Cyclophenil, a non-steroidal compound with a higher central than peripheral oestrogenic activity: study of its effects on uterine growth and on some central parameters in castrated female rats
Celotti, F.; Avogadri, N.; Melcangi, R.C.; Milani, S.; Negri-Cesi, P.
Acta Endocrinologica 107(3): 340-345
1984
ISSN/ISBN: 0001-5598 PMID: 6438973 Document Number: 240400
The estrogenic activity of cyclophenil, a non-steroidal compound which has structural analogies with both stilbene and triphenylethylene, was reevaluated using both central and peripheral parameters. The central parameters considered were LH FSH, prolactin secretion and 2 enzymatic systems known to be estrogen-sensitive: hypophyseal 5.alpha.-reductase and hypothalamic aromatase. The uterine growth test was used to determine estrogenic peripheral activity. The compound was administered at various doses in comparison with estradiol benzoate (EB) to long-term castrated female rats. Cyclophenil has an activity 1/8110 times that of EB on uterine growth, and 1/1660 and 1/550 times that of EB in inhibiting LH and FSH, respectively. The hypophyseal 5.alpha.-reductase (expressed as DHT formation) was inhibited 1710 times less by cyclophenil than by EB. The other parameters considered were unsuitable to provide a statistically reliable estimate of the potency ratios between the 2 compounds. Evidently cyclophenil is an estrogenic compound with peculiar characteristics. This substance is more effective in expressing its estrogenic activity in central structures than in the peripheral ones.