De la Cruz A, Coy D H, Vilchez-Martinez J A, Arimura A, Schelly A V
Science. 1976 Jan 16;191(4223):195-7. doi: 10.1126/science.1108196.
An antagonist of luteinizing hormone-releasing hormone (LH-RH). [D-Phe2-Phe3-D-Phe6]-LH-RH (Phe, phenylalanine), suppressed luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release in male rats in response to LH-RH for at least 4 hours. Three subcutaneous injection of 1 milligram of this antagonist into rats during proestrus completely suppressed ovulation, while a single injection of 1.5 milligrams per rat inhibited 95.3 percent of the preovulatory surge of LH, 84.2 percent of the FSH surge, and suppressed ovulation by 86.4 percent.
促黄体生成素释放激素（LH-RH）的拮抗剂。[D-苯丙氨酸2-苯丙氨酸3-D-苯丙氨酸6]-LH-RH（苯丙氨酸，Phe）可抑制雄性大鼠对LH-RH产生反应时促黄体生成素（LH）和促卵泡激素（FSH）的释放，且这种抑制作用至少持续4小时。在大鼠动情前期皮下注射3次，每次1毫克这种拮抗剂，可完全抑制排卵；而每只大鼠单次注射1.5毫克，则可抑制95.3%的LH排卵前峰、84.2%的FSH峰，并使排卵抑制86.4%。
