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State University of New York at Buffalo, New York
Correspondence: For reprints contact: Hank F. Kung, Dept. of Nuclear Medicine, Veterans' Administration Hospital, 3495 Bailey Ave., Buffalo, NY 14215.
ABSTRACT
Bidentate monophosphatesphosphonoacetate (PAA), 2-phosphonoproprionate (PPA), 2-methyl-2-phosphonoproprionate (MPPA), and carbamyl phosphate (CAP)which are pyrophosphate analogs, were successfully labeled with Sn(II)-reduced [99mTc] pertechnetate in high yield (>95%).
Biodistribution studies show that these Tc-99m-labeled monophosphates do localize in bone. At 2 hr after injection, Tc-99m CAP has average femur uptakes of 1.9% in rats and 2.9% in rabbits, which correspond to calculated total-bone uptakes of 38% and .58%, respectively. These are comparable with the femur uptakes for Tc-99m methylene diphosphonate (MDP), which are 1.8% in rats and 2.7% in rabbits. However, the blood clearance rate for Tc-99m CAP was slower than that observed for Tc-99m MDP making the former less desirable for use as a bone-scanning agent. The femur uptakes for Tc-99m PAA are 0.9% in rats and 1.2% in rabbits, corresponding to 18% and 24% in total bone, respectively. The PAA derivatives PPA and MPPA have much lower bone uptake.
Technetium-99m CAP also concentrates in necrotic myocardium in rats, in amounts comparable to Tc-99m pyrophosphate.
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