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

  title={An Inverse Agonist Selective for α5 Subunit-Containing GABAA Receptors Enhances Cognition},
  author={G. R. Dawson and K. Maubach and N. Collinson and M. Cobain and B. Everitt and A. Macleod and H. Choudhury and L. McDonald and G. Pillai and W. Rycroft and A. Smith and F. Sternfeld and F. Tattersall and K. Wafford and D. Reynolds and G. Seabrook and J. Atack},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  pages={1335 - 1345}
  • G. R. Dawson, K. Maubach, +14 authors J. Atack
  • Published 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… CONTINUE READING
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