Hoet B, Arnout J, Deckmyn H, Vermylen J
Center for Molecular and Vascular Biology, University Leuven, Belgium.
Thromb Haemost. 1993 Nov 15;70(5):822-5.
Ridogrel, a combined thromboxane receptor antagonist and thromboxane synthase inhibitor (1), inhibits platelet aggregation. Following stimulation with arachidonic acid, cAMP-levels are increased in human platelets preincubated with ridogrel, this is due to the known reorientation of the metabolism of the formed endoperoxides towards adenylate cyclase stimulating prostaglandins. Pretreatment of resting platelets with UDCG-212, a cAMP-phosphodiesterase inhibitor (2), also inhibits platele aggregation induced by arachidonic acid, concomitant with an increase in cAMP levels, due to an inhibition of its breakdown. Under basal conditions, cAMP also is increased. By combining the two drugs, a more than additive action was observed on platelet aggregation and on both resting and stimulated platelet cAMP content. The appropriate combination may result in a more effective antiplatelet strategy.
利度格雷是一种血栓素受体拮抗剂和血栓素合酶抑制剂的复方制剂（1），可抑制血小板聚集。在用利度格雷预孵育的人血小板中，花生四烯酸刺激后，环磷酸腺苷（cAMP）水平升高，这是由于已知生成的内过氧化物代谢重新导向刺激腺苷酸环化酶的前列腺素。用cAMP磷酸二酯酶抑制剂UDCG - 212（2）预处理静息血小板，也可抑制花生四烯酸诱导的血小板聚集，同时cAMP水平升高，这是由于其分解受到抑制。在基础条件下，cAMP也会升高。通过联合使用这两种药物，在血小板聚集以及静息和刺激血小板的cAMP含量方面观察到了超相加作用。适当的联合可能会产生更有效的抗血小板策略。
