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首页 > 医学词汇大全 > mifepristone
mifepristone

妇产

关键词妇产 药物 抗孕酮药物

词汇介绍

拓展阅读

解析

mifepristone    [mɪ'fɛprɪ,ston]

释    义   n. 米非司酮;美服培酮

例    句   Objective: To observe the effect and safety of mifepristone in combination with Ethacridine in terminating intermediate pregnancy.

目的:观察米非司酮联合依沙吖啶终止中期妊娠的临床效果及安全性。

概述

米非司酮具有强烈的抗孕酮活性,动物实验表明,米非司酮对孕酮受体的结合力比孕酮高3~5倍。米非司酮主要作用于子宫内膜,在分子水平与内源性孕酮竞争结合受体,产生较强的抗孕酮作用,而产生如下的生理活性:1、竞争性占据蜕膜中孕酮受体,引起孕酮作用撤退,蜕膜组织变性坏死、绒毛继发受损、剥离,引起HCG水平下降,黄体溶解。其机制是米非司酮可直接作用于合体细胞滋养层,引起剂量依赖性HCG、HPL和P生成速率下降。2、促使内源性前列腺素释放,导致子宫收缩。3、同时也作用于下丘脑垂体前叶,促使FSH、LH下降

Resetting the Stress System with a Mifepristone Challenge.复制标题

用米非司酮攻击重置应激系统。

发表时间:2019-05-15

影响因子:3.8

作者: Dalm S

期刊:Cell. Mol. Neurobiol

Psychotic depression is characterized by elevated circulating cortisol, and high daily doses of the glucocorticoid/progesterone antagonist mifepristone for 1 week are required for significant improvement. Using a rodent model, we find that such high doses of mifepristone are needed because the antagonist is rapidly degraded and poorly penetrates the blood-brain barrier, but seems to facilitate the entry of cortisol.  To explain this rapid reset of corticosterone secretion upon recurrent mifepristone administration, we suggest the following: (i) A rebound glucocorticoid feedback after cessation of mifepristone treatment. (ii) Glucocorticoid agonism in transrepression and recruitment of cell-specific coregulator cocktails. (iii) A more prominent role of brain MR function in control of stress circuit activity. An overview table of neuroendocrine MIF effects is provided. The data are of interest for understanding the mechanistic underpinning of stress system reset as treatment strategy for stress-related diseases.

译文

精神病性抑郁症的特征在于循环皮质醇升高,并且需要高剂量的糖皮质激素/孕酮拮抗剂米非司酮1周才能显着改善。使用啮齿动物模型,我们发现需要如此高剂量的米非司酮,因为拮抗剂迅速降解并且很难穿透血脑屏障,但似乎促进了皮质醇的进入。为了解释复发米非司酮给药后皮质酮分泌的快速复位,我们建议如下:(i)米非司酮治疗停止后反弹性糖皮质激素反馈。 (ii)转录抑制和募集细胞特异性共调节剂混合物中的糖皮质激素激动作用。 (iii)脑MR功能在控制应激回路活动中的更突出作用。提供了神经内分泌MIF效应的概述表。这些数据对于理解应力系统重置的机制基础作为压力相关疾病的治疗策略是有意义的。