Sumatriptan is a potent vasoconstrictor of human dural arteries via a 5-HT1-like receptor.
The action of sumatriptan, putatively a selective 5-HT1D or 5-HT1-like receptor agonist which is effective in the treatment of migraine, has been studied on fresh human dural (middle meningeal) arteries. In low concentrations (10(-8)-10(-7) M) it was found to be a significantly stronger vasoconstrictor of dural arteries compared to cerebral and temporal arteries. However, its potency was less than that of 5-HT. The sumatriptan-induced vasoconstriction was antagonized by methiothepin (10(-9)-10(-8) M), but not by ketanserin (10(-7) M). The observations suggest that the sumatriptan-induced contraction of the dural artery is mediated via activation of 5-HT1D or 5-HT1-like receptors, whereas it does not appear to activate the 5-HT2 receptors.
Jansen
I
I
Department of Experimental Research, Malmö General Hospital, Sweden.
Edvinsson
L
L
Mortensen
A
A
Olesen
J
J
D002536:Cerebral Arteries / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D007211:Indoles / Q000494:pharmacology*; D007650:Ketanserin / Q000494:pharmacology; D008576:Meningeal Arteries / Q000187:drug effects*; D008719:Methiothepin / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000187:drug effects*; D013449:Sulfonamides / Q000494:pharmacology*; D018170:Sumatriptan; D013699:Temporal Arteries / Q000187:drug effects; D014662:Vasoconstrictor Agents / Q000494:pharmacology*
D007211:Indoles; D011985:Receptors, Serotonin; D013449:Sulfonamides; D014662:Vasoconstrictor Agents; D008719:Methiothepin; D018170:Sumatriptan; D007650:Ketanserin