3-二甲基氨基-5-(2',6'-二氯亚苄基)-6-甲基(4H)-哒嗪（PC 89）增强前列环素生物合成并减少血栓素生成
Enhanced prostacyclin biosynthesis and decreased thromboxane formation by 3-dimethylamino 5-(2',6'-dichlorobenzylidene) 6-methyl (4H)-pyridazine (PC 89).
作者信息
Pham H C, Lasserre B, Tronche P, Couquelet J, Dossou-Gbete V, Palhares de Miranda A L
出版信息
Prostaglandins Leukot Med. 1985 Jul;19(1):37-49. doi: 10.1016/0262-1746(85)90159-3.
The effects of 3-dimethylamino 5-(2',6'-dichlorobenzylidene) 6-methyl (4H)-pyridazine (PC 89) on the biosynthesis of PG I2 and TX A2 using horse aorta and horse platelet microsomes as sources of enzymes and arachidonic acid as substrate, were investigated. PC 89 (1.10(-6) M- 1.10(-3) M) dose-dependently - enhanced the biosynthesis of PG I2: the AD50 was 6.8 X 10(-6) M +/- 1.2 X 10(-9) M, the Vmax did not vary significantly with concentrations: PC 89 increased the affinity of enzyme for substrate - but inhibited TX A2 biosynthesis (ID50 = 3.31 X 10(-3) M +/- 4.8 X 10(-7) M): this inhibiting action was not of competitive type. Owing to this dual activity of preventing TX A2 formation and stimulating PG I2 biosynthesis, PC 89 could be a valuable drug for myocardial ischemia and atherosclerosis therapeutics.
以马主动脉和马血小板微粒体作为酶源，花生四烯酸作为底物，研究了3-二甲氨基-5-（2'，6'-二氯亚苄基）-6-甲基（4H）哒嗪（PC 89）对前列环素I2（PG I2）和血栓素A2（TX A2）生物合成的影响。PC 89（1.10（-6）M - 1.10（-3）M）剂量依赖性地增强PG I2的生物合成：半数有效剂量（AD50）为6.8×10（-6）M±1.2×10（-9）M，最大反应速度（Vmax）随浓度变化不显著；PC 89增加了酶对底物的亲和力，但抑制TX A2的生物合成（半数抑制剂量（ID50） = 3.31×10（-3）M±4.8×10（-7）M）：这种抑制作用不是竞争性的。由于PC 89具有防止TX A2形成和刺激PG I2生物合成的双重活性，它可能是治疗心肌缺血和动脉粥样硬化的一种有价值的药物。
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