Dihydroergotoxine mesylate

Biological Activity

Dihydroergotoxine mesylate is a complex of closely related alkaloid salts. Binds with high affinity to the GABA_A 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.

Technical Data

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.

Background References

1. Expression of gamma-aminobutyric acid receptor (subtype A) in prostate cancer
   Abdul et al.
   Acta Oncol., 2008;47:1546
2. Dihydrogenated ergot compounds bind with high affinity to GABA_A receptor-associated Cl^- ionophore.
   Tvrdeic and Perici
   Eur.J.Pharmacol., 1991;202:109
3. Dihydroergotoxine modulation of the GABA_A receptor-associated Cl^- ionophore in mouse brain.
   Tvrdeic and Perici
   Eur.J. Pharmacol., 1992;221:139
4. Effects of ergot alkaloids on 3H-flunitrazepam binding to mouse brain GABAA receptors.
   Tvredic and Perici
   Coll.Antropol., 2003;27:S175

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