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XB-ART-1117
J Med Chem 2005 Nov 17;4823:7089-92. doi: 10.1021/jm058034a.
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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: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.

Carling RW , Madin A , Guiblin A , Russell MG , Moore KW , Mitchinson A , Sohal B , Pike A , Cook SM , Ragan IC , McKernan RM , Quirk K , Ferris P , Marshall G , Thompson SA , Wafford KA , Dawson GR , Atack JR , Harrison T , Castro JL , Street LJ .


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There is increasing evidence that compounds with selectivity for gamma-aminobutyric acid(A) (GABA(A)) alpha2- and/or alpha3-subtypes may retain the desirable anxiolytic activity of nonselective benzodiazepines but possess an improved side effect profile. Herein we describe a novel series of GABA(A) alpha2/alpha3 subtype-selective agonists leading to the identification of the development candidate 17, a nonsedating anxiolytic in preclinical animal assays.

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???displayArticle.link??? J Med Chem