Dihydroergotamine (mesylate)

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).1 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).2 Dihydroergotamine also binds to α-adrenergic receptors.3 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.4WARNING This product is not for human or veterinary use.

An agonist of 5-HT1B and 5-HT1D receptors

679.8

≥98%

Biochemicals/Receptor Pharmacology/Agonists

Formal_Name:(5'α,10α)-9,10-dihydro-12'-hydroxy-2'-methyl-5'-(phenylmethyl)-ergotaman-3',6',18-trione, methanesulfonate;Synonyms:(+)-Dihydroergotamine

CN1[C@]([C@]2([H])C[C@@H](C(N[C@@]3(C)C(N([C@@H](CC4=CC=CC=C4)C(N5[C@@]6([H])CCC5)=O)[C@@]6(O)O3)=O)

C33H37N5O5 • CH3SO3H

6190-39-2

≥ 4 years

DMF: 20 mg/ml DMSO: 20 mg/ml DMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml Ethanol: 1 mg/ml