The development of a highly selective 5‐HT₁ receptor agonist, sumatriptan, for the treatment of migraine

Sumatriptan is a highly selective 5‐HT 1 receptor agonist and an effective treatment for migraine. It causes constriction of cranial blood vessels. In anaesthetised animals, it selectively constricts parts of the carotid vasculature and has been shown to inhibit plasma protein extravasation from blood vessels of the dura mater induced by antidromic stimulation of the trigeminal nerve. This effect may result from a localised vasoconstriction of the meningeal vessels and/or a direct inhibitory effect on adventitial nerve endings. Sumatriptan penetrates the blood brain barrier poorly. These findings are consistent with the view that the locus of action of sumatriptan is at the level of the wall of cranial blood vessels that are distended and edematous during a migraine headache.