Guglietta A, Irons B J, Lazarus L H, Melchiorri P
Endocrinology. 1987 May;120(5):2137-43. doi: 10.1210/endo-120-5-2137.
The amphibian skin heptapeptide dermorphin (DM) administered intracerebroventricularly to rats significantly reduces gastric secretion. Dermorphin and 19 DM homologs and analogs were tested for their effect on gastric volume, pH, H+ ion concentration, and gastric acid output. DM, DM N-terminal pentapeptide and tetrapeptide amides, [D-Met2]DM, [Sar4]DM, [Trp5]DM, [Phe5]DM, [Gly7]DM, [Ser(Bzl)7]DM, and deamidated-DM significantly (P less than 0.01) reduced gastric acid output 2 h after injection. These data provide evidence for the following conclusions on the effect of DM on gastric secretion: ability to inhibit gastric secretion depends on the presence of the D-isomer of Ala at position 2, since [L-Ala2]DM is inactive; the shortest sequence with significant bioactivity is DM N-terminal tetrapeptide amide; the single replacement of amino acid residues in DM elicits a wide range of activities, varying from full biological activity of [Gly7]DM to those analogs with a complete lack of activity, such as [Pro4]DM and [Gly6]DM; and 4) coupling of protective groups to amino and hydroxyl groups of DM results in a significant loss of activity.
向大鼠脑室内注射两栖动物皮肤七肽（ dermorphin, DM）可显著减少胃酸分泌。测试了DM及其19种同系物和类似物对胃容积、pH值、H⁺离子浓度和胃酸分泌量的影响。DM、DM N端五肽和四肽酰胺、[D - Met²]DM、[Sar⁴]DM、[Trp⁵]DM、[Phe⁵]DM、[Gly⁷]DM、[Ser(Bzl)⁷]DM和脱酰胺化 - DM在注射后2小时显著（P < 0.01）降低胃酸分泌量。这些数据为以下关于DM对胃酸分泌影响的结论提供了证据：抑制胃酸分泌的能力取决于2位Ala的D - 异构体的存在，因为[L - Ala²]DM无活性；具有显著生物活性的最短序列是DM N端四肽酰胺；DM中氨基酸残基的单取代引发了广泛的活性，从[Gly⁷]DM的完全生物活性到完全无活性的类似物，如[Pro⁴]DM和[Gly⁶]DM；以及4）DM的氨基和羟基与保护基团偶联会导致活性显著丧失。
