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Cationic technetium-99m complexes of N-substituted pyridoxal derivatives as renal function agents

Journal Article · · Journal of Nuclear Medicine
OSTI ID:458865
New cationic technetium-chelating agents containing a pyridinium group have been synthesized and evaluated as potential renal radiopharmaceuticals. The pyridinium compounds used in the study are N-methyl pyridoxal chloride, N-ethyl pyridoxal chloride, N-propyl pyridoxal chloride, 1-methyl-3-hydroxy-4-formylpyridinium chloride, 1-methyl-2-formyl-3-hydroxpyridinium chloride and the Schiff`s bases of N-methyl pyridoxal chloride with amino acid, amino acid ester and amino acid amide. Complexes of these chelating agents with {sup 22m}Tc were prepared using a Na{sub 2}S{sub 2}O{sub 4} or a SnCl{sub 2} solution as a reducing agent. The purity of the {sup 99m}Tc complexes was determined by paper electrophoresis in 0.1 Mtris buffer. Electrophoresis indicates slightly positive-charged species. The log P values of these complexes showed a hydrophilic nature. Urinary excretion of the {sup 99m}Tc N-alkylated pyridoxal derivatives, {sup 99m}Tc-diethylenetriaminepentaacetic acid, {sup 99m}Tc-mercaptoacetylglycylglycylglycine (MAG3) and {sup 131}I-o-iodohippurate were determined in mice and rats at different time intervals. In a rat model, the pyridoxal-derived {sup 99m}Tc complexes are rapidly excreted in urine and provide clear renal scintigrams. Hepatobiliary excretion was negligible, reducing scan interference from the intestines. Total clearances were lower than that of {sup 131}I-hippurate and {sup 99m}Tc-MAG3. The rate of urinary clearance of the new tracers was not significantly faster than {sup 99m}Tc diethylenetriaminepentaacetic acid and the inhibitor N{sup 1}-methylnicotinamide had only a minimal effect on the renal behavior. Though the new tracers have cationic properties, the pyridinium group did not contribute largely to the excretion of active transport. 21 refs., 4 figs., 4 tabs.
OSTI ID:
458865
Journal Information:
Journal of Nuclear Medicine, Journal Name: Journal of Nuclear Medicine Journal Issue: 10 Vol. 35; ISSN JNMEAQ; ISSN 0161-5505
Country of Publication:
United States
Language:
English

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