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- W4247560468 abstract "AA-2414, (±)-7-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)-7-phenyl heptanoic acid, inhibited the aggregation of guinea pig platelets induced by a prostaglandin endoperoxide (PGH2) analogue, U-44069 and the specific binding of another analogue, [3H]U-46619 to washed guinea pig platelets with IC50 values of 3.1 × 10−7 and 8.2 × 10−9 M. respectively. AA-2414 competitively inhibited the contraction of rabbit aorta and pig coronary arteries induced by U-44069 with pA2 values of 8.3 and 9.0, respectively. AA-2414 also inhibited the contraction of rabbit aorta induced by PGF2α (pA2: 7.8) and the contraction of pig coronary arteries induced by PGF2α, PGD2 and 9α, 11β-PGF2 with pA2 values of 7.8, 8.6 and 7.8, respectively. But, AA-2414 had no effect on the antiaggregatory effect of PGD2 on the aggregation of guinea pig platelets. In experiments with guinea pigs ex vivo, AA-2414 (0.1–1 mg/kg, p.o.) dose-dependently inhibited the platelet aggregation induced by U-44069; the inhibition at a dose of 1 mg/kg was 100% at 1 hr and was 89% even at 24 hr after the administration. The thromboxane (TX) A2/PGH2 receptor antagonistic action of AA-2414 was stereospecific. These results show that AA-2414 is a potent, orally active and long acting TXA2/PGH2 receptor antagonist. In addition, AA-2414 has PGF2α, PGD2 and 9α,11β-PGF2 antagonistic effects." @default.
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- W4247560468 date "1990-01-01" @default.
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- W4247560468 title "Antagonistic Action of AA-2414 on Thromboxane A2/Prostaglandin Endoperoxide Receptor in Platelets and Blood Vessels" @default.
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- W4247560468 doi "https://doi.org/10.1016/s0021-5198(19)37765-0" @default.
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