Migraine enters the molecular era

Migraine headache is the first neurological condition treatable by a drug targeted to a specific receptor binding site. Originally viewed as a disorder of brain blood vessels, migraine may have as its biological basis a disturbance in brain function. Regarding therapy, recent molecular data document that 5-HT_1D receptors on primary afferent fibers are coupled to inhibition of neuropeptide release, blockade of neurogenic inflammation, and c-fos expression within the trigeminal nucleus caudalis after noxious meningeal stimulation in experimental animals. The 5-HT_1Dα receptor subtype (as opposed to the 5-HT_1Dβ receptor) has emerged as an important therapeutic target aimed at blocking trigeminal nerve fibers without constricting vascular smooth muscle.