Cat. No. 0505
Biological ActivityA 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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
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.
Tvredic and Perici (2003) Effects of ergot alkaloids on 3H-flunitrazepam binding to mouse brain GABAA receptors. Coll.Antropol. 27 S175. PMID: 12955907.
Tvrdeic and Perici (1992) Dihydroergotoxine modulation of the GABAA receptor-associated Cl- ionophore in mouse brain. Eur.J. Pharmacol. 221 139. PMID: 1333969.
Tvrdeic and Perici (1991) Dihydrogenated ergot compounds bind with high affinity to GABAA receptor-associated Cl- ionophore. Eur.J.Pharmacol. 202 109. PMID: 1664802.
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Keywords: Dihydroergotoxine mesylate, supplier, Binds, GABAA, receptor, Cl-, channel, allosteric, modulators, benzodiazepine, site, Receptors, Tocris Bioscience, GABAA Receptor Benzodiazepine products
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July 8 - 12, 2017