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Synthesis of [ 3 H]proadifen for studying binding to liver membranes
Author(s) -
Werner Tom,
Gawell Lars,
Ross Svante B.
Publication year - 1993
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.2580330709
Subject(s) - chemistry , membrane , tritium , chromatography , hydrochloride , nuclear chemistry , organic chemistry , biochemistry , physics , nuclear physics
Tritium‐labelled proadifen (1, SKF 525A, 2‐(N,N‐diethylamino)‐ethyl‐2,2‐di‐diphenylpentanoate hydrochloride), a potent inhibitor of microsomal drug metabolism in the liver, was synthesized by hydrogenation of the corresponding allylic derivative with tritium gas. The specific activity of the compound obtained was 65 Ci/mmol. [ 3 H]Proadifen was found to bind to washed rat liver membranes with high affinity (K D 1.3 nM) and large capacity B max 1300 pmol/g wet weight tissue.