6-Methyl-3'-bromoflavone, a high-affinity ligand for the benzodiazepine binding site of the GABA(A) receptor with some antagonistic properties.

@article{Viola19996Methyl3bromoflavoneAH,
  title={6-Methyl-3'-bromoflavone, a high-affinity ligand for the benzodiazepine binding site of the GABA(A) receptor with some antagonistic properties.},
  author={Hayd{\'e}e Viola and Mariel Marder and Jorge Nu{\~n}ez and Luciana A. Izquierdo and Cristina Wasowski and Claudia Wolfman and Patr{\'i}cia Grolli Ardenghi and D Barros and Jorge H. Medina and Alejandro C. Paladini},
  journal={Biochemical and biophysical research communications},
  year={1999},
  volume={262 3},
  pages={
          643-6
        }
}
  • H. Viola, M. Marder, A. Paladini
  • Published 7 September 1999
  • Biology, Psychology, Chemistry
  • Biochemical and biophysical research communications
6-Methyl-3'-bromoflavone inhibited [(3)H]flunitrazepam binding to the benzodiazepine binding site of the GABA(A) receptor (BDZ-bs) with Ki values between 10 and 50 nM in different brain regions. The GABA ratio of 1.03 for [(3)H]flunitrazepam binding to cerebral cortex, 0.76 for cerebellum, 0.7 for hippocampus, 0.7 for striatum, and 0.8 for spinal cord indicated an antagonistic or weak inverse agonistic profile of 6-methyl-3'-bromoflavone on BDZ-bs. Unlike classical benzodiazepines, it had no… 
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6‐Methylflavone, a benzodiazepine receptor ligand with antagonistic properties on rat brain and human recombinant GABAA receptors in vitro
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The modulation of GABA‐induced chloride currents by 6‐methylflavone suggests that the compound is an antagonist at human GABAA receptor subtypes, and some general structure–activity relationships are discussed.
Relationship between benzodiazepine receptor occupancy and potentiation of gamma-aminobutyric acid-stimulated chloride flux in vitro of four ligands of differing intrinsic efficacies.
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The rank order of relative intrinsic efficacy determined in this study was: triazolam congruent to diazepam much greater than Ro 19-8022 greater than bretazenil.
6-Bromoflavone, a high affinity ligand for the central benzodiazepine receptors is a member of a family of active flavonoids.
6-Bromoflavone, obtained by bromination of flavanone, binds to central benzodiazepine receptors with a Ki=70 nM and has a clear anxiolytic activity in mice, at 0.5 mg/kg i.p. A survey of the
Apigenin, a component of Matricaria recutita flowers, is a central benzodiazepine receptors-ligand with anxiolytic effects.
TLDR
It is demonstrated that apigenin is a ligand for the central benzodiazepine receptors exerting anxiolytic and slight sedative effects but not being anticonvulsant or myorelaxant.
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