Corbin A, Beattie C W, Yardley J, Foell T J
Endocr Res Commun. 1976;3(6):359-76. doi: 10.3109/07435807609073910.
An analogue of synthetic hypothalamic LRH, D-[ALA]6-DES-[GLY]10-PRO9-ethylamide-LRH (Wy-18,481) was evaluated for agonistic (in vivo LH-releasing and ovulation-inducing), post-coital contraceptive and reproductive target organ effects. Both LRH and the analogue terminated pregnancy; there appeared to be a direct relationship between agonistic and post-coital contraceptive potency and activity. The analogue proved to be a potent agonist and both a pre-and post-implantational post-coital anti-fertility agent. In contrast to LRH, the congener did not produce a uterotrophic effect in the hypophysectomized rat. The data suggest that agonist analogue(s) of LRH can terminate pregnancy via hyperstimulation of the pituitary-ovarian-reproductive complex and the use of members of this neurohormonal class as potential clinical pro-fertility agents should be weighted with caution.
对合成下丘脑促黄体激素释放激素(LRH)的类似物D-[丙氨酸]6-去-[甘氨酸]10-脯氨酸9-乙酰胺-LRH(Wy-18,481)进行了激动作用(体内促黄体生成素释放和诱导排卵)、性交后避孕及生殖靶器官效应的评估。LRH及其类似物均能终止妊娠;激动作用与性交后避孕效力和活性之间似乎存在直接关系。该类似物被证明是一种强效激动剂,并且是植入前和植入后性交后抗生育剂。与LRH不同,该同系物在垂体切除的大鼠中未产生子宫肥大效应。数据表明,LRH激动剂类似物可通过过度刺激垂体-卵巢-生殖复合体来终止妊娠,将这类神经激素成员用作潜在的临床促生育剂时应谨慎权衡。