Calcitonin gene-related peptide receptor (CGRP receptor) (CGRP receptor)

The Calcitonin gene-related peptide (CGRP) receptor is a heteromeric protein complex consisting of the calcitonin receptor-like receptor (CLR), a Class B G protein-coupled receptor, and the receptor activity-modifying protein 1 (RAMP1) (Source: UniProt Q16602). It requires the intracellular receptor component protein (RCP) for efficient coupling to G proteins and subsequent signaling (Source: PubMed PMC3133754). Primarily located in the trigeminal ganglion and cranial blood vessels, the receptor mediates the potent vasodilatory and pro-nociceptive effects of the CGRP neuropeptide (Source: StatPearls, Migraine Pathophysiology). In migraine pathology, CGRP release leads to neurogenic inflammation and sensitization of pain pathways, making the receptor a focal point for therapeutic intervention (Source: PubMed PMC6734061). Modern treatments include monoclonal antibodies like erenumab, which binds directly to the receptor, and small-molecule antagonists known as gepants, such as ubrogepant and rimegepant (Source: FDA, Aimovig and Ubrelvy labels). These drugs provide relief by inhibiting the receptor's activation, thereby reducing the frequency and intensity of migraine attacks.

Other names

CGRPRCLR/RAMP1 complexCalcitonin receptor-like receptor/Receptor activity-modifying protein 1 complex

Competitive antagonism or allosteric inhibition of the CGRP receptor complex to block CGRP-mediated vasodilation and nociceptive signaling (Source: PubMed PMC6734061).