下丘脑产生的促性腺激素释放激素(GnRH)调节垂体前叶促性腺激素(GTH)分泌,从而调节性腺功能。自1971年 Schally与 Guillemin 阐明其结构并人工合成以来,曾试图用它治疗因缺乏 GnRH 而引起的下丘脑性闭经和不育症,并为此合成了数以千计的 GnRH 激动性类似物。但临床工作表明,反复给予大剂量 GnRH 或其激动剂不仅不能使 GTH 低下的患者恢复垂体功能,反能导致正常性腺功能的抑制。在此基础上,近年来对 GnRH 及其激动剂的异相抗生育作用进行了广泛的实验与临床研究,目的在于发展 Hypothalamic gonadotropin-releasing hormone (GnRH) regulates gonadal function by regulating the secretion of the anterior pituitary gonadotropin (GTH). Since 1971, Schally and Guillemin elucidated their structure and synthesized them, attempts have been made to treat hypothalamic amenorrhea and infertility caused by the lack of GnRH and to this end, thousands of GnRH agonistic analogs have been synthesized. However, clinical work shows that repeated administration of large doses of GnRH or its agonists not only fails to restore pituitary function in patients with low GTH, but leads to inhibition of normal gonadal function. On this basis, a wide range of experimental and clinical studies have been conducted on out-of-phase anti-fertility effects of GnRH and its agonists in recent years with the aim of developing