Ito K, Nose T
Nihon Yakurigaku Zasshi. 1982 Nov;80(5):341-8.
The effects of KB-1043, a new non-steroidal anti-inflammatory agent, on prostaglandin (PG) and SRS-A synthesis were investigated and compared with those of reference drugs. KB-1043 (3 X 10(-5) approximately 3 X 10(-4)M) inhibited the PG synthesis induced by PG synthetase prepared from bovine seminal vesicles. The IC50 value was 1.33 X 10(-4)M. The activity of KB-1043 was less than that of indomethacin, but was about 8 times stronger than that of aspirin. However, KB-1043 (10(-6) and 10(-5)M) did not increase the SRS-A released from sensitized guinea pig lung. With a concentration of 10(-4), KB-1043 decreased the SRS-A release. On the other hand, indomethacin (10(-6) and 10(-5)M), mefenamic acid (10(-6) and 10(-5)M), phenylbutazone (10(-5) and 10(-4)M) and aspirin (10(-4) and 10(-3)M) distinctly increased the SRS-A release from sensitized guinea pig lung.
研究了新型非甾体抗炎药KB - 1043对前列腺素（PG）和慢反应物质A（SRS - A）合成的影响，并与参比药物进行了比较。KB - 1043（3×10⁻⁵ 至 3×10⁻⁴M）抑制了由牛精囊制备的PG合成酶诱导的PG合成。IC50值为1.33×10⁻⁴M。KB - 1043的活性低于吲哚美辛，但比阿司匹林强约8倍。然而，KB - 1043（10⁻⁶和10⁻⁵M）并未增加致敏豚鼠肺释放的SRS - A。在浓度为10⁻⁴时，KB - 1043减少了SRS - A的释放。另一方面，吲哚美辛（10⁻⁶和10⁻⁵M）、甲芬那酸（10⁻⁶和10⁻⁵M）、保泰松（10⁻⁵和10⁻⁴M）和阿司匹林（10⁻⁴和10⁻³M）显著增加了致敏豚鼠肺释放的SRS - A。
