title: Uptake of technetium-99m-tetrofosmin, technetium-99m-MIBI and thallium-201 in tumor cell lines.
abstract: We investigated the kinetics, cellular uptake and intracellular distribution of 99mTc-tetrofosmin in tumor cell lines and compared them with those of 99mTc-MIBI and 201TI.
  
  
  METHODS
  At specific intervals after incubation with radiotracers, cellular uptake was determined. Cells were also treated with nigericin, carbonyl cyanide m-chloro-phenylhydrazone (CCCP) and ouabain to determine their effects on the uptake of the tracers.
  
  
  RESULTS
  Each tracer showed similar uptake kinetics in both cell lines, and a steady-state was maintained for at least 4 hr. Nigericin stimulated the uptake of both 99mTc-tetrofosmin and 99mTc-MIBI in HBL-2 cells, although it inhibited their uptake in SW-13 cells. Nigericin also inhibited 90% of 201TI uptake in both cell lines. Addition of CCCP caused 73%-97% release of accumulated 99mTc-MIBI from both cell lines with or without nigericin pretreatment, indicating that most of the accumulated 99mTc-MIBI was related to mitochondria. The effect of CCCP on accumulated 99mTc-tetrofosmin was less marked than that on 99mTc-MIBI in both cell lines, indicating that only a part of accumulated 99mTc-tetrofosmin, was related to mitochondria. Ouabain preincubation inhibited 74%-77% and 51%-53% of 201TI uptake in HBL-2 and SW-13 cells, respectively, as well as inhibited 22%-31% uptake of 99mTc-tetrofosmin in both HBL-2 and SW-13 cells. Uptake by the dead cells of either cell line was negligible for each tracer.
  
  
  CONCLUSIONS
  Technetium-99m-tetrofosmin uptake depends on both cell membrane and mitochondrial potentials. Only a small fraction of 99mTc-tetrofosmin accumulates inside the mitochondria, while most 99mTc-MIBI accumulates inside the mitochondria. Thallium-201 uptake is partly independent of the Na+, K+ pump.
authors.affiliation: Department of Radiology, Yamanashi Medical University, Japan.
authors.forename: A S
authors.initials: AS
authors.lastname: Arbab
authors.forename: K
authors.initials: K
authors.lastname: Koizumi
authors.forename: K
authors.initials: K
authors.lastname: Toyama
authors.forename: T
authors.initials: T
authors.lastname: Araki
mesh_terms: D002258:Carbonyl Cyanide m-Chlorophenyl Hydrazone / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006801:Humans; D007476:Ionophores / Q000494:pharmacology; D009550:Nigericin / Q000494:pharmacology; D009943:Organophosphorus Compounds / Q000493:pharmacokinetics*; D015609:Organotechnetium Compounds / Q000493:pharmacokinetics*; D010042:Ouabain / Q000494:pharmacology; D000254:Sodium-Potassium-Exchanging ATPase / Q000037:antagonists & inhibitors; D017256:Technetium Tc 99m Sestamibi / Q000493:pharmacokinetics*; D013794:Thallium Radioisotopes / Q000493:pharmacokinetics*; D014407:Tumor Cells, Cultured; D014475:Uncoupling Agents / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D007476:Ionophores; D009943:Organophosphorus Compounds; D015609:Organotechnetium Compounds; D013794:Thallium Radioisotopes; D014475:Uncoupling Agents; C078700:technetium tc-99m tetrofosmin; D002258:Carbonyl Cyanide m-Chlorophenyl Hydrazone; D010042:Ouabain; D017256:Technetium Tc 99m Sestamibi; D000254:Sodium-Potassium-Exchanging ATPase; D009550:Nigericin