Abstract
In this study, we evaluate the utility of 4-[{sup 18}F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([{sup 18}F]FITM) as a positron emission tomography (PET) ligand for imaging of the metabotropic glutamate receptor subtype 1 (mGluR1) in rat and monkey brains. In vivo distribution of [{sup 18}F]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. 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{sub T}) was detected in the cerebellum (V{sub T} = 11.5). [{sup 18}F ]FITM has an excellent profile as a PET ligand for mGluR1 imaging. PET with [{sup 18}F ]FITM may prove useful for determining the regional distribution and density of mGluR1 and the mGluR1 occupancy of drugs in human brains. (orig.)
Yamasaki, Tomoteru;
[1]
Tohoku University, Graduate School of Pharmaceutical Sciences, Sendai (Japan)];
Fujinaga, Masayuki;
Maeda, Jun;
Kawamura, Kazunori;
Yui, Joji;
Hatori, Akiko;
Nagai, Yuji;
Tokunaga, Masaki;
Higuchi, Makoto;
Suhara, Tetsuya;
Fukumura, Toshimitsu;
[1]
Yoshida, Yuichiro;
[2]
Zhang, Ming-Rong;
[1]
National Institute of Radiological Sciences, Department of Molecular Probes, Molecular Imaging Centre, Chiba (Japan)]
- National Institute of Radiological Sciences, Molecular Imaging Centre, Chiba (Japan)
- SHI Accelerator Service Co. Ltd., Tokyo (Japan)
Citation Formats
Yamasaki, Tomoteru, Tohoku University, Graduate School of Pharmaceutical Sciences, Sendai (Japan)], Fujinaga, Masayuki, Maeda, Jun, Kawamura, Kazunori, Yui, Joji, Hatori, Akiko, Nagai, Yuji, Tokunaga, Masaki, Higuchi, Makoto, Suhara, Tetsuya, Fukumura, Toshimitsu, Yoshida, Yuichiro, Zhang, Ming-Rong, and National Institute of Radiological Sciences, Department of Molecular Probes, Molecular Imaging Centre, Chiba (Japan)].
Imaging for metabotropic glutamate receptor subtype 1 in rat and monkey brains using PET with [{sup 18}F]FITM.
Germany: N. p.,
2012.
Web.
doi:10.1007/S00259-011-1995-6.
Yamasaki, Tomoteru, Tohoku University, Graduate School of Pharmaceutical Sciences, Sendai (Japan)], Fujinaga, Masayuki, Maeda, Jun, Kawamura, Kazunori, Yui, Joji, Hatori, Akiko, Nagai, Yuji, Tokunaga, Masaki, Higuchi, Makoto, Suhara, Tetsuya, Fukumura, Toshimitsu, Yoshida, Yuichiro, Zhang, Ming-Rong, & National Institute of Radiological Sciences, Department of Molecular Probes, Molecular Imaging Centre, Chiba (Japan)].
Imaging for metabotropic glutamate receptor subtype 1 in rat and monkey brains using PET with [{sup 18}F]FITM.
Germany.
https://doi.org/10.1007/S00259-011-1995-6
Yamasaki, Tomoteru, Tohoku University, Graduate School of Pharmaceutical Sciences, Sendai (Japan)], Fujinaga, Masayuki, Maeda, Jun, Kawamura, Kazunori, Yui, Joji, Hatori, Akiko, Nagai, Yuji, Tokunaga, Masaki, Higuchi, Makoto, Suhara, Tetsuya, Fukumura, Toshimitsu, Yoshida, Yuichiro, Zhang, Ming-Rong, and National Institute of Radiological Sciences, Department of Molecular Probes, Molecular Imaging Centre, Chiba (Japan)].
2012.
"Imaging for metabotropic glutamate receptor subtype 1 in rat and monkey brains using PET with [{sup 18}F]FITM."
Germany.
https://doi.org/10.1007/S00259-011-1995-6.
@misc{etde_21568775,
title = {Imaging for metabotropic glutamate receptor subtype 1 in rat and monkey brains using PET with [{sup 18}F]FITM}
author = {Yamasaki, Tomoteru, Tohoku University, Graduate School of Pharmaceutical Sciences, Sendai (Japan)], Fujinaga, Masayuki, Maeda, Jun, Kawamura, Kazunori, Yui, Joji, Hatori, Akiko, Nagai, Yuji, Tokunaga, Masaki, Higuchi, Makoto, Suhara, Tetsuya, Fukumura, Toshimitsu, Yoshida, Yuichiro, Zhang, Ming-Rong, and National Institute of Radiological Sciences, Department of Molecular Probes, Molecular Imaging Centre, Chiba (Japan)]}
abstractNote = {In this study, we evaluate the utility of 4-[{sup 18}F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([{sup 18}F]FITM) as a positron emission tomography (PET) ligand for imaging of the metabotropic glutamate receptor subtype 1 (mGluR1) in rat and monkey brains. In vivo distribution of [{sup 18}F]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. 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{sub T}) was detected in the cerebellum (V{sub T} = 11.5). [{sup 18}F ]FITM has an excellent profile as a PET ligand for mGluR1 imaging. PET with [{sup 18}F ]FITM may prove useful for determining the regional distribution and density of mGluR1 and the mGluR1 occupancy of drugs in human brains. (orig.)}
doi = {10.1007/S00259-011-1995-6}
journal = []
issue = {4}
volume = {39}
place = {Germany}
year = {2012}
month = {Apr}
}
title = {Imaging for metabotropic glutamate receptor subtype 1 in rat and monkey brains using PET with [{sup 18}F]FITM}
author = {Yamasaki, Tomoteru, Tohoku University, Graduate School of Pharmaceutical Sciences, Sendai (Japan)], Fujinaga, Masayuki, Maeda, Jun, Kawamura, Kazunori, Yui, Joji, Hatori, Akiko, Nagai, Yuji, Tokunaga, Masaki, Higuchi, Makoto, Suhara, Tetsuya, Fukumura, Toshimitsu, Yoshida, Yuichiro, Zhang, Ming-Rong, and National Institute of Radiological Sciences, Department of Molecular Probes, Molecular Imaging Centre, Chiba (Japan)]}
abstractNote = {In this study, we evaluate the utility of 4-[{sup 18}F]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([{sup 18}F]FITM) as a positron emission tomography (PET) ligand for imaging of the metabotropic glutamate receptor subtype 1 (mGluR1) in rat and monkey brains. In vivo distribution of [{sup 18}F]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. 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{sub T}) was detected in the cerebellum (V{sub T} = 11.5). [{sup 18}F ]FITM has an excellent profile as a PET ligand for mGluR1 imaging. PET with [{sup 18}F ]FITM may prove useful for determining the regional distribution and density of mGluR1 and the mGluR1 occupancy of drugs in human brains. (orig.)}
doi = {10.1007/S00259-011-1995-6}
journal = []
issue = {4}
volume = {39}
place = {Germany}
year = {2012}
month = {Apr}
}