抑制排卵的孕酮类似物(受体激动剂和拮抗剂):行动的初步证据,不同的网站和机制。

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Heikinheimo O戈登·K·威廉姆斯射频,霍金GD

抑制排卵的孕酮类似物(受体激动剂和拮抗剂):行动的初步证据,不同的网站和机制。

避孕措施。1996年1月,53 (1):55 - 64。

PubMed ID

8631191 (在PubMed

]

文摘

持续管理antiprogesterone RU486抑制排卵的女性和猴子;在这方面RU486可能充当黄体酮受体激动剂而不是对手。我们比较了网站(s)和机制(s)与levonorgestrel RU486-induced排卵抑制(液化天然气)。定期6个月经来潮猕猴每个接受安慰剂,RU486(1毫克/公斤/天)或液化天然气(2 g / kg / d)天(cd)之间的即时消息2-22三个月经周期。血清雌二醇(E2)、孕酮(P4),分析了雄烯二酮、LH和FSH的ria每日血液样本。基底和GnRH-stimulated(1激性腺素释放素注射和50克。2 h)评估了LH和FSH的分泌使用串行血液样本收集12 h cd 10。意思是周期长度延长RU486和液化天然气治疗从32 d到70 d和52个d,分别(p < 0.02)。排卵是抑制在RU486的灵长类动物的六个方面中的五个,并在所有六个液化天然气治疗。RU486治疗期间,血清E2水平类似的控制周期;尽管E2分泌高峰,没有看到LH峰。 In contrast, E2 concentrations were profoundly suppressed during LNG treatment (p < 0.005). The reduction in serum E2 was accompanied by lower levels of androstenedione, and suppressed ratio of E2/androstenedione (p < 0.02) suggesting both reduced synthesis and aromatization of androgen precursors during administration of LNG. Consequently, LNG treatment was associated with higher levels of serum FSH and LH (p < 0.001; 1-way ANOVA). Similarly, as during the luteal phase of the menstrual cycle, the amplitude of basal LH-pulses was increased during LNG treatment (p < 0.05), whereas RU486 treatment did not affect basal LH secretion. The GnRH-stimulated release of LH was similar during the placebo, RU486 and LNG cycles; enhanced release of FSH was seen during administration of LNG. Thus, in the present model system, RU486 seems to inhibit ovulation mainly at the level of hypothalamus, possibly by interfering with the steroidal positive feedback signals from the ovary. However, LNG inhibits ovulation differently, most likely via direct progesterone-like effects on folliculogenesis and the hypothalamus. The pituitary does not appear to be the major site of action(s) of RU486 or LNG. Thus, the differential mechanisms of ovulation inhibition by RU486 and LNG seem to result from lesser intraovarian impact of RU486 as well as dissimilar influences on tonic gonadotropin secretory levels. We conclude that when inhibiting ovulation, RU486 does not act as a progestin agonist, but rather, functions through a hypothalamic mechanism(s), which might be unique to RU486 as a progesterone antagonist.

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药物酶

药物	酶	类	生物	药理作用	行动
甲基炔诺酮	细胞色素P450 19 a1	蛋白质	人类	未知的	抑制剂	细节