Synthesis and biodistribution of new oxo and nitrido 99mTc complexes with asymmetrical potentially dianionic or trianionic tetradentate SNNO ligands derived from methyl-2-aminocyclopentene-1-dithiocarboxylic acid

In this work, 10 new asymmetrical tetradentate SNNO ligands were prepared by reaction of the amine function of methyl 2-[(β-aminoethyl)amino]cyclopentene-1-dithiocarboxylate with various bifunctional substituents bearing hydroxyl/ketone and hydroxyl/aldehyde functional groups and with diethyl oxalat...

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Bibliographic Details
Published in:Nuclear medicine and biology 1998, Vol.25 (1), p.65-69
Main Authors: Belhadj-Tahar, H., Ouhayoun, E., Cros, G., Darbieu, M.H., Tafani, J.A.M., Fabre, J., Esquerre, J.P., Coulais, Y.
Format: Article
Language:English
Subjects:
2-Aminocyclopentene-1-dithiocarboxylic acid
Aminothiol
Animals
Biodistribution
Biological and medical sciences
Complexes
Contrast media. Radiopharmaceuticals
Cyclopentanes - chemical synthesis
Cyclopentanes - chemistry
Cyclopentanes - pharmacokinetics
Drug Stability
Ethylenediamines - chemical synthesis
Ethylenediamines - pharmacokinetics
Hydrogen-Ion Concentration
Isotope Labeling
Ligands
Male
Medical sciences
Nitridotechnetium
Oxotechnetium
Pharmacology. Drug treatments
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - pharmacokinetics
Rats
Rats, Wistar
Technetium Compounds - chemical synthesis
Technetium Compounds - pharmacokinetics
Technetium-99m
Temperature
Thiones - chemical synthesis
Thiones - chemistry
Thiones - pharmacokinetics
Tissue Distribution
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Summary:In this work, 10 new asymmetrical tetradentate SNNO ligands were prepared by reaction of the amine function of methyl 2-[(β-aminoethyl)amino]cyclopentene-1-dithiocarboxylate with various bifunctional substituents bearing hydroxyl/ketone and hydroxyl/aldehyde functional groups and with diethyl oxalate. 99mTc labeling efficiency was optimized by adjusting temperature and pH conditions. Seven nitrido and two oxo 99mTc complexes were isolated. Six of them proved to be stable near physiological conditions. Biodistribution studies in the rat showed a significant heart uptake for four of them and strong kidney and liver uptake for the other two.
ISSN:0969-8051
1872-9614
DOI:10.1016/S0969-8051(97)00138-8