Nishihira J, Hayakawa T, Suzuki K, Kato K, Ishibashi T
Department of Biochemistry, Hokkaido University School of Medicine, Sapporo, Japan.
Int Arch Allergy Appl Immunol. 1989;90(3):285-90. doi: 10.1159/000235039.
Azelastine, a newly synthesized antiallergic agent, strikingly inhibited the production of leukotriene B4 and C4 (LTB4 and LTC4) in murine peritoneal cells which had been stimulated by calcium ionophore A23187. The 50% inhibitory concentrations (IC50) of the agent were approximately 1.0 x 10(-5) M. In addition, azelastine significantly inhibited also 5-lipoxygenase activity in peritoneal cells with an IC50 of 1.0 x 10(-5) M, but not on LTC4 synthetase, LTA4 hydrolase or phospholipase A2 activity. Furthermore, azelastine showed little effect on either 12-lipoxygenase activity or thromboxane synthesis in human platelets. These results suggest that at least the drug's antiallergic effects can be attributed to its inhibiting action of 5-lipoxygenase in regard to arachidonate metabolism.
氮卓斯汀是一种新合成的抗过敏药，能显著抑制钙离子载体A23187刺激的小鼠腹腔细胞中白三烯B4和C4（LTB4和LTC4）的产生。该药物的50%抑制浓度（IC50）约为1.0×10⁻⁵M。此外，氮卓斯汀还能显著抑制腹腔细胞中的5-脂氧合酶活性，IC50为1.0×10⁻⁵M，但对LTC4合成酶、LTA4水解酶或磷脂酶A2活性无影响。此外，氮卓斯汀对人血小板中的12-脂氧合酶活性或血栓素合成几乎没有影响。这些结果表明，至少该药物的抗过敏作用可归因于其在花生四烯酸代谢方面对5-脂氧合酶的抑制作用。
