Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABAA receptors

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

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

Harvard

Nilsson, J, Nielsen, EØ, Liljefors, T, Nielsen, MPC & Sterner, O 2008, 'Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABAA receptors', Bioorganic & Medicinal Chemistry Letters, vol. 18, no. 21, pp. 5713-5716. https://doi.org/10.1016/j.bmcl.2008.09.092

APA

Nilsson, J., Nielsen, E. Ø., Liljefors, T., Nielsen, M. P. C., & Sterner, O. (2008). Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABAA receptors. Bioorganic & Medicinal Chemistry Letters, 18(21), 5713-5716. https://doi.org/10.1016/j.bmcl.2008.09.092

Vancouver

Nilsson J, Nielsen EØ, Liljefors T, Nielsen MPC, Sterner O. Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABAA receptors. Bioorganic & Medicinal Chemistry Letters. 2008;18(21):5713-5716. https://doi.org/10.1016/j.bmcl.2008.09.092

Author

Nilsson, Jakob ; Nielsen, Elsebet Østergaard ; Liljefors, Tommy ; Nielsen, Mogens Peter Cherly ; Sterner, Olov. / Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABAA receptors. In: Bioorganic & Medicinal Chemistry Letters. 2008 ; Vol. 18, No. 21. pp. 5713-5716.

Bibtex

@article{2e30a9f0f43811ddbf70000ea68e967b,
title = "Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABAA receptors",
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.",
keywords = "Former Faculty of Pharmaceutical Sciences",
author = "Jakob Nilsson and Nielsen, {Elsebet {\O}stergaard} and Tommy Liljefors and Nielsen, {Mogens Peter Cherly} and Olov Sterner",
note = "Keywords: Flavone; Azaflavone; GABA(A); Benzodiazepine binding site",
year = "2008",
doi = "10.1016/j.bmcl.2008.09.092",
language = "English",
volume = "18",
pages = "5713--5716",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Pergamon Press",
number = "21",

}

RIS

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