Platelet and cardiovascular activity of the hydantoin BW245C, a potent prostaglandin analogue

https://doi.org/10.1016/0090-6980(83)90105-3Get rights and content

Abstract

The platelet anti-aggregating, cardiovascular and gastro-intestinal actions of a hydantoin prostaglandin analogue, BW245C have been compared with prostaglandin and PGD2 several species. In human plasma in vitro, BW245C was 0.2 times as active as prostacyclin and 8 times as active as PGD2 in inhibiting platelet aggregation. In rat and rabbit plasma, BW245C was only weakly active but was more potent in sheep and horse plasma. Since the acivity of PGD2 varied in a parallel fashion, BW245C may interactive with PGD2 binding sites on platelets. The potency of BW245C as a vasodepressor also varied between species, being 0.5, 0.1, 0.06 and < 0.02 times as active as prostacyclin in the aneasthetised dog, monkey, rat and rabbit respectively.

The relative activity of BW245C as an inhibitor of platelet aggregation ex vivo was more comparable, being 0.08, 0.04 and 0.05 times as active as prostacyclin following intravenous infusion in the rabbit dog and monkey respectively. In the rabbit, BW245C was a highly selective platelet inhibitor with minimal cardiovascular actions, whereas in the dog and monkey, BW245C lowered BP in anti-aggregating doses. The potent platlet anti-aggregating actions of BW245C following parenteral or oral administration makes this hydantoin a potentially-useful anti-thrombotic prostaglandin analogue.

References (20)

There are more references available in the full text version of this article.

Cited by (0)

View full text