Radiolabeling with fluorine-18 of a protein, interleukin-1 receptor antagonist

C. Prenant, C. Cawthorne, M. Fairclough, N. Rothwell, H. Boutin

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IL-1RA is a naturally occurring antagonist of the pro-inflammatory cytokine interleukin-1 (IL-1) with high therapeutic promise, but its pharmacokinetic remains poorly documented. In this report, we describe the radiolabeling of recombinant human interleukin-1 receptor antagonist (rhIL-1RA) with fluorine-18 to allow pharmacokinetic studies by positron emission tomography (PET). rhIL-1RA was labeled randomly by reductive alkylation of free amino groups (the ε-amino group of lysine residues or amino-terminal residues) using [ 18F]fluoroacetaldehyde under mild reaction conditions. Radiosyntheses used a remotely controlled experimental rig within 100min and the radiochemical yield was in the range 7.1-24.2% (decay corrected, based on seventeen syntheses). We showed that the produced [ 18F]fluoroethyl-rhIL-1ra retained binding specificity by conducting an assay on rat brain sections, allowing its pharmakokinetic study using PET. © 2010 Elsevier Ltd.
Original languageEnglish
Pages (from-to)1721-1727
Number of pages6
JournalApplied Radiation and Isotopes
Issue number9
Publication statusPublished - Sept 2010


  • [ 18F]fluoroacetaldehyde
  • [ 18F]rhIL-1RA
  • IL-1
  • Inflammation
  • PET.


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