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(4-[18F]fluoro-3-iodobenzyl)guanidine, a potential MIBG analogue for positron emission tomography.

Publication ,  Journal Article
Vaidyanathan, G; Affleck, DJ; Zalutsky, MR
Published in: J Med Chem
October 14, 1994

The aims of this investigation were to develop a no-carrier-added (nca) synthesis of (4-[18F]-fluoro-3-iodobenzyl)guanidine ([18F]FIBG) and to evaluate its potential as an MIBG analogue useful for positron emission tomography. [18F]FIBG was prepared in four steps starting from 4-cyano-2-iodo-N,N,N-trimethylanilinium trifluoromethanesulfonate in 5% decay-corrected radiochemical yield in a total synthesis time of 130 min. The specific activity was more than 1500 Ci per mmol. In vitro binding studies showed that the percent binding of [18F]FIBG to SK-N-SH human neuroblastoma cells remained constant over a 3-log activity range and was similar to that of nca [131I]MIBG. Specific and high uptake of FIBG was also seen in mouse heart and adrenals. The in vitro and in vivo properties of [18F]FIBG suggest that this compound may be a useful positron-emitting analogue of MIBG.

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Published In

J Med Chem

DOI

ISSN

0022-2623

Publication Date

October 14, 1994

Volume

37

Issue

21

Start / End Page

3655 / 3662

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Tomography, Emission-Computed
  • Tissue Distribution
  • Neuroblastoma
  • Myocardium
  • Mice, Inbred BALB C
  • Mice
  • Medicinal & Biomolecular Chemistry
  • Lipid Metabolism
  • Iodobenzenes
 

Citation

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Vaidyanathan, G., Affleck, D. J., & Zalutsky, M. R. (1994). (4-[18F]fluoro-3-iodobenzyl)guanidine, a potential MIBG analogue for positron emission tomography. J Med Chem, 37(21), 3655–3662. https://doi.org/10.1021/jm00047a022
Vaidyanathan, G., D. J. Affleck, and M. R. Zalutsky. “(4-[18F]fluoro-3-iodobenzyl)guanidine, a potential MIBG analogue for positron emission tomography.J Med Chem 37, no. 21 (October 14, 1994): 3655–62. https://doi.org/10.1021/jm00047a022.
Vaidyanathan G, Affleck DJ, Zalutsky MR. (4-[18F]fluoro-3-iodobenzyl)guanidine, a potential MIBG analogue for positron emission tomography. J Med Chem. 1994 Oct 14;37(21):3655–62.
Vaidyanathan, G., et al. “(4-[18F]fluoro-3-iodobenzyl)guanidine, a potential MIBG analogue for positron emission tomography.J Med Chem, vol. 37, no. 21, Oct. 1994, pp. 3655–62. Pubmed, doi:10.1021/jm00047a022.
Vaidyanathan G, Affleck DJ, Zalutsky MR. (4-[18F]fluoro-3-iodobenzyl)guanidine, a potential MIBG analogue for positron emission tomography. J Med Chem. 1994 Oct 14;37(21):3655–3662.
Journal cover image

Published In

J Med Chem

DOI

ISSN

0022-2623

Publication Date

October 14, 1994

Volume

37

Issue

21

Start / End Page

3655 / 3662

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Tomography, Emission-Computed
  • Tissue Distribution
  • Neuroblastoma
  • Myocardium
  • Mice, Inbred BALB C
  • Mice
  • Medicinal & Biomolecular Chemistry
  • Lipid Metabolism
  • Iodobenzenes