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Updated: Jun 12, 2026

Ex Vivo Release of Calcitonin Gene-Related Peptide from the Trigeminovascular System in Rodents
Published on: May 16, 2022
Calcitonin gene-related peptide receptor antagonists for migraine
1Department of Pharmacology, University of Cambridge, Cambridge, UK. mjmf2@cam.ac.uk
Importance Of The Field:
Migraine is a highly prevalent disabling condition, and the current treatment options are not satisfactory. The role of calcitonin gene-related peptide (CGRP) in migraine pathophysiology is well established. CGRP receptor antagonists address this new target and have the potential to improve therapy for both responders and non-responders to previous options.
Areas Covered In This Review:
This review describes CGRP, its receptors and their role in the pathophysiology of migraine. CGRP receptor antagonists are a recent development; all reported antagonists are reported in chronological order. The experimental evidence, as well as all clinical trials since the first proof-of-concept study in 2004, is discussed.
What The Reader Will Gain:
An overview of the CGRP system and why it provides an attractive drug target for headache. The main focus is on the currently presented CGRP receptor antagonists and clinical evidence for this new therapeutic option.
Take Home Message:
CGRP receptor antagonists will provide an additional and valuable therapeutic option for the treatment of headaches.
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