Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABAA receptors
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Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABAA receptors. / Nilsson, Jakob; Nielsen, Elsebet Østergaard; Liljefors, Tommy; Nielsen, Mogens Peter Cherly; Sterner, Olov.
In: Bioorganic & Medicinal Chemistry Letters, Vol. 18, No. 21, 2008, p. 5713-5716.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABAA receptors
AU - Nilsson, Jakob
AU - Nielsen, Elsebet Østergaard
AU - Liljefors, Tommy
AU - Nielsen, Mogens Peter Cherly
AU - Sterner, Olov
N1 - Keywords: Flavone; Azaflavone; GABA(A); Benzodiazepine binding site
PY - 2008
Y1 - 2008
N2 - 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.
AB - 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.
KW - Former Faculty of Pharmaceutical Sciences
U2 - 10.1016/j.bmcl.2008.09.092
DO - 10.1016/j.bmcl.2008.09.092
M3 - Journal article
C2 - 18851913
VL - 18
SP - 5713
EP - 5716
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
SN - 0960-894X
IS - 21
ER -
ID: 10161029