The paper describes the role of serotonin (5-hydroxytryptamine, 5-HT) in the pathophysiology of migraine. Serotonin exerts many various effects depending on activation of different types of serotonin (5-HT) receptors. According to our contemporary knowledge human 5-HT2B (or 5-HT2C) receptors localized on the endothelial cells of vessels play the most important role in the initiation of the painful phase of migraine. Activation of these receptors in cranial vessels leads via the release of nitric oxide (NO) to the vasodilatation and painful sterile inflammation in the vessel wall. Some anti-migraine prophylactic drugs are 5-HT2 antagonists. On the contrary 5-HT1D/1B agonists such as sumatriptan and other triptans are the most effective drugs in abolition of an acute attack. These receptors are responsible for cranial vasoconstriction and blockade of the neurogenic inflammation in the vessel wall during the activation of the trigeminovascular system.

        Key words: migraine, serotonin (5-hydroxytryptamine, 5-HT), serotonin (5-hydroxytryptamine, 5-HT) receptors, nitric oxide (NO), trigeminovascular systém