Synthesis, characterization, and biodistribution of oxo complexes of technetium-99m with biguanide and N1-Substituted ligands

We report the synthesis, characterization, and biodistribution of 99mTc-complexes with the bidentate- N,N chelate biguanide (Big) and the N1- substituted ligands dimethyl (DMBig), phenyl (PBig), and phenethyl (PEBig). Dynamic gamma-camera studies with 99mTc-Big and 99mTc-DMSA in rabbits indicated di...

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Bibliographic Details
Published in:Nuclear medicine and biology 1999, Vol.26 (1), p.79-83
Main Authors: Neves, M, Gano, L, Ribeiro, M.João, Santos, A.Cristina, Marchi, A, Sawas-Dimopolou, C, Pedroso de Lima, J.J
Format: Article
Language:English
Subjects:
99mTc-Biguanides
99mTc-DMSA
Animals
Biguanides - chemical synthesis
Biguanides - pharmacokinetics
Biological and medical sciences
Contrast media. Radiopharmaceuticals
Female
Kidney - diagnostic imaging
Medical sciences
Mice
Organotechnetium Compounds - chemical synthesis
Organotechnetium Compounds - pharmacokinetics
Pharmacology. Drug treatments
Protein Binding
Rabbits
Radionuclide Imaging
Radiopharmaceuticals - pharmacokinetics
Rats
Rats, Wistar
Renal imaging
Technetium Tc 99m Dimercaptosuccinic Acid - pharmacokinetics
Whole-Body Counting
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Summary:We report the synthesis, characterization, and biodistribution of 99mTc-complexes with the bidentate- N,N chelate biguanide (Big) and the N1- substituted ligands dimethyl (DMBig), phenyl (PBig), and phenethyl (PEBig). Dynamic gamma-camera studies with 99mTc-Big and 99mTc-DMSA in rabbits indicated distinct renal and urinary excretion profiles. 99mTc-Big was cleared more quickly than 99mTc-DMSA, and for the same acquisition times, the contrast in whole-body images favored 99mTc-Big. Also, the estimated radiation absorbed doses by kidneys and blood for 99mTc-DMSA were significantly higher than for 99mTc-Big. These preliminary studies show that 99mTc-Big has favourable practical and dosimetric features for renal imaging as an alternative to 99mTc-DMSA.
ISSN:0969-8051
1872-9614
DOI:10.1016/S0969-8051(98)00074-2