Sydbom A, Terenius L
Agents Actions. 1985 Apr;16(3-4):269-72. doi: 10.1007/BF01983157.
The basic opioid peptide dynorphin was tested for histamine-releasing activity on peritoneal rat mast cells. Dynorphin was found to induce a dose-dependent histamine release from the mast cells. The threshold concentration was 2 X 10(-7) M and release was maximal (40% of total) at 2 X 10(-6) M of the peptide. The dynorphin-induced histamine release was a very rapid process completed within 10 seconds at 37 degrees C. The release was independent of extracellular calcium. Experiments with naloxone and a specific kappa-agonist (U-50,488H) gave results indicating that the dynorphin induced histamine release was probably not mediated through opioid kappa-receptors. A couple of other Arg-Pro containing peptides of different origin were also screened for histamine-releasing activity. Most of these peptides elicited a more or less pronounced histamine release, provided the peptide contained more than 5 amino acids, suggesting that the Arg-Pro sequence is of importance for the histamine-releasing effect of peptides such as dynorphin.
对基本阿片肽强啡肽进行了对大鼠腹膜肥大细胞组胺释放活性的测试。发现强啡肽可诱导肥大细胞释放组胺，且呈剂量依赖性。阈值浓度为2×10⁻⁷ M，在该肽浓度为2×10⁻⁶ M时释放量最大（占总量的40%）。强啡肽诱导的组胺释放是一个非常快速的过程，在37℃下10秒内即可完成。该释放与细胞外钙无关。用纳洛酮和一种特异性κ激动剂（U-50,488H）进行的实验结果表明，强啡肽诱导的组胺释放可能不是通过阿片κ受体介导的。还对其他几种不同来源的含精氨酸-脯氨酸的肽进行了组胺释放活性筛选。只要这些肽含有超过5个氨基酸，大多数都会或多或少地引起明显的组胺释放，这表明精氨酸-脯氨酸序列对于强啡肽等肽的组胺释放作用很重要。
