抄録
Acetyl Salicylic Acid (ASA) have been recently used as one of the antithrombotic agents. However it has provided a few problems for the choice of its adequet dose and usage which will inhibit platelet TXA2 synthesis leaving the vascular PGI2 synthesis unimpaired. This paper reports the effect of OKY-1581, pyridine derivatives, which is a new TXA2 synthetase inhibitor, on the platelet aggregation, platelet AA metabolism, and PGI2 generation of vessel wall. The interaction of platelet and vessel wall was also discussed.
OKY-1581 inhibited platelet TXA2 generation, while PGE2, PGD2, and PGF2α synthesis were increased instead, and it inhibited ADP induced secondary aggregation, collagen or AA induced platelet aggregations, while it did not affect PGI2 generation of rat aorta in vitro, but it increased PGI2 generation in vivo.
When TXA2 generation was inhibited by OKY-1581, the increased PG endoperoxides originated from the activated platelet were speculated to be utilized for PGI2 synthesis by bovine arterial microsome.
From these results, it is concluded that OKY-1581 plays an important role as the antithrombotic agents through the inhibition of platelet TXA2 synthesis snd also the enhanced PGI2 generation of vessel wall.
