Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one.

@article{Fukuda2009IdentificationOA,
  title={Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one.},
  author={Junko Fukuda and Gentaroh Suzuki and Toshifumi Kimura and Yasushi Nagatomi and Satoru Ito and Hiroshi Kawamoto and Satoshi Ozaki and Hisashi Ohta},
  journal={Neuropharmacology},
  year={2009},
  volume={57 4},
  pages={438-45}
}
Currently tested allosteric modulators for metabotropic glutamate receptor 1 (mGluR1) are known to regulate the activity of mGluR1 mainly through transmembrane (TM) domain 6 and/or 7. We identified a novel interaction site, N760 in TM5, which negatively regulates activation of mGluR1 with a newly discovered selective mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one (CFMMC). CFMMC inhibited L-glutamate-induced intracellular Ca(2+) mobilization ([Ca(2… CONTINUE READING

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