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Uptake of Technetium-99m-Teboroxime in Cultured Myocardial Cells: Comparison with Thallium-201 and Technetium-99m-Sestamibi

Division of Nuclear Medicine, Centre Jean Perrin and INSERM U195 and U71, Faculty of Medicine, Université d'Auvergne, 63011 Clermont-Ferrand, France

Correspondence: For correspondence and reprints contact: Jean C. Maublant, MD, PhD, Division of Nuclear Medicine, Centre Jean Perrin, 63011 Clermont-Ferrand, France.

ABSTRACT

The effects of metabolic inhibition on the uptake of ^99mTc-teboroxime were assessed in cultured myocardial cells and compared with ²⁰¹Tl and ^99mTc-sestamibi. Metabolic impairment was induced by cyanide (CN), a blocker of the mitochondrial respiratory chain, iodoacetate (IAA), an inhibitor of the glycolytic pathway, and ouabain, an inhibitor of Na⁺-K⁺ sarcolemmal ATPase. Cellular viability was appreciated by the trypan blue exclusion method. The effects of low temperature and of cellular death resulting from osmotic lysis were also assessed. Net cellular uptake of the radiotracers and the amount of proteins in the culture dishes were measured. All experiments were performed in parallel with control conditions and the results were expressed relatively to the control values. Teboroxime uptake was clearly decreased at low temperature (29.6% ± 2.2% at 0°C, p < 0.001), while metabolic inhibition or osmotic lysis had no definite effect. The uptake of ²⁰¹Tl and sestamibi was severely diminished in the presence of a mixture of 5 mM CN and 0.1 mM IAA, but ²⁰¹Tl was less resistant than sestamibi (13.7% ± 0.3% and 73.5% ± 3.3%, respectively, after 1 hr of preincubation, p < 0.001 for both). Uptake of both tracers was very low in the presence of dead cells (12.1% ± 1.3% for ²⁰¹Tl and 4.1% ± 0.2% for sestamibi, p < 0.001 for both). Ouabain had a detrimental effect only on ²⁰¹Tl uptake at doses higher than 100 µM. Of these three currently available coronary blood flow imaging agents, teboroxime shows the lowest sensitivity to metabolic impairment.

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