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Evaluation in dogs and humans of three potential technetium-99m myocardial perfusion agents

Journal Article · · J. Nucl. Med.; (United States)
OSTI ID:5270734

The biodistribution of the three cationic /sup 99m/Tc complexes (/sup 99m/Tc(TMP)6)+, (/sup 99m/Tc(POM-POM)3)+, and (/sup 99m/Tc(TBIN)6)+--where TMP represents trimethylphosphite, POM-POM represents 1,2-bis(dimethyoxyphosphino)ethane, and TBIN represents t-butylisonitrile--have been evaluated in humans and dogs. Each agent was studied in three normal volunteers at rest, while (/sup 99m/Tc(POM-POM)3)+ and (/sup 99m/Tc(TBIN)6)+ were each studied in one normal volunteer at exercise. Even though all three agents yield good myocardial images in dogs, none appear suitable for clinical use as myocardial perfusion imaging radiopharmaceuticals. In humans, (/sup 99m/Tc(TMP)6)+ and (/sup 99m/Tc(POM-POM)3)+ clear very slowly from the blood and provide myocardial images only several hours after injection. (/sup 99m/Tc(TBIN)6)+ clears rapidly from the blood, but accumulation in the lung obscures the myocardial image for the first hour after injection; at later times, activity in the liver and spleen masks the apical wall. These results correlate with the blood-binding properties of the three complexes. (/sup 99m/Tc(TMP)6)+ and (/sup 99m/Tc(POM-POM)3)+ bind tightly to the plasma of human blood, but not to the plasma of dog blood; (/sup 99m/Tc(TBIN)6)+ does not bind tightly to the plasma of either dog or human blood. Among the Tc(I) complexes studied to date in humans, (/sup 99m/Tc(TBIN)6)+ appears to be unique in biodistribution pattern, blood-binding properties, and the fact that exercise improves the ultimate myocardial image. All the Tc(I) complexes appear to undergo myocardial accumulation by a mechanism different from that utilized by Tc(III) complexes. Animal studies alone are not adequate to evaluate the potential utility of /sup 99m/Tc cationic complexes for myocardial perfusion studies.

Research Organization:
Univ. of Milan, Italy
OSTI ID:
5270734
Journal Information:
J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 3; ISSN JNMEA
Country of Publication:
United States
Language:
English