Calcitonin Gene-Related Peptide Receptor (CGRP Receptor)

The calcitonin gene-related peptide receptor (CGRP receptor) is a heteromeric G protein-coupled receptor that mediates the effects of CGRP, a neuropeptide involved in vasodilation, pain transmission, and migraine pathophysiology. It consists of CLR, RAMP1, and RCP subunits. Activation of the receptor leads to increased cAMP and PKA activation, resulting in vasodilation. The CGRP receptor is a key therapeutic target for migraine, with antagonists and monoclonal antibodies developed to block its activity.

Other names

CGRP-RCalcitonin Receptor-Like Receptor/Receptor Activity-Modifying Protein 1/Receptor Component Protein complexCLR/RAMP1/RCP complex

CGRP receptor antagonists block the binding of CGRP to its receptor, preventing the activation of adenylyl cyclase and subsequent downstream signaling pathways, ultimately reducing vasodilation and pain transmission. CGRP monoclonal antibodies bind to the CGRP ligand, preventing it from binding to the receptor.