Forskning ved Københavns Universitet - Københavns Universitet

Forside

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

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

  • 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.
OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry Letters
Vol/bind18
Udgave nummer21
Sider (fra-til)5713-5716
ISSN0960-894X
DOI
StatusUdgivet - 2008

ID: 10161029