Synthesis, characterization and evaluation of 99Tc/99mTc DIARS and DMPE complexes containing pentadecanoic acid.
The synthesis and purification of two new ligands, 15-[bis(3,4-dimethyl arsino)phenyl] pentadecanoic acid (FA-DIARS) and [bis(16,17-dimethyl phosphino)] heptadecanoic acid (FA-DMPE) and the preparation of their corresponding 99Tc/99mTc complexes of the general formula [Tc(III)L2Cl2]+, wherein L is FA-DIARS or FA-DMPE are reported. After careful purification by preparative HPLC, the 99Tc complexes were characterized by spectroscopy, while the 99mTc complexes were used to determine the biodistribution in mice. The results of the organ distribution studies indicated a relatively high uptake in heart (5-7% dose/g). The complexes were, however, found to be very slowly cleared from the blood, probably due to strong binding to serum proteins. Further, the heart to liver and heart to lung ratios were unfavourable. Attempts to improve the efficacy by synthesizing complexes containing one fatty acid per molecule are also described.
Institut für Chemie 1 (Nuklearchemie), Kernforschungsanlage Jülich GmbH, F.R.G.
L
L
Astheimer
K H
KH
Linse
N
N
Ramamoorthy
K
K
Schwochau
D000818:Animals; D001152:Arsenicals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D006321:Heart / Q000000981:diagnostic imaging*; D007202:Indicators and Reagents; D008024:Ligands; D008099:Liver / Q000378:metabolism*; D008168:Lung / Q000378:metabolism*; D051379:Mice; D009206:Myocardium / Q000378:metabolism*; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D009943:Organophosphorus Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D015609:Organotechnetium Compounds; D010720:Phosphines; D011877:Radionuclide Imaging; D014018:Tissue Distribution
D001152:Arsenicals; D007202:Indicators and Reagents; D008024:Ligands; D009942:Organometallic Compounds; D009943:Organophosphorus Compounds; D015609:Organotechnetium Compounds; D010720:Phosphines; C054747:technetium Tc 99m 15-(bis(3,4-dimethyl arsino)phenyl)pentadecanoic acid; C054748:technetium Tc 99m bis(16,17-dimethylphosphino)heptadecanoic acid