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2-[4-(2-N-哌啶基乙氧基)苯基]-3-苯基(2H)苯并(b)吡喃的生物学特性——一种强效的大鼠抗着床剂。

Biological profile of 2-[4-(2-N-piperidinoethoxy) phenyl]-3-phenyl (2H) benzo (b) pyran--a potent antiimplantation agent in rat.

作者信息

Dhar J D, Setty B S, Duran S, Kapil R S

机构信息

Division of Endocrinology, Central Drug Research Institute, Lucknow, India.

出版信息

Contraception. 1991 Oct;44(4):461-72. doi: 10.1016/0010-7824(91)90036-f.

Abstract

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 activities. The results suggest that the compound exerts its antiimplantation acivity in rat by virtue of its antiestrogenic activity [corrected].

摘要

化合物CDRI-85/287:2-[4-(2-N-哌啶基乙氧基)苯基]-3-苯基(2H)苯并(b)吡喃已被确认为一种对大鼠有效的抗着床剂。在妊娠第1、2或3天单次口服该化合物(2.5毫克/千克体重),或在交配后第5至7天多次给药(0.05毫克/千克/天),均可有效防止妊娠。在交配后第5至7天给药时,即使剂量高达20毫克/千克,也未能终止妊娠。该化合物是一种强效抗雌激素,子宫营养活性非常弱;它不会在未成熟去卵巢大鼠中诱导阴道角化。此外,它没有孕激素、抗孕激素、雄激素、抗雄激素和抗促性腺激素活性。结果表明,该化合物凭借其抗雌激素活性在大鼠中发挥抗着床活性[已修正]。

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