Pharmacological characterisation of erenumab, Aimovig, at two calcitonin gene-related peptide responsive receptors.
amylin
calcitonin gene-related peptide
calcitonin receptor
calcitonin receptor-like receptor
erenumab
migraine
receptor activity-modifying protein
Journal
British journal of pharmacology
ISSN: 1476-5381
Titre abrégé: Br J Pharmacol
Pays: England
ID NLM: 7502536
Informations de publication
Date de publication:
Jan 2024
Jan 2024
Historique:
revised:
30
06
2023
received:
30
01
2023
accepted:
02
08
2023
medline:
6
12
2023
pubmed:
15
8
2023
entrez:
15
8
2023
Statut:
ppublish
Résumé
Calcitonin gene-related peptide (CGRP) is involved in migraine pathophysiology. CGRP can signal through two receptors. The canonical CGRP receptor comprises the calcitonin receptor-like receptor and receptor activity-modifying protein 1 (RAMP1); the AMY Erenumab antagonism was quantified through IC Erenumab antagonised both the CGRP and AMY Despite being designed to target the CGRP receptor, erenumab can antagonise the AMY
Sections du résumé
BACKGROUND AND PURPOSE
OBJECTIVE
Calcitonin gene-related peptide (CGRP) is involved in migraine pathophysiology. CGRP can signal through two receptors. The canonical CGRP receptor comprises the calcitonin receptor-like receptor and receptor activity-modifying protein 1 (RAMP1); the AMY
EXPERIMENTAL APPROACH
METHODS
Erenumab antagonism was quantified through IC
KEY RESULTS
RESULTS
Erenumab antagonised both the CGRP and AMY
CONCLUSION AND IMPLICATIONS
CONCLUSIONS
Despite being designed to target the CGRP receptor, erenumab can antagonise the AMY
Substances chimiques
Receptors, Calcitonin Gene-Related Peptide
0
Calcitonin Gene-Related Peptide
JHB2QIZ69Z
erenumab
I5I8VB78VT
Calcitonin Gene-Related Peptide Receptor Antagonists
0
Receptors, Calcitonin
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
142-161Subventions
Organisme : New Zealand Neurological Foundation First Fellowship
Organisme : University of Otago Doctoral Scholarship
Organisme : Fred Fastier Summer Studentship Scholarship
Organisme : National Institute of Neurological Disorders And Stroke of the National Institutes of Health
ID : RF1NS113839
Informations de copyright
© 2023 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.
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