TY - JOUR
T1 - Imaging for metabotropic glutamate receptor subtype 1 in rat and monkey brains using PET with [ 18F]FITM
AU - Yamasaki, Tomoteru
AU - Fujinaga, Masayuki
AU - Maeda, Jun
AU - Kawamura, Kazunori
AU - Yui, Joji
AU - Hatori, Akiko
AU - Yoshida, Yuichiro
AU - Nagai, Yuji
AU - Tokunaga, Masaki
AU - Higuchi, Makoto
AU - Suhara, Tetsuya
AU - Fukumura, Toshimitsu
AU - Zhang, Ming Rong
PY - 2012/4
Y1 - 2012/4
N2 - Purpose In this study, we evaluate the utility of 4-[ 18F]fluoro- N-[4-[6-(isopropylamino) pyrimidin-4-yl]-1,3-thiazol-2-yl]-Nmethylbenzamide ([ 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.
AB - Purpose In this study, we evaluate the utility of 4-[ 18F]fluoro- N-[4-[6-(isopropylamino) pyrimidin-4-yl]-1,3-thiazol-2-yl]-Nmethylbenzamide ([ 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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U2 - 10.1007/s00259-011-1995-6
DO - 10.1007/s00259-011-1995-6
M3 - Article
C2 - 22113620
AN - SCOPUS:84862518776
SN - 1619-7070
VL - 39
SP - 632
EP - 641
JO - European Journal of Nuclear Medicine and Molecular Imaging
JF - European Journal of Nuclear Medicine and Molecular Imaging
IS - 4
ER -