Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABAA receptors

Research output: Contribution to journalJournal articleResearchpeer-review

  • Jakob Nilsson
  • Elsebet Østergaard Nielsen
  • Tommy Liljefors
  • Mogens Peter Cherly Nielsen
  • Olov Sterner
A series of azaflavone derivatives and analogues were prepared and evaluated for their affinity to the benzodiazepine binding site of the GABA(A) receptor, and compared to their flavone counterparts. Three of the compounds, the azaflavones 9 and 12 as well as the new flavone 13, were also assayed on GABA(A) receptor subtypes (alpha(1)beta(3)gamma(2s), alpha(2)beta(3)gamma(2s), alpha(4)beta(3)gamma(2s) and alpha(5)beta(3)gamma(2s)), displaying nanomolar affinities as well as selectivity for alpha1- versus alpha2- and alpha3-containing receptors by a factor of between 14 and 26.
Original languageEnglish
JournalBioorganic & Medicinal Chemistry Letters
Issue number21
Pages (from-to)5713-5716
Publication statusPublished - 2008

Bibliographical note

Keywords: Flavone; Azaflavone; GABA(A); Benzodiazepine binding site

ID: 10161029