942436-93-3Relevant articles and documents
Development and SAR of functionally selective allosteric modulators of GABAA receptors
Alhambra, Cristobal,Becker, Chris,Blake, Timothy,Chang, Amy,Damewood Jr., James R.,Daniels, Thalia,Dembofsky, Bruce T.,Gurley, David A.,Hall, James E.,Herzog, Keith J.,Horchler, Carey L.,Ohnmacht, Cyrus J.,Schmiesing, Richard Jon,Dudley, Adam,Ribadeneira, Maria D.,Knappenberger, Katherine S.,MacIag, Carla,Stein, Mark M.,Chopra, Maninder,Liu, Xiaodong F.,Christian, Edward P.,Arriza, Jeffrey L.,Chapdelaine, Marc J.
, p. 2927 - 2938 (2011/06/21)
Positive modulators at the benzodiazepine site of α2- and α3-containing GABAA receptors are believed to be anxiolytic. Through oocyte voltage clamp studies, we have discovered two series of compounds that are positive modulators at α2-/α3-containing GABAA receptors and that show no functional activity at α1-containing GABA A receptors. We report studies to improve this functional selectivity and ultimately deliver clinical candidates. The functional SAR of cinnolines and quinolines that are positive allosteric modulators of the α2- and α3-containing GABAA receptors, while simultaneously neutral antagonists at α1-containing GABAA receptors, is described. Such functionally selective modulators of GABAA receptors are expected to be useful in the treatment of anxiety and other psychiatric illnesses.
Compounds and Uses Thereof
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Page/Page column 30; 90-91, (2008/06/13)
This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of anxiety disorders, cognitive disorders, and/or mood disorders.
