Background:

Dihydroergotoxine mesylate is 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.IC50 value:Target: Dihydroergotoxine mesylate also interacts with central dopaminergic, serotonergic and adrenergic (α1) receptors. Dihydroergotoxine mesylate displays antiproliferative activity in vitro (IC50 = 18 - 38 μM in prostate cancer cells) and exhibits cognition-enhancing, anticonvulsant and sedative activity in vivo.

参考文献:
[1]. Tvrdeic A, et al. Dihydrogenated ergot compounds bind with high affinity to GABAA receptor-associated Cl- ionophore. Eur J Pharmacol. 1991 Sep 4;202(1):109-11.
[2]. Tvrdeic A, et al. Dihydroergotoxine modulation of the GABAA receptor-associated Cl- ionophore in mouse brain. Eur J Pharmacol. 1992 Oct 6;221(1):139-43.
[3]. Tvrdeic A, et al. Effect of ergot alkaloids on 3H-flunitrazepam binding to mouse brain GABAA receptors. Coll Antropol. 2003;27 Suppl 1:175-82.
[4]. Abdul M, et al. Expression of gamma-aminobutyric acid receptor (subtype A) in prostate cancer. Acta Oncol. 2008;47(8):1546-50.