The Discovery of a New Drug Class for the Acute Treatment of Migraine

• Published in: Headache Vol. 47; no. s1; pp. S10 - S19
• Main Author: Humphrey, Patrick P.A.
• Format: Journal Article
• Language: English
• Published: Malden, USA Blackwell Publishing Inc 01.04.2007; Blackwell
• Subjects: adenosine A1 receptors; Biological and medical sciences; Cardiovascular system; GTP-Binding Proteins - physiology; History, 20th Century; Humans; Medical sciences; Migraine Disorders - drug therapy; Migraine Disorders - physiopathology; Neurology; Neuropharmacology; Neurotransmitters. Neurotransmission. Receptors; Pharmacology. Drug treatments; Receptors, Serotonin - physiology; Serotonin - physiology; serotonin receptors; Serotoninergic system; somatostatin sst2; sumatriptan; triptans; Tryptamines - history; Tryptamines - therapeutic use; Vascular diseases and vascular malformations of the nervous system; Vasodilator agents. Cerebral vasodilators; Headache; Agonist; Sumatriptan; Peptide hormone; Cardiovascular disease; 5-HT1 Serotonine receptor; Serotonin agonist; triptans; Vascular disease; Pain; Triptan derivatives; Somatostatin; Neurological disorder; Cerebrovascular disease; Nervous system diseases; serotonin receptors; Serotonin; somatostatin sst2; Antimigrainous agent; Migraine; Cerebral disorder; Treatment; Central nervous system disease; Neurotransmitter; Adenosine receptor; adenosine A1 receptors
• ISSN: 0017-8748; 1526-4610
• DOI: 10.1111/j.1526-4610.2007.00672.x

The history of the scientific ideas and events that led to the discovery of sumatriptan is outlined with personal reminiscences about individuals who influenced the approach. The development of sumatriptan revolutionized the acute treatment of migraine and led to the availability of a number of other triptans. The anti‐migraine effects of all the triptans are mediated via 5‐HT1B, and possibly 5‐HT1D receptors, which transduce their effects via G; proteins. This suggests that agonists at other Gi protein‐coupled receptor types appropriately located (eg, somatostatin sst2, adenosine A1) should be examined for their effects on the trigeminovascular system, Studies on such receptor targets may provide insight into a novel approach towards the design of new anti‐migraine drugs.