首页> 美国卫生研究院文献>British Journal of Pharmacology and Chemotherapy >Comparison of the actions of U-46619 a prostaglandin H2-analogue with those of prostaglandin H2 and thromboxane A2 on some isolated smooth muscle preparations.
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Comparison of the actions of U-46619 a prostaglandin H2-analogue with those of prostaglandin H2 and thromboxane A2 on some isolated smooth muscle preparations.

机译:比较前列腺素H2类似物U-46619与前列腺素H2和血栓烷A2在某些分离的平滑肌制剂上的作用。

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摘要

1 The actions of the prostaglandin H2 (PGH2) analogue, U-46619, have been compared with those of PGH2 on thromboxane A2 (TxA2) on a range of isolated smooth muscle preparations in a superfusion cascade system. 2 U-46619 was a potent agonist on guinea-pig lung strip, dog saphenous vein and rat and rabbit aortae. In contrast, U-46619 was weak or inactive on guinea-pig ileum and fundic strip, cat trachea and dog and cat iris sphincter muscles, preparations on which either PGE2 or PGF2 alpha was the most potent agonist studied. 3 PGH2 was active on all of the preparations and displayed little selectivity. On some of the preparations, the actions of PGH2 may have been mediated indirectly by conversion to other prostanoids. 4 In contrast, TxA2 displayed the same pattern of selectivity as U-46619, being a potent agonist on the lung strip and vascular preparations but weak or inactive on the others. 5 It is suggested that U-46619 is a selective TxA2-mimetic and that it should therefore be a valuable tool in the study of the actions of TxA2.
机译:1已将前列腺素H2(PGH2)类似物U-46619的作用与PGH2对血栓烷A2(TxA2)的作用进行了比较,该作用是在超融合级联系统中的一系列分离的平滑肌制剂上进行的。 2 U-46619是豚鼠肺带,犬大隐静脉以及大鼠和兔主动脉的强效激动剂。相比之下,U-46619在豚鼠回肠和胃底条带,猫气管以及狗和猫虹膜括约肌上较弱或没有活性,其中以PGE2或PGF2α为最有效的激动剂。 3 PGH2在所有制剂中均具有活性,并显示出很小的选择性。在某些制剂中,PGH2的作用可能是通过转化为其他类前列腺素间接介导的。 4相反,TxA2表现出与U-46619相同的选择性模式,是在肺带和血管制剂上的强效激动剂,而对其他物质则弱或无活性。 5建议U-46619是一种选择性的TxA2模拟物,因此,它应该是研究TxA2作用的有价值的工具。

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