Naqvi T, Raghubir R, Haq W, Tripathi A, Patnaik G K, Mathur K B
Division of Biopolymers, Central Drug Research Institute, Lucknow, India.
Neuropeptides. 1998 Aug;32(4):333-8. doi: 10.1016/s0143-4179(98)90056-7.
Seven new tetrapeptides analogous to (1-4) sequence of dermorphin were synthesized and evaluated for their opioid activity. The peptides were synthesized by the solution phase method. Their opioid activity revealed that peptides II and V were the most potent in the analgesia test as well as in the peripheral assays. Peptide II was most active in the guinea pig ileum assay, whereas peptide VI was 2763 times more selective for mu-receptors.
合成了七种与皮啡肽（1-4）序列类似的新四肽，并对其阿片样活性进行了评估。这些肽通过溶液相法合成。它们的阿片样活性表明，肽II和肽V在镇痛试验以及外周试验中活性最强。肽II在豚鼠回肠试验中活性最高，而肽VI对μ受体的选择性高2763倍。
