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Synthesis of isotopically labelled αCGRP8-37 and its lipidated analogue.

Journal of labelled compounds & radiopharmaceuticals (2020-03-27)
Benjamin L Lu, Kerry M Loomes, Debbie L Hay, Paul W R Harris, Margaret A Brimble
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 .

MATERIALS
Product Number
Brand
Product Description

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2,2′-(Ethylenedioxy)diethanethiol, 95%
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(2S)-6-Amino-2-{[(9H-fluoren-9-ylmethoxy)carbonyl]amino}hexanoic acid