Nekola M B, Horvath A, Ge L J, Coy D H, Schally A V
Science. 1982 Oct 8;218(4568):160-2. doi: 10.1126/science.6750790.
A synthetic antagonist of luteinizing hormone-releasing hormone blocked ovulation in rats in a dose-dependent manner when given by gavage on the afternoon of proestrus. Ovulation was delayed for at least 1 day in all animals given 2 milligrams of antogonist and in some of the animals treated with 1 or 0.5 milligram. Oral administration of 2 milligrams also blocked the preovulatory surge of luteinizing hormone. This demonstration that antagonists of luteinizing hormone-releasing hormone can have oral antiovulatory activity clearly enhances their therapeutic potential.
促黄体生成素释放激素的一种合成拮抗剂，在动情前期下午经口给药时，能以剂量依赖方式阻断大鼠排卵。给予2毫克拮抗剂的所有动物以及接受1毫克或0.5毫克治疗的部分动物，排卵至少延迟1天。口服2毫克也能阻断促黄体生成素的排卵前激增。促黄体生成素释放激素拮抗剂具有口服抗排卵活性这一证明，明显提高了它们的治疗潜力。
