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
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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DOI：
10.1111/j.1476-5381.1981.tb16814.x
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发表时间：
1981-01-01
影响因子：
7.3
通讯作者：
LUMLEY, P
中科院分区：
文献类型：
--
作者：
COLEMAN, RA;HUMPHREY, PPA;LUMLEY, P
[1]在一系列离体平滑肌标本上，比较了前列腺素H_2（PGH_2）类似物U-46619和PGH_2对血栓素A_2（TxA_2）的作用。2U-46619对豚鼠肺条、犬隐静脉、大鼠和家兔肺动脉均为强激动剂。相比之下，U-46619对豚鼠回肠和胃底带、猫气管以及犬和猫虹膜括约肌（PGE 2或PGF 2 α是研究的最有效激动剂的制剂）的作用较弱或无活性。3 PGH 2对所有制剂都有活性，并且显示出很小的选择性。在某些制剂中，PGH 2的作用可能通过转化为其他前列腺素类间接介导。[4]与此相反，TxA 2显示出与U-46619相同的选择性模式，对肺条和血管制备物是有效的激动剂，但对其他制备物是弱的或无活性的。[5] U-46619是一种选择性的TxA 2模拟物，因此它应该是研究TxA 2作用的一个有价值的工具。
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.