Chorev M, Rubini E, Gilon C, Wormser U, Selinger Z
J Med Chem. 1983 Feb;26(2):129-35. doi: 10.1021/jm00356a003.
Partial retro-inverso modification of a single peptide bond was applied to pGlu-Phe-Phe-Gly-Leu-Met-NH2 (I), a C-terminal hexapeptide analogue of the neuropeptide substance P. Two analogues with reversed peptide bonds, between the pGlu-Phe and Phe-Gly residues, were prepared, purified and characterized. The analogue gpGlu-(RS)-mPhe-Phe-Gly-Leu-Met-NH2 (II) was devoid of either agonistic or antagonistic activity. The second pseudopeptide analogue, i.e., pGlu-Phe-gPhe-mGly-Leu-Met-NH2 (III), was found to be a full agonist with 22% of the potency of I in the guinea pig ileum assay.
对神经肽P物质的C端六肽类似物pGlu-Phe-Phe-Gly-Leu-Met-NH2（I）进行了单个肽键的部分逆反向修饰。制备、纯化并表征了两种在pGlu-Phe和Phe-Gly残基之间具有反向肽键的类似物。类似物gpGlu-(RS)-mPhe-Phe-Gly-Leu-Met-NH2（II）既没有激动活性也没有拮抗活性。发现第二种拟肽类似物，即pGlu-Phe-gPhe-mGly-Leu-Met-NH2（III），在豚鼠回肠试验中是一种完全激动剂，其效力为I的22%。
