[125I], [127I]-and [14C]-Labelling of the GLP-1-(7-37) derivative NN2211

✍ Scribed by Jesper B. Kristensen; Mette L. Pedersen; Ulla D. Larsen; Lars Martiny; Louis B. Hansen; Christian Foged

• Publisher: John Wiley and Sons
• Year: 2003
• Tongue: French
• Weight: 121 KB
• Volume: 46
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.689

✦ Synopsis

Abstract

Arg^34^Lys^26^(N^ε^‐(γ‐L‐glutamyl(N^α^‐palmitoyl)))‐GLP‐1(7‐37) (NN2211) is currently in development as a diabetes type 2 drug. The fatty acid attached to the GLP‐1(7‐37) ensures a long and controlled duration of action. The synthesis of [^125^I]NN2211, [^127^I]NN2211 and [^14^C]NN2211 used for preclinical ADME studies are described. NN2211 was iodinated using the lactoperoxidase/hydrogen peroxide method, and [^14^C]NN2211 was synthesized in 4 steps by two routes both starting from an α‐protected [U‐^14^C]glutamic acid. Copyright © 2003 John Wiley & Sons, Ltd.