Allosteric modulators of group I metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives.

@article{Gasparini2002AllostericMO,
  title={Allosteric modulators of group I metabotropic glutamate receptors: novel subtype-selective ligands and therapeutic perspectives.},
  author={Fabrizio Gasparini and Rainer Kuhn and Jean-Philippe Pin},
  journal={Current opinion in pharmacology},
  year={2002},
  volume={2 1},
  pages={43-9}
}
Recent drug discovery programs aimed at identifying selective metabotropic mGlu receptor ligands by high-throughput functional screening efforts have revealed subtype-selective allosteric modulators of mGlu1 and mGlu5 receptors that are structurally unrelated to glutamate. In contrast to competitive ligands, which bind to the glutamate binding site located in the large N-terminal extracellular domain, these modulators act as non-competitive antagonists, inverse agonists or positive modulators… CONTINUE READING