13-氮杂前列腺酸：一种人血小板血栓素/内过氧化物受体的特异性拮抗剂。
13-Azaprostanoic acid: a specific antagonist of the human blood platelet thromboxane/endoperoxide receptor.
作者信息
Le Breton G C, Venton D L, Enke S E, Halushka P V
出版信息
Proc Natl Acad Sci U S A. 1979 Aug;76(8):4097-101. doi: 10.1073/pnas.76.8.4097.
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.
摘要
一种新合成的前列腺酸13-氮杂衍生物（13-APA）特异性抑制由花生四烯酸、前列腺素H2或稳定的内过氧化物类似物（15S）-羟基-9α，11α-（环氧亚甲基）-前列腺-5Z，13E-二烯酸诱导的人血小板聚集。13-APA还抑制因花生四烯酸、ADP或凝血酶引起的[14C]5-羟色胺释放，但不抑制由ADP或凝血酶诱导的初始聚集。13-APA完全阻断了吲哚美辛处理的重悬血小板中前列腺素H2诱导的聚集，但不抑制血栓素的合成。因此，我们得出结论，13-APA作为血小板血栓素/内过氧化物受体的直接拮抗剂发挥作用。
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