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Journal of Endocrinology (1975) 64, 193-194       DOI: 10.1677/joe.0.0640193
© 1975 Society for Endocrinology
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INHIBITION OF OESTRADIOL BINDING TO MOUSE UTERINE AND VAGINAL OESTROGEN RECEPTORS BY TRIPHENYLETHYLENES

V. C. JORDAN and S. KOERNER

Worcester Foundation for Experimental Biology, Shrewsbury, Massachusetts 01545, U.S.A.

(Received 28 August 1974)

Harper & Walpole (1967 reported the potent antioestrogenic activity of ICI 46,474, the trans-isomer of 1-(p-β-dimethylaminoethoxyphenyl)-1,2-diphenylbut-1-ene, in the rat; however, in the mouse the compound exhibited only oestrogenic properties. However, Emmens (1971) showed that large doses of ICI 46,474 or the related compound H774 (1-(p-β-diethylaminoethoxyphenyl)-1,2-di(p-methoxyphenyl)-but-1-ene citrate) caused vaginal refractoriness to oestradiol for several weeks after s.c. administration to ovariectomized mice. The present study was undertaken to determine the ability of ICI 46,474 and H774 to inhibit binding of [3H]oestradiol to the 8 S oestrogen receptor derived from ovariectomized mouse uterus and vagina.

Mature, Charges River CD strain mice were ovariectomized under ether anaesthesia, primed with 1 µg oestradiol-17β in 0·05 ml peanut oil and used for experimentation 2 weeks later. Animals were killed by cervical dislocation and the uteri and vaginae were dissected out, weighed and immediately




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[Abstract] [Full Text] [PDF]




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