Validation of 4-(Fluorine-18)Fluoro-3-iodobenzylguanidine as a positron-emitting analog of MIBG
- Duke Univ. Medical Center, Durham, NC (United States)
This study evaluates the potential utility of 4-({sup 13}F)fluoro-3-iodo-benzylguanidine (({sup 18}F)FIBG) as an MIBG analog. In vitro assays of tracer binding were carried out using the SK-N-SH human neuroblastoma cell line in a paired-label format to compare ({sup 18}F)FIBG directly with no-carrier-added ({sup 125}I)MIBG. To ascertain whether ({sup 18}F)FIBG, like MIBG, is taken up by the uptake-1 mechanism, the effects of desipramine, norepinephrine, and carrier MIBG and FIBG on cell binding were determined. Preincubation with ouabain and incubation at 4{degrees}C was used to evaluate the energy-dependence of ({sup 18}F)FIBG uptake by SK-N-SH cells. The tissue distribution of ({sup 18}F)FIBG in mice was compared with no-carrier-added ({sup 125}I)MIBG in a paired-label study. In paired-label binding studies, the percent binding of ({sup 18}F)FIBG to neuroblastoma cells remained constant over a three-log activity range and the level was somewhat higher than that of no-carrier-added ({sup 125}I)MIBG. Binding was blocked by desipramine, norepinephrine, carrier MIBG and FIBG, ouabain and by incubating at 4{degrees}C, suggesting that ({sup 18}F)FIBG is taken up by the uptake-1 mechanism. Radiation dosimetry calculations suggest that higher doses of ({sup 18}F)FIBG, unlike ({sup 124}I)MIBG, could be administered to patients. These in vitro and in vivo evaluations show that ({sup 18}F)FIBG is an excellent analog of MIBG, suggesting that ({sup 18}F)FIBG should be further evaluated for use in PET imaging of neuroendocrine tumors and cardiac abnormalities. 33 refs., 4 figs., 2 tabs.
- DOE Contract Number:
- FG05-89ER60789
- OSTI ID:
- 250015
- Journal Information:
- Journal of Nuclear Medicine, Vol. 36, Issue 4; Other Information: PBD: Apr 1995
- Country of Publication:
- United States
- Language:
- English
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