Hispidulin

Biological Activity

Hispidulin is a 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-β2 γ2S GABA_A receptors. Brain penetrant; oral administration reduces seizures in a gerbil model of epilepsy. Also has antifungal, antiproliferative, antioxidant and antithrombotic properties.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Hispidulin, a natural flavone, inhibits human platelet aggregation by increasing cAMP levels.
   Bourdillat et al.
   Eur.J.Pharmacol., 1988;147:1
2. Constituents of sage (Salvia officinalis) with in vitro affinity to human brain benzodiazepine receptor.
   Kavvadias et al.
   Planta Med., 2003;69:113
3. The flavone hispidulin, a benzodiazepine receptor ligand with positive allosteric properties, traverses the blood-brain barrier and exhibits anticonvulsive effects.
   Kavvadias et al.
   Br.J.Pharmacol., 2004;142:811

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