Serotonin receptor ligands: treatments of acute migraine and cluster headache.
Fuelled by the development of the serotonin 5-HT(1B/1D) receptor agonists, the triptans, the last 15 years has seen an explosion of interest in the treatment of acute migraine and cluster headache. Sumatriptan was the first of these agonists, and it launched a wave of therapeutic advances. These medicines are effective and safe. Triptans were developed as cranial vasoconstrictors to mimic the desirable effects of serotonin, while avoiding its side-effects. It has subsequently been shown that the triptans' major action is neuronal, with both peripheral and central trigeminal inhibitory effects, as well as actions in the thalamus and at central modulatory sites, such as the periaqueductal grey matter. Further refinements may be possible as the 5-HT(1D) and 5-HT(1F) receptor agonists are explored. Serotonin receptor pharmacology has contributed much to the better management of patients with primary headache disorders.
Goadsby
P J
PJ
Institute of Neurology, Queen Square, London WC1N 3BG, UK. peterg@ion.ucl.ac.uk
D000208:Acute Disease; D000818:Animals; D002490:Central Nervous System / Q000187:drug effects; D003027:Cluster Headache / Q000188:drug therapy*; D006801:Humans; D008024:Ligands; D008881:Migraine Disorders / Q000188:drug therapy*; D017933:Peripheral Nervous System / Q000187:drug effects; D044302:Receptor, Serotonin, 5-HT1B / Q000187:drug effects; D044346:Receptor, Serotonin, 5-HT1D / Q000187:drug effects; D011985:Receptors, Serotonin / Q000187:drug effects*; D017366:Serotonin Receptor Agonists / Q000627:therapeutic use*; D014363:Tryptamines / Q000627:therapeutic use*; D000096642:Receptor, Serotonin, 5-HT1F
D008024:Ligands; D044302:Receptor, Serotonin, 5-HT1B; D044346:Receptor, Serotonin, 5-HT1D; D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D014363:Tryptamines; D000096642:Receptor, Serotonin, 5-HT1F