Chemical Name:5,7-Dihydroxy-2-(4-hydroxyphenyl)-6-methoxy-4H-1-benzop
yran-4-one
Biological Activity:
Partial positive allosteric modulator at the
benzodiazepine receptor (IC50 = 1.3 μM for
inhibition of flumazenil binding); natural sage flavone. Stimulates
GABA-induced chloride currents in Xenopus oocytes expressing α1
α2-,
α3-,
α5-
or α6-β2γ2S GABAA
receptors. Brain penetrant; oral administration reduces seizures in a gerbil
model of epilepsy. Also has antifungal, antiproliferative, antioxidant and
antithrombotic properties.
Bourdillatet al (1988) Hispidulin, a
natural flavone, inhibits human platelet aggregation by increasing cAMP levels.
Eur.J.Pharmacol. 147 1. Kavvadiaset al (2003)
Constituents of sage (Salvia officinalis) with in vitro affinity to human brain
benzodiazepine receptor. Planta Med. 69 113. Kavvadiaset
al (2004) The flavone hispidulin, a benzodiazepine receptor ligand with
positive allosteric properties, traverses the blood-brain barrier and exhibits
anticonvulsive effects. Br.J.Pharmacol. 142 811.
Selective antagonist of neuro-steroid potentiation and direct gating of GABAA receptors. Selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids & displays no effect on potentiation evoked by barbiturates & benzodiazepines. Attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.
