一些京都啡肽-促吞噬肽类似物的镇痛活性。
The analgesic activity of some kyotorphin-tuftsin analogs.
作者信息
Siemion I Z, Kubik A, Nawrocka E, Obuchowicz E, Gołba K, Herman Z S
机构信息
Institute of Chemistry, Wrocław University, Poland.
出版信息
Pol J Pharmacol Pharm. 1990 Mar-Apr;42(2):177-84.
The analgesic potency of the C-terminal dipeptide of tuftsin (Pro-Arg) was found to be much stronger than that of the C-terminal of bradykinin dipeptide Phe-Arg. It was also found that the tripeptide fragment of bradykinin (Pro-Phe-Arg) and its D-Pro analog (D-Pro-Phe-Arg) are deprived of analgesic activity. The attempt to synthesize kyotorphin analogs containing fluorescence label (DMAPhe-Arg and D-DMAPhe-Arg; DMAPhe: 4'-dimethylamino-phenylalanine) resulted in inactive compounds.
发现促吞噬素的C末端二肽（脯氨酸-精氨酸）的镇痛效力比缓激肽二肽苯丙氨酸-精氨酸的C末端强得多。还发现缓激肽的三肽片段（脯氨酸-苯丙氨酸-精氨酸）及其D-脯氨酸类似物（D-脯氨酸-苯丙氨酸-精氨酸）没有镇痛活性。合成含有荧光标记的强啡肽类似物（4'-二甲基氨基苯丙氨酸-精氨酸和D-4'-二甲基氨基苯丙氨酸-精氨酸；4'-二甲基氨基苯丙氨酸：4'-二甲基氨基苯丙氨酸）的尝试得到了无活性的化合物。
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