Document Report Card
Basic Information
ID: ALA1681636
Journal: Bioorg Med Chem Lett
Title: Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.
Authors: Hintermann S, Hurth K, Nozulak J, Tintelnot-Blomley M, Aichholz R, Blanz J, Kaupmann K, Mosbacher J.
Abstract: A novel series of agonists at the benzodiazepine binding site of the GABA(A) 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 GABA(A) 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.
CiteXplore: 21277199