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[ 125 I], [ 127 I]‐and [ 14 C]‐Labelling of the GLP‐1‐(7‐37) derivative NN2211
Author(s) -
Kristensen Jesper B.,
Pedersen Mette L.,
Larsen Ulla D.,
Martiny Lars,
Hansen Louis B.,
Foged Christian
Publication year - 2003
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.689
Subject(s) - chemistry , labelling , hydrogen peroxide , adme , derivative (finance) , lactoperoxidase , combinatorial chemistry , stereochemistry , biochemistry , pharmacology , enzyme , peroxidase , medicine , economics , financial economics , in vitro
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.