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note
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® AD column with the eluent, hexane/isopropanol/AcOH, 980:20:1. The (-)-isomer was first eluted, and the (+)-isomer used in Scheme 3 was eluted second.
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13
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33746789559
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note
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Antiestrogen activity was determined as anti-uterotrophic effect of the test compound in ovariectomized (OVX) mice. OVX mice were treated with 0.1 μg of 17β-estradiol benzoate in peanut oil solution subcutaneously along with the indicated dose of the test compound in 5% gum arabic-water suspension orally once a day for three consecutive days. Approximately 24 h after the last administration, mice were euthanized, and their uterine weights were measured. Antiestrogen activity, determined by percent inhibition of estrogen-stimulated uterine weight gain by the test compound, was calculated according to the following equation: % inhibition = 100 × (1 - (T - C)/(E - C)). Estrogen activity was determined as uterotrophic effect of the test compound in OVX mice. OVX mice were treated with the indicated dose of the test compound in 10% EtOH-peanut oil solution subcutaneously once a day for three consecutive days. Approximately 24 h after the last administration, mice were euthanized, and their uterine weights were measured. Estrogen activity, determined by percent uterine weight gain by the test compound, was calculated according to the following equation: % uterine weight gain = 100 × (T - C)/(E - C). T, E, and C refer to uterine weight gain per body weight by the test compound, by 17β-estradiol benzoate, and by vehicle, respectively.
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14
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33746825620
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note
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The RBA value for ICI182,780 we obtained appears higher than other published values, which may be due to the experimental condition. The condition we used mainly differs from other reports in that the temperature we used is 25 °C, whereas the temperature other reports used is 0 or 4 °C. We speculate that ER degradation by ICI182,780 at 25 °C proceeded faster than at 0 or 4 °C, which led to high RBA value for ICI182,780 compared to those reported in the literature.
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