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Synthesis of isotopically labelled αCGRP8-37 and its lipidated analogue
Benjamin L Lu1,2, Kerry M Loomes2,3, Debbie L Hay2,3
1School of Chemical Sciences, The University of Auckland, Auckland, New Zealand.
Abstract:
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, αCGRP8-37 , as well as lipidated αCGRP8-37 with comparable antagonistic activity. These isotopically labelled peptides can be employed in assays to determine the metabolic stability of the lipidated αCGRP8-37 and compare this with the stability of known αCGRP8-37 .

