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

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    Authors
    Prenant, C
    Cawthorne, Christopher
    Fairclough, M
    Rothwell, N
    Boutin, H
    Affiliation
    Wolfson Molecular Imaging Centre, University of Manchester, Manchester, UK. cprenant@cyclopharma.fr
    Issue Date
    2010-09
    
    Metadata
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    Abstract
    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 epsilon-amino group of lysine residues or amino-terminal residues) using [(18)F]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 [(18)F]fluoroethyl-rhIL-1ra retained binding specificity by conducting an assay on rat brain sections, allowing its pharmakokinetic study using PET.
    Citation
    Radiolabeling with fluorine-18 of a protein, interleukin-1 receptor antagonist. 2010, 68 (9):1721-7 Appl Radiat Isot
    Journal
    Applied Radiation and Isotopes
    URI
    http://hdl.handle.net/10541/111114
    DOI
    10.1016/j.apradiso.2010.04.007
    PubMed ID
    20435481
    Type
    Article
    Language
    en
    ISSN
    0969-8043
    EISSN
    1872-9800
    ae974a485f413a2113503eed53cd6c53
    10.1016/j.apradiso.2010.04.007
    Scopus Count
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    All Christie Publications
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