Mezö I, Seprödi J, Erchegyi J, Teplán I, Kovacs M, Flerkó B
Peptides. 1983 Mar-Apr;4(2):149-51. doi: 10.1016/0196-9781(83)90105-5.
Inhibitory analogues of luteinizing hormone-releasing hormone (LH-RH) were prepared with formyl-D-Trp1, acetyl-D-Trp1, valeryl-D-Trp1, tartaryl-D-Trp1, diacetyl-tartaryl-D-Trp1, acetyl-Gly1, and acetyl-Sar1 successively replacing the position one in the analogue [D-Trp1, D-p-Cl-Phe2, D-Trp3, D-Phe6, D-Ala10]-LH-RH. The formyl-D-Trp1 and acetyl-D-Trp1 analogues yielded 100% blockade of ovulation at the 10 micrograms dose; the others were less potent and inhibited ovulation at the 50 micrograms dose. The inhibitory potency seems to correlate with the polarity of the acyl group.
用甲酰基 - D - 色氨酸1、乙酰基 - D - 色氨酸1、戊酰基 - D - 色氨酸1、酒石酰基 - D - 色氨酸1、二乙酰基 - 酒石酰基 - D - 色氨酸1、乙酰基 - 甘氨酸1和乙酰基 - 肌氨酸1依次取代类似物[D - 色氨酸1，D - 对氯苯丙氨酸2，D - 色氨酸3，D - 苯丙氨酸6，D - 丙氨酸10] - 促黄体生成激素释放激素（LH - RH）中的第1位，制备了促黄体生成激素释放激素（LH - RH）的抑制类似物。甲酰基 - D - 色氨酸1和乙酰基 - D - 色氨酸1类似物在10微克剂量时可使排卵完全被阻断；其他类似物活性较低，在50微克剂量时抑制排卵。抑制活性似乎与酰基的极性相关。
