Abstract
A series of novel zoledronic acid (ZL) derivatives 1-hydroxy-3-(2-methyl-1H-imidazol-1-yl)propane-1,1-diyldiphosphonic acid (MIPrDP), 1-hydroxy-4-(2-methyl-1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (MIBDP), and 1-hydroxy-5-(2-methyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (MIPeDP) were prepared and successfully labeled with 99mTc in high labeling yields. The in vitro stability and in vivo biodistribution of 99mTc-MIPrDP, 99mTc-MIBDP and 99mTc-MIPeDP were investigated and compared. The biodistribution studies indicate that the radiotracer 99mTc-MIPrDP has highly selective uptake in the skeletal system and rapid clearance from soft tissues. The present findings indicate that 99mTc-MIPrDP holds great potential for use in bone imaging.
Highlights
Technetium-99m, with its excellent physical characteristics and easy availability from a generator, has become the most important nuclide for organ imaging in nuclear medicine
Based on our primary studies, we found that optimization of imidazolyl ring or extension of the linker chain between the imidazolyl and geminal bisphosphonate group in the zoledronic acid (ZL) to be labeled with technetium-99m can bring significant influence on the biological properties of the bone resorption and the clearance from blood and soft tissues [15,16]
MIPrDP, MIBDP and MIPeDP were synthesized by three step reactions from the starting material
Summary
Technetium-99m, with its excellent physical characteristics and easy availability from a generator, has become the most important nuclide for organ imaging in nuclear medicine. Complexes of technetium-99m labeled with methylenediphosphonate (99mTc-MDP) and hydroxymethylenediphosphonate (99mTc-HMDP) have been widely used, both experimentally and clinically, for detection of skeletal metastases and other focal bone lesions [4,6,7]. An interval of 2–6 h is needed between injecting these agents into the patient and bone scanning [8]. Shorting this interval would lessen the burden on patients in terms of the total length of the examination. To enable imaging at an earlier time after injection, a radiopharmaceutical with higher affinity for bone, larger ratio of bone-to-soft tissue uptake and more rapid clearance from blood is required, [9]. The nature of ligands (diphosphonic acid) is a key factor to determine the advantages of the radiopharmaceuticals
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