Correlation of receptor occupancy of metabotropic glutamate receptor subtype 1 (mGluR1) in mouse brain with in vivo activity of allosteric mGluR1 antagonists.

@article{Suzuki2009CorrelationOR,
  title={Correlation of receptor occupancy of metabotropic glutamate receptor subtype 1 (mGluR1) in mouse brain with in vivo activity of allosteric mGluR1 antagonists.},
  author={Gentaroh Suzuki and Hiroko Kawagoe-Takaki and Takao Inoue and Toshifumi Kimura and Hirohiko Hikichi and Takashi Murai and Akio Satow and Mikiko Hata and Shunsuke Maehara and Satoru Ito and Hiroshi Kawamoto and Satoshi Ozaki and Hisashi Ohta},
  journal={Journal of pharmacological sciences},
  year={2009},
  volume={110 3},
  pages={
          315-25
        }
}
The aim of this study was to clarify the relationship between receptor occupancy and in vivo pharmacological activity of mGluR1 antagonists. The tritiated mGluR1-selective allosteric antagonist [(3)H]FTIDC (4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide) was identified as a radioligand having high affinity for mGluR1-expressing CHO cells (K(D) = 2.1 nM) and mouse cerebellum (K(D) = 3.7 nM). [(3)H]FTIDC bound to mGluR1 was… 

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