孕二烯酮（Gestodene）对大鼠垂体LH的分泌与垂体胞浆孕激素受体结合的影响

The Effect of Gestodene on the Pituitary LH Secretion and Cytosol Progestogenic Receptor in Rat

孕二烯酮（Ｇｅｓｔｏｄｅｎｅ）是一种合成的孕激素，有强抗雌激素活性，为了研究其对生殖激素调节的影响，我们利用垂体对ＧｎＲＨ的激发效应为模型，观察Ｇｅｓｔｏｄｅｎｅ对垂体功能及其垂体孕激素受体结合活性的影响。结果显示：１．Ｇｅｓｔｏｄｅｎｅ处理后大鼠垂体对ＧｎＲＨ激发效应有明显的抑制作用。２．Ｇｅｓｔｏｄｅｎｅ能与垂体胞液孕激素受体相结合，其竞争结合力强于Ｒ５０２０和１８－甲基炔诺酮，由此可见该药物作用对垂体分泌机能的调节有一定程度的影响。

Gestodene is a synthetic progestogenic compound with potent anti-estrogenic activity. The pituitary priming effect model in rat induced by GnRH was used to study the effect of the drug on regulatory function of reproductive endocrine. The results of Gestodene affecting the pituitary function and its binding capacity to progestogenic receptors in pituitary gland were as follows: 1.After treatment with Gestodene the rat pituitary responsiveness to GnRH was inhibited remarkably,the inhibitory extent being much greater than that of Levonorgestrel.2. Gestodene could be bound to the progestogenic receptors in pituitary cytosol,and the binding competitive capacity was morepoment than those of R5020 and Levonorgestrel. It is obvious that Gestodene couldinfluence the pituitary secretory function to a certain extent.