• G Vaidyanathan, X G Zhao, D K Strickland, and M R Zalutsky.
• Department of Radiology, Duke University Medical Center, Durham, North Carolina 27710, USA.
• J. Nucl. Med. 1997 Feb 1; 38 (2): 330-4.

UnlabelledThe purpose of this study was to evaluate the properties of 4-fluoro-3-[131I]iodobenzylguanidine ([131I]FIBG), a potential neuroendocrine tumor and myocardial imaging radiopharmaceutical.MethodsThe binding of [131I]FIBG and [125I]MIBG was compared in vitro using the SK-N-SH human neuroblastoma cell line. The role of the active uptake-1 mechanism was investigated by determining the effect on cell binding of desipramine (DMI), ouabain, norepinephrine (NE), unlabeled MIBG and FIBG and by incubation at 4 degrees C. Finally, the tissue distributions of [131I]FIBG and [125I]MIBG were compared in normal mice.ResultsThe specific binding of [131I]FIBG remained fairly constant (45%-60%) over a 2-3-log activity range and consistently was 11%-14% higher (p < 0.05) than that of [125I]MIBG. The uptake of [131I]FIBG was reduced to 13% of control values by 1.5 microM DMI, to 31% by 1 mM ouabain, to 8% by lower temperature, to 8% by 50 microM NE and to 6% and 5% by 10 microM each of unlabeled MIBG and FIBG, respectively. The amount of [131I]FIBG retained by SK-N-SH cells was significantly higher than that of [125I]MIBG with the maximum difference observed at 72 hr. In mice, the uptake of [131I]FIBG was higher than that of [125I]MIBG not only in target tissues (heart and adrenals) but also in many other normal tissues; conversely, thyroidal uptake of [131I]FIBG was 2-3-fold lower than that of [125I]MIBG. The uptake of [131I]FIBG in the heart and adrenals was reduced by DMI.ConclusionIodine-131-FIBG is an analog of MIBG with prolonged binding to neuroblastoma cells in vitro and retention in the myocardium in vivo.

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