Nillius S J, Bergquist C, Wide L
Int J Fertil. 1980;25(3):239-46.
The stimulatory analogue of luteinizing hormone-releasing hormone (LRH) D-Ser(TBU)6-EA10-LRH was administered subcutaneously (sc) or intranasally to 10 women with amenorrhea and to 44 healthy female and male volunteers. The LRH agonist evoked a pronounced initial release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) but the gonadotropin response decreased during the course of the chronic treatment. Ovulation could not be induced in seven amenorrheic women who were given prolonged treatment with the analogue. In normally ovulating women, ovulation was inhibited during chronic treatment with a daily sc dose of 5 microgram or a daily intranasal dose of 400 microgram. In four healthy men treated with 5 microgram of the LRH agonist daily over 17 weeks basal FSH, LH, and testosterone levels decreased but spermatogenesis and potency were unaffected. The negative effects on testosterone secretion may limit the use of the LRH agonist for male contraception. Chronic intranasal administration of the stimulatory LRH analogue paradoxically inhibited ovulation and proved to be a safe and effective new approach to contraception in women.
将促黄体生成素释放激素（LRH）的刺激类似物D - Ser（TBU）6 - EA10 - LRH皮下或经鼻给予10名闭经女性以及44名健康的女性和男性志愿者。LRH激动剂引发了促卵泡生成素（FSH）和促黄体生成素（LH）明显的初始释放，但在长期治疗过程中促性腺激素反应降低。在接受该类似物长期治疗的7名闭经女性中未能诱导排卵。在正常排卵的女性中，每日皮下注射5微克或每日经鼻给予400微克进行长期治疗期间排卵受到抑制。在4名健康男性中，每天给予5微克LRH激动剂治疗17周，基础FSH、LH和睾酮水平降低，但精子发生和性功能未受影响。对睾酮分泌的负面影响可能会限制LRH激动剂在男性避孕中的应用。长期经鼻给予刺激型LRH类似物反而抑制了排卵，并且被证明是一种安全有效的女性避孕新方法。
