title: CDRI-85/287: studies on competition to estrogen binding sites in the immature rat uterus.
abstract: Ability of compound CDRI-85/287, a new nonsteroidal antiestrogen with negligible inherent estrogenicity, to inhibit uptake of 3H-estradiol (3H-E2) by the immature rat uterus in vivo was investigated. Different doses of 85/287 were administered either intraperitoneally 30 min before 3H-E2 or orally 1 and 6 hr before 3H-E2. A dose dependent inhibition in 3H-E2 uptake was observed after administration of the compound by either route and was 69% at 50 micrograms/rat ip dose and 80% at 2.5 mg/kg po dose. In in vitro competitive binding assay, however, the compound showed poor affinity (RBA 0.42% of estradiol-17 beta) for cytosolic estrogen receptors. Considering the potent anti-estrogenic as well as anti-implantation efficacy of the compound, its action in vivo appears to be mediated via its active metabolite(s).
authors.affiliation: Division of Endocrinology, Central Drug Research Institute, Lucknow, India.
authors.forename: S
authors.initials: S
authors.lastname: Sreenivasulu
authors.forename: A
authors.initials: A
authors.lastname: Dwivedi
authors.forename: M M
authors.initials: MM
authors.lastname: Singh
authors.forename: B S
authors.initials: BS
authors.lastname: Setty
authors.forename: V P
authors.initials: VP
authors.lastname: Kamboj
mesh_terms: D000818:Animals; D001578:Benzopyrans / Q000494:pharmacology*; D001665:Binding Sites; D001667:Binding, Competitive; D003600:Cytosol / Q000378:metabolism; D004958:Estradiol / Q000378:metabolism*; D004965:Estrogen Antagonists / Q000494:pharmacology*; D005260:Female; D007700:Kinetics; D010880:Piperidines / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011960:Receptors, Estrogen / Q000187:drug effects / Q000378:metabolism; D014599:Uterus / Q000187:drug effects / Q000378:metabolism*
chemical_list: D001578:Benzopyrans; D004965:Estrogen Antagonists; D010880:Piperidines; D011960:Receptors, Estrogen; C066624:CDRI 85-287; D004958:Estradiol