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更现代的颉抗物随后的工作是继续在第1和2位上的取代,特别是D-苯丙氨酸残基的苯环上予以不同置换的影响,人们发现对氯-多肽具有促进抑制的活性。Channabasavaiah和Stewart报导第1位上乙酰D-氨基酸的取代,包括D-苯丙氨酸,导致良好的抑制物。按照我们的做法,注射低到62微克剂量的N-乙酰D-苯丙,D-对氯苯丙,D-色-LH-RH于丙二醇-生理盐水的溶液或31微克于玉米油的注液,均产生良好的阻断排卵效果。第1位上D-苯丙氨酸被D-对氯苯丙氨酸取代能提高抑制活性约2倍。含对氟苯丙氨酸的多肽约有相等效果。乙酰D-色,D-对氯苯丙,D-苯丙-LH-RH也很活跃。当D-丙氨酸掺入更活跃的顺
Subsequent work by the more modern gui-chi-ku continued the substitution at positions 1 and 2, in particular the substitution of different substitutions on the benzene ring of the D-phenylalanine residue. It was found that the p-chloro-polypeptide has the effect of promoting inhibition Activity. Channabasavaiah and Stewart report that the substitution of acetyl D-amino acids at position 1, including D-phenylalanine, results in a good inhibitor. As per our practice, a solution of N-acetyl D-phenylpropyl, D-p-chlorpropyl, D-color-LH-RH in propylene glycol-saline, or a solution of 31 micrograms of corn oil , Have a good effect of blocking ovulation. Substitution of D-phenylalanine at position 1 with D-p-chlorophenylalanine increased the inhibitory activity by about 2-fold. Equivalent effects on polypeptides containing para-fluorophenylalanine. Acetyl D-color, D-p-chlorpheniramine, D-phenylpropionate-LH-RH are also very active. D-alanine incorporates more active cis