ANIMAL EVALUATION OF TC-99M TRIAMIDE MERCAPTIDE COMPLEXES AS POTENTIAL RENAL IMAGING AGENTS

  • 1 July 1987
    • journal article
    • research article
    • Vol. 28  (7) , 1180-1186
Abstract
Technetium-99m mercaptoacetylglycylglycylglycine (MAG3), a [99mTc]triamide mercaptide (N3S) compound has been synthesized in an attempt to obviate the stereochemistry problems associates with the diamide dimercaptide (N2S2) ligands. Because initial studies have been promising, the terminal glycine on the MAG3 compound has been varied to create a new series of N3S compounds. Twelve new N3S complexes were initially screened in mice and the more promising complexes, 99mTc mercaptoacetylglycylglycyl-glycine ([99mTc]MAG3), 99mTc mercaptoacetygylcylglycyl-L-alanine ([99mTc]MAG2-Ala), and both complexes of 99mTc mercaptoeacetylglycylglycyl-L-asparagine ([99mTc]MAG2-Asn) and 99mTc mercaptoacetylglycylglycyl-L-glutamine ([99mTc]MAG2-Gln), were further evaluated in rats utilizing constant infusion blood clearances, extraction efficiencies and protein binding assays. The renal excretion of all these complexes compared favorably with simultaneously administered [131I]OIH and [125I]iothalamate. The triamide mercaptide complexes represent a new ligand class for 99mTc, which may provide a variety of complexes for the evaluation of renal tubular function.