Small molecule
PubChem CID 5358
Sumatriptan
Imitrex
- Mechanism of action
- Selective 5-HT1B/1D receptor agonist
- In plain language
- Narrows blood vessels in the brain and calms overactive pain-signaling nerves to stop a migraine in progress.
- How it works
- Sumatriptan is a selective agonist at 5-HT1B and 5-HT1D serotonin receptor subtypes, binding with high affinity to these receptors on intracranial blood vessels and on sensory nerve terminals of the trigeminal system. Activation of 5-HT1B receptors on vascular smooth muscle produces constriction of dilated cranial vessels. Activation of 5-HT1D receptors on trigeminal nerve endings inhibits the release of pro-inflammatory neuropeptides, reducing neurogenic inflammation and pain transmission. Sumatriptan has minimal affinity for other 5-HT receptor subtypes, giving it a targeted action on the trigeminovascular pathway implicated in migraine.
- Therapeutic applications
- Indicated for the acute treatment of migraine, with or without aura, in adults. Not indicated for migraine prophylaxis and has not been established as effective for cluster headache.
- Class
- Small molecule
- Therapeutic area
- CNS / Neurology
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