A complex of closely related alkaloid salts. Binds with high affinity to the GABAA receptor Cl- channel, producing an allosteric interaction with the benzodiazepine site. Also interacts with central dopaminergic, serotonergic and adrenergic (α1) receptors. Displays antiproliferative activity in vitro (IC50 = 18 - 38 μM in prostate cancer cells) and exhibits cognition-enhancing, anticonvulsant and sedative activity in vivo. Orally active.
|Storage||Store at RT|
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||Soluble in ethanol|
References are publications that support the products' biological activity.
Abdul et al (2008) Expression of gamma-aminobutyric acid receptor (subtype A) in prostate cancer Acta Oncol. 47 1546 PMID: 18607852
Tvrdeic and Perici (1991) Dihydrogenated ergot compounds bind with high affinity to GABAA receptor-associated Cl- ionophore. Eur.J.Pharmacol. 202 109 PMID: 1664802
Tvrdeic and Perici (1992) Dihydroergotoxine modulation of the GABAA receptor-associated Cl- ionophore in mouse brain. Eur.J. Pharmacol. 221 139 PMID: 1333969
Tvredic and Perici (2003) Effects of ergot alkaloids on 3H-flunitrazepam binding to mouse brain GABAA receptors. Coll.Antropol. 27 S175 PMID: 12955907
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Keywords: Dihydroergotoxine mesylate, supplier, Binds, GABAA, receptor, Cl-, channel, allosteric, modulators, benzodiazepine, site, Receptors, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
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