Menu

Javascript is not activated in your browser. This website needs javascript activated to work properly.
You are here

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

Author:
  • Jakob Nilsson
  • Elsebet Østergaard Nielsen
  • Tommy Liljefors
  • Mogens Nielsen
  • Olov Sterner
Publishing year: 2008
Language: English
Pages: 5713-5716
Publication/Series: Bioorganic & Medicinal Chemistry Letters
Volume: 18
Issue: 21
Document type: Journal article
Publisher: Elsevier

Abstract 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.

Keywords

  • Organic Chemistry

Other

Published
  • ISSN: 1090-2120
Olov Sterner
E-mail: olov.sterner [at] science.lu.se

Dean

Faculty of Science

+46 46 222 82 13

+46 70 530 66 49

B127

Sölvegatan 27, Lund

39

Professor

Centre for Analysis and Synthesis

+46 46 222 82 13

1