-muscle and bone-to-blood uptake ratios were 61.32 and 13.21, respectively. The clear bone image of rabbit was obtained at 120 min after injection of 99 Tc m -TADP and clearance in soft tissue was visible. The preparation of 99 Tc m -TADP was convenient and 99 Tc m -TADP exhibited high uptake in bone, and it would be a potential new bone imaging agent. Bone-imaging agent 99 Tc m -labeled TADP Bio-evaluation References SUN Da . Skeletal imaging of radionuclide . Hangzhou : Zhejiang University Press (in Chinese) , 2000 : 12 - 24 . Skeletal imaging of radionuclide Vasireddy S , Talwakar A , Miller H , et al . Clin Rheumatol , 2003 , 22 : 376 - 380 . Clin Rheumatol Dawson N A . Expert Opin Pharmacother , 2003 , 4 : 705 - 716 . Expert Opin Pharmacother WANG Hongyong , LUO Shineng , XIE Minhao , et al . Nucl Tech (in Chinese) , 2006 , 29 : 438 - 441 . Nucl Tech (in Chinese) LUO Shineng , WANG Hongyong , XIE Minhao , et al . Chin J Nucl Med , 2005 , 25 : 341 - 343 . Chin J Nucl Med GUO Xuehua , LUO Shineng , XIE Minhao , et al . Nuclear Science and Techniques , 2006 , 17 : 285 - 288 . Nuclear Science and Techniques Widler L , Jaeggi K A , Glatt M , et al . J Med Chem , 2002 , 45 : 3721 - 3738 . J Med Chem Jaeggi K A , Widler L . USP 4939130 , 1990 . Liu Liqin , Yang Jianquan , Li Ye , et al . Journal of Beijing Normal University (Natural Science Edition) , 2003 , 39 : 230 - 234 . Journal of Beijing Normal University (Natural Science Edition) 10.1016/S1001-8042(08)60044-5 R817 Supported by Wu Jieping Medical Found (32067500615) 2008-04-08 2008-06-20 2021-01-19 2008 Nuclear Science and Techniques 03 19