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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6,3'-dibromoflavone and 6-nitro-3'-bromoflavone: new additions to the 6,3'-disubstituted flavone family of high-affinity ligands of the brain benzodiazepine binding site with agonistic properties.
TLDR
These synthetic flavone derivatives join an existing family of 6,3'-disubstituted flavone compounds with high affinity for the benzodiazepine binding site and partial agonistic profiles.
Behavioral effects of 6-bromoflavanone and 5-methoxy-6,8-dibromoflavanone as anxiolytic compounds
5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic properties.
Molecular modeling and QSAR analysis of the interaction of flavone derivatives with the benzodiazepine binding site of the GABA(A) receptor complex.
Flavonoids as GABAA receptor ligands: the whole story?
TLDR
Flavonoids are prominent drugs in the treatment of mental disorders, and can also be used as tools to study modulatory sites at GABA type A receptors and to develop GABAtype A selective agents further.
Antitumor activity of some natural flavonoids and synthetic derivatives on various human and murine cancer cell lines.

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6-Bromoflavone, a high affinity ligand for the central benzodiazepine receptors is a member of a family of active flavonoids.
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TLDR
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