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

Biochemical and Biophysical Research Communications
H ViolaJ H Medina

Abstract

6,3'-dibromoflavone and 6-nitro-3'-bromoflavone inhibited [(3)H]flunitrazepam binding to the benzodiazepine binding site of the gamma amino butyric acid receptor complex with K(i) values between 17 and 36 nM in different brain regions. Their gamma amino butyric acid ratio for [(3)H]flunitrazepam binding to cerebral cortex membranes indicated partial agonistic properties. Both compounds had similar pharmacological effects: they produced anxiolytic-like effects at low doses but did not alter locomotor activity or muscle tonicity; sedation was caused only at doses higher than 30 mg/kg in mice. 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.

References

Jan 1, 1983·Advances in Biochemical Psychopharmacology·C BraestrupT Honoré
Dec 8, 1995·Journal of Medicinal Chemistry·J J AresW C Kershaw

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Citations

May 10, 2011·Neurochemical Research·Jader NonesFlávia Carvalho Alcantara Gomes
Aug 3, 2012·Cell and Tissue Research·Jader NonesAndréa Gonçalves Trentin
Sep 25, 2007·Progress in Neuro-psychopharmacology & Biological Psychiatry·Elisa OgnibeneGiovanni Laviola
Sep 12, 2009·Journal of Neuroscience Research·Tânia Cristina Leite de Sampaio e SpohrFlávia Carvalho Alcantara Gomes
Jul 14, 2004·European Journal of Pharmacology·Daniele V S LopesFrançois Noël
Sep 15, 2011·European Journal of Pharmacology·Lihuan RenHong Xue
Mar 21, 2019·International Journal of Food Sciences and Nutrition·Rafael Fernández-DemeneghiSocorro Herrera-Meza

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