An Inverse Agonist Selective for α5 Subunit-Containing GABAA Receptors Enhances Cognition

@article{Dawson2006AnIA,
  title={An Inverse Agonist Selective for $\alpha$5 Subunit-Containing GABAA Receptors Enhances Cognition},
  author={Gerard R Dawson and Karen A. Maubach and Neil Collinson and Matthew R D Cobain and Barry J. Everitt and Angus Murray Macleod and Hedaythul I Choudhury and Louise M. McDonald and Goplan V Pillai and W. Stanley Rycroft and Alison J. Smith and Francine Sternfeld and F. David Tattersall and Keith A. Wafford and David S. Reynolds and Guy R. Seabrook and J. R. Atack},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2006},
  volume={316},
  pages={1335 - 1345}
}
  • G. Dawson, K. Maubach, +14 authors J. Atack
  • Published 1 March 2006
  • Chemistry, Medicine
  • Journal of Pharmacology and Experimental Therapeutics
α5IA is a compound that binds with equivalent subnanomolar affinity to the benzodiazepine (BZ) site of GABAA receptors containing an α1, α2, α3, or α5 subunit but has inverse agonist efficacy selective for the α5 subtype. As a consequence, the in vitro and in vivo effects of this compound are mediated primarily via GABAA receptors containing an α5 subunit. In a mouse hippocampal slice model, α5IA significantly enhanced the θ burst-induced long-term potentiation of the excitatory postsynaptic… Expand
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