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A novel zoledronic acid (ZL) derivative, 1-hydroxy-2-(2,4-dimethyl-1 H -imidazol-1-yl)-ethane-1,1-diyldiphosphonic acid (DMIDP, dimezoledronate), was successfully prepared and labeled with  99m Tc in a high labeling yield. The biodistribution in mice shows that  99m Tc-DMIDP has significant advantage regarding bone resorption and clearance from soft tissues compared with  99m Tc-ZL and the clinically widely-used bone-imaging agent  99m Tc-MDP (methylenediphosphonic acid). Kinetics of blood clearance displayed that distribution half-life ( T  1/2 α  ) and elimination half-life ( T  1/2 β  ) of  99m Tc-DMIDP were 2.53 min and 23.53 min, while those of  99m Tc-ZL were 2.28 and 52.63 min, respectively. Excellent images of the rabbit skeleton can be quickly obtained from  99m Tc-DMIDP, which was faster than  99m Tc-ZL and  99m Tc-MDP. The present findings indicate that  99m Tc-DMIDP possesses excellent potential for application as a novel bone scanning agent.

A novel 99m Tc-labeled dimethyl-substituted zoledronic acid (DMIDP) with improved bone imaging efficiency