Formulation: A crystalline solid
Formal Name: (5'α,10α)-9,10-dihydro-12'-hydroxy-2'-methyl-5'-(phenylmethyl)-ergotaman-3',6',18-trione, methanesulfonate
Purity: ≥98%
Formula Markup: C33H37N5O5 • CH3SO3H
Formula Weight: 679,8
Shelf life (days): 1460
CAS Number: 6190-39-2
Notes: Dihydroergotamine is a derivative of ergotamine and an agonist of the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D (Kis = 0.3 and 2.5 nM, respectively, for human receptors).{41322} It binds to dopamine D2 and D3 as well as 5-HT2A receptors (K0.5s = 5, 16, and 38 nM, respectively) but has lower affinity for D1, 5-HT2C, and 5-HT3 receptors (K0.5s = 2,779, 298, and >10,000 nM, respectively).{41323} Dihydroergotamine also binds to α-adrenergic receptors.{41324} Dihydroergotamine (50 and 100 mg/kg) increases the mechanical pain threshold in a rat model of neuropathic pain following chronic constriction injury to the infraorbital nerve. Formulations containing dihydroergotamine have been used in the treatment of migraine headaches.{41321}