Validation of 4-[fluorine-18]fluoro-3-iodobenzylguanidine as a positron-emitting analog of MIBG.

Published

Journal Article

UNLABELLED: This study evaluates the potential utility of 4-[18F]fluoro-3-iodobenzylguanidine ([18F]FIBG) as an MIBG analog. METHODS: 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 [18F]FIBG directly with no-carrier-added [125I]MIBG. To ascertain whether [18F]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 [18F]FIBG uptake by SK-N-SH cells. The tissue distribution of [18F]FIBG in mice was compared with no-carrier-added [125I]MIBG in a paired-label study. RESULTS: In paired-label binding studies, the percent binding of [18F]FIBG to neuroblastoma cells remained constant over a three-log activity range and the level was somewhat higher than that of no-carrier-added [125I]MIBG. Binding was blocked by desipramine, norepinephrine, carrier MIBG and FIBG, ouabain and by incubating at 4 degrees C, suggesting that [18F]FIBG is taken up by the uptake-1 mechanism. Radiation dosimetry calculations suggest that higher doses of [18F]FIBG, unlike [124I]MIBG, could be administered to patients. CONCLUSION: These in vitro and in vivo evaluations show that [18F]FIBG is an excellent analog of MIBG, suggesting that [18F]FIBG should be further evaluated for use in PET imaging of neuroendocrine tumors and cardiac abnormalities.

Full Text

Duke Authors

Cited Authors

  • Vaidyanathan, G; Affleck, DJ; Zalutsky, MR

Published Date

  • April 1995

Published In

Volume / Issue

  • 36 / 4

Start / End Page

  • 644 - 650

PubMed ID

  • 7699460

Pubmed Central ID

  • 7699460

International Standard Serial Number (ISSN)

  • 0161-5505

Language

  • eng

Conference Location

  • United States