Labelling of a potent glucagon receptor antagonist with tritium, carbon-14 and stable isotopes

摘要

3-{4-[l-(4-Cyclohex-l-enylphenyl)-3-(3,5-dichlorophenyl) ureidomethyl]-benzoylamino}propionic acid (1) is a potent glucagon receptor antagonist, which has been investigated in pre-clinical trials for the treatment of type 2 diabetes (Scheme 1). Here, we present the syntheses of tritium, carbon-14 and stable isotope labelled 1 for use in a range of preclinical studies.