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Dihydroergotoxine mesylate
Biological Activity:
A complex of closely related
alkaloid salts. Binds with high affinity to the GABAA receptor Cl-
channel and has anticonvulsant and sedative activity. May also interact with
central dopaminergic, serotonergic and adrenergic (α1) receptors. Inhibits
prolactin.
Tvrdeic and Pericic (1991) Dihydrogenated ergot compounds bind with
high affinity to GABAA receptor-associated Cl- ionophore. Eur.J.Pharmacol. 202
109. Tvrdeic and Pericic (1992) Dihydroergotoxine modulation of the GABAA receptor-associated Cl- ionophore in mouse
brain. Eur.J. Pharmacol. 221 139.
Selective antagonist of neuro-steroid potentiation and direct gating of GABAA receptors. Selectively reduces the effects of 5α-reduced steroids compared to 5β-reduced steroids & displays no effect on potentiation evoked by barbiturates & benzodiazepines. Attenuates 3α,5α-THP-induced loss of righting reflex and total sleep time following i.c.v administration in rats.