A novel zoledronic acid derivative,1-hydroxy-2-(2-propyl-1H-imidazol-1-yl)ethane-1,1-diyldiphosphonic acid (PIDP), was synthesized by three-step reactions from 2-propyl-1H-imidazole. It was labeled with 99Tcm in condi...A novel zoledronic acid derivative,1-hydroxy-2-(2-propyl-1H-imidazol-1-yl)ethane-1,1-diyldiphosphonic acid (PIDP), was synthesized by three-step reactions from 2-propyl-1H-imidazole. It was labeled with 99Tcm in conditions of 0.1 mg SnCl2.2H2O at pH 6.0 and 99TcmO4? in aqueous solution for 20 min at room temperature. The labeling yield and radiochemical purity of 99Tcm-PIDP are both higher than 95%. The biodistribution results show that the bone uptake is up to 8.47% ID/g which is the maximum of bone uptake at 30 min after injection of 99Tcm-PIDP in mice. The pharmacokinetic parameters can be estimated from the exponential equation of C=59.565e-11.307t+2.069e-1.211t. The clear bone image of rabbit was obtained at 120 min after injection of 99Tcm-PIDP. The results indicate that 99Tcm-PIDP has highly selective uptake in the skeletal and low uptake, rapid clearance in soft tissues, so it would be a potential novel bone imaging agent.展开更多
99mTc-HMIBP, a new bone-imaging agent, was prepared by the reduction of 99mTc-pertechnetate in the presence of SnCl2?2H2O. The effects of the amounts of SnCl2?2H2O and HMIBP and the pH value on the labeling yield and ...99mTc-HMIBP, a new bone-imaging agent, was prepared by the reduction of 99mTc-pertechnetate in the presence of SnCl2?2H2O. The effects of the amounts of SnCl2?2H2O and HMIBP and the pH value on the labeling yield and radiochemical purity of 99mTc-HMIBP were investigated. When the amounts of SnCl2?2H2O and HMIBP were more than 10 μg and 2.5 mg, respectively, the pH value was between 2 and 7, and the labeling reaction contin- ued for 10 min, both labeling yield and radiochemical purity of 99mTc-HMIBP were more than 90%. The biodistribu- tion in rats and bone scan in rabbits were also studied. The results showed that the bone uptake is up to 7.94%ID/g at 30 min after injection of 99mTc-HMIBP, bone-to-muscle and bone-to-blood uptake ratios were 20.89 and 16.89, re- spectively. The clear bone image was obtained at 120 min after injection of 99mTc-HMIBP and clearance in soft tissue was visible. All of the above-mentioned results suggested that 99mTc-HMIBP may be a potential bone-imaging agent.展开更多
基金Supported by the National Natural Science Foundation of China (No.20801024)Wu Jieping Medical Found(No.32067500615)
文摘A novel zoledronic acid derivative,1-hydroxy-2-(2-propyl-1H-imidazol-1-yl)ethane-1,1-diyldiphosphonic acid (PIDP), was synthesized by three-step reactions from 2-propyl-1H-imidazole. It was labeled with 99Tcm in conditions of 0.1 mg SnCl2.2H2O at pH 6.0 and 99TcmO4? in aqueous solution for 20 min at room temperature. The labeling yield and radiochemical purity of 99Tcm-PIDP are both higher than 95%. The biodistribution results show that the bone uptake is up to 8.47% ID/g which is the maximum of bone uptake at 30 min after injection of 99Tcm-PIDP in mice. The pharmacokinetic parameters can be estimated from the exponential equation of C=59.565e-11.307t+2.069e-1.211t. The clear bone image of rabbit was obtained at 120 min after injection of 99Tcm-PIDP. The results indicate that 99Tcm-PIDP has highly selective uptake in the skeletal and low uptake, rapid clearance in soft tissues, so it would be a potential novel bone imaging agent.
文摘99mTc-HMIBP, a new bone-imaging agent, was prepared by the reduction of 99mTc-pertechnetate in the presence of SnCl2?2H2O. The effects of the amounts of SnCl2?2H2O and HMIBP and the pH value on the labeling yield and radiochemical purity of 99mTc-HMIBP were investigated. When the amounts of SnCl2?2H2O and HMIBP were more than 10 μg and 2.5 mg, respectively, the pH value was between 2 and 7, and the labeling reaction contin- ued for 10 min, both labeling yield and radiochemical purity of 99mTc-HMIBP were more than 90%. The biodistribu- tion in rats and bone scan in rabbits were also studied. The results showed that the bone uptake is up to 7.94%ID/g at 30 min after injection of 99mTc-HMIBP, bone-to-muscle and bone-to-blood uptake ratios were 20.89 and 16.89, re- spectively. The clear bone image was obtained at 120 min after injection of 99mTc-HMIBP and clearance in soft tissue was visible. All of the above-mentioned results suggested that 99mTc-HMIBP may be a potential bone-imaging agent.
