GABAA receptor subtype-selective modulators. I. α2/α3-selective agonists as non-sedating anxiolytics.

@article{Atack2011GABAARS,
  title={GABAA receptor subtype-selective modulators. I. $\alpha$2/$\alpha$3-selective agonists as non-sedating anxiolytics.},
  author={J. Atack},
  journal={Current topics in medicinal chemistry},
  year={2011},
  volume={11 9},
  pages={
          1176-202
        }
}
  • J. Atack
  • Published 2011
  • Chemistry, Medicine
  • Current topics in medicinal chemistry
The prototypic benzodiazepines, such as diazepam, are not only anxiolytic but also produce sedation. These effects are mediated by GABA(A) receptors containing either an α1, α2, α3 or α5 subunit at which the positive modulatory effects (i.e., agonist efficacy) of benzodiazepines are mediated via a specific benzodiazepine recognition site. Recent molecular genetic and pharmacological data point to α1-containing GABA(A) receptors as the "sedative" and α2- and/or α3-containing receptors as the… Expand
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