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Dihydroergotamine

Name: Dihydroergotamine
Description: A 9,10alpha-dihydro derivative of ergotamine. It is used as a vasoconstrictor, specifically for the therapy of migraine disorders. (PubChem) Pharmacology: Dihydroergotamine is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. Dihydroergotamine binds with high affinity to 5-HT1Da and 5-HT1Db receptors. It also binds with high affinity to serotonin 5-HT1A, 5-HT2A, and 5-HT2C receptors, noradrenaline a2A, a2B and a receptors, and dopamine D2L and D3 receptors. The therapeutic activity of Dihydroergotamine in migraine is generally attributed to the agonist effect at 5-HT1D receptors. Mechanism of action: Two theories have been proposed to explain the efficacy of 5-HT1D receptor agonists in migraine: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release. Drug type: Approved. Small Molecule. Drug category: Analgesics. Analgesics, Non-Narcotic. Anti-migraine Agents. Dopamine Agonists. Sympatholytics. Vasoconstrictor Agents
Synonym(s): 9, 10-dihydro-ergotamine, Dihidroergotamina (INN-Spanish), Dihydroergotamine mesylate, Dihydroergotamine methanesulfonate, Dihydroergotamine monomethanesulfonate, Dihydroergotaminum (INN-Latin), Agit, Angionorm, D, H, E, D, H, E, 45, DET MS, DHE-45, Dergotamine, Diergo, Dihydergot, Dirgotarl, Endophleban, Ergomimet, Ergont, Ergotonin, Ikaran, Migranal, Morena, Orstanorm, Tonopres, Verladyn
Related to: 5-hydroxytryptamine 2A receptor, 5-hydroxytryptamine 1D receptor, 5-hydroxytryptamine 1B receptor
Has role: Drug, Dopamine agonist role
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB00320
Id: DB00320
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Contributors

Ccdbuser, Memartone, Nifbot2



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Commenttaken from DrugBank
CurationStatusuncurated  +
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB00320  +
DefinitionA 9,10alpha-dihydro derivative of ergotami A 9,10alpha-dihydro derivative of ergotamine. It is used as a vasoconstrictor, specifically for the therapy of migraine disorders. (PubChem) Pharmacology: Dihydroergotamine is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. Dihydroergotamine binds with high affinity to 5-HT1Da and 5-HT1Db receptors. It also binds with high affinity to serotonin 5-HT1A, 5-HT2A, and 5-HT2C receptors, noradrenaline a2A, a2B and a receptors, and dopamine D2L and D3 receptors. The therapeutic activity of Dihydroergotamine in migraine is generally attributed to the agonist effect at 5-HT1D receptors. Mechanism of action: Two theories have been proposed to explain the efficacy of 5-HT1D receptor agonists in migraine: 1) activation of 5-HT1D receptors located on intracranial blood vessels, including those on arterio-venous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache and 2) activation of 5-HT1D receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release. Drug type: Approved. Small Molecule. Drug category: Analgesics. Analgesics, Non-Narcotic. Anti-migraine Agents. Dopamine Agonists. Sympatholytics. Vasoconstrictor Agents ts. Sympatholytics. Vasoconstrictor Agents
Has roleDrug  +, and Dopamine agonist role  +
IdDB00320  +
LabelDihydroergotamine  +
ModifiedDate14 April 2014  +
RelatedTo5-hydroxytryptamine 2A receptor  +, 5-hydroxytryptamine 1D receptor  +, and 5-hydroxytryptamine 1B receptor  +
SuperCategoryMolecular entity  +
Synonym9  +, 10-dihydro-ergotamine  +, Dihidroergotamina (INN-Spanish)  +, Dihydroergotamine mesylate  +, Dihydroergotamine methanesulfonate  +, Dihydroergotamine monomethanesulfonate  +, Dihydroergotaminum (INN-Latin)  +, Agit  +, Angionorm  +, D  +, H  +, E  +, 45  +, DET MS  +, DHE-45  +, Dergotamine  +, Diergo  +, Dihydergot  +, Dirgotarl  +, Endophleban  +, Ergomimet  +, Ergont  +, Ergotonin  +, Ikaran  +, Migranal  +, Morena  +, Orstanorm  +, Tonopres  +, and Verladyn  +