血栓素合成酶抑制剂（OKY - 046、OKY - 1580）对豚鼠气管条中支气管活性剂作用及豚鼠肺叶中花生四烯酸代谢的影响。

Effect of thromboxane synthetase inhibitors (OKY-046, OKY-1580) on the action of bronchoactive agents in guinea pig tracheal strips and on arachidonate metabolism in guinea pig lung lobes.

作者信息

Kitamura S, Ishihara Y, Takaku F

出版信息

Prostaglandins Leukot Med. 1984 Jun;14(3):341-50. doi: 10.1016/0262-1746(84)90118-5.

Abstract

We investigated the effect of the thromboxane synthetase inhibitors, OKY-046 and OKY-1580, on the action of bronchoactive agents in guinea pig tracheal strips, and on arachidonic acid metabolism in isolated perfused guinea pig lung lobes. OKY-046 and OKY-1580 attenuated histamine-, serotonin-, acetylcholine-, bradykinin- and prostaglandin F2- induced contractile responses in guinea pig tracheal strips dose-dependently and potentiated isoproterenol-, salbutamol- and prostaglandin E2-induced relaxation in guinea pig tracheal strips dose-dependently. In addition, OKY-046 and OKY-1580 inhibited the biosynthesis of thromboxane A2 and accelerated the production of 6-keto prostaglandin F1 from arachidonic acid in isolated perfused guinea pig lung lobes. The above results suggest that OKY-046 and OKY-1580 might be useful therapeutic agents for the treatment of pulmonary thromboembolism and chronic obstructive lung diseases.

摘要

我们研究了血栓素合成酶抑制剂OKY - 046和OKY - 1580对豚鼠气管条中支气管活性剂作用以及对离体灌注豚鼠肺叶中花生四烯酸代谢的影响。OKY - 046和OKY - 1580剂量依赖性地减弱组胺、5 - 羟色胺、乙酰胆碱、缓激肽和前列腺素F2诱导的豚鼠气管条收缩反应，并剂量依赖性地增强异丙肾上腺素、沙丁胺醇和前列腺素E2诱导的豚鼠气管条舒张反应。此外，OKY - 046和OKY - 1580抑制离体灌注豚鼠肺叶中血栓素A2的生物合成，并加速花生四烯酸生成6 - 酮前列腺素F1。上述结果表明，OKY - 046和OKY - 1580可能是治疗肺血栓栓塞和慢性阻塞性肺疾病的有用治疗药物。