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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solubility||Soluble in ethanol|
References are publications that support the biological activity of the product.
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, Dihydroergotoxine mesylate supplier, Binds, GABAA, receptor, Cl-, channel, allosteric, modulators, benzodiazepine, site, Receptors, 0505, 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!
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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.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
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.