Synthesis of isotopically labelled αCGRP8-37 and its lipidated analogue,Journal of Labelled Compounds and Radiopharmaceuticals

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Synthesis of isotopically labelled αCGRP8-37 and its lipidated analogue
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2020-03-25 , DOI: 10.1002/jlcr.3838
Benjamin L Lu _{1,

2} , Kerry M Loomes _{2,

3} , Debbie L Hay _{2,

3} , Paul W R Harris _{1,

2,

3} , Margaret A Brimble _{1,

2,

3}

Affiliation

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 .

中文翻译：

同位素标记的αCGRP8-37及其脂化类似物的合成

α-降钙素基因相关肽（αCGRP）抑制剂由于能够产生抗偏头痛作用而成为重要的医学靶点，因此，长效αCGRP抑制剂的发现具有重要意义。在此，我们报告了众所周知的 CGRP 受体拮抗剂 αCGRP8-37 的同位素标记形式的合成，以及具有相当拮抗活性的脂化 αCGRP8-37 。这些同位素标记的肽可用于测定脂化 αCGRP8-37 的代谢稳定性，并将其与已知的 αCGRP8-37 的稳定性进行比较。

更新日期：2020-03-25

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