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)alph 2/alpha 3-Subtype Selective Agonist That Exhibits Potent Anxiolytic Activ

摘要

There is increasing evidence that compounds with selectivity for gamma-aminobutyric acidA(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.