An agonist of 5-HT1B and 5-HT1D receptors (Kis = 0.3 and 2.5 nM

Dihydroergotamine (mesylate) – 250 mg

Brand:
Cayman
CAS:
6190-39-2
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

An agonist of 5-HT1B and 5-HT1D receptors (Kis = 0.3 and 2.5 nM, respectively, for human receptors); 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); binds to α-adrenergic receptors; increases the mechanical pain threshold in a rat model of neuropathic pain when used at doses of 50 and 100 mg/kg

Formal name: (5’α,10α)-9,10-dihydro-12′-hydroxy-2′-methyl-5′-(phenylmethyl)-ergotaman-3′,6′,18-trione, methanesulfonate

Synonyms:  (+)-Dihydroergotamine

Molecular weight: 679.8

CAS: 6190-39-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Cardiovascular Diseases||Research Area|Neuroscience|Pain Research

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