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Target intelligence / Profile preview
Calcitonin Gene-Related Peptide (CGRP)
- Target
- CGRP
- Molecular classification
- Neuropeptide
01
Overview
Calcitonin gene-related peptide (CGRP) is a 37-amino acid neuropeptide primarily produced by alternative splicing of the calcitonin gene. It exists in two major isoforms, α-CGRP and β-CGRP. CGRP is a potent vasodilator and is implicated in pain pathways, particularly in migraine pathophysiology. CGRP antagonists have proven efficacy for migraine treatment.
- Other names
- alpha-CGRPβ-CGRP
02
Mechanism of action
CGRP exerts its effects via a unique heteromeric receptor complex (CLR/RAMP1/RCP), activating Gs subunit → stimulates adenylyl cyclase → increases cAMP → activates PKA → downstream phosphorylation events including opening of KATP channels and activation of CREB transcription factor.
03
Biological functions
VasodilationPain modulationImmune regulationGastrointestinal motilityBone growthNociceptionParacrine regulation of pituitary hormone release
04
Disease associations
MigraineInflammatory PainNeuropathic PainCardiovascular stress
05
Interacting drugs
Gepants
1 more in the full profile.
06
Biomarkers
CGRP levels (elevated in migraine)
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