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 } }
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…
6 Citations
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.
- Biology, ChemistryBiochemical and biophysical research communications
- 2000
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
- Biology, PsychologyProgress in Neuro-Psychopharmacology and Biological Psychiatry
- 2008
5,7-Dihydroxy-6-methoxyflavone, a benzodiazepine site ligand isolated from Scutellaria baicalensis Georgi, with selective antagonistic properties.
- Biology, ChemistryBiochemical pharmacology
- 2003
Molecular modeling and QSAR analysis of the interaction of flavone derivatives with the benzodiazepine binding site of the GABA(A) receptor complex.
- Biology, ChemistryBioorganic & medicinal chemistry
- 2001
Flavonoids as GABAA receptor ligands: the whole story?
- BiologyJournal of experimental pharmacology
- 2012
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.
- Biology, ChemistryBioorganic & medicinal chemistry
- 2006
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