ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization.

@article{Kalinichev2013ADX71743AP,
  title={ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization.},
  author={Mikhail Kalinichev and M{\'e}lanie Rouillier and Françoise Girard and Isabelle Royer-Urios and Bruno Bournique and Terry Finn and Delphine Charvin and Brice Campo and Emmanuel Le Poul and Vincent Mutel and Sonia Maria Poli and Stuart A Neale and Thomas E. Salt and Robert L{\"u}tjens},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2013},
  volume={344 3},
  pages={624-36}
}
Metabotropic glutamate receptor 7 (mGlu(7)) has been suggested to be a promising novel target for treatment of a range of disorders, including anxiety, post-traumatic stress disorder, depression, drug abuse, and schizophrenia. Here we characterized a potent and selective mGlu(7) negative allosteric modulator (NAM) (+)-6-(2,4-dimethylphenyl)-2-ethyl-6,7-dihydrobenzo[d]oxazol-4(5H)-one (ADX71743). In vitro, Schild plot analysis and reversibility tests at the target confirmed the NAM properties of… CONTINUE READING
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Development of a cAMP BRET cellular HTS assay to characterize pharmacological properties of mGlu 7 ligands

  • R Lütjens, M Becker, +7 authors D Charvin
  • Poster presented at the Annual Meeting of the…
  • 2010
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