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={H. Viola and M. Marder and J. Nunez and L. Izquierdo and C. Wasowski and C. Wolfman and P. Ardenghi and D. Barros and J. Medina and A. Paladini},
  journal={Biochemical and biophysical research communications},
  year={1999},
  volume={262 3},
  pages={
          643-6
        }
}
  • H. Viola, M. Marder, +7 authors A. Paladini
  • Published 1999
  • Biology, Medicine
  • 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… CONTINUE READING
    View on PubMed
    doi.org
    6 Citations
    Background Citations
    2
    6 Citations
    Citation Type

    Citation Type

    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.
    • 16
    Behavioral effects of 6-bromoflavanone and 5-methoxy-6,8-dibromoflavanone as anxiolytic compounds
    • 33
    5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic properties.
    • 76
    Molecular modeling and QSAR analysis of the interaction of flavone derivatives with the benzodiazepine binding site of the GABA(A) receptor complex.
    • 69
    Flavonoids as GABAA receptor ligands: the whole story?
    • 52
    • PDF
    Antitumor activity of some natural flavonoids and synthetic derivatives on various human and murine cancer cell lines.
    • 199

    References

    SHOWING 1-10 OF 17 REFERENCES
    Anxioselective properties of 6,3'-dinitroflavone, a high-affinity benzodiazepine receptor ligand.
    • 66
    Pharmacological Characterization of 6-Bromo-3′-nitroflavone, a Synthetic Flavonoid with High Affinity for the Benzodiazepine Receptors
    • 18
    6-Bromo-3′-nitroflavone, a new high affinity benzodiazepine receptor agonist recognizes two populations of cerebral cortical binding sites
    • 19
    6‐Methylflavone, a benzodiazepine receptor ligand with antagonistic properties on rat brain and human recombinant GABAA receptors in vitro
    • 43
    Chrysin (5,7-di-OH-flavone), a naturally-occurring ligand for benzodiazepine receptors, with anticonvulsant properties.
    • 163
    Possible anxiolytic effects of chrysin, a central benzodiazepine receptor ligand isolated from Passiflora Coerulea
    • 325
    Relationship between benzodiazepine receptor occupancy and potentiation of gamma-aminobutyric acid-stimulated chloride flux in vitro of four ligands of differing intrinsic efficacies.
    • 47
    6-Bromoflavone, a high affinity ligand for the central benzodiazepine receptors is a member of a family of active flavonoids.
    • 60
    • PDF
    6,3'-Dinitroflavone, a novel high affinity ligand for the benzodiazepine receptor with potent anxiolytic properties
    • 30
    Apigenin, a component of Matricaria recutita flowers, is a central benzodiazepine receptors-ligand with anxiolytic effects.
    • 314
    • PDF