Antifertility potential of 2-[piperdinoethoxyphenyl]-3-[4- methoxyphenyl]-2H benzopyran: a potent anti-oestrogenic compound in rats.
The present study was carried out to investigate the artifertility potential of 2-[piperdinoethoxyphenyl]-3-[4-methoxyphenyl]-2H benzopyran (K-7) in rats. A single oral administration of 250 micrograms K-7 kg-1 body mass after coitus prevented pregnancy in rats. The minimum effective dose in rats given K-7 orally for 1-4 days after coitus was 100 micrograms kg-1 body mass. K-7 had weak oestrogenicity in ovariectomized immature rats but had no androgenic or anti-gonadotrophic activity. Studies in vivo showed that K-7 was a potent anti-oestrogenic compound and that at 100 micrograms kg-1 it could mitigate the effect of 1.0 microgram oestradiol. On the basis of the above results, K-7 appeared to exert its antifertility action(s) by its weak oestrogenic and its strong anti-oestrogenic activity. The anti-oestrogenic activity of K-7 was substantiated further by performing studies on the competition of K-7 for binding of [3H]oestradiol to rat uterine oestrogen receptors. A high affinity for binding to oestrogen receptors was displayed by K-7, with a relative binding affinity of 71%. These findings show that K-7 is an effective anti-oestrogenic compound and is a potent antifertility agent.
Singh
R
R
Centre for Cellular and Molecular Biology, Hyderabad, India.
D000818:Animals; D001578:Benzopyrans / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001667:Binding, Competitive; D003280:Contraceptives, Oral, Synthetic / Q000378:metabolism / Q000494:pharmacology*; D004958:Estradiol / Q000378:metabolism; D004965:Estrogen Antagonists / Q000378:metabolism / Q000494:pharmacology*; D004967:Estrogens / Q000494:pharmacology; D005260:Female; D008297:Male; D010052:Ovariectomy; D010880:Piperidines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011960:Receptors, Estrogen / Q000378:metabolism; D014599:Uterus / Q000378:metabolism
D001578:Benzopyrans; D003280:Contraceptives, Oral, Synthetic; D004965:Estrogen Antagonists; D004967:Estrogens; D010880:Piperidines; D011960:Receptors, Estrogen; C099947:2-(4-(2-piperidinoethoxy)phenyl)-3-(4-methoxyphenyl)-2H-benzopyran; D004958:Estradiol