title: Synthesis and biological evaluation of novel (99m)Tc-labelled bisphosphonates as superior bone imaging agents.
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 (99m)Tc in high labeling yields. The in vitro stability and in vivo biodistribution of (99m)Tc-MIPrDP, (99m)Tc-MIBDP and (99m)Tc-MIPeDP were investigated and compared. The biodistribution studies indicate that the radiotracer (99m)Tc-MIPrDP has highly selective uptake in the skeletal system and rapid clearance from soft tissues. The present findings indicate that (99m)Tc-MIPrDP holds great potential for use in bone imaging.
authors.affiliation: Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China.
authors.forename: Ling
authors.initials: L
authors.lastname: Qiu
authors.forename: Wen
authors.initials: W
authors.lastname: Cheng
authors.forename: Jianguo
authors.initials: J
authors.lastname: Lin
authors.forename: Shineng
authors.initials: S
authors.lastname: Luo
authors.forename: Li
authors.initials: L
authors.lastname: Xue
authors.forename: Jing
authors.initials: J
authors.lastname: Pan
mesh_terms: D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D050071:Bone Density Conservation Agents / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D001842:Bone and Bones / Q000000981:diagnostic imaging*; D002851:Chromatography, High Pressure Liquid; D004164:Diphosphonates / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D004355:Drug Stability; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007093:Imidazoles / Q000737:chemistry; D007275:Injections, Intravenous; D051379:Mice; D008813:Mice, Inbred ICR; D057054:Molecular Imaging / Q000379:methods*; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D011485:Protein Binding; D011877:Radionuclide Imaging / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D013667:Technetium / Q000737:chemistry / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D001798:Blood Proteins; D050071:Bone Density Conservation Agents; D004164:Diphosphonates; D007093:Imidazoles; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D013667:Technetium