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Erschienen in:
01.11.2005 | Short Communication
Demonstration of pulmonary β2-adrenergic receptor binding in vivo with [18F]fluoroethyl-fenoterol in a guinea pig model
Erschienen in: European Journal of Nuclear Medicine and Molecular Imaging | Ausgabe 11/2005
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Purpose
The new β2 radioligand (R,R)(S,S) 5-(2-(2-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylethylamino)-1-hydroxyethyl)-benzene-1,3-diol ([18F]FE-fenoterol; [18F]FEFE), a fluoroethylated derivative of racemic fenoterol, was evaluated in vivo and ex vivo using a guinea pig model.
Methods
Dynamic PET studies over 60 min with [18F]FEFE were performed in nine Hartley guinea pigs in which a baseline (group 1, n=3), a predose (group 2, n=3; 2 mg/kg fenoterol 5 min prior to injection of [18F]FEFE) or a displacement study (group 3, n=3; 2 mg/kg fenoterol 5 min post injection of [18F]FEFE) was conducted.
Results
In all animal groups, the lungs could be visualised and semi-quantified separately by calculating uptake ratios to non-specific binding in the neck area. Premedication with non-radioactive fenoterol and displacement tests showed significant reduction of lung uptake, by 94% and 76%, respectively.
Conclusion
These data demonstrate specific binding of the new radioligand to the pulmonary β2-receptors in accordance with ex vivo measurements. Therefore, [18F]FEFE seems to be suitable for the in vivo visualisation and quantification of the pulmonary β2-receptor binding in this animal model.