Tai H H, Lee N, Tai C L
Adv Prostaglandin Thromboxane Res. 1980;6:447-52.
Pyridine inhibited the conversion of PG endoperoxide to TXA2 catalyzed by TX synthetase from human platelet and swine lung microsomes. The inhibitory potency of pyridine is abolished by derivatizing pyridine at the 2-position but is increased by introducing hydrophobic substituents at 3- or 4-positions, with 3-substituted pyridines being the most potent inhibitors. Inhibition by pyridine and its derivatives was also selective, since other enzymes in the arachidonic acid cascade were not significantly affected. Pyridine and the active derivatives also inhibited human platelet aggregation induced by arachidonic acid or ADP.
吡啶抑制了由人血小板和猪肺微粒体中的血栓素合成酶催化的前列腺素内过氧化物向血栓素A2的转化。吡啶在2-位衍生化后其抑制效力消失，但在3-或4-位引入疏水取代基后抑制效力增强，其中3-取代吡啶是最有效的抑制剂。吡啶及其衍生物的抑制作用也是具有选择性的，因为花生四烯酸级联反应中的其他酶未受到显著影响。吡啶及其活性衍生物还抑制了由花生四烯酸或二磷酸腺苷诱导的人血小板聚集。
