Department of Chemistry "G. Ciamician", University of Bologna , via Selmi 2, 40126 Bologna, Italy.
J Med Chem. 2014 Aug 14;57(15):6861-6. doi: 10.1021/jm5002925. Epub 2014 Jul 30.
The noncationizable tripeptide Ac-D-Trp-Phe-GlyNH2 was recently proposed as a novel minimal recognition motif for μ-opioid receptor. The introduction of different substituents (methyl, halogens, nitro, etc.) at the indole of D-Trp significantly influenced receptor affinities and resulted in serum stability and in a measurable effect on central antinociception in mice after ip administration.
最近，非离子化三肽 Ac-D-Trp-Phe-GlyNH2 被提出作为 μ 阿片受体的新型最小识别基序。在 D-Trp 的吲哚上引入不同的取代基（甲基、卤素、硝基等）会显著影响受体亲和力，并导致其在血清中的稳定性以及在腹腔给药后对小鼠中枢性镇痛作用的可测量影响。
