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

Nilsson, Jakob LU ; Nielsen, Elsebet Østergaard; Liljefors, Tommy; Nielsen, Mogens and Sterner, Olov LU (2008) In Bioorganic & Medicinal Chemistry Letters 18(21). p.5713-5716
Abstract
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.
Please use this url to cite or link to this publication:
author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Bioorganic & Medicinal Chemistry Letters
volume
18
issue
21
pages
5713 - 5716
publisher
Elsevier
external identifiers
  • wos:000260227400001
  • pmid:18851913
  • scopus:53949112240
ISSN
1090-2120
DOI
10.1016/j.bmcl.2008.09.092
language
English
LU publication?
yes
id
18ffec1a-5541-4036-84fa-5cd21d6d84d8 (old id 1262278)
date added to LUP
2008-11-25 18:04:51
date last changed
2017-07-30 04:08:30
@article{18ffec1a-5541-4036-84fa-5cd21d6d84d8,
  abstract     = {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.},
  author       = {Nilsson, Jakob and Nielsen, Elsebet Østergaard and Liljefors, Tommy and Nielsen, Mogens and Sterner, Olov},
  issn         = {1090-2120},
  language     = {eng},
  number       = {21},
  pages        = {5713--5716},
  publisher    = {Elsevier},
  series       = {Bioorganic & Medicinal Chemistry Letters},
  title        = {Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABA(A) receptors.},
  url          = {http://dx.doi.org/10.1016/j.bmcl.2008.09.092},
  volume       = {18},
  year         = {2008},
}