title: Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.
abstract: Calcitonin gene-related peptide (CGRP) is a potent neuromodulator and vasodilator. It has been implicated in the pathogenesis of migraine by a number of lines of evidence, although its precise role has yet to be fully defined. Compelling evidence for the importance of CGRP in migraine has been provided by clinical trials with multiple small molecule CGRP receptor antagonists. These clinical studies have shown that blockade of the CGRP receptor can produce antimigraine efficacy comparable to that of the gold standard triptan class of drugs with an incidence of adverse events that appears to be relatively low. The present review describes the discovery and development of these new antimigraine agents and highlights the challenges of identifying orally acting drugs that target a family B G-protein-coupled receptor.
authors: Department of Discovery Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, United States.
authors: Ian M
authors: IM
authors: Bell
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D015740:Calcitonin Gene-Related Peptide / Q000502:physiology; D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D002986:Clinical Trials as Topic; D055808:Drug Discovery; D006801:Humans; D008881:Migraine Disorders / Q000188:drug therapy*; D008969:Molecular Sequence Data; D018015:Receptors, Calcitonin Gene-Related Peptide / Q000737:chemistry / Q000502:physiology; D013329:Structure-Activity Relationship
chemical_list: D000077221:Calcitonin Gene-Related Peptide Receptor Antagonists; D018015:Receptors, Calcitonin Gene-Related Peptide; D015740:Calcitonin Gene-Related Peptide