Mechanisms of Action of the 5-HT1B/1D Receptor Agonists | Clinical Pharmacy and Pharmacology | JAMA Neurology | JAMA Network
[Skip to Navigation]
Access to paid content on this site is currently suspended due to excessive activity being detected from your IP address Please contact the publisher to request reinstatement.
Neurological Review
July 2002

Mechanisms of Action of the 5-HT1B/1D Receptor Agonists

Author Affiliations

From the New England Center for Headache, Stamford, Conn (Drs Tepper, Rapoport, and Sheftell); the Department of Neurology, Yale University School of Medicine, New Haven, Conn (Drs Tepper and Rapoport); and the Department of Psychiatry, New York Medical College, Valhalla (Dr Sheftell). Drs Tepper, Rapoport, and Sheftell are consultants for GlaxoSmithKline, Merck, AstraZeneca, and Pharmacia; conduct research for GlaxoSmithKline, Merck, AstraZeneca, Pharmacia, Allergan, Elan, and OrthoMcNeill; and are on the speakers bureau for GlaxoSmithKline, Merck, and AstraZeneca. Dr Rapoport is also a consultant for Abbott, Pfizer, Forest Laboratories, Elan, and Bristol-Myers Squibb. Dr Sheftell is also a consultant for Pfizer.



Arch Neurol. 2002;59(7):1084-1088. doi:10.1001/archneur.59.7.1084

Recent studies of the pathophysiology of migraine provide evidence that the headache phase is associated with multiple physiologic actions. These actions include the release of vasoactive neuropeptides by the trigeminovascular system, vasodilation of intracranial extracerebral vessels, and increased nociceptive neurotransmission within the central trigeminocervical complex. The 5-HT1B/1D receptor agonists, collectively known as triptans, are a major advance in the treatment of migraine. The beneficial effects of the triptans in patients with migraine are related to their multiple mechanisms of action at sites implicated in the pathophysiology of migraine. These mechanisms are mediated by 5-HT1B/1D receptors and include vasoconstriction of painfully dilated cerebral blood vessels, inhibition of the release of vasoactive neuropeptides by trigeminal nerves, and inhibition of nociceptive neurotransmission. The high affinity of the triptans for 5-HT1B/1D receptors and their favorable pharmacologic properties contribute to the beneficial effects of these drugs, including rapid onset of action, effective relief of headache and associated symptoms, and low incidence of adverse effects.