Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.

@article{Lindsley2004DiscoveryOP,
  title={Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.},
  author={Craig W Lindsley and David D. Wisnoski and William H. Leister and Julie A O'brien and Wei Lemaire and David L Williams and Maryann Burno and Cyrille Sur and Gene G. Kinney and Doug J Pettibone and Philip R. Tiller and Sheri Lee Smith and Mark E. Duggan and George D. Hartman and P Jeffrey Conn and Joel R. Huff},
  journal={Journal of medicinal chemistry},
  year={2004},
  volume={47 24},
  pages={
          5825-8
        }
}
  • Craig W Lindsley, David D. Wisnoski, +13 authors Joel R. Huff
  • Published in
    Journal of medicinal…
    2004
  • Chemistry, Medicine
  • This report describes the discovery of the first centrally active allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5). Appropriately substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides (e.g., 8) have been identified as a novel class of potent positive allosteric modulators of mGluR5 that potentiate the response to glutamate. An iterative analogue library synthesis approach provided potentiators with excellent potency and selectivity for mGluR5 (vs mGluRs 1-4, 7, 8… CONTINUE READING

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