Seratrodast

Description

Seratrodast, a novel benzoquinone derivative, is the first thromboxane A₂ (TxA₂) receptor antagonist to reach the market. It is orally active for the treatment of bronchospastic disorders such as asthma. TxA₂, a metabolite of the arachidonate cascade, is involved in several cardiovascular and respiratory diseases through its potent biological effects on platelet aggregation and constriction of vascular and respiratory smooth muscles. Seratrodast potently inhibits platelet aggregation and bronchoconstriction induced by a TxA₂ mimic and by a variety of spasmogenic prostanoids including PGF_2α, PGD₂ and 9α,11β-PGF₂. Seratrodast shows excellent efficacy in asthma and has been reported to be potentially useful in hyper-responsive disorder. The R-(+)- seratrodast was reported to be the active isomer.

Chemical properties

Pale Orange Solid

Originator

Takeda (Japan)

The Uses of Seratrodast

Thromboxane A2-receptor antagonist. Antiasthmatic.

The Uses of Seratrodast

antibacterial

The Uses of Seratrodast

Thromboxane A2-receptor antagonist. Antiasthmatic

Definition

ChEBI: Seratrodast is an organic molecular entity.

What are the applications of Application

Seratrodast is a potent and selective thromboxane A2 receptor (TP) antagonist

brand name

Bronica

Biological Activity

Thromboxane A 2 (TP) receptor antagonist. Antiasthmatic agent; inhibits platelet aggregation and bronchoconstriction induced by a TXA 2 mimetic in guinea pigs.

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].

References

[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).