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Synthesis and Renal Excretion of Technetium 99m-Labeled Organic Cations

College of Pharmacy and Biomedical Chemistry Research Center, Department of Chemistry, University of Cincinnati, Cincinnati, Ohio

Correspondence: For reprints contact: William Cacini, PhD., College of Pharmacy, University of Cincinnati, Cincinnati, OH 45267-0004.

ABSTRACT

Organic cations are excreted more efficiently than organic anions in uremia suggesting superiority as renal imaging agents. In this study, three ^99mTc-labeled cationic cyclam complexes were synthesized and their renal clearance quantified in rats. The complexes are cleared at a rate of about 2.5–3 times that of inulin and about 60% that of p-aminohippurate. Inhibition of ^99mTc-cyclam excretion by quinine indicates transport by the organic cation process. Comparative in vivo imaging experiments demonstrated that in normal rats ^99mTc-cyclam reached peak renal activity 1.8 ± 0.6 min after injection, a value intermediate between that for [¹³¹I]OIH (1.0 ± 0) and ^99mTc-MAG3 (2.8 ± 0.6). In rats injected with the acute nephrotoxin cisplatin, the times to peak were lengthened with the relative order being ^99mTc-cyclam > ^99mTc-MAG3 > [¹³¹I]OIH. The results demonstrate that cationic complexes may be useful for renal imaging diagnostic applications.