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Synthesis of isotopically labelled αCGRP8-37 and its lipidated analogue

Authors :
Kerry M. Loomes
Debbie L. Hay
Margaret A. Brimble
Paul W. R. Harris
Benjamin L. Lu
Source :
Journal of Labelled Compounds and Radiopharmaceuticals. 63:325-332
Publication Year :
2020
Publisher :
Wiley, 2020.

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 .

Details

ISSN :
03624803
Volume :
63
Database :
OpenAIRE
Journal :
Journal of Labelled Compounds and Radiopharmaceuticals
Accession number :
edsair.doi...........c16408cbb9631830e5ba87ef82156f4c
Full Text :
https://doi.org/10.1002/jlcr.3838