TPA023 [7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an Agonist Selective for α2- and α3-Containing GABAA Receptors, Is a Nonsedating Anxiolytic in Rodents and Primates

@article{Atack2006TPA023A,
  title={TPA023 [7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine], an Agonist Selective for $\alpha$2- and $\alpha$3-Containing GABAA Receptors, Is a Nonsedating Anxiolytic in Rodents and Primates},
  author={J. Atack and K. Wafford and S. Tye and S. Cook and B. Sohal and A. Pike and C. Sur and D. Melillo and L. Bristow and F. Bromidge and I. Ragan and J. Kerby and L. Street and R. Carling and J. Castro and P. Whiting and G. Dawson and R. Mckernan},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2006},
  volume={316},
  pages={410 - 422}
}
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023) is a triazolopyridazine that binds with equivalent high (subnanomolar) affinity to the benzodiazepine binding site of recombinant human GABAA receptors containing an α1, α2, α3, or α5 subunit but has partial agonist efficacy at the α2 and α3 subtypes and essentially antagonist efficacy at the α1 and α5 subtypes. In rats, TPA023 gave time- and dose-dependent occupancy after… Expand

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