Demonstration of pulmonary beta2-adrenergic receptor binding in vivo with [18F]fluoroethyl-fenoterol in a guinea pig model

The new beta2 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. Dynamic PET studies over 60...

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Bibliographic Details
Published in:European journal of nuclear medicine and molecular imaging 2005-11, Vol.32 (11), p.1324-1328
Main Authors: Helisch, A, Schirrmacher, E, Thews, O, Schirrmacher, R, Buchholz, H G, Dillenburg, W, Höhnemann, S, Tillmanns, J, Wessler, I, Buhl, R, Rösch, F, Bartenstein, P
Format: Article
Language:English
Subjects:
Animals
Feasibility Studies
Fenoterol - analogs & derivatives
Fenoterol - pharmacokinetics
Guinea Pigs
Lung - diagnostic imaging
Lung - metabolism
Metabolic Clearance Rate
Models, Animal
Organ Specificity
Radionuclide Imaging
Radiopharmaceuticals - pharmacokinetics
Receptors, Adrenergic, beta-2 - metabolism
Tissue Distribution
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Summary:The new beta2 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. Dynamic PET studies over 60 min with [(18)F]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. 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. These data demonstrate specific binding of the new radioligand to the pulmonary beta2-receptors in accordance with ex vivo measurements. Therefore, [18F]FEFE seems to be suitable for the in vivo visualisation and quantification of the pulmonary beta2-receptor binding in this animal model.
ISSN:1619-7070