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.
|Storage||Desiccate at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 300.27. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.33 mL||16.65 mL||33.3 mL|
|5 mM||0.67 mL||3.33 mL||6.66 mL|
|10 mM||0.33 mL||1.67 mL||3.33 mL|
|50 mM||0.07 mL||0.33 mL||0.67 mL|
References are publications that support the products' biological activity.
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
If you know of a relevant reference for Hispidulin, please let us know.
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Keywords: Hispidulin, supplier, Partial, positive, allosteric, modulators, benzodiazepine, receptor, GABAA, Receptors, GABAC, Dinatin, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
GABA Receptors Scientific Review
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.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.