The Non-competitive Antagonists 2-Methyl-6-(phenylethynyl)pyridine and 7-Hydroxyiminocyclopropan[b]chromen-1a-carboxylic Acid Ethyl Ester Interact with Overlapping Binding Pockets in the Transmembrane Region of Group I Metabotropic Glutamate Receptors*

@article{Pagano2000TheNA,
  title={The Non-competitive Antagonists 2-Methyl-6-(phenylethynyl)pyridine and 7-Hydroxyiminocyclopropan[b]chromen-1a-carboxylic Acid Ethyl Ester Interact with Overlapping Binding Pockets in the Transmembrane Region of Group I Metabotropic Glutamate Receptors*},
  author={A. Pagano and D. Rüegg and S. Litschig and N. Stoehr and C. Stierlin and M. Heinrich and P. Floersheim and L. Prézeau and F. Carroll and J. Pin and A. Cambria and I. Vranesic and P. Flor and F. Gasparini and R. Kuhn},
  journal={The Journal of Biological Chemistry},
  year={2000},
  volume={275},
  pages={33750 - 33758}
}
We have investigated the mechanism of inhibition and site of action of the novel human metabotropic glutamate receptor 5 (hmGluR5) antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP), which is structurally unrelated to classical metabotropic glutamate receptor (mGluR) ligands. Schild analysis indicated that MPEP acts in a non-competitive manner. MPEP also inhibited to a large extent constitutive receptor activity in cells transiently overexpressing rat mGluR5, suggesting that MPEP acts as an… Expand
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