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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.
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author
; ; ; and
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
  • pmid:18851913
ISSN
0960-894X
DOI
10.1016/j.bmcl.2008.09.092
language
English
LU publication?
yes
additional info
The information about affiliations in this record was updated in December 2015. The record was previously connected to the following departments: Organic chemistry (S/LTH) (011001240)
id
18ffec1a-5541-4036-84fa-5cd21d6d84d8 (old id 1262278)
date added to LUP
2016-04-01 13:50:42
date last changed
2022-01-27 21:27:11
@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         = {{0960-894X}},
  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}},
  doi          = {{10.1016/j.bmcl.2008.09.092}},
  volume       = {{18}},
  year         = {{2008}},
}