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  • Title: 13-Azaprostanoic acid: a specific antagonist of the human blood platelet thromboxane/endoperoxide receptor.
    Author: Le Breton GC, Venton DL, Enke SE, Halushka PV.
    Journal: Proc Natl Acad Sci U S A; 1979 Aug; 76(8):4097-101. PubMed ID: 291066.
    Abstract:
    A newly synthesized 13-aza derivative of prostanoic acid (13-APA) specifically inhibited human platelet aggregation induced by arachidonic acid, prostaglandin H2, or the stable endoperoxide analog (15S)-hydroxy-9 alpha,11 alpha-)epoxymethano)-prosta-5Z,13E-dienoic acid. 13-APA also inhibited [14C]serotonin release in response to arachidonic acid, ADP, or thrombin, but did not inhibit primary aggregation induced by ADP or thrombin. 13-APA completely blocked prostaglandin H2-induced aggregation in indomethacin-treated resuspended platelets but did not inhibit thromboxane synthesis. We therefore conclude that 13-APA acts as a direct antagonist of the platelet thromboxane/endoperoxide receptor.
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