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Synthesis of [3H]proadifen for studying binding to liver membranes

✍ Scribed by Tom Werner; Lars Gawell; Svante B. Ross

Publisher
John Wiley and Sons
Year
1993
Tongue
French
Weight
216 KB
Volume
33
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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.

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