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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 |
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| Authors: | Hintermann Samuel Hurth Konstanze Nozulak Joachim Tintelnot-Blomley Marina Aichholz Reiner Blanz Joachim Kaupmann Klemens Mosbacher Johannes |
| Affiliation: | a Novartis Institutes for BioMedical Research, Neuroscience Research, CH-4002 Basel, Switzerland b Novartis Institutes for BioMedical Research, Metabolism and Pharmacokinetics, CH-4002 Basel, Switzerland |
| Abstract: | 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. |
| Keywords: | GABAA ligands Subtype selectivity Metabolic stability |
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