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- Title
Synthesis of C-14 radiolabeled glucagon receptor antagonist and its use in a human mass balance study.
- Authors
Czeskis, Boris A.; Satonin, Darlene K.
- Abstract
The synthesis of the radiolabeled glucagon receptor antagonist 1-[ 14 C ] was accomplished based on decarboxylative iodination of acid 2 followed by 'reattachment' of 14C carboxylic function. The method allowed a significant reduction in the number of steps in preparation of the radiolabeled compound. Iodide 4, obtained by the halodecarboxylation, was converted to cyanide 5-[ 14 C ], which was hydrolyzed to provide the radiolabeled acid 2-[ 14 C ]. Coupling with β-alanine fragment and hydrolysis of ester 6-[ 14 C ] completed the synthesis of the target molecule 1-[ 14 C ]. The resulting compound was utilized in a mass balance and metabolism study where hepatic oxidation followed by a trace amount of sulfate conjugation and elimination was the main clearance pathway for 1 in humans.
- Subjects
PROGLUCAGON; PEPTIDE hormones; GLUCAGON-like peptides; G protein coupled receptors; RADIOPHARMACEUTICALS
- Publication
Journal of Labelled Compounds & Radiopharmaceuticals, 2017, Vol 60, Issue 2, p110
- ISSN
0362-4803
- Publication type
Article
- DOI
10.1002/jlcr.3477