Chemical and biological studies of Tc-99m N,N'-bis(mercaptoacetamido)-ethylenediamine: a potential replacement for I-131 iodohippurate.
The tetradentate chelating agent N,N'-bis(benzoylmercaptoacetamido)ethylenediamine was synthesized for evaluation as a potential technetium-99m renal-function radiopharmaceutical. Complexes were prepared using different reducing agents and analyzed by high-performance liquid chromatography. Biological studies were performed in mice, rats, and rabbits and indicated that the new agent is cleared by the kidneys significantly faster than Tc-99m DTPA (p less than 0.01) and slightly slower than I-131 o-iodohippuric acid (p greater than 0.05). There was no evidence of significant renal retention. Renal excretion in all species studied was 70--75% of the injected dose in 30 min; biliary excretion in rats was 7% in animals with normal renal function and 18% in 90 min in the absence of renal function. We conclude that limited clinical trials are warranted.
D000818:Animals; D004353:Drug Evaluation, Preclinical; D005029:Ethylenediamines / Q000138:chemical synthesis / Q000378:metabolism* / Q000633:toxicity; D005260:Female; D006207:Half-Life; D007553:Isotope Labeling; D007668:Kidney / Q000000981:diagnostic imaging* / Q000378:metabolism; D007684:Kidney Tubules / Q000378:metabolism; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D015609:Organotechnetium Compounds; D004369:Pentetic Acid / Q000378:metabolism; D011817:Rabbits; D011877:Radionuclide Imaging; D051381:Rats; D013667:Technetium / Q000378:metabolism* / Q000633:toxicity; D014018:Tissue Distribution
D005029:Ethylenediamines; D015609:Organotechnetium Compounds; D013667:Technetium; C028923:technetium Tc 99m N,N'-bis(mercaptoacetamido)ethylenediamine; D004369:Pentetic Acid