Rivier C, Rivier J, Vale W
Endocrinology. 1981 May;108(5):1998-2001. doi: 10.1210/endo-108-5-1998.
Daily treatment with 1 mg of the GnRH antagonist [Ac-delta 3-Pro1,pC1-D-Phe2,D-Trp3,6,N alpha MeLeu7]-GnRH abolished mating behavior and disrupted spermatogenesis in male rats within 2 weeks. This was accompanied by a sharp decrease in plasma testosterone (T) levels as well as sexual organ weights while body weight remained normal. Following cessation of treatment, T levels returned to control values within 5 days, while sexual organ weights were still slightly depressed after 6 weeks. In rats having been treated for either 2 weeks or 4 months, mating behavior and fertility were restored between the 4th and 8th week after the last injection. Antagonist-treated animals who concomitantly received high doses of exogenous testosterone were sexually active as well as fertile, while lower doses of testosterone maintained sexual activity but not fertility. These data indicate that GnRH antagonists may be used to control male fertility.
每天用1毫克促性腺激素释放激素（GnRH）拮抗剂[Ac-δ3-Pro1，pC1-D-Phe2，D-Trp3,6，Nα-MeLeu7]-GnRH对雄性大鼠进行治疗，在2周内可消除其交配行为并破坏精子发生。这伴随着血浆睾酮（T）水平以及性器官重量的急剧下降，而体重保持正常。停止治疗后，T水平在5天内恢复到对照值，而6周后性器官重量仍略有降低。在接受2周或4个月治疗的大鼠中，末次注射后第4至8周交配行为和生育能力得以恢复。同时接受高剂量外源性睾酮治疗的拮抗剂处理动物具有性活性且可育，而较低剂量的睾酮可维持性活动但不能维持生育能力。这些数据表明GnRH拮抗剂可用于控制雄性生育能力。
