Synthesis and biological evaluation of technetium-99m MAG3 as a hippuran replacement

J Nucl Med. 1986 Jan;27(1):111-6.

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 omicron-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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Female
  • Iodohippuric Acid*
  • Kidney / diagnostic imaging*
  • Male
  • Mice
  • Oligopeptides / chemical synthesis*
  • Probenecid / pharmacology
  • Radionuclide Imaging
  • Rats
  • Rats, Inbred Strains
  • Technetium / chemical synthesis*
  • Technetium Tc 99m Mertiatide
  • Tissue Distribution

Substances

  • Oligopeptides
  • Iodohippuric Acid
  • Technetium Tc 99m Mertiatide
  • Technetium
  • Probenecid