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Synthesis of isotopically labelled αCGRP 8‐37 and its lipidated analogue
Author(s) -
Lu Benjamin L.,
Loomes Kerry M.,
Hay Debbie L.,
Harris Paul W.R.,
Brimble Margaret A.
Publication year - 2020
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3838
Subject(s) - calcitonin gene related peptide , calcitonin , chemistry , antagonist , metabolic stability , receptor , peptide , biochemistry , neuropeptide , endocrinology , biology , in vitro
α‐Calcitonin gene related peptide (αCGRP) inhibitors are important medicinal targets due to their ability to produce antimigraine effects, thus, the discovery of long‐acting αCGRP inhibitors is of significant interest. Herein we report the synthesis of an isotopically labelled version of the well‐known CGRP receptor antagonist, αCGRP 8‐37 , as well as lipidated αCGRP 8‐37 with comparable antagonistic activity. These isotopically labelled peptides can be employed in assays to determine the metabolic stability of the lipidated αCGRP 8‐37 and compare this with the stability of known αCGRP 8‐37 .