Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.

Article Details

Citation

Hanrahan JR, Chebib M, Davucheron NL, Hall BJ, Johnston GA

Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors.

Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.

PubMed ID
12824018 [ View in PubMed
]
Abstract

Amentoflavone is found in a number of plants with medicinal properties, including Ginkgo biloba and Hypericum perforatum (St. John's Wort). We have developed a rapid and economic semi-synthetic preparation of amentoflavone from biflavones isolated from autumnal Ginkgo biloba leaves. Several studies have shown that amentoflavone binds to benzodiazepine receptors. Using two electrode voltage-clamp methodology, amentoflavone has been shown to be a negative modulator of GABA at GABA(A) alpha(1)beta(2)gamma(2L) receptors expressed in Xenopus laevis oocytes This action appears to be independent of the flumazenil-sensitive benzodiazepine modulatory sites on the GABA(A) receptor.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
Ginkgo bilobaGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Unknown
Negative modulator
Details
Ginkgo bilobaGamma-aminobutyric acid receptor subunit beta-2ProteinHumans
Unknown
Negative modulator
Details
Ginkgo bilobaGamma-aminobutyric acid receptor subunit gamma-2ProteinHumans
Unknown
Negative modulator
Details