IC50: 7.4 nM for guinea pig platelets

Seratrodast is a thromboxane A2 (TXA2) receptor antagonist.

Thromboxane A2, a type of thromboxane, is produced by activated platelets and has prothrombotic properties, such as stimulating activation of new platelets and increasing platelet aggregation.

In vitro: Seratrodast was found to inhibit the aggregation of guinea pig platelets induced by a prostaglandin endoperoxide analogue, U-44069 and the specific binding of another analogue, [3H]U-46619 to washed guinea pig platelets. Seratrodast could competitively inhibit the contraction of rabbit aorta and pig coronary arteries induced by U-44069. Seratrodast also inhibited the contraction of rabbit aorta induced by PGF2 alpha and the contraction of pig coronary arteries. However, seratrodast had no effect on the antiaggregatory effect of guinea pig platelets [1].

In vivo: In experiments with guinea pigs, oral seratrodast at 0.1-1 mg/kg could dose-dependently inhibit the platelet aggregation induced by U-44069; the inhibition at 1 mg/kg was 100% at 1 hr and was 89% even at 24 hr after seratrodast administration [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Imura, Y. ,Terashita, Z.,Shibouta, Y., et al. Antagonistic action of AA-2414 on thromboxane A2/prostaglandin endoperoxide receptor in platelets and blood vessels. Japanese Journal of Pharmacology 52(1), 35-53 (1990).