AbstractOf all known neurotransmitters, 5-HT is the one most frequently mentioned in the pathophysiology of migraine. This review focuses on the relationship between the efficacy of sumatriptan and other migraine agents and their effects on specific 5-HT receptors in rodent models. These agents are seen to have effects on vascular constriction and the release of vasoactive and inflammatory peptides from trigeminovascular sensory neurons. Specific subtypes of the 5-HT₁ receptors appear to mediate these effects.