Internal medicine

Receptor

Neuropeptide

Endocrinology

Calcitonin gene-related peptide

Receptor antagonist

Antagonist

Antagonism

Migraine

Competitive antagonist

Medicine

Pharmacology

British Journal of Pharmacology

The development of several drugs that target the calcitonin gene-related peptide (CGRP) system has been a major breakthrough in the pharmacological management of migraine. These are divided into two major classes, antibodies which bind to the CGRP peptide, preventing it from activating CGRP receptors and receptor antagonists. Within the receptor antagonist class, there are two mechanisms of action, small molecule receptor antagonists and an antibody antagonist. This mini-review considers the pharmacology of these receptor targeted antagonist drugs at the CGRP receptor and closely related AMY1 receptor, at which CGRP may also act. The antagonists are most potent at the CGRP receptor but can also show antagonism of the AMY1 receptor. However, important data are missing and selectivity parameters cannot be provided for all antagonists. The clinical implications of AMY1 receptor antagonism are unknown, but we urge consideration of this receptor as a potential contributing factor to CGRP and antagonist drug actions. LINKED ARTICLES: This article is part of a themed issue on Advances in Migraine and Headache Therapy (BJP 75th Anniversary). To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v179.3/issuetoc.

CGRP receptor antagonists for migraine. Are they also AMY<sub>1</sub> receptor antagonists?

CGRP receptor antagonists for migraine. Are they also AMY1 receptor antagonists?

CGRP receptor antagonists for migraine. Are they also AMY₁ receptor antagonists?