Basic Information
ID: ALA1629416
Journal: Bioorg Med Chem
Title: Developing dual functional allosteric modulators of GABA(A) receptors.
Authors: Liu XF, Chang HF, Schmiesing RJ, Wesolowski SS, Knappenberger KS, Arriza JL, Chapdelaine MJ.
Abstract: Positive modulators at benzodiazepine sites of α2- and α3-containing GABA(A) receptors are believed to be anxiolytic. Negative allosteric modulators of α5-containing GABA(A) receptors enhance cognition. By oocyte two-electrode voltage clamp and subsequent structure-activity relationship studies, we discovered cinnoline and quinoline derivatives that were both positive modulators at α2-/α3-containing GABA(A) receptors and negative modulators at α5-containing GABA(A) receptors. In addition, these compounds showed no functional activity at α1-containing GABA(A) receptors. Such dual functional modulators of GABA(A) receptors might be useful for treating comorbidity of anxiety and cognitive impairments in neurological and psychiatric illnesses.
CiteXplore: 20980155
DOI: 10.1016/j.bmc.2010.09.058
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets