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Mechanisms of action of serotonin 5-HT1B/D agonists: insights into migraine pathophysiology using rizatriptan.
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2000
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Pain MedicinePsychotropic MedicationNeurotransmitterPsychopharmacologyPharmacotherapySocial SciencesMolecular PharmacologyNeurologyAcute MigraineNeurochemistryVascular ChangeCluster HeadacheMigraine HeadacheNeuropharmacologyNervous SystemPharmacologyPain ResearchSerotonin 5-Ht1b/d AgonistsNeurophysiologyNeuroanatomyNeuroscienceMigraine PathophysiologyMedicineNeuropeptides
Current theories on the etiology of migraine headache suggest that it is a neurovascular disorder (i.e., vascular change secondary to neural activation), with a primary CNS dysfunction giving rise to headache pain as a result of local intracranial vasodilatation and release of sensory neuropeptides from nerve endings in an activated trigeminal system. The serotonin 5-HT1B/1D agonists, known as the triptans, represent a major advance in the treatment of acute migraine. This article describes their mechanisms of action. The development of 5-HT1B/1D agonist drugs, such as rizatriptan, and the study of their pharmacology have enhanced our understanding of the mechanisms involved in the pathophysiology of migraine.