CGRP (Calcitonin Gene-Related Peptide)
Also known as: α-CGRP, β-CGRP, Calcitonin Gene-Related Peptide-1
Overview
Calcitonin Gene-Related Peptide (CGRP) is a 37-amino acid neuropeptide produced by alternative splicing of the calcitonin gene, expressed abundantly in trigeminal sensory neurons. It is the most potent endogenous vasodilator known and plays a central role in migraine pathophysiology. CGRP itself is not used therapeutically; rather, anti-CGRP monoclonal antibodies (erenumab, fremanezumab, galcanezumab) and CGRP receptor antagonists ('gepants': rimegepant, ubrogepant) targeting this peptide have revolutionized migraine prevention and acute treatment.
Mechanism of Action
CGRP binds a heterodimeric GPCR complex consisting of calcitonin receptor-like receptor (CLR) combined with receptor activity-modifying protein 1 (RAMP1). Activation stimulates adenylyl cyclase (cAMP/PKA) in vascular smooth muscle, causing potent and prolonged vasodilation. In the trigeminal system, CGRP is released from trigeminal ganglion neurons during migraine attacks, promoting neurogenic inflammation, mast cell degranulation, and sensitization of central pain pathways (central sensitization/allodynia). Blocking CGRP signaling with antibodies or small molecule antagonists interrupts this cascade.
Potential Benefits
- As target: anti-CGRP biologics prevent 50%+ of migraine days in responders
- Gepant CGRP antagonists provide acute migraine abortion
- Understanding CGRP enabled development of the first mechanism-specific migraine drugs
- CGRP itself has vasodilatory and cardioprotective roles in ischemia
- Research target for cluster headache and other trigeminovascular conditions
Dosage Protocols
The following reflects doses used in published research studies. This is not medical advice. Consult a qualified healthcare professional.
| Beginner | Research tool only |
| Intermediate | N/A |
| Advanced | N/A |
| Cycle Duration | N/A |
CGRP itself is a research peptide. Clinical therapeutics are monoclonal antibodies (erenumab, fremanezumab, galcanezumab, eptinezumab) and small-molecule antagonists (rimegepant, ubrogepant, atogepant) that BLOCK CGRP for migraine.
Use our Reconstitution Calculator to determine exact syringe units for your protocol.
Routes of Administration
Intravenous (research provocation studies) 100%
Used to reliably provoke migraine in susceptible subjects.
Read our full Routes of Administration Guide for detailed comparison of all delivery methods.
Stacking Protocols
Popular research stacks involving CGRP (Calcitonin Gene-Related Peptide):
Research Context Only
CGRP is not used therapeutically — blocking it is. Stacking not applicable.
Explore our complete Peptide Stacking Guide for more combinations and safety considerations.
Reconstitution
| Storage | Refrigerate at 2-8°C after reconstitution. Do not freeze reconstituted solution. |
|---|
Typical vial sizes: 0.5-1 mg (research). Add bac water slowly down the side of the vial, swirl gently — do not shake. Use insulin syringe for precise dosing.
Need exact syringe measurements?
Amino Acid Sequence
Ala-Cys-Asp-Thr-Ala-Thr-Cys-Val-Thr-His-Arg-Leu-Ala-Gly-Leu-Leu-Ser-Arg-Ser-Gly-Gly-Val-Val-Lys-Asn-Asn-Phe-Val-Pro-Thr-Asn-Val-Gly-Ser-Lys-Ala-Phe-NH2
Side Effects & Safety
- CGRP itself: hypotension at pharmacological doses, flushing
- Anti-CGRP antibodies: constipation, injection site reactions
Safety & Contraindications
This information is for educational purposes only. Consult a qualified healthcare provider before using any peptide.
Pregnancy / Lactation
Bleeding Disorders
Active Skin Infection at Injection Site
Pharmacokinetics
| Half-Life | Not well characterized for this peptide; consult primary literature |
|---|---|
| Storage | Store lyophilized peptide at -20°C (long-term) or 2-8°C (short-term, under 30 days). Reconstituted: refrigerate at 2-8°C and use within 28-30 days. Protect from light. Do not freeze reconstituted solution. |
Synergistic Compounds
The following compounds have been studied alongside CGRP (Calcitonin Gene-Related Peptide) for potential complementary or synergistic effects:
Learn More
References & Further Reading
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