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Submit ReviewHispidulin 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 GABAA receptors. Brain penetrant; oral administration reduces seizures in a gerbil model of epilepsy. Also has antifungal, antiproliferative, antioxidant and antithrombotic properties.
M. Wt | 300.27 |
Formula | C16H12O6 |
Storage | Desiccate at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1447-88-7 |
PubChem ID | 5281628 |
InChI Key | IHFBPDAQLQOCBX-UHFFFAOYSA-N |
Smiles | OC1=CC2=C(C(C=C(C3=CC=C(O)C=C3)O2)=O)C(O)=C1OC |
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.
References are publications that support the biological activity of the product.
Bourdillat et al (1988) Hispidulin, a natural flavone, inhibits human platelet aggregation by increasing cAMP levels. Eur.J.Pharmacol. 147 1 PMID: 2836213
Kavvadias et al (2003) Constituents of sage (Salvia officinalis) with in vitro affinity to human brain benzodiazepine receptor. Planta Med. 69 113 PMID: 12624814
Kavvadias et 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 PMID: 15231642
Keywords: Hispidulin, Hispidulin supplier, Partial, positive, allosteric, modulators, benzodiazepine, receptor, GABAA, Receptors, GABAC, PAM, Dinatin, 2174, Tocris Bioscience
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Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.