Antifertility Agents

Emmens, C W

doi:10.1146/annurev.pa.10.040170.001321

Cited by 37 publications

(9 citation statements)

References 39 publications

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“…Since Lerner, Holthaus & Thompson (1958) described MER-25 {l-[p-{2-diethylaminoethoxy) phenyl] -2-(^-methoxyphenyl) -1 -phenylethanol), various triarylethane and triarylethylene derivatives with basic ether groups have been found to possess both antioestrogenic and antifertility activity (see Emmens, 1970, for a recent review). Antioestrogenic activity has usually been detected by administering an oestrogen and potential antagonist simultaneously in uterine weight or vaginal smear tests, and antifertility activity by administering the compounds before or shortly after coitus.…”

Section: Introductionmentioning

confidence: 99%

Compounds Exhibiting Prolonged Antioestrogenic and Antifertility Activity in Mice and Rats

Emmens¹

1971

Reproduction

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Section: Introductionmentioning

confidence: 99%

Compounds Exhibiting Prolonged Antioestrogenic and Antifertility Activity in Mice and Rats

Emmens¹

1971

Reproduction

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“…Plants that exhibit antiestrogenic activity have the capacity of interrupting the gestation of rats and mice, by the inhibition of the estrogen necessary for implantation (Ghandi et al, 1991). In mice and humans, estrogen has an important role in implantation, as it participates in the estrogen/progesterone balance and in the receptivity of the uterus to the embryo (Ements, 1970).…”

Section: Resultsmentioning

confidence: 99%

Study of reproductive toxicity of Combretum leprosum Mart and Eicher in female Wistar rats

Oliveira¹,

Santos²,

Cardoso³

et al. 2013

Afr. J. Biotechnol.

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Most plants culturally used in Brazil for medicine do not have pre-clinical studies of reproductive toxicity, therefore risks of using such products on the reproductive system are unknown. The aim of the study was to evaluate possible reproductive toxicity of ethanolic extract of Combretum leprosum Mart and Eicher (EECL) in female Wistar rats. The animals, weighing between 180 to 250 g, were maintained in controlled environmental conditions of temperature, humidity, light/dark cycle of 12/12 h, water ad libitum and fed with commercial diet for rats. To verify the estrogenic activity of EECL, four groups of ovariectomized rats were used: saline + corn oil; saline + estradiol; EECL (500 mg/kg) + corn oil; EECL (500 mg/kg) + estradiol. To study the reproductive toxicity during the fecundation and implantation phases of the embryos and also during the organogenesis phase, two groups were used for each experiment, saline and EECL (500 mg/Kg). No estrogenic or anti-estrogenic activities were observed in the EECL. The ingestion of EECL did not cause modification in the number of implantation sites, which indicates a lack of toxicity during this phase. The EECL administered orally in the dose of 500 mg/kg did not produce adverse effects on the reproductive system of the female rats.

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“…Various in vivo and in vitro methods have been proposed for the evaluation of antiestrogens [1,4,5,7]. The events occurring in the uterus and vagina follow different time sequences of action following administration of estrogen and/or antiestrogens [14].…”

Section: Methods O F Evaluationmentioning

confidence: 99%

A Critique on the Evaluation and Mode of Action of Antiestrogens

Sankaran¹,

Prasad²

1972

Gynecol Obstet Invest

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(1) The ‘true antiestrogens’ are estrogenic and are competitive inhibitors of estrogen action at the estrogen-sensitive target organs. The estrogenicity of a compound needs to be specified with reference to (a) the target tissue, (b) parameter used, (c) route of administration, (d) dose of the compound, (e) time sequence of action. The degree of antiestrogenicity is directly proportional to the, estrogenicity of the compound. The antiestrogenic action of a compound is related to its affinity with the receptor sites in the target organ: (a) compounds which are bound to the receptors for brief periods are weakly estrogenic (DMS, cis-clomiphene), (b) compounds which have greater binding affinity with the receptors in the target organ are strongly estrogenic and antiestrogenic (CN 55, 945–27; trans-clomiphene, DES, MER-25 at high doses). The duration of antiestrogenic action of a compound is related to the duration of its binding with the receptor in the target organ.

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Antifertility Agents

Cited by 37 publications

References 39 publications

Compounds Exhibiting Prolonged Antioestrogenic and Antifertility Activity in Mice and Rats

Compounds Exhibiting Prolonged Antioestrogenic and Antifertility Activity in Mice and Rats

Study of reproductive toxicity of Combretum leprosum Mart and Eicher in female Wistar rats

A Critique on the Evaluation and Mode of Action of Antiestrogens

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