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Demonstration of pulmonary β2-adrenergic receptor binding in vivo with [18F]fluoroethyl-fenoterol in a guinea pig model

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Abstract

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.

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Acknowledgements

This study was supported by the German Research Foundation (DFG grant FOR 474). Additionally, the authors thank Boehringer Ingelheim Pharma, Germany, for providing (R,R)(S,S)-fenoterol hydrobromide. Studies had previously been approved by the regional ethics committee and were conducted according to the German Law for Animal Protection.

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Authors and Affiliations

  1. Department of Nuclear Medicine, University Hospital, Langenbeckstrasse 1, 55101, Mainz, Germany

    A. Helisch, E. Schirrmacher, R. Schirrmacher, H. G. Buchholz & P. Bartenstein

  2. Institute of Physiology and Pathophysiology, University of Mainz, Mainz, Germany

    O. Thews, W. Dillenburg & J. Tillmanns

  3. Institute of Nuclear Chemistry, University of Mainz, Mainz, Germany

    S. Höhnemann & F. Rösch

  4. Institute of Pharmacology, University of Mainz, Mainz, Germany

    I. Wessler

  5. Pulmonary Division, University Hospital, Mainz, Germany

    R. Buhl

Authors
  1. A. Helisch
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  2. E. Schirrmacher
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  3. O. Thews
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  4. R. Schirrmacher
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  5. H. G. Buchholz
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  6. W. Dillenburg
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  7. S. Höhnemann
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  8. J. Tillmanns
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  9. I. Wessler
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  10. R. Buhl
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  11. F. Rösch
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  12. P. Bartenstein
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Corresponding author

Correspondence to A. Helisch.

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Helisch, A., Schirrmacher, E., Thews, O. et al. Demonstration of pulmonary β2-adrenergic receptor binding in vivo with [18F]fluoroethyl-fenoterol in a guinea pig model. Eur J Nucl Med Mol Imaging 32, 1324–1328 (2005). https://doi.org/10.1007/s00259-005-1914-9

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  • DOI: https://doi.org/10.1007/s00259-005-1914-9

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