Boutin, H.

Cawthorne, C.

Fairclough, M.

Prenant, C.

Rothwell, N.

English

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

The University of Manchester - Institutional Repository

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

https://pure.manchester.ac.uk/ws/files/29573855/POST-PEER-REVIEW-PUBLISHERS-DOCUMENT.PDF

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

Abstract

Similar works

Full text

Available Versions

The University of Manchester - Institutional Repository