醋酸诺美孕酮：在中国仓鼠卵巢细胞中的甾体受体转激活特性和在大鼠与猴中的排卵抑制作用。
Nomegestrol acetate: steroid receptor transactivation profile in Chinese hamster ovary cells and ovulation inhibition in rat and monkey.
机构信息
Women's Health Department, Merck Research Laboratories, Oss, The Netherlands.
出版信息
Contraception. 2011 Aug;84(2):199-204. doi: 10.1016/j.contraception.2010.11.017. Epub 2011 Jan 20.
BACKGROUND
Activity of nomegestrol acetate (NOMAC), levonorgestrel (LNG), drospirenone (DRSP), dienogest (DNG) and progesterone on human steroid receptor transactivation was investigated. Ovulation inhibition by NOMAC, LNG and progesterone was tested.
STUDY DESIGN
The progestogen receptor profile was determined in Chinese hamster ovary cells transfected with human progesterone B (PRB), androgen, estrogen (ER(α) and ER(β)), glucocorticoid (GR) and mineralocorticoid (MR) receptors, respectively. Ovulation inhibition was tested in rats and monkeys.
RESULTS
Agonistic potency rankings for PRB were LNG=NOMAC≫progesterone≫DRSP>DNG. No antagonistic activity at PRB was observed. Only LNG had androgenic activity. Antiandrogenic potency rankings were LNG≫NOMAC>progesterone>DNG>DRSP. All agents were devoid of activity at ER(α), ER(β) and GR. Only progesterone, DRSP and LNG had anti-MR activity. The NOMAC dose inhibiting ovulation at 50% ranged from 0.14 mg/kg (monkey) to 1.25 to 5.0 mg/kg (rat).
CONCLUSION
Nomegestrol acetate is a selective progestogen and a potent inhibitor of ovulation in the rat and monkey.
背景
研究了醋酸诺美孕酮（NOMAC）、左炔诺孕酮（LNG）、屈螺酮（DRSP）、地诺孕素（DNG）和孕酮对人甾体激素受体转激活的作用。测试了 NOMAC、LNG 和孕酮对排卵的抑制作用。
研究设计
在中国仓鼠卵巢细胞中转染人孕激素 B（PRB）、雄激素、雌激素（ER（α）和 ER（β））、糖皮质激素（GR）和盐皮质激素（MR）受体，分别确定孕激素受体谱。在大鼠和猴子中测试排卵抑制。
结果
PRB 的激动效力排名为 LNG=NOMAC≫孕酮≫DRSP>DNG。在 PRB 上未观察到拮抗活性。只有 LNG 具有雄激素活性。抗雄激素效力排名为 LNG≫NOMAC>孕酮>DNG>DRSP。所有药物均无 ER（α）、ER（β）和 GR 活性。只有孕酮、DRSP 和 LNG 具有抗 MR 活性。抑制 50%排卵的 NOMAC 剂量范围为 0.14mg/kg（猴子）至 1.25-5.0mg/kg（大鼠）。
结论
醋酸诺美孕酮是一种选择性孕激素，能有效抑制大鼠和猴子的排卵。
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