雄マウスにおけるヘキセストロールジカプリレートの類似体ジエチルスチルベストロールジカプリレートの代謝と生物活性について

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  • Metabolism and biological effectiveness of di-ethylstilbestrol dicaprylate in male mice
  • オス マウス ニ オケル Hexestrol dicaprylate ノ ルイジタイ Diethylstilbestrol dicaprylate ノ タイシャ ト セイブツ カッセイ ニ ツイテ

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To investigate more about the long acting effect of esterified estorogen on the inhibition of gonadal activities, diethylstilbestrol dicaprylate (D8) was synthesized and the mode of conversion from storage to effective forms of D8 was compared with that of hexestrol dicaprylate (H8).<BR>Estrus-inducing dose of D8 was 20 μg for spayed rats by the vaginal smear test; a dose which was close to that of H8. Spermatogenesis was inhibited by the injection of 0.5 mg/kg of D8 in dogs and 15 mg/kg of D8 in mice. Following the injection of 1.5 mg/0.2 μCi of D8 to mice, more than 80% of the injected dose of D8 was found at the injection site on the 30th day. Two days after the [3H]-D8 injection, the visceral content of radioactive compounds was less than 30×10-6 of the injected dose. In the liver, kidney, and blood, relatively high concentrations of radioactive compounds were found in the dicaprylate form. Rat uterus cytosol was incubated with either D8, H8, diethylstilbestrol, or hexestrol in the presence of [3H]-estradio1-17β at 4 C for 18 hours. Diethylstilbestrol and hexestrol strongly competed with [3H]-estradio1-17β for binding to cytosol estrogen receptor, while D8 and H8 weakly competed with it.<BR>These findings demonstrate that D8 is absorbed slowly from the injection site and acts to the target organs after being hydrolyzed, and thus manifests long acting effect in vivo.

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