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Technetium-99m-L,L-Ethylenedicysteine: A Renal Imaging Agent. I. Labeling and Evaluation in Animals

Laboratory of Radiopharmaceutical Chemistry I.F.W., K. U. Leuven
Department of Nuclear Medicine, U.Z. Gasthuisberg, Leuven, Belgium
Mallinckrodt Medical, Inc., St. Louis, Missouri

Correspondence: For reprints contact: A.M. Verbruggen, PhD, U.Z. Gasthuisberg, Radiopharmacy, B-3000 Leuven, Belgium.

ABSTRACT

L,L-ethylenedicysteine (L,L-EC) can be labeled efficiently with ^99mTc at pH 12 to obtain a highly pure and very stable tracer agent (^99mTc-L,L-EC). The biological behavior of ^99mTc-L,L-EC was studied in mice and a baboon. In mice, ^99mTc-L,L-EC demonstrated a more rapid urinary excretion and less retention in the kidneys, the liver, the intestines, and the blood than did ^99mTc-MAG₃ at 10 and 60 min p.i. Urinary excretion decreased in probenecid pretreated mice, which indicates active tubular transport. In the baboon, the renograms for ^99mTc-MAG₃ and ^99mTc-L,L-EC were comparable. Plasma-protein binding of ^99mTc-L,L-EC was lower than that of ^99mTc-MAG₃ while its distribution volume and 1-hr plasma clearance were clearly higher. The promising results of the animal experiments suggest that ^99mTc-L,L-ethylenedicysteine may be a useful alternative to ^99mTc-MAG₃ for renal function studies in humans.

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