title: A novel (99m)Tc-labeled diphosphonic acid as potential bone seeking agent: synthesis and biological evaluation.
abstract: A novel zoledronate derivative, 1-hydroxy-4-(2-butyl-1H-imidazol-1-yl)butane-1,1- diyldiphosphonic acid (BIBDP) was prepared and labeled with (99m)Tc successfully in a high radiochemical purity and good stability in vitro. The biodistribution in mice shows that (99m)Tc-BIBDP has high specificity and efficacy in bone uptake with a maximum of 12.14 ± 0.53 %ID/g at 120 min. Kinetics of blood clearance showed that distribution half life (T(1/2α)), elimination half life (T(1/2β)) and total clearance rate (CL) of (99m)Tc-BIBDP were 4.67 min, 91.9 min and 1.21 %ID/g·min(-1), respectively. Moreover, (99m)Tc-BIBDP has higher uptake in the bone and faster clearance from soft tissues than (99m)Tc-MDP and (99m)Tc-ZL. A plain and clear bone image was obtained at 1 h with SPECT bone imaging. The present findings indicate that (99m)Tc- BIBDP holds great potential for bone imaging.
authors.affiliation: Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China. linjianguo@jsinm.org.
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: Shu
authors.initials: S
authors.lastname: Zhang
authors.forename: Shineng
authors.initials: S
authors.lastname: Luo
mesh_terms: D000818:Animals; D050071:Bone Density Conservation Agents / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics*; D001842:Bone and Bones / Q000000981:diagnostic imaging*; D004164:Diphosphonates / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics*; D007093:Imidazoles / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics*; D008657:Metabolic Clearance Rate; D051379:Mice; D018482:Muscle, Skeletal / Q000000981:diagnostic imaging*; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics*; D011817:Rabbits; D013667:Technetium / Q000378:metabolism / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon; D000077211:Zoledronic Acid
chemical_list: D050071:Bone Density Conservation Agents; D004164:Diphosphonates; D007093:Imidazoles; D015609:Organotechnetium Compounds; C583427:technetium 99m 1-hydroxy-4-(2-butyl-1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid; D000077211:Zoledronic Acid; D013667:Technetium