کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
3914660 1251480 2011 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Nomegestrol acetate: steroid receptor transactivation profile in Chinese hamster ovary cells and ovulation inhibition in rat and monkey
موضوعات مرتبط
علوم پزشکی و سلامت پزشکی و دندانپزشکی زنان، زایمان و بهداشت زنان
پیش نمایش صفحه اول مقاله
Nomegestrol acetate: steroid receptor transactivation profile in Chinese hamster ovary cells and ovulation inhibition in rat and monkey
چکیده انگلیسی

BackgroundActivity of nomegestrol acetate (NOMAC), levonorgestrel (LNG), drospirenone (DRSP), dienogest (DNG) and progesterone on human steroid receptor transactivation was investigated. Ovulation inhibition by NOMAC, LNG and progesterone was tested.Study DesignThe progestogen receptor profile was determined in Chinese hamster ovary cells transfected with human progesterone B (PRB), androgen, estrogen (ERα and ERβ), glucocorticoid (GR) and mineralocorticoid (MR) receptors, respectively. Ovulation inhibition was tested in rats and monkeys.ResultsAgonistic potency rankings for PRB were LNG=NOMAC≫progesterone≫DRSP>DNG. No antagonistic activity at PRB was observed. Only LNG had androgenic activity. Antiandrogenic potency rankings were LNG≫NOMAC>progesterone>DNG>DRSP. All agents were devoid of activity at ERα, ERβ and GR. Only progesterone, DRSP and LNG had anti-MR activity. The NOMAC dose inhibiting ovulation at 50% ranged from 0.14 mg/kg (monkey) to 1.25 to 5.0 mg/kg (rat).ConclusionNomegestrol acetate is a selective progestogen and a potent inhibitor of ovulation in the rat and monkey.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Contraception - Volume 84, Issue 2, August 2011, Pages 199–204
نویسندگان
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