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Synthesis of β‐ 3 H‐mitotane for use in a rapid assay for mitotane metabolism
Author(s) -
PiñeiroSánchez Mayra L.,
Vaz Alfin D. N.,
Counsell Raymond E.,
Ruyan Mohamed,
Schteingart David E.,
Sinsheimerl Joseph E.
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.2580360204
Subject(s) - mitotane , chemistry , hydroxylation , metabolism , adrenocortical carcinoma , drug metabolism , chromatography , pharmacology , biochemistry , endocrinology , enzyme , medicine
A 3 H + ‐release method has been developed for the assay of β‐hydroxylation of the adrenolytic drug mitotane. β‐ 3 H‐mitotane was synthesized by the reduction of 1‐(2‐chlorophenyl)‐1‐(4‐chlorophenyl)‐2,2,2‐trichloroethane by an aluminium‐Hg 2 Cl 2 couple in the presence of 3 H 2 O. For β‐hydroxylation of mitotane, the 3 H + ‐release assay is more efficient and sensitive than a method utilizing 14 C‐mitotane and chromatographic separation of metabolites by HPLC. The 3 H + ‐release assay has been used to evaluate the ability of adrenal tumors to metabolize mitotane via the β‐ hydroxylation route.