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CGRP blockers in migraine therapy: where do they act?
1Department of Medicine, Institute of Clinical Sciences, Lund University Hospital, Lund, Sweden. lars.edvinsson@med.lu.se
British Journal of Pharmacology
|September 9, 2008
Summary
Calcitonin gene-related peptide (CGRP) antagonists and CGRP-reducing antibodies show promise for migraine treatment. Reducing CGRP availability may be more effective for prophylaxis than acute therapy due to the blood-brain barrier.
Area of Science:
- Neuroscience
- Pharmacology
Background:
- Calcitonin gene-related peptide (CGRP) plays a key role in the central and peripheral nervous systems, influencing functions like vasodilation and nociception.
- AlphaCGRP is concentrated in sensory nerve fibers, and its release is triggered by trigeminal nerve activation, impacting the trigeminovascular pathway.
Purpose of the Study:
- To explore the therapeutic potential of targeting CGRP mechanisms for migraine treatment.
- To evaluate the efficacy of CGRP receptor antagonists and CGRP availability reduction strategies.
Main Methods:
- Investigated the effects of CGRP1 receptor antagonists on trigeminovascular signaling.
- Examined the impact of CGRP antibodies and RNA-Spiegelmers on CGRP availability and neurogenic inflammation.
Main Results:
- CGRP1 receptor antagonists effectively reduce trigeminovascular pathway signaling and can abort acute migraine attacks.
- Strategies limiting CGRP availability decrease neurogenic inflammation and attenuate trigeminovascular signaling.
Conclusions:
- Targeting CGRP offers a promising therapeutic avenue for migraine management.
- Reducing CGRP availability may be more beneficial for migraine prophylaxis than for acute treatment due to limitations imposed by the blood-brain barrier.
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