N-Adamantane-substituted tetrapeptide amides and the pharmacologically acceptable salts thereof are disclosed herein. These compounds are analogs of enkephalin wherein the methionine or leucine of position 5 has been substituted by an adamantyl amide and the glycine of position 2 has been substituted by various amino acid residues. Optionally the tyrosine of position 1 and the phenylalanine of position 4 may be substituted by various amino acid residues. These compounds exhibit agonist activity at opiate receptor sites and are useful as analgesics.
本文披露了N-
金刚烷取代的四肽酰胺及其药理学上可接受的盐。这些化合物是
脑啡肽的类似物,其中第5位的蛋
氨酸或亮
氨酸被
金刚烷酰胺替代,第2位的甘
氨酸被各种
氨基酸残基替代。选项地,第1位的
酪氨酸和第4位的苯丙
氨酸可以被各种
氨基酸残基替代。这些化合物在鸦片受体位点表现出激动剂活性,并可用作镇痛剂。