Preparation and preclinical pharmacological study on a novel bone imaging agent (99m)Tc-EMIDP.
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.
Lin
Jianguo
J
Key Laboratory of Nuclear Medicine, Ministry of Health & Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, PR China.
Luo
Shineng
S
Chen
Chuanqing
C
Qiu
Ling
L
Wang
Yan
Y
Cheng
Wen
W
Ye
Wanzhong
W
Xia
Yongmei
Y
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
D004164:Diphosphonates; D007093:Imidazoles; D019275:Radiopharmaceuticals; D000077211:Zoledronic Acid; D013667:Technetium