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European Journal of Nuclear Medicine and Molecular Imaging

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01-04-2012 | Original Article

Imaging for metabotropic glutamate receptor subtype 1 in rat and monkey brains using PET with [¹⁸F]FITM

Authors: Tomoteru Yamasaki, Masayuki Fujinaga, Jun Maeda, Kazunori Kawamura, Joji Yui, Akiko Hatori, Yuichiro Yoshida, Yuji Nagai, Masaki Tokunaga, Makoto Higuchi, Tetsuya Suhara, Toshimitsu Fukumura, Ming-Rong Zhang

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 4/2012

Abstract

Purpose

In this study, we evaluate the utility of 4-[¹⁸F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([¹⁸F]FITM) as a positron emission tomography (PET) ligand for imaging of the metabotropic glutamate receptor subtype 1 (mGluR1) in rat and monkey brains.

Methods

In vivo distribution of [¹⁸F]FITM in brains was evaluated by PET scans with or without the mGluR1-selective antagonist (JNJ16259685). Kinetic parameters of monkey PET data were obtained using the two-tissue compartment model with arterial blood sampling.

Results

In PET studies in rat and monkey brains, the highest uptake of radioactivity was in the cerebellum, followed by moderate uptake in the thalamus, hippocampus and striatum. The lowest uptake of radioactivity was detected in the pons. These uptakes in all brain regions were dramatically decreased by pre-administration of JNJ16259685. In kinetic analysis of monkey PET, the highest volume of distribution (V _T) was detected in the cerebellum (V _T = 11.5).

Conclusion

[¹⁸F]FITM has an excellent profile as a PET ligand for mGluR1 imaging. PET with [¹⁸F]FITM may prove useful for determining the regional distribution and density of mGluR1 and the mGluR1 occupancy of drugs in human brains.

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Title: Imaging for metabotropic glutamate receptor subtype 1 in rat and monkey brains using PET with [18F]FITM
Authors: Tomoteru Yamasaki
Masayuki Fujinaga
Jun Maeda
Kazunori Kawamura
Joji Yui
Akiko Hatori
Yuichiro Yoshida
Yuji Nagai
Masaki Tokunaga
Makoto Higuchi
Tetsuya Suhara
Toshimitsu Fukumura
Ming-Rong Zhang
Publication date: 01-04-2012
Publisher: Springer-Verlag
Published in: European Journal of Nuclear Medicine and Molecular Imaging / Issue 4/2012
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI: https://doi.org/10.1007/s00259-011-1995-6

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Imaging for metabotropic glutamate receptor subtype 1 in rat and monkey brains using PET with [¹⁸F]FITM

Abstract

Purpose

Methods

Results

Conclusion

Keynote webinar | Spotlight on medication adherence

Springer Medicine

Abstract

Purpose

Methods

Results

Conclusion

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