Antagonists for gynecological therapy

摘要: Progesterone antagonists (antiprogestions) can completely or partially inhibit progesterone effects at the receptor level. Accordingly, two types of antiprogestins, type I (pure and II (partial agonists) have been proposed. Compounds with absent much reduced represent a special subgroup antiprogestins. Their abortifacient activity is drastically because high partial progestagenic activity. Antiprogestins modulate function receptors in tissue-specific manner. Type antiprogestins interact co-repressors transcription can, therefore, exert inhibitory even presence strong DNA binding PR-antiprogestin complex. On other hand, prevent complex to DNA. The „pure“ be particularly useful for obstetrical indications such as cervical ripening labor induction term. Surprisingly pure induce myometrial responsiveness oxytocic stimuli but uterine PGF2α secretion. This may reason why combination prostaglandins essential. „Pure“ mesoprogestins exhibit antiovulatory activities endometrial proliferation primates. Some compounds complete atrophy endometrium circulating estrogens. effect, which mechanism remains unclear, surprising. There are ongoing studies aimed determine antiprogestin suitable bleeding-free estrogen replacement therapy endometriosis treatment.