Duration of anti-implantation action of the triphenylethylene anti-oestrogen centchroman in adult female rats.
The duration of the anti-implantation action of a single oral post-coital dose (1.25 mg kg-1) of a triphenylethylene anti-oestrogen, centchroman, was determined in adult rats. The effects of centchroman were compared with those of tamoxifen. In rats undergoing delay, centchroman administered orally on day 7 post-coitum prevented the induction of implantation of delayed blastocysts by an implantation inducing dose (1 micrograms per rat, s.c.) of oestrone which was administered earlier than 120 h after centchroman treatment. In tamoxifen (0.2 mg kg-1, orally) pretreated rats, oestrone administered at 144 h or later induced implantation. In cyclic rats treated with centchroman at intervals of 168 h and mated with males of proven fertility, implantation was prevented only when the interval between centchroman treatment and nidatory oestrogen secretion was less than 120 h. None of the females conceived when treated regularly at intervals of 120 h during exposure to fertile males. Discontinuation of treatment resulted in the occurrence of normal implantations in rats that mated 48 h or later after the last dose of centchroman, since in these animals the interval between anti-oestrogen treatment and nidatory oestrogen secretion was greater than 120 h. These findings suggest that the duration of the anti-implantation action of a single oral antifertility dose of centchroman in rats is about 120 h. Recovery of normal blastocysts from rats treated continuously with this dose of centchroman at these intervals suggests lack of significant effect on follicular maturation, ovulation, fertilization, preimplantation development or mating behaviour.(ABSTRACT TRUNCATED AT 250 WORDS)
Central Drug Research Institute, Lucknow, India.
M M
MM
Singh
S
S
Sreenivasulu
V P
VP
Kamboj
D000284:Administration, Oral; D000818:Animals; D002486:Centchroman / Q000008:administration & dosage / Q000494:pharmacology*; D010064:Embryo Implantation / Q000187:drug effects*; D010065:Embryo Implantation, Delayed / Q000187:drug effects; D005260:Female; D051381:Rats; D017207:Rats, Sprague-Dawley; D013629:Tamoxifen / Q000494:pharmacology; D013997:Time Factors
D013629:Tamoxifen; D002486:Centchroman