Preparation and biodistribution of 99Tcm-PIDP as bone imaging agent

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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 SnCI2.2H2Cl2·2H2O 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.
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