Structure-Activity Relationships of Flavonoids, Isolated from Scutellaria baicalensis, Binding to Benzodiazepine Site of GABA_A Receptor Complex

Abstract

Twenty-six flavonoids were isolated from Scutellaria baicalensis. Their affinities for the benzodiazepine (BDZ) binding site of GABA_A receptor have been studied using [³ H]flunitrazepam binding to rat cortical membranes in vitro. The structure-activity relationships suggested that 2′-OH flavones exhibited the most potent binding affinity, which could lead to the design and discovery of new BDZ receptor ligands.

Key words

Flavonoids - Scutellaria baicalensis - Lamiaceae - BDZ receptor ligands - structure-activity relationship

References

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