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Imaging agents for myeloperoxidase
Author(s) -
Malmquist Jonas,
Bernlind Alexandra,
Johansson Maria,
Juréus Anders,
Nilsson Maria
Publication year - 2012
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.2961
Subject(s) - chemistry , myeloperoxidase , isotopologue , formate , potassium cyanide , in vivo , in vitro , cyanide , potassium , radiochemistry , catalysis , biochemistry , organic chemistry , molecule , medicine , microbiology and biotechnology , inflammation , biology
The myeloperoxidase (MPO) inhibitors 1 and 2 were prepared as their isotopologues with carbon‐14, carbon‐13, and nitrogen‐15 or tritium with high specific activity and purity. Starting from potassium [ 14 C]cyanide or [ 14 C]formate provided metabolically stable 14 C‐labels on [ 14 C]‐1 and [ 14 C]‐2. Catalytic hydrogenation was used for the preparation of [ 3 H]‐2, giving multiple enriched positions as shown by 3 H NMR. 1 and 2 are promising in vitro and in vivo imaging radioligands and have the potential to provide key information with regard to MPO expression, function, stoichiometry, and pharmacology.