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Synthesis and characterization of tritium‐labeled RU486
Author(s) -
Mais Dale E.,
Chen LianZhi,
Wagoner Murriel A.,
Hayes J. Scott,
Wang MingWei
Publication year - 1995
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.2580361210
Subject(s) - chemistry , tritium , desmethyl , ligand (biochemistry) , amine gas treating , mifepristone , receptor , progesterone receptor , stereochemistry , iodide , radiochemistry , biochemistry , organic chemistry , medicine , physics , nuclear physics , pregnancy , cancer , estrogen receptor , biology , breast cancer , metabolite , genetics
[ 3 H]RU38486 (RU486) was synthesized from its penultimate precursor, desmethyl RU486, by substitution of the secondary amine with tritiated methyl iodide; specific activity 85 Ci/mmol. Ligand binding studies confirm that RU486 binds with high affinity to human progesterone receptor type A (PR‐A) and progesterone receptor type B (PR‐B).