title: Synthesis and pharmacological evaluation of 99mTc-labeled imidazolyl-containing diphosphonic acid as a novel bone imaging agent.
abstract: In order to develop a superior bone imaging agent, a new radiotracer (99m)Tc-1-hydroxy-5-(2-butyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (BIPeDP) was designed and prepared with good radiochemical yield and stability. The biodistribution in mice shows that (99m)Tc-BIPeDP has high specificity in the skeleton with the maximum uptake of 17.30 ± 0.14 injected dose per gram at 60 min. Kinetics of blood clearance shows that the distribution half-life (T1/2α) and elimination half-life (T1/2β) of (99m)Tc-BIPeDP are 3.7 and 49.7 min, respectively. An excellent image can be obtained at 1-h post-injection with the single photon emission computed tomography bone scanning, which is clearer and quicker than (99m)Tc-zoledronic acid, (99m)Tc-1-hydroxy-5-(1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid, and (99m)Tc-methylenediphosphonic acid All results indicate that (99m)Tc-BIPeDP holds great potential as a novel promising bone imaging agent.
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: Shu
authors.initials: S
authors.lastname: Zhang
authors.forename: Shineng
authors.initials: S
authors.lastname: Luo
mesh_terms: D000818:Animals; D001842:Bone and Bones / Q000000981:diagnostic imaging*; D004164:Diphosphonates / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D007093:Imidazoles / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D051379:Mice; D015609:Organotechnetium Compounds / Q000138:chemical synthesis*; D049268:Positron-Emission Tomography; D011817:Rabbits; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics*
chemical_list: D004164:Diphosphonates; D007093:Imidazoles; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C000589726:technetium 99m 1-hydroxy-5-(2-butyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid
keywords: 99mTc-labeled imidazolyl-containing diphosphonic acid; biodistribution; bone scanning; pharmacokinetics; stability