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Chemical and Biological Studies of Tc-99m N,N'-Bis(mercaptoacetamido)ethylenediamine: A Potential Replacement for I-131 Iodohippurate

University of Colorado Health Sciences Center and Veterans Administration Medical Center, Denver, Colorado

Correspondence: For reprints contact: Alan R. Fritzberg, PhD, Dept. of Radiology, Univ. of Colo. Health Sciences Ctr., 4200 E. 9th, Denver, CO 80262.

ABSTRACT

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 < 0.01) and slightly slower than I-131 o-iodohippuric acid (p > 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.