Сератродаст

Описание

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.

Химические свойства

Pale Orange Solid

Биологическая активность

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