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

Journal Article · Wed Jan 01 04:00:00 EST 1986 · J. Nucl. Med.; (United States)

OSTI ID:5684621

Fritzberg, A R; Kasina, S; Eshima, D; Johnson, D L

A new technetium-chelating agent based on a triamide monomercaptide tetradentate set of donor groups, mercaptoacetylglycylglycylglycine (MAG3), was synthesized and evaluated. Chelation with /sup 99m/Tc resulted in a single radiochemical product as expected. Studies in mice of (/sup 99m/Tc)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 (/sup 99m/Tc)MAG3, 2.17 for OIH, and 1.29 for (125I)iothalamate. Extraction efficiencies were 85% for (/sup 99m/Tc)MAG3, 69% for OIH and 39% for (125I)iothalamate. Probenicid depressed the clearance both of (/sup 99m/Tc)MAG3 and OIH at 25 and 50 mg/kg/hr, but to a greater extent with (/sup 99m/Tc)MAG3. The greater effect is offset, however, by the larger fraction secreted by the renal tubular cells. The animal results suggest that (/sup 99m/Tc)MAG3 may be a useful alternative to (131I)OIH.

• Research Organization: Univ. of Utah School of Medicine, Salt Lake City
• OSTI ID: 5684621
• Journal Information: J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 1; ISSN JNMEA
• Country of Publication: United States
• Language: English

Related Subjects

560172* -- Radiation Effects-- Nuclide Kinetics & Toxicology-- Animals-- (-1987)
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
CHELATING AGENTS
CLEARANCE
CONTRAST MEDIA
DAYS LIVING RADIOISOTOPES
DISTRIBUTION
EXCRETION
HIPPURAN
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
IODINE 131
IODINE ISOTOPES
ISOMERIC TRANSITION ISOTOPES
ISOTOPES
KIDNEYS
MAMMALS
MICE
NUCLEI
ODD-EVEN NUCLEI
ORGANS
RADIOISOTOPES
RATS
RENAL CLEARANCE
RODENTS
SYNTHESIS
TECHNETIUM 99
TECHNETIUM ISOTOPES
TESTING
TISSUE DISTRIBUTION
VERTEBRATES
YEARS LIVING RADIOISOTOPES