Phillips A, Hahn D W, McGuire J L
R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869-0602.
Am J Obstet Gynecol. 1992 Oct;167(4 Pt 2):1191-6. doi: 10.1016/s0002-9378(12)90410-x.
Norgestimate is a novel progestin with highly selective progestational activity and minimal androgenicity. In rabbits, norgestimate binds to uterine progestin receptors, stimulates the endometrium, and inhibits ovulation. Norgestimate acts directly on target organs, stimulating rabbit endometrium when injected into the uterine cavity and inhibiting luteinizing hormone-releasing hormone-stimulated luteinizing hormone release in dispersed rat pituitary cells in culture. Norgestimate has no estrogenic activity, and like other progestins, it suppresses the action of estrogen. Unlike some other progestins, it is relatively free of androgenic activity. Norgestimate and its 17-deacetylated metabolite demonstrate very poor affinity for androgen receptors compared with levonorgestrel and gestodene and do not exhibit androgenic activity when measured as the stimulation of prostatic growth in immature rats. Norgestimate's lack of affinity for human sex hormone-binding globulin is further evidence of its minimal androgenicity.
诺孕酯是一种新型孕激素，具有高度选择性的孕激素活性且雄激素活性极小。在兔子身上，诺孕酯与子宫孕激素受体结合，刺激子宫内膜，并抑制排卵。诺孕酯直接作用于靶器官，注入子宫腔时可刺激兔子子宫内膜，并在培养的分散大鼠垂体细胞中抑制促黄体生成激素释放激素刺激的促黄体生成激素释放。诺孕酯无雌激素活性，与其他孕激素一样，它会抑制雌激素的作用。与其他一些孕激素不同，它相对没有雄激素活性。与左炔诺孕酮和孕二烯酮相比，诺孕酯及其17-脱乙酰代谢产物对雄激素受体的亲和力非常低，在以未成熟大鼠前列腺生长刺激来衡量时，不表现出雄激素活性。诺孕酯对人性激素结合球蛋白缺乏亲和力，这进一步证明了其极小的雄激素活性。
