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Inhibition of [methyl-3H]diazepam binding to rat brain membranes in vitro by dinatin and skrofulein

Shen, X L; Nielsen, M; Witt, M R; Sterner, Olov LU ; Bergendorff, Ola LU and Khayyal, M (1994) In Zhongguo Yaoli Xuebao (China) 1980-01-01+01:002000-01-01+01:00 15(5). p.385-388
Abstract
Two flavones, 4',5,7-trihydroxy-6-methoxy flavone (dinatin) and 4',5-dihydroxy-6, 7-dimethoxy flavone (skrofulein), were extracted from Artemisia herba alba L. Dinatin and skrofulein inhibited the binding of [methyl-3H]diazepam to rat brain membranes in vitro with IC50 of 1.3 and 23 mumol.L-1, respectively. The GABA-ratios (the ratio of IC50 values in the absence/presence of GABA in the binding assay) were 1.1 and 1.2 for dinatin and skrofulein, respectively. Both flavones induced a slight increase in [35S] TBPS binding. The data suggest that the flavones are antagonists or partial agonists of benzodiazepine receptors.
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Zhongguo Yaoli Xuebao (China) 1980-01-01+01:002000-01-01+01:00
volume
15
issue
5
pages
385 - 388
publisher
Nature Publishing Group
external identifiers
  • pmid:7717057
  • scopus:0028024756
ISSN
0253-9756
language
English
LU publication?
yes
id
686438fe-2b43-43f3-bf5d-c3667f8648b7 (old id 1108261)
date added to LUP
2008-07-23 16:19:31
date last changed
2017-01-01 06:47:01
@article{686438fe-2b43-43f3-bf5d-c3667f8648b7,
  abstract     = {Two flavones, 4',5,7-trihydroxy-6-methoxy flavone (dinatin) and 4',5-dihydroxy-6, 7-dimethoxy flavone (skrofulein), were extracted from Artemisia herba alba L. Dinatin and skrofulein inhibited the binding of [methyl-3H]diazepam to rat brain membranes in vitro with IC50 of 1.3 and 23 mumol.L-1, respectively. The GABA-ratios (the ratio of IC50 values in the absence/presence of GABA in the binding assay) were 1.1 and 1.2 for dinatin and skrofulein, respectively. Both flavones induced a slight increase in [35S] TBPS binding. The data suggest that the flavones are antagonists or partial agonists of benzodiazepine receptors.},
  author       = {Shen, X L and Nielsen, M and Witt, M R and Sterner, Olov and Bergendorff, Ola and Khayyal, M},
  issn         = {0253-9756},
  language     = {eng},
  number       = {5},
  pages        = {385--388},
  publisher    = {Nature Publishing Group},
  series       = {Zhongguo Yaoli Xuebao (China) 1980-01-01+01:002000-01-01+01:00},
  title        = {Inhibition of [methyl-3H]diazepam binding to rat brain membranes in vitro by dinatin and skrofulein},
  volume       = {15},
  year         = {1994},
}