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Target intelligence / Profile preview
Calcitonin Gene-Related Peptide Type 1 Receptor (CGRP receptor)
- Target
- CGRP receptor
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor, Heteromeric receptor complex, Family B GPCR
01
Overview
The calcitonin gene-related peptide type 1 receptor (CGRP receptor) is a heteromeric G protein-coupled receptor (GPCR) that mediates the physiological effects of the neuropeptide CGRP. This receptor plays a central role in regulating vascular tone, modulating inflammatory and metabolic responses, and is critically implicated in migraine pathophysiology. The receptor is composed of Calcitonin Receptor-Like Receptor (CLR), Receptor Activity-Modifying Protein 1 (RAMP1), and Receptor Component Protein (RCP). Upon CGRP binding, the receptor activates Gs proteins, leading to increased cAMP production and PKA activation. CGRP receptors are widely distributed and involved in vasodilation, pain modulation, and other processes. Therapeutic targeting of CGRP or its receptor has proven effective for migraine treatment.
- Other names
- CGRPRCalcitonin Receptor-Like Receptor/RAMP1 complex
02
Mechanism of action
Inhibition of CGRP binding to the receptor or downstream signaling.
03
Biological functions
VasodilationPain modulationInflammation regulationSignal transductionAdenylyl cyclase activationcAMP productionProtein kinase A (PKA) activation
04
Disease associations
MigraineCardiovascular diseaseInflammation
05
Interacting drugs
Rimegepant
5 more in the full profile.
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