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Selective inhibition of thromboxane A2 biosynthesis in blood platelets

Nature volume 267, pages 627–628 (1977)Cite this article

Abstract

SAMUELSSON'S group1,2 showed that human platelets convert arachidonic acid and prostaglandin (PG) endoperoxides3 to thromboxane A2 (TXA2). TXA2 strongly aggregates platelets1 and contracts vascular strips1,4,5. Vane's group5,6 has identified TXA2 synthetase in platelet microsomes—this enzyme generates TXA2 from PG endoperoxides. Aspirin-like drugs inhibit generation of PGs (refs 7, 8) and TXA2 (ref. 9) in platelets at the early stage of cyclooxygenation of arachidonic acid10,11. It is through this activity that aspirin, indomethacin, naproxen and other acidic anti-inflammatory drugs are anti-aggregatory11,12—they have little or no effect on generation of TXA2 from PG endoperoxides6. We report here that the non-acidic anti-inflammatory compound 2-isopropyl-3-nicotinyl-indole (L 8027) (refs 13, 14) is a selective TXA2, synthetase inhibitor in platelets and a potent anti-aggregatory agent.

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Authors and Affiliations

  1. Department of Pharmacology, Copernicus Academy of Medicine in Cracow, 31-531 Cracow, 16, Grzegorzecka, Poland

    R. J. GRYGLEWSKI, A. ZMUDA, R. KORBUT, E. KRECIOCH & K. BIERON

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  1. R. J. GRYGLEWSKI
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GRYGLEWSKI, R., ZMUDA, A., KORBUT, R. et al. Selective inhibition of thromboxane A2 biosynthesis in blood platelets. Nature 267, 627–628 (1977). https://doi.org/10.1038/267627a0

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