Article thumbnail

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

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

Publisher: Elsevier
Year: 2010
DOI identifier: 10.1016/j.bmcl.2010.12.107
OAI identifier: oai:oak.novartis.com:3677
Download PDF:
Sorry, we are unable to provide the full text but you may find it at the following location(s):
  • https://oak.novartis.com/3677/ (external link)
  • Suggested articles


    To submit an update or takedown request for this paper, please submit an Update/Correction/Removal Request.