ATC Group: N02CC Selective serotonin (5HT1) agonists

Almotriptan is a selective 5-HT_1B and 5-HT_1D receptor agonist. These receptors mediate vasoconstriction of certain cranial vessels, as demonstrated in studies using isolated human tissue preparations.

Eletriptan is a selective agonist at the vascular 5-HT_1B and neuronal 5-HT_1D receptors. Eletriptan also exhibits high affinity for the 5-HT_1F receptor which may contribute to its anti-migraine mechanism of action.

Frovatriptan is a selective agonist for 5-HT receptors. Frovatriptan is believed to act selectively on extracerebral, intracranial arteries to inhibit the excessive dilatation of these vessels in migraine.

Naratriptan has been shown to be a selective agonist for 5 hydroxytryptamine₁ (5-HT₁) receptors mediating vascular contraction. This receptor is found predominantly in intracranial (cerebral and dural) blood vessels. Naratriptan is indicated for the acute treatment of migraine attacks with or without aura.

Rizatriptan binds selectively with high affinity to human 5-HT_1B and 5-HT_1D receptors. The therapeutic activity of rizatriptan in treating migraine headache may be attributed to its agonist effects at 5-HT_1B and 5-HT_1D receptors on the extracerebral intracranial blood vessels that are thought to become dilated during an attack and on the trigeminal sensory nerves that innervate them.

Sumatriptan has been demonstrated to be a specific and selective 5-Hydroxytryptamine₁ (5HT_1D) receptor agonist with no effect on other 5HT receptor (5-HT₂ - 5-HT₇) subtypes. The vascular 5-HT_1D receptor is found predominantly in cranial blood vessels and mediates vasoconstriction.

Zolmitriptan has been demonstrated to be a selective agonist for the vascular human recombinant 5HT_1B and 5HT_1D receptor subtypes. Zolmitriptan is a high affinity 5HT_1B/1D receptor agonist with modest affinity for 5HT_1A receptors.