title: Preparation and preclinical pharmacological study on a novel bone imaging agent (99m)Tc-EMIDP.
abstract: A novel zoledronic acid (ZL) derivative, 1-hydroxy-2-(2-ethyl-4-methyl-1H-imidazol-1-yl)ethane-1,1-diyldiphosphonic acid (EMIDP), was prepared and labeled with (99)(m)Tc successfully in a high labeling yield and good stability in vitro. The preclinical pharmacological properties of (99)(m)Tc-EMIDP were investigated and compared with (99)(m)Tc-MDP and (99)(m)Tc-ZL. The studies of biodistribution in mice and SPECT bone imaging of the rabbit suggest that (99)(m)Tc-EMIDP has highly selective uptake in the skeletal system and rapid clearance in the soft tissues. The present findings indicate that (99)(m)Tc-EMIDP holds great potential for bone scintigraphy.
authors.affiliation: Key Laboratory of Nuclear Medicine, Ministry of Health & Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, PR China.
authors.forename: Jianguo
authors.initials: J
authors.lastname: Lin
authors.forename: Shineng
authors.initials: S
authors.lastname: Luo
authors.forename: Chuanqing
authors.initials: C
authors.lastname: Chen
authors.forename: Ling
authors.initials: L
authors.lastname: Qiu
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.forename: Wen
authors.initials: W
authors.lastname: Cheng
authors.forename: Wanzhong
authors.initials: W
authors.lastname: Ye
authors.forename: Yongmei
authors.initials: Y
authors.lastname: Xia
mesh_terms: D000818:Animals; D004164:Diphosphonates / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D005269:Femur / Q000000981:diagnostic imaging* / Q000378:metabolism*; D007093:Imidazoles / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D007553:Isotope Labeling / Q000379:methods; D008657:Metabolic Clearance Rate; D051379:Mice; D009928:Organ Specificity; D011817:Rabbits; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics; D013667:Technetium / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D000077211:Zoledronic Acid
chemical_list: D004164:Diphosphonates; D007093:Imidazoles; D019275:Radiopharmaceuticals; D000077211:Zoledronic Acid; D013667:Technetium