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Towards functional selectivity for α6β3γ2 GABAA receptors: a series of novel pyrazoloquinolinones.

Marco TrevenDavid C B SiebertRaphael HolzingerKonstantina BampaliJure FabjanZdravko VaragicLaurin WimmerFriederike SteudlePetra ScholzeMichael SchnürchMarko D MihovilovicMargot Ernst
Published in: British journal of pharmacology (2017)
These results constitute a major step towards a potential selective positive modulation of certain α6-containing GABAA receptors, which might be useful to elicit their physiological role. Furthermore, these studies pave the way towards insights into molecular principles that drive positive versus negative allosteric modulation of specific GABAA receptor isoforms.
Keyphrases
  • small molecule
  • risk assessment