(4-[18F]fluoro-3-iodobenzyl)guanidine, a potential MIBG analogue for positron emission tomography.
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.
Vaidyanathan
G
G
Department of Radiology, Duke University Medical Center, Durham, North Carolina 27710.
Affleck
D J
DJ
Zalutsky
M R
MR
D019797:3-Iodobenzylguanidine; D000311:Adrenal Glands / Q000378:metabolism; D000818:Animals; D003287:Contrast Media; D005462:Fluorine Radioisotopes; D006801:Humans; D007462:Iodobenzenes / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D050356:Lipid Metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D009206:Myocardium / Q000378:metabolism; D009447:Neuroblastoma / Q000378:metabolism; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed; D014407:Tumor Cells, Cultured
D003287:Contrast Media; D005462:Fluorine Radioisotopes; D007462:Iodobenzenes; C090053:(4-fluoro-3-iodobenzyl)guanidine; D019797:3-Iodobenzylguanidine