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ONO-1078是一种新型白三烯(LT)拮抗剂,可显著抑制LTC_4、LTD_4诱发的豚鼠支气管收缩;但对LTC_4、LTD_4以及抗原诱发的人游离支气管收缩作用的抑制与反转效应,尚待研究。支气管组织来源于肺癌术者。ONO-1078(10~(-8)M~10~(-6)M)对LTC_4、LTD_4诱发的支气管收缩的抑制作用具有浓度依赖性,浓度-反应曲线平行右移,提示为非竞争性,且这种非竞争性的抑制不受I-丝氨酸硼酸酯复合物(可抑制LTC_4转化为LTD_4)的影响,表明ONO-1078是人气管平滑肌中LTC_4和LTD_4的拮
ONO-1078 is a novel antagonist of leukotriene (LT), which can significantly inhibit bronchoconstriction induced by LTC_4 and LTD_4 in guinea pigs. However, inhibition and reversal effect of LTC_4, LTD_4 and antigen-induced free bronchoconstriction To be studied. Bronchial tissue from lung cancer who. The inhibitory effect of ONO-1078 (10 -8 M 10 -6 M) on bronchoconstriction induced by LTC_4 and LTD_4 was concentration-dependent and the concentration-response curve shifted parallel to the right, indicating a non-competitive, And this noncompetitive inhibition is not affected by the I-serine boronate complex (which inhibits the conversion of LTC_4 to LTD_4), suggesting that ONO-1078 is an antagonist of LTC_4 and LTD_4 in human bronchial smooth muscle