Effect of the infusion of OKY-046, a thromboxane A2 synthase inhibitor, on urinary metabolites of prostacyclin and thromboxane A2 in healthy human subjects. 1993

H Morio, and A Hirai, and T Terano, and Y Tamura, and S Yoshida
Second Department of Internal Medicine, Chiba University Medical School, Japan.

The influence of OKY-046, a selective thromboxane synthase inhibitor, on prostanoid formation in healthy human subjects was studied. Vehicle (5% glucose solution) or OKY-046 in 5% glucose solution at 15 micrograms kg-1 min-1 was intravenously administered to five male healthy volunteers for 6 h. Platelet aggregation and thromboxane B2 (TXB2) formation induced by collagen and arachidonic acid were suppressed by the infusion of OKY-046, while both were not affected by the infusion of vehicle. Urinary excretion of 11-dehydro-thromboxane B2, one of major urinary metabolites of thromboxane A2 (TXA2) was decreased by the infusion of OKY-046, while that of 2,3-dinor-6-keto-prostaglandin F1 alpha, one of major urinary metabolites of prostacyclin (PGI2) was increased. The present study demonstrated that the infusion of OKY-046 improved the balance of TXA2/PGI2 into antithrombotic state in healthy subjects. It was also suggested that endogenously produced (probably platelet-derived) endoperoxides could be redirected into prostacyclin in vivo.

UI MeSH Term Description Entries
D008297 Male Males
D008689 Methacrylates Acrylic acids or acrylates which are substituted in the C-2 position with a methyl group. Methacrylate
D010974 Platelet Aggregation The attachment of PLATELETS to one another. This clumping together can be induced by a number of agents (e.g., THROMBIN; COLLAGEN) and is part of the mechanism leading to the formation of a THROMBUS. Aggregation, Platelet
D011464 Epoprostenol A prostaglandin that is a powerful vasodilator and inhibits platelet aggregation. It is biosynthesized enzymatically from PROSTAGLANDIN ENDOPEROXIDES in human vascular tissue. The sodium salt has been also used to treat primary pulmonary hypertension (HYPERTENSION, PULMONARY). Prostacyclin,Prostaglandin I2,Epoprostanol,Epoprostenol Sodium,Epoprostenol Sodium Salt, (5Z,9alpha,11alpha,13E,15S)-Isomer,Flolan,Prostaglandin I(2),Veletri
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D013928 Thromboxane A2 An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS). Rabbit Aorta Contracting Substance,A2, Thromboxane
D013929 Thromboxane B2 A stable, physiologically active compound formed in vivo from the prostaglandin endoperoxides. It is important in the platelet-release reaction (release of ADP and serotonin). B2, Thromboxane
D013930 Thromboxane-A Synthase An enzyme found predominantly in platelet microsomes. It catalyzes the conversion of PGG(2) and PGH(2) (prostaglandin endoperoxides) to thromboxane A2. EC 5.3.99.5. Thromboxane Synthetase,Thromboxane A Synthase,Thromboxane A2 Synthetase,A2 Synthetase, Thromboxane,Synthase, Thromboxane A,Synthase, Thromboxane-A,Synthetase, Thromboxane,Synthetase, Thromboxane A2
D015121 6-Ketoprostaglandin F1 alpha The physiologically active and stable hydrolysis product of EPOPROSTENOL. Found in nearly all mammalian tissue. 6-Keto-PGF1 alpha,6-Oxo-PGF1 alpha,6-Oxoprostaglandin F1 alpha,6 Ketoprostaglandin F1 alpha,6 Keto PGF1 alpha,6 Oxo PGF1 alpha,6 Oxoprostaglandin F1 alpha,F1 alpha, 6-Ketoprostaglandin,F1 alpha, 6-Oxoprostaglandin,alpha, 6-Keto-PGF1,alpha, 6-Ketoprostaglandin F1,alpha, 6-Oxo-PGF1,alpha, 6-Oxoprostaglandin F1

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