The browser you are using is not supported by this website. All versions of Internet Explorer are no longer supported, either by us or Microsoft (read more here: https://www.microsoft.com/en-us/microsoft-365/windows/end-of-ie-support).

Please use a modern browser to fully experience our website, such as the newest versions of Edge, Chrome, Firefox or Safari etc.

Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABA(A) receptors.

På svenska

Author

  • Jakob Nilsson
  • Elsebet Østergaard Nielsen
  • Tommy Liljefors
  • Mogens Nielsen
  • Olov Sterner

Summary, in English

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.

Publishing year

2008

Language

English

Pages

5713-5716

Publication/Series

Bioorganic & Medicinal Chemistry Letters

Volume

18

Issue

21

Document type

Journal article

Publisher

Elsevier

Topic

  • Organic Chemistry

Status

Published

ISBN/ISSN/Other

  • ISSN: 0960-894X