Dihydroergotamine mesylate

Dihydroergotamine mesylate (6190-39-2) is a full agonist at serotonin 5HT1B and 5HT1D receptors, IC50= 2 and 2.2 nM respectively1 and also at 5HT1A and 5HT1F receptors2. One of the oldest agents for treatment of migraine.3 Also acts as a potent vasoconstrictor and alpha-adrenergic antagonist.4

White to Off-White Solid

α-Androgenic blocker with selective venoconstrictor properties. Also binds to serotonin 5HT1-receptors. Antimigraine.

Agonist at vascular serotonin receptors; partial agonist at alpha-adrenergic and dopamine D2 receptors

vasoconstrictor, antimigraine

ChEBI: The methanesulfonic acid salt of dihydroergotamine, a semisynthetic ergot alkaloid with weaker oxytocic and vasoconstrictor properties than ergotamine. Both the mesylate and the tartrate salts are used for the treatment of migraine and orthostatic hypotens on.

D.H.E. 45 (Valeant); Migranal (Valeant) .

Partial α -adrenergic agonist. Partial D 2 dopaminergic receptor agonist. Competitive 5-HT antagonist.

Room temperature

[1] ANNE S. LESAGE. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines[J]. British Journal of Pharmacology, 2009, 123 8: 1655-1665. DOI:10.1038/sj.bjp.0701766
[2] SILBERSTEIN S D. The pharmacology of ergotamine and dihydroergotamine.[J]. Headache, 1997, 37 Suppl 1: S15-25.
[3] STEPHEN D SILBERSTEIN  Douglas C M. Ergotamine and dihydroergotamine: history, pharmacology, and efficacy.[J]. Headache, 2003, 43 2: 144-166. DOI:10.1046/j.1526-4610.2003.03034.x
[4] LIPTON R B. Ergotamine tartrate and dihydroergotamine mesylate: safety profiles.[J]. Headache, 1997, 37 Suppl 1: S33-41.