The 5-HT1D Receptor Subtype and Migraine Headache

Abstract

Serotonin (5-hydroxytryptamine, 5-HT) is involved in a wide variety of physiological functions and pathological states, including migraine. Fourteen subtypes of 5-HT receptors have been identified as of this writing (see Humphrey et al., 1993); while several of them might be the target of prophylactic anti-migraine drugs, the 5-HTm subtype appears most relevant among the known receptor subtypes, and this is based on the clinical efficacy of the receptor agonists sumatriptan and ergot alkaloids in aborting migraine headache (Deliganis and Peroutka, 1991). Accordingly, this chapter will briefly review current knowledge of the 5-HT1D receptor subtype with particular emphasis on its ligand binding properties, second messengers, molecular biology and mechanism of action.