Description: Positive allosteric modulator of GABAA receptors
Chemical Name: (2E)-3-[(4S,7R,7aR)-2,4,5,6,7,7a-Hexadydro-3,7-dimethyl-1H-inden-4-yl]-2-methyl-2-propenoic acid
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Positive allosteric modulator of GABAA receptors that displays preference for receptors containing β2 or β3 subunits. Directly activates the receptor and blocks the channel at high concentrations. Displays sedative, anticonvulsant and anxiolytic activity in vivo. Also acts as a partial agonist of 5-HT5A receptors.
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.
Solubility Data
Solubility
Soluble in ethanol
Preparing Stock Solutions
The following data is based on the product molecular weight 234.33. 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
4.27 mL
21.34 mL
42.67 mL
5 mM
0.85 mL
4.27 mL
8.53 mL
10 mM
0.43 mL
2.13 mL
4.27 mL
50 mM
0.09 mL
0.43 mL
0.85 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Dietzet al (2005) Valerian extract and valerenic acid are partial agonists of the 5-HT5a receptor in vitro. Brain Res.Mol.Brain Res. 138 191 PMID: 15921820
Benkeet al (2008) GABAA receptors as in vivo substrate for the anxiolytic action of valerenic acid, a major constituent of valerian root extracts. Neuropharmacology 56 174 PMID: 18602406
Khomet al (2007) Valerenic acid potentiates and inhibits GABAA receptors: molecular mechanism and subunit specificity. Neuropharmacol. 53 178 PMID: 17585957
Khomet al (2016) Analysis of β-subunit-dependent GABAA receptor modulation and behavioral effects of valerenic acid derivatives. J.Pharmacol.Exp.Ther. 357 580 PMID: 27190170