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. 2012;2(1):55-76.
Epub 2011 Dec 15.

Positron emission tomography (PET) imaging with (18)F-based radiotracers

Mian M Alauddin  1
Affiliations

Positron emission tomography (PET) imaging with (18)F-based radiotracers

Mian M Alauddin. Am J Nucl Med Mol Imaging. 2012.

Abstract

Positron Emission Tomography (PET) is a nuclear medicine imaging technique that is widely used in early detection and treatment follow up of many diseases, including cancer. This modality requires positron-emitting isotope labeled biomolecules, which are synthesized prior to perform imaging studies. Fluorine-18 is one of the several isotopes of fluorine that is routinely used in radiolabeling of biomolecules for PET; because of its positron emitting property and favorable half-life of 109.8 min. The biologically active molecule most commonly used for PET is 2-deoxy-2-(18)F-fluoro-β-D-glucose ((18)F-FDG), an analogue of glucose, for early detection of tumors. The concentrations of tracer accumulation (PET image) demonstrate the metabolic activity of tissues in terms of regional glucose metabolism and accumulation. Other tracers are also used in PET to image the tissue concentration. In this review, information on fluorination and radiofluorination reactions, radiofluorinating agents, and radiolabeling of various compounds and their application in PET imaging is presented.

Keywords: Fluorine-18; PET radiopharmaceuticals; positron emission tomography (PET).

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Figures

Figure 1
Figure 1
Electrophilic fluorination; Syntheses of 18F-5-fluorouracil (A), 18F-a-trifluoromethyl ketones (B), and 18F-fluorodopa (C).
Figure 2
Figure 2
Electrophilic fluorination with 18F-perchloryl fluoride (A), synthesis of 18F-FDG (B), and radiosynthesis of the fluorinated A-ring of vitamin D3 (C).
Figure 3
Figure 3
Nucleophilic fluorination; synthesis of 18F-FDG (A), and 18F-FHPG & 18F-FHBG (B).
Figure 4
Figure 4
synthesis of 2′- deoxy-2′-18F-fluoro-arabino-adenosine (A) and 3′- deoxy-3′-18F-fluoro-xylo-adenosine (B).
Figure 5
Figure 5
Four-step synthesis of 2′-deoxy-2′-18F-fluoro-1-β-D-5-substituted-arabionofuranosyluracil (A), and two-step synthesis of 2′-deoxy-2′-18F-fluoro-1-β-D-5-methyl-arabionofuranosyluracil (B).
Figure 6
Figure 6
Synthesis of 18F-FMXU (A), and 18F-FLT (B) and (C).
Figure 7
Figure 7
Nucleophilic fluorination, synthesis of synthesis of N3-substituted thymidine analogues.
Figure 8
Figure 8
Radiosynthesis of Et-18FDL (A) and 18F-FEL (B).
Figure 9
Figure 9
Nucleophilic fluorination, synthesis of 18F-F-PEG6-IPQA.
Figure 10
Figure 10
Radiosynthesis of 18F-fluoroacetate (A), synthesis of 18F-Fmiso (B) and (C).
Figure 11
Figure 11
PET images of tumor-bearing mice using 18F-L-FMAU (A), 18F-D-FMAU (B), 18F-FLT (C), N3-18F-FET (D) and N3-18F-FPrT (E).
Figure 12
Figure 12
PET images of wild-type tumor (left flank) and HSV1-tk expressing tumor (right flank) on nude mice using 18F-FFAU (A), 18F-FCAU (B), 18F-FBAU (C), 18F-FIAU (D), 18F-FMAU (E), and 18F-FEAU (F). PET images of HSV1-tk and HSV1-A168Htk gene expression using 18F-FDG (G), 18F-FEAU (H) and 18F-FHBG (I).
Figure 13
Figure 13
PET images of 18F-FAA (A) and 18F-FXA (B); PET image of an orthotopically implanted pancreatic tumor xenograft in a nude mouse (C); and PET images of xenografts expressing EGFR using 18F-PEG6-IPQA in mice before therapy (D) and after therapy (E).
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