Present and future of 5-HT receptor agonists as antimigraine drugs.

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Pauwels PJ, John GW

Present and future of 5-HT receptor agonists as antimigraine drugs.

Clin Neuropharmacol. 1999 May-Jun;22(3):123-36.

PubMed ID

10367177 [ View in PubMed

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Abstract

Serotonin (5-hydroxytryptamine; 5-HT) is thought to play an important role in the pathogenesis of migraine. The discovery of the 5-HT1B/1D/1F agonist sumatriptan constitutes a substantial advance in the acute treatment of migraine, though it displays a number of nonnegligible shortcomings. Today, a number of second-generation drugs derived from tryptamine are under advanced clinical development or are about to be marketed worldwide for the acute treatment of migraine. These tryptamine derivatives display partial agonist properties at 5-HT1B/1D receptors. It is not yet clearly established whether these agents represent a major improvement over sumatriptan in therapeutic effectiveness. Most of them also show affinity for 5-ht1F binding sites and have better oral pharmacokinetics than sumatriptan. The acute antimigraine effects of this second-generation of triptans seem to be obtained in largely the same way as with sumatriptan: by cranial vasoconstriction and inhibition of trigeminovascular activation from both peripheral and central projections. Future directions in migraine therapy should focus on agents that exhibit high intrinsic activity at 5-HT1B/1D receptors, offer a good safety profile, and demonstrate long-lasting action which might also be considered in migraine prophylaxis.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Sumatriptan	5-hydroxytryptamine receptor 1F	Protein	Humans	Yes	Agonist	Details