Abstract
Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [(18)F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solution-phase (18)F-"click" radiolabeling and solid-phase radiolabeling using 4-[(18)F]fluorobenzoic and 2-[(18)F]fluoropropionic acids. Here we compare the three different radiolabeling approaches and report the effects on PET imaging and pharmacokinetics. The prosthetic groups did have an effect; metabolites with significantly different polarities were observed.
Publication types
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Comparative Study
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Evaluation Study
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Antigens, Neoplasm / chemistry
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Antigens, Neoplasm / drug effects*
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Antigens, Neoplasm / metabolism
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Benzoates / chemistry*
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Cell Line, Tumor
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Fluorine Radioisotopes
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Humans
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Integrins / chemistry
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Integrins / drug effects*
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Integrins / metabolism
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Male
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Mice
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Mice, Nude
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Molecular Structure
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Neoplasms / diagnosis*
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Peptides* / chemistry
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Peptides* / pharmacokinetics
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Positron-Emission Tomography / methods*
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Propionates / chemistry*
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Radiopharmaceuticals* / chemistry
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Radiopharmaceuticals* / pharmacokinetics
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Sensitivity and Specificity
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Stereoisomerism
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Tissue Distribution
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Xenograft Model Antitumor Assays
Substances
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Antigens, Neoplasm
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Benzoates
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Fluorine Radioisotopes
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Integrins
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Peptides
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Propionates
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Radiopharmaceuticals
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integrin alphavbeta6
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4-fluorobenzoic acid