SYNTHESIS AND BIOLOGICAL EVALUATION OF TC-99M MAG3 AS A HIPPURAN REPLACEMENT

  • 1 January 1986
    • journal article
    • research article
    • Vol. 27  (1) , 111-116
Abstract
A new technetium-chelating agent based on a triamide monomercaptide tetradentate set of donor groups, mercaptoacetylglycylglycylglycine (MAG3), was synthesized and evaluated. Chelation with 99mTc resulted in a single radiochemical product as expected. Studies in mice of [99mTc]MAG3 indicated excretion rates faster than o-iodohippurate (OIH) both in normal and in probenecid treated animals. Specificity for renal excretion was essentially complete. Clearance studies in rats resulted in 2.84 ml/min/100 g for [99mTc]MAG3, 2.17 for OIH, and 1.29 for [125I]iothalamate. Extraction efficiencies were 85% for [99mTc]MAG3 69% for OIH and 39% for [125I]iothalamate. Probenicid depressed the clearance both of [99mTC]MAG3 and OIH at 25 and 50 mg/kg/hr, but to a greater extent with [99mTC]MAG3. The greater effect is offset, however, by the larger fraction secreted by the renal tubular cells. The animal results suggest that [99mTc]MAG3 may be a useful alternative to [131I]OIH.