Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABAA receptor α1 subtype

@article{McKernan2000SedativeBN,
  title={Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABAA receptor $\alpha$1 subtype},
  author={R M McKernan and Thomas W. Rosahl and David S. Reynolds and Cyrille Sur and K. A. Wafford and J. R. Atack and Sophie J. Farrar and Janice Myers and Gina P Cook and Pushpinder Ferris and L. Garrett and L J Bristow and George R. Marshall and Alison J. Macaulay and N A Brown and Owain Howell and Kevin W. Moore and Robert W. Carling and L Street and Jos{\'e} L. Castro and C. Ian Ragan and G. R. Dawson and P J Whiting},
  journal={Nature Neuroscience},
  year={2000},
  volume={3},
  pages={587-592}
}
Inhibitory neurotransmission in the brain is largely mediated by GABAA receptors. Potentiation of GABA receptor activation through an allosteric benzodiazepine (BZ) site produces the sedative, anxiolytic, muscle relaxant, anticonvulsant and cognition-impairing effects of clinically used BZs such as diazepam. We created genetically modified mice (α1 H101R) with a diazepam-insensitive α1 subtype and a selective BZ site ligand, L-838,417, to explore GABAA receptor subtypes mediating specific… 

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Selective anxiolysis produced by ocinaplon, a GABA(A) receptor modulator.

  • A. LippaP. Czobor P. Skolnick
  • Psychology, Biology
    Proceedings of the National Academy of Sciences of the United States of America
  • 2005
It is reported that the pyrazolo[1,5-a]-pyrimidine, ocinaplon, exhibits an anxioselective profile in both preclinical procedures and in patients with generalized anxiety disorder, the most common of the anxiety disorders.

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It may be possible to develop effective anxiolytic compounds that have a much reduced side-effect profile compared with existing drugs, according to the phenotypic analysis of transgenic knock-in and knock-out mice.
...

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