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hljmmj

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Key results: Pre-incubation of neutrophils with montelukast resulted in dose-related inhibition of the generation of reactive oxygen species and leukotriene B4 by chemoattractant-activated neutrophils, as well as release of elastase, all of which were maximal at 2 mmol·L-1 (mean percentages of the control values of 30  1, 12  3 and 21  3 respectively; P < 0.05). From a mechanistic perspective, treatment of chemoattractant-activated neutrophils with montelukast resulted in significant reduc-
tions in both post-peak cytosolic Ca2+ concentrations and store-operated Ca2+ influx. These montelukast-mediated alterations in Ca2+ handling by the cells were associated with a significant elevation in basal cAMP levels, which resulted from inhibition of cyclic nucleotide phosphodiesterases.
Conclusions and implications: Montelukast, primarily a cysteinyl leukotriene (CysLT1) receptor antagonist, exhibited previously undocumented, secondary, neutrophil-directed anti-inflammatory properties, which appeared to be cAMP-dependent.

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baoshanqiu

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hljmmj: 金币+10, 翻译EPI+1, ★★★★★最佳答案 2016-01-04 09:01:20
主要结果:将中性粒细胞与孟鲁司特预培养导致剂量相关地抑制化学趋化剂激活中性粒细胞活性氧簇和白三烯B4的产生及弹性蛋白酶的释放,所有值均在2 mmol·L-1达高峰(对照值的平均百分率分别为 30.1, 12.3 和 21.3; P < 0.05)。从机理上看,化学趋化剂激活的中性粒细胞经孟鲁斯特处理导致峰后细胞质钙离子浓度和钙池调控钙离子内流均显著减少。这些由孟鲁司特介导的细胞对钙离子处理能力的改变与环核苷酸磷酸二酯酶抑制引起cAMP基础水平显著升高有关。
结论及含意:首先,孟鲁司特作为半胱氨酰白三烯 (CysLT1)受体拮抗剂先前未有报道,其次,对中性粒细胞的抗炎症特性表现为 cAMP依赖性。
2楼2015-12-31 01:40:44
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