首页> 美国卫生研究院文献>British Journal of Pharmacology and Chemotherapy >Apomorphine-induced inhibition of histamine release in rat peritoneal mast cells.
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Apomorphine-induced inhibition of histamine release in rat peritoneal mast cells.

机译:阿扑吗啡对大鼠腹膜肥大细胞中组胺释放的抑制作用。

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摘要

The apomorphine-induced inhibition of histamine release in rat peritoneal mast cells was studied by means of secretagogues stimulating different pathways of mast cell activation. Apomorphine inhibited the mast cell response to all releasing agents (lysophosphatidylserine plus nerve growth factor, compound 48/80, substance P, ATP, tetradecanoylphorbolacetate, melittin). The IC50 ranged from 4 microM to 24 microM at concentrations of secretagogues releasing 30-50% of mast cell histamine. However, the potency of the drug decreased at higher secretagogue concentrations. Mast cells, pretreated with apomorphine and washed, released little histamine upon stimulation. The secretory response could be partially restored on increasing the concentration of secretagogues. The results suggest that apomorphine affects a regulatory step controlling the terminal sequence of mast cell secretory activity. As indicated by the reduced potency of the drug, the control by the apomorphine-sensitive reaction loses efficiency under conditions of massive histamine release.
机译:阿朴吗啡诱导的组胺在大鼠腹膜肥大细胞中的抑制作用是通过促泌剂刺激肥大细胞活化的不同途径研究的。阿扑吗啡抑制肥大细胞对所有释放剂的反应(溶血磷脂酰丝氨酸加神经生长因子,化合物48/80,物质P,ATP,十四烷酰佛波乙酸酯,蜂毒肽)。在分泌促泌剂的浓度下,IC50范围从4 microM到24 microM,释放出30-50%的肥大细胞组胺。但是,在较高促分泌剂浓度下,药物的效力会降低。用阿扑吗啡预处理并洗涤的肥大细胞在刺激后几乎不释放组胺。随着促分泌素浓度的增加,分泌反应可以部分恢复。结果表明,阿扑吗啡影响控制肥大细胞分泌活性末端序列的调控步骤。如药物效力降低所表明,在大量组胺释放的条件下,阿扑吗啡敏感反应的控制失去了效率。

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