An inverse agonist selective for alpha5 subunit-containing GABAA receptors enhances cognition.

@article{Dawson2006AnIA,
  title={An inverse agonist selective for alpha5 subunit-containing GABAA receptors enhances cognition.},
  author={G. R. Dawson and Karen A Maubach and Neil Collinson and M. R. D. Cobain and Barry J. Everitt and Angus M Macleod and Hedaythul I Choudhury and Louise M McDonald and G. Rajasekharan Pillai and Wayne Rycroft and Alison J. Smith and Francine Sternfeld and Frederick D Tattersall and Keith A Wafford and David W. Reynolds and Guy R. Seabrook and John R. Atack},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2006},
  volume={316 3},
  pages={1335-45}
}
Alpha5IA is a compound that binds with equivalent subnanomolar affinity to the benzodiazepine (BZ) site of GABA(A) receptors containing an alpha1, alpha2, alpha3, or alpha5 subunit but has inverse agonist efficacy selective for the alpha5 subtype. As a consequence, the in vitro and in vivo effects of this compound are mediated primarily via GABA(A) receptors containing an alpha5 subunit. In a mouse hippocampal slice model, alpha5IA significantly enhanced the burst-induced long-term potentiation… CONTINUE READING
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