阿扑吗啡对大鼠腹膜肥大细胞组胺释放的抑制作用。
Apomorphine-induced inhibition of histamine release in rat peritoneal mast cells.
作者信息
Battistella A, Boarato E, Bruni A, Mietto L, Palatini P, Toffano G
出版信息
Br J Pharmacol. 1986 Jun;88(2):457-62. doi: 10.1111/j.1476-5381.1986.tb10224.x.
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.
通过刺激肥大细胞激活不同途径的促分泌剂，研究了阿扑吗啡对大鼠腹膜肥大细胞组胺释放的抑制作用。阿扑吗啡抑制肥大细胞对所有释放剂（溶血磷脂酰丝氨酸加神经生长因子、化合物48/80、P物质、ATP、十四酰佛波醇乙酸酯、蜂毒肽）的反应。在释放30 - 50%肥大细胞组胺的促分泌剂浓度下，IC50范围为4 microM至24 microM。然而，在更高的促分泌剂浓度下，该药物的效力降低。用阿扑吗啡预处理并洗涤后的肥大细胞，在刺激时释放的组胺很少。增加促分泌剂浓度可部分恢复分泌反应。结果表明，阿扑吗啡影响控制肥大细胞分泌活动终末序列的调节步骤。正如该药物效力降低所表明的，在大量组胺释放的情况下，阿扑吗啡敏感反应的控制失去效率。
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