Preparation and preclinical pharmacological study on a novel bone imaging agent 99mTc-EMIDP

Abstract: A novel zoledronic acid (ZL) derivative, 1-hydroxy-2-(2-ethyl-4-methyl-1H-imidazol-1-yl)ethane-1,1-diyldiphosphonic acid (EMIDP), was prepared and labeled with 99 mTc successfully in a high labeling yield and good stability in vitro. The preclinical pharmacological properties of 99 mTc-EMIDP were investigated and compared with 99 mTc-MDP and 99 mTc-ZL. The studies of biodistribution in mice and SPECT bone imaging of the rabbit suggest that 99 mTc-EMIDP has highly selective uptake in the skeletal system and rapid clearance in the soft tissues. The present findings indicate that 99 mTc-EMIDP holds great potential for bone scintigraphy. [Copyright &y& Elsevier]