Duration of antiestrogenecity of compound CDRI-85/287: a new orally active nonsteroidal antiimplantation agent
Sreenivasulu, S.; Singh, M.M.; Dwivedi, A.; Setty, B.S.; Kamboj, V.P.
Indian Journal of Experimental Biology 30(11): 968-971
1992
ISSN/ISBN: 0019-5189 PMID: 1293041 Document Number: 404919
Duration of antiestrogenic and antiimplantation action of CDRI-85/287, (2-(4-(2-N-piperidino)ethoxy phenyl)-3-phenyl(2H)benzo(2)pyran), was studied in rat. Pretreatment of ovariectomized immature rats with this compound caused translocation of cytoplasmic estrogen receptor (ER) to the nucleus and a marked depletion of cytoplasmic ER pool resulting in a nonresponsive state of the uterus to subsequent estrogen administration until day 4. While in rats pretreted with estradiol, increased cytoplasmic ER level made the uterus responsive to a second injection of estrogen. In the delayed implantation model, 85/287 pretreated rats were given estrone on days 4,5 or 6 post-antiestrogen treatment. No implantations were observed after estrone administration on day 4, but were present when estrone was given on days 5 or 6. Summation of these results suggests the duration of action of 85/287 to be 3-4 days in rat.