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 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.
Neves
M
M
Departamento de Química, Instituto Tecnológico e Nuclear, Sacavém, Portugal. mneves@itn1.itn.pt
Gano
L
L
Ribeiro
M J
MJ
Santos
A C
AC
Marchi
A
A
Sawas-Dimopolou
C
C
Pedroso de Lima
J J
JJ
D000818:Animals; D001645:Biguanides / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D005260:Female; D007668:Kidney / Q000000981:diagnostic imaging*; D051379:Mice; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011485:Protein Binding; D011817:Rabbits; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar; D019783:Technetium Tc 99m Dimercaptosuccinic Acid / Q000493:pharmacokinetics; D014915:Whole-Body Counting
D001645:Biguanides; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D019783:Technetium Tc 99m Dimercaptosuccinic Acid