title: Development of superior bone scintigraphic agent from a series of (99m)Tc-labeled zoledronic acid derivatives.
abstract: Two novel zoledronic acid (ZL) derivatives, 1-hydroxy-4-(1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (IBDP) and 1-hydroxy-5-(1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (IPeDP), were prepared and labeled with the radionuclide technetium-99m in a high labeling yield. In vitro stabilities of these radiolabeled complexes were measured by the radio-HPLC analysis as a function of time, which showed excellent stability with the radiochemical purity of over 95% at 6h post preparation. Their in vivo biological performances were evaluated and compared with those of (99m)Tc-ZL and (99m)Tc-MDP (methylenediphosphonic acid). The biodistribution in mice and scintigraphic images of the rabbit showed that the tracer agent (99m)Tc-IPeDP had highly selective uptake in the skeletal system and rapid clearance from the blood and soft tissues and an excellent scintigraphic image can be obtained in a shorter time post injection with clear visualization of the skeleton and low soft tissue activity. These preclinical studies suggest that (99m)Tc-IPeDP would be a novel superior bone scintigraphic agent.
authors.affiliation: Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi, PR China.
authors.forename: Jianguo
authors.initials: J
authors.lastname: Lin
authors.forename: Ling
authors.initials: L
authors.lastname: Qiu
authors.forename: Wen
authors.initials: W
authors.lastname: Cheng
authors.forename: Shineng
authors.initials: S
authors.lastname: Luo
authors.forename: Li
authors.initials: L
authors.lastname: Xue
authors.forename: Shu
authors.initials: S
authors.lastname: Zhang
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004164:Diphosphonates / Q000737:chemistry*; D007093:Imidazoles / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D015609:Organotechnetium Compounds / Q000737:chemistry*; D011817:Rabbits; D011874:Radiometry; D011877:Radionuclide Imaging; D021241:Spectrometry, Mass, Electrospray Ionization; D000077211:Zoledronic Acid
chemical_list: D004164:Diphosphonates; D007093:Imidazoles; D015609:Organotechnetium Compounds; D000077211:Zoledronic Acid