论文部分内容阅读
Norgestimate(NGM)是一种新的具有高度选择性的促孕活性及最低的雄激素活性的孕激素。在家兔,NGM与子宫孕激素受体结合,剌激子宫内膜,抑制排卵。NGM直接作用于靶器官,当注入宫腔的,可剌激家兔子宫内膜,而注入培养中的分散的大鼠垂体细胞中,则抑制LHRH对LH释放的刺激作用。NGM无雌激素活性,相反,与其它孕激素一样,抑制雌激素的作用。而与其它一些孕激素不同的是,NGM相对无雄激素活性。与左旋18甲基炔诺酮(LNG)及gestodene和比,NGM及其17-去乙酰代谢物对雌激素受体的亲和力很弱,当其作为未成熟大鼠前列腺生长的刺激物时,未显示出雄激素活性。NGM缺乏与人类性激素结合球蛋白的亲和力,这一点是其具有最低的雌激素活性的更有力的证据。
Norgestimate (NGM) is a new progestin with a highly selective progestogen activity and lowest androgen activity. In rabbits, NGM binds to uterine progesterone receptors, stimulating the endometrium and inhibiting ovulation. NGM acts directly on the target organ. When injected into the uterine cavity, NGM stimulates the rabbit’s endometrium and injects into dispersed rat pituitary cells in culture to inhibit LHRH stimulation of LH release. NGM has no estrogenic activity, on the contrary, like other progestins, inhibits the action of estrogen. And unlike some other progestins, NGM has relatively no androgenic activity. The affinity of NGM and its 17-deacetyl metabolites for estrogen receptors was weaker than that of LN-18 and gestodene, and when it was used as an irritant to prostatic growth in immature rats, no Show androgen activity. NGM lacks affinity for the human sex hormone-binding globulin, which is evidence that it has the strongest evidence of the lowest estrogenic activity.