雄マウス臓器におけるヘキセストロール　ジカプリレートのインビトロ代謝およびエストロジェンリセプターへの結合について

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  • <I>In vitro</I> metabolism of Hexestrol dicaprylate in mouse organs and its binding to estrogen receptor
  • ユウ マウス ゾウキ ニ オケル hexestrol dicaprylate

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Hundred mg each of various tissues obtained from 60 days old mice was incubated with either [14C]hexestrol dicaprylate (H8; 115 nmol, 4 nCi) or [3H]-H8 (10 nmol, 0.1 μCi) at 37 C for 1 h. Following incubation, radioactive metabolites were extracted, isolated, and identified with the method of re-crystallization to constant specific activity.<BR>Only small amounts of radioactive H8 were metabolized by mouse tissues-adrenal, pancreas, intestine, fat, spleen, lung, muscle, testis, and kidney. It was observed that no radioactive H8 was metabolized by plasma.<BR>Rat uterus cytosol was incubated with either H8 or H0 and [3H]-estradiol-17 β ([3H]-E2) at 4 C for 18 h. Following incubation, [3H]-E2 binding to estrogen receptor was separated from free [3H]-E2 using dextran coated charcoal. Five nm H0 strongly competed with 0. 8 nm [3H]-E2 for binding to estrogen receptor, while 25 nm H8 weakly competed with 0.2 nm [3H]-E2.<BR>These findings will suggest that the injected H8 to animals will be slowly converted to H0 and act to the target organs after being hydrolyzed to H0.

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