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dihydroergotamine
- Development stage
- Approved
- Lead developer
- Valeant Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Intravenous, Intramuscular, Subcutaneous, Intranasal
01
Overview
Dihydroergotamine is an ergot alkaloid used for the acute treatment of migraine headaches (with or without aura) and cluster headaches. It acts primarily as an agonist at serotonin 5-HT1D receptors, leading to vasoconstriction of intracranial blood vessels and inhibition of pro-inflammatory neuropeptide release in the trigeminal system. Dihydroergotamine also binds with high affinity to other serotonin receptors (5-HT1A, 5-HT2A, 5-HT2C), noradrenaline alpha receptors (α2A, α2B), and dopamine D2L and D3 receptors. The drug is not indicated for migraine prevention or for hemiplegic/basilar migraines. Its use has largely been supplanted by triptans due to their greater selectivity and improved side effect profile[1][2][6].
- Brand names
- D.H.E. 45MigranalTrudhesa
- Other names
- dihydroergotamineDHE
02
Targets
HTR1D (5-hydroxytryptamine receptor 1D)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))ADRA2B (α2B)ADRA2A (α2A)DRD2 (Dopamine D2 Receptor)HTR2C (5-hydroxytryptamine 2C receptor)HTR2A (Serotonin receptor 5-HT2A)DRD3 (Dopamine receptor D3)
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