Binding of hexestrol dicaprylate on estrogen receptor in the canine prostate.
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Binding of hexestrol dicaprylate (H<SUB>8</SUB>) on the estrogen receptor in the canine prostate was investi-gated. Six male dogs were injected with a single dose of 20mg/kg of H<SUB>8</SUB> 25 days after castration. On the 28th day after H<SUB>8</SUB> injection, the prostate was removed. In the dogs treated with H<SUB>8</SUB>, the size of the prostate gland exceeded that of the castrated control dogs by 3 times, and the epithelial proli-feration with stratified squamous metaplasia and the dilated acinar lumina filled with keratinized epithelial detritus were found histologically.<BR>Canine prostate cytosol was incubated with either H<SUB>8</SUB> or hexestrol (H<SUB>0</SUB>) and [<SUP>3</SUP>H]-estradiol ([<SUP>3</SUP>]-E<SUB>2</SUB>) at 4C for 18h. Following incubation, [<SUP>3</SUP>H]-E<SUB>2</SUB> binding to the estrogen receptor was separated from free [<SUP>3</SUP>H]-E<SUB>2</SUB> using dextran coated charcoal. H<SUB>0</SUB> strongly competed with [<SUP>3</SUP>H]-E<SUB>2</SUB> for binding to the estrogen receptor, while H<SUB>8</SUB> weakly competed with [<SUP>3</SUP>H]-E<SUB>2</SUB>. Prostate cytosol was also incubated with either H<SUB>8</SUB> or H<SUB>0</SUB> and [<SUP>3</SUP>H]-R1881 (the synthetic androgen) at 4C for 24h. Neither H<SUB>8</SUB> nor H<SUB>0</SUB> competed with [<SUP>3</SUP>H]-R1881 for binding to the androgen receptor.<BR>These results indicated that H<SUB>8</SUB> after being hydrolyzed to H<SUB>0</SUB> bound to the estrogen receptor in the prostate gland and caused the enlargement of the gland.
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