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Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor

By Samuel Hintermann, Konstanze Hurth, Joachim Nozulak, Marina Tintelnot-Blomley, Reiner Aichholz, Joachim Blanz, Klemens Kaupmann and Johannes Mosbacher


A novel series of agonists at the benzodiazepine binding site of the GABAA receptor was prepared by functionalizing a known template. Adding substituents to the pyrazolone-oxygen of CGS-9896 led to a number of compounds with selectivities for either α2- or α1-containing GABAA receptor subtypes offering an entry into indications such as anxiety and insomnia. In this communication, structure-activity relationship and efforts to increase in vitro stabilities are discussed

Publisher: Elsevier
Year: 2010
DOI identifier: 10.1016/j.bmcl.2010.12.107
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