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前列腺素H2类似物U-46619与前列腺素H2及血栓素A2对某些离体平滑肌制剂作用的比较。

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.

作者信息

Coleman R A, Humphrey P P, Kennedy I, Levy G P, Lumley P

出版信息

Br J Pharmacol. 1981 Jul;73(3):773-8. doi: 10.1111/j.1476-5381.1981.tb16814.x.

Abstract

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.

摘要
  1. 在一个灌注级联系统中,已将前列腺素H2(PGH2)类似物U - 46619的作用与PGH2以及血栓素A2(TxA2)在一系列离体平滑肌制剂上的作用进行了比较。2. U - 46619对豚鼠肺条、犬隐静脉以及大鼠和兔主动脉是一种强效激动剂。相比之下,U - 46619对豚鼠回肠和胃底条、猫气管以及犬和猫虹膜括约肌肌肉作用较弱或无活性,而在这些制剂上,PGE2或PGF2α是所研究的最有效的激动剂。3. PGH2对所有制剂均有活性,且几乎没有选择性。在某些制剂上,PGH2的作用可能是通过转化为其他前列腺素间接介导的。4. 相比之下,TxA2表现出与U - 46619相同的选择性模式,对肺条和血管制剂是强效激动剂,但对其他制剂作用较弱或无活性。5. 提示U - 46619是一种选择性TxA2模拟物,因此它应是研究TxA2作用的一种有价值的工具。

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