Action of an estrogen antagonist in intact and ovariectomized rats

Perry, Kenneth W.; DiPasquale, G.; Ferguson, Evan R.; Pozzi, Charles; Rassaert, Charles L.

doi:10.1016/0010-7824(73)90014-0

Cited by 10 publications

(4 citation statements)

References 27 publications

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“…Previous studies of the effect of the antioestrogens upon the uptake of [3H]-oestradiol into the target areas of the brain are inconsistent. Workers have reported that either the antioestrogens interact with only the peripheral tissues (Perry, Dipasquale, Ferguson, Pozzi & Rassaert, 1973;Whalen & Gorzalka, 1973;Chazal, Faudon, Gogan & Rotsztyn, 1975), or both peripheral and central tissues (Maurer & Woolley, 1971;Luttge, Gray & Hughes, 1976;Roy & Wade, 1977). The experiments described here show that there is a dose-related depletion of the cytosol HAR in all tissues but at low doses the brain HAR are not affected, findings which help to clarify the anomalous results.…”

Section: Discussionsupporting

confidence: 52%

DIFFERENTIAL DEPLETION OF CYTOPLASMIC HIGH AFFINITY OESTROGEN RECEPTORS AFTER THE in vivo ADMINISTRATION OF THE ANTIOESTROGENS, CLOMIPHENE, MER‐25 AND TAMOXIFEN

Kurl

Morris

1978

British J Pharmacology

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1 The in vivo actions of the oestrogen antagonists, MER-25 and tamoxifen upon the cytosol oestrogen receptors prepared from amygdala, hypothalamus, pituitary and uterus of rats were studied 24 h after drug administration. 2 There was a dose-related depletion of cytosol oestrogen receptors. However, the uterine and pituitary receptors were consistently affected at a lower dose than were those from the brain. 3 The ratios of the combined central ED50 to the combined peripheral ED50 were clomiphene 169 greater than MER-25 19.2 greater than tamoxifen 2.13. 4 The receptor changes were not related to biological activity monitored by serum luteinizing hormone levels and uterotrophic response. 5 The possible role of these drug effects in the induction of ovulation and future developments are discussed.

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Section: Discussionsupporting

confidence: 52%

DIFFERENTIAL DEPLETION OF CYTOPLASMIC HIGH AFFINITY OESTROGEN RECEPTORS AFTER THE in vivo ADMINISTRATION OF THE ANTIOESTROGENS, CLOMIPHENE, MER‐25 AND TAMOXIFEN

Kurl

Morris

1978

British J Pharmacology

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“…Non-steroidal anti-oestrogens block the binding of oestradiol by target tissues in vivo (Roy, Mahesh & Greenblatt, 1964;Perry, DiPasquale, Ferguson, Pozzi & Rassaert, 1973) and in vitro (Terenius 19716). In the present study, tamoxifen inhibited increases in uterine weight, and the binding of oestradiol to uterine oestrogen-binding components in vivo (Fig.…”

Section: Discussionmentioning

confidence: 98%

Tamoxifen as an Anti-Tumour Agent: Effect on Oestrogen Binding

Jordan¹,

Dowse²

1976

Journal of Endocrinology

137

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Tamoxifen (ICI 46,474) has been shown to possess anti-tumour properties in the dimethylbenz(a)anthracene (DMBA)-induced rat mammary carcinoma model. During tamoxifen therapy the binding of [3H]oestradiol in vivo to uterine (P less than 0-001), vaginal (P less than 0 X 01) and tumour (P less than 0-001) tissues was significantly reduced. Tamoxifen therapy was without effect on the binding of [3H]oestradiol in heart tissue. The determination of specific oestrogen-binding components in vitro was significantly reduced (P less than 0-01) in tumours from tamoxifen-treated rats and tamoxifen inhibited the binding of [3H]oestradiol to 8S oestrogen-binding components, derived from rat uteri and DMBA-induced tumours, in vitro.

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“…There is some suggestion that CI 628 may not inhibit estradiol uptake in the central nervous system (Whalen and Gorzalka, 1973). However, others have demonstrated that CI 628 can suppress hypothalamic estradiol uptake (Perry, DiPasquale, Ferguson, Pozzi, and Rassaert, 1973) although this inhibition occurred in intact, but not in ovariectomized, females. There is little doubt that other pharmacologic agents can effectively compete for estradiol receptors in brain (Kahwanago, Heinrichs, and Hermann, 1970;van Kordelaar, Broekman, and van Rossum, 1975;Maurer and Wooley, 1971).…”

Section: Discussionmentioning

confidence: 98%

Anti-estrogenic suppression of the lordosis response in female rats

1975

Hormones and Behavior

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The anti-estrogen, Cl 628, was used to suppress the lordosis response induced by sequential injections of estrogen and progesterone in ovariectomired (OVX) female rats. Appropriate doses of Cl 628 completely abolished sexual receptivity in females administered estradiol benzoate (EB) in sesame oil. This behavioral effect could be attenuated by providing increased quantities of EB or decreased quantities of CI 628. Antiestrogenic effects on lordosis induced by free estradiol in saline (E) were assessed after first establishing behaviorally equivalent doses of EB and E. This was accomplished by determining thresholds for E-induced lordosis. OVX females were approximately seven times less sensitive to E than to EB. CI 628 had no significant effects on E-induced lordosis, in contrast to the complete abolition of lordosis in females treated with behaviorally equivalent EB doses. A possible mechanism to explain this differential responsiveness of EB-and E-treated females is discussed.

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Action of an estrogen antagonist in intact and ovariectomized rats

Cited by 10 publications

References 27 publications

DIFFERENTIAL DEPLETION OF CYTOPLASMIC HIGH AFFINITY OESTROGEN RECEPTORS AFTER THE in vivo ADMINISTRATION OF THE ANTIOESTROGENS, CLOMIPHENE, MER‐25 AND TAMOXIFEN

DIFFERENTIAL DEPLETION OF CYTOPLASMIC HIGH AFFINITY OESTROGEN RECEPTORS AFTER THE in vivo ADMINISTRATION OF THE ANTIOESTROGENS, CLOMIPHENE, MER‐25 AND TAMOXIFEN

Tamoxifen as an Anti-Tumour Agent: Effect on Oestrogen Binding

Anti-estrogenic suppression of the lordosis response in female rats

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