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Imaging the norepinephrine transporter with positron emission tomography: initial human studies with (S,S)-[18F]FMeNER-D2

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Abstract

Introduction

(S,S)-[18F]FMeNER-D2 is a recently developed positron emission tomography (PET) ligand for in vivo quantification of norepinephrine transporter. A monkey occupancy study with the radioligand indicated that (S,S)-[18F]FMeNER-D2 can be useful for quantitative PET analysis. In this preliminary study, regional distributions in the living human brain were evaluated.

Materials and methods

Brain PET measurements were performed for a total of 255 min after the injection of 188.3 ± 5.7 MBq of (S,S)-[18F]FMeNER-D2 in four healthy male subjects. Regions of interests were drawn on the thalamus and the caudate in the coregistered MRI/PET images.

Results

(S,S)-[18F]FMeNER-D2 displayed good brain penetration and selective retention in regions rich in norepinephrine reuptake sites. The transient peak equilibrium was reached during the PET measurements. The ratios of radioactivity uptake in the thalamus to that in the caudate were 1.50 ± 0.06 for the time period of 90–255 min.

Conclusion

The present preliminary investigation indicates that (S,S)-[18F]FMeNER-D2 has suitable characteristics for probing the norepinephrine reuptake system with PET in the human brain.

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Acknowledgement

The authors would like to thank Lilly Research Laboratories for providing the precursors and standards. We are grateful to all the members of the PET group at the Karolinska Institutet. We are also grateful to Dr. Pierre Lafolie at Karolinska Clinical Research for subject recruitment.

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Authors and Affiliations

  1. Psychiatry Section, Department of Clinical Neuroscience, Karolinska Institutet, 171 76, Stockholm, Sweden

    Akihiro Takano, Balázs Gulyás, Andrea Varrone, Per Karlsson, Magnus Schou, Anu J. Airaksinen & Christer Halldin

  2. Lilly Research Laboratories, Mont-Saint-Guibert, Belgium

    Francois Vandenhende

  3. Lilly Research Laboratories, Indianapolis, IN, USA

    Johannes Tauscher

Authors
  1. Akihiro Takano
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  2. Balázs Gulyás
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  3. Andrea Varrone
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  4. Per Karlsson
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  5. Magnus Schou
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  6. Anu J. Airaksinen
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  7. Francois Vandenhende
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  8. Johannes Tauscher
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  9. Christer Halldin
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Corresponding author

Correspondence to Christer Halldin.

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Takano, A., Gulyás, B., Varrone, A. et al. Imaging the norepinephrine transporter with positron emission tomography: initial human studies with (S,S)-[18F]FMeNER-D2 . Eur J Nucl Med Mol Imaging 35, 153–157 (2008). https://doi.org/10.1007/s00259-007-0598-8

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  • DOI: https://doi.org/10.1007/s00259-007-0598-8

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