Description
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
Chemical Properties
White to Off-White Solid
Uses
Agonist at vascular serotonin receptors; partial agonist at alpha-adrenergic and dopamine D2 receptors
Uses
vasoconstrictor, antimigraine
Uses
α-Androgenic blocker with selective venoconstrictor properties. Also binds to serotonin 5HT1-receptors. Antimigraine.
Definition
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.
Brand name
D.H.E. 45 (Valeant); Migranal (Valeant)
.
Biological Activity
Partial α -adrenergic agonist. Partial D 2 dopaminergic receptor agonist. Competitive 5-HT antagonist.
References
Lesage et al. (1998), Agnostic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines; J. Pharmacol., 123 1655
Silberstein (1997), The pharmacology of ergotamine and dihydroergotamine; Headache, 37 Suppl 1 S15
Silberstein and McCrory (2003), Ergotamine and dihydroergotamine: history, pharmacology, and efficacy; Headache, 43 144
Lipton (1997), Ergotamine tartrate and dihydroergotamine mesylate: safety profiles; Headache, 37 Suppl.1 S33
