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Synthesis of β-3H-mitotane for use in a rapid assay for mitotane metabolism

✍ Scribed by Mayra L. Piñeiro-Sánchez; Alfin D. N. Vaz; Raymond E. Counsell; Mohamed Ruyan; David E. Schteingart; Joseph E. Sinsheimerl

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
316 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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.

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