Identification of novel positive allosteric modulators and null modulators at the GABA A receptor α+β− interface
British Journal of Pharmacology2013Vol. 169(2), pp. 371–383
Citations Over TimeTop 23% of 2013 papers
Zdravko Varagić, Laurin Wimmer, Michael Schnürch, Marko D. Mihovilovič, Shengming Huang, Sundari Rallapalli, James M. Cook, Pantea Mirheydari, Gerhard F. Ecker, Werner Sieghart, Margot Ernst
Abstract
Pyrazoloquinolinones and pyrazolopyridinones represent the first prototype of drug candidates mediating benzodiazepine like modulatory effects via the α+β-interface of GABAA receptors. The discovery of null modulators acting as inhibitors of the plus modulators provides a highly useful tool for the discovery of additional classes of compounds that can modulate GABAA receptors via this site, which may lead to novel therapeutic principles.
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