Molecular and Cellular Mechanisms of CGRP Antagonists

Abstract

Calcitonin gene–related peptide (CGRP) receptor antagonists are increasingly becoming more important as treatments for acute migraine. These antagonists bind the CGRP receptor but could also interact with the amylin receptors. They relieve migraine pain in clinical trials, and their molecular mechanisms involve binding and inhibiting CGRP receptors in the trigeminovascular system. The current data on migraine pathology suggest that binding to CGRP receptors on the Aδ-neurons is the main molecular and cellular pathways through which they excise their effects.