Biological profile of 2-[4-(2-n-piperidinoethoxy) phenyl]-3-phenyl (2h) benzo (b) pyran — A potent antiimplantation agent in rat

• Published in: Contraception (Stoneham) Vol. 44; no. 4; pp. 461 - 472
• Main Authors: Dhar, J.D., Setty, B.S., Duran, S., Kapil, R.S.
• Format: Journal Article
• Language: English
• Published: New York, NY Elsevier Inc 01.10.1991; Elsevier Science
• Subjects: Animals; Benzopyrans - pharmacology; Benzopyrans - standards; Biological and medical sciences; Birth control; Contraceptives, Postcoital - pharmacology; Contraceptives, Postcoital - standards; Dose-Response Relationship, Drug; Embryo Implantation - drug effects; Estrogen Antagonists - pharmacology; Estrogen Antagonists - standards; Female; Gynecology. Andrology. Obstetrics; Medical sciences; Other methods of contraception. Sterilization; Piperidines - pharmacology; Piperidines - standards; Pregnancy; Rabbits; Rats; Rats, Inbred Strains; Pregnancy; Vertebrata; Mammalia; Postcoital; Rat; Animal; Rodentia; Antiestrogen; Oral administration; Implantation; Contraceptive
• ISSN: 0010-7824; 1879-0518
• DOI: 10.1016/0010-7824(91)90036-F

Compound CDRI-85/287: 2-[4-(2-N-piperidinoethoxy) phenyl]-3-phenyl (2H) benzo (b) pyran has been identified as a potent antiimplantation agent in rat. A single oral dose (2.5 mg/kg body weight) of the compound administered on days 1, 2 or 3 of pregnancy or multiple dosing (0.05 mg/kg daily) on days 5–7 postcoitum effectively prevented pregnancy. When administered on days 5–7 postcoitum, it failed to interrupt pregnancy even at 20 mg/kg dose. The compound is a potent antiestrogen, with very weak uterotrophic activity; it does not induce vaginal cornification in immature ovariectomised rat. Also, it is devoid of progestational, antiprogestational, androgenic, antiandrogenic and antigonadotrophic activity in rat by virtue of its antiestrogenic activity.