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1
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.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。
Br J Pharmacol. 1981 Jul;73(3):773-8. doi: 10.1111/j.1476-5381.1981.tb16814.x.
2
Actions of the novel thromboxane A2 receptor antagonist sodium (E)-11-[2-(5,6-dimethyl-1-benzimidazolyl)-ethylidene]-6,11- dihydrodibenz[b,e]oxepine-1-carboxylate monohydrate on smooth muscle preparations.新型血栓素A2受体拮抗剂(E)-11-[2-(5,6-二甲基-1-苯并咪唑基)-亚乙基]-6,11-二氢二苯并[b,e]氧杂卓-1-羧酸酯钠一水合物对平滑肌制剂的作用
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3
EP 171: a high affinity thromboxane A2-mimetic, the actions of which are slowly reversed by receptor blockade.EP 171:一种高亲和力的血栓素A2模拟物,其作用可通过受体阻断缓慢逆转。
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4
Antagonism of the thromboxane-sensitive contractile systems of the rabbit aorta, dog saphenous vein and guinea-pig trachea.兔主动脉、犬隐静脉和豚鼠气管中血栓素敏感性收缩系统的拮抗作用。
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5
Heterogeneity of thromboxane A2 (TP-) receptors: evidence from antagonist but not agonist potency measurements.血栓素A2(TP-)受体的异质性:来自拮抗剂而非激动剂效价测量的证据。
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6
U-46619, a selective thromboxane A2-like agonist? [proceedings].U - 46619,一种选择性血栓素A2样激动剂?[会议论文集]
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7
Thromboxane A2/prostaglandin H2 directly stimulates platelet shape change independent of secreted ADP.血栓素A2/前列腺素H2直接刺激血小板形态改变,与分泌的ADP无关。
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8
Thromboxane A2/prostaglandin H2 mobilizes calcium in human blood platelets.血栓素A2/前列腺素H2可动员人血小板中的钙。
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BAY u3405, a potent and selective thromboxane A2 receptor antagonist on airway smooth muscle in vitro.BAY u3405,一种在体外对气道平滑肌具有强效且选择性的血栓素A2受体拮抗剂。
Br J Pharmacol. 1991 Nov;104(3):585-90. doi: 10.1111/j.1476-5381.1991.tb12473.x.
10
Characterization of a thromboxane A2/prostaglandin H2 receptor in guinea pig lung membranes using a radioiodinated thromboxane mimetic.使用放射性碘化血栓素类似物对豚鼠肺膜中血栓素A2/前列腺素H2受体的表征
Mol Pharmacol. 1991 Jan;39(1):72-8.

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本文引用的文献

1
A COMPARISON OF THE ACTIONS OF PROSTAGLANDINS F2-ALPHA AND E1 ON SMOOTH MUSCLE.前列腺素F2-α与E1对平滑肌作用的比较
Br J Pharmacol Chemother. 1965 Apr;24(2):470-6. doi: 10.1111/j.1476-5381.1965.tb01736.x.
2
THE USE OF ISOLATED ORGANS FOR DETECTING ACTIVE SUBSTANCES IN THE CIRCULATING BLOOD.利用离体器官检测循环血液中的活性物质
Br J Pharmacol Chemother. 1964 Oct;23(2):360-73. doi: 10.1111/j.1476-5381.1964.tb01592.x.
3
A sensitive method for the assay of 5-hydroxytryptamine.一种测定5-羟色胺的灵敏方法。
Br J Pharmacol Chemother. 1957 Sep;12(3):344-9. doi: 10.1111/j.1476-5381.1957.tb00146.x.
4
Reactions of strips of rabbit aorta to epinephrine, isopropylarterenol, sodium nitrite and other drugs.兔主动脉条对肾上腺素、异丙肾上腺素、亚硝酸钠及其他药物的反应。
J Pharmacol Exp Ther. 1953 Jun;108(2):129-43.
5
U-46619, a selective thromboxane A2-like agonist? [proceedings].U - 46619,一种选择性血栓素A2样激动剂?[会议论文集]
Br J Pharmacol. 1980 Jan;68(1):127P-128P.
6
Isolation and structure of two prostaglandin endoperoxides that cause platelet aggregation.两种引起血小板聚集的前列腺素内过氧化物的分离与结构
Proc Natl Acad Sci U S A. 1974 Feb;71(2):345-9. doi: 10.1073/pnas.71.2.345.
7
Detection and isolation of an endoperoxide intermediate in prostaglandin biosynthesis.前列腺素生物合成中一种内过氧化物中间体的检测与分离。
Proc Natl Acad Sci U S A. 1973 Mar;70(3):899-903. doi: 10.1073/pnas.70.3.899.
8
Evidence for nonadrenergic inhibitory nerves in the guinea pig trachealis muscle.豚鼠气管平滑肌中非肾上腺素能抑制性神经的证据。
Am J Physiol. 1973 May;224(5):1072-80. doi: 10.1152/ajplegacy.1973.224.5.1072.
9
Some biological effects of prostaglandin endoperoxide analogs.前列腺素内过氧化物类似物的一些生物学效应。
Life Sci. 1976 Jan 15;18(2):169-76. doi: 10.1016/0024-3205(76)90021-7.
10
Activity of prostaglandin E, F, A and B on sphincter, dilator and ciliary muscle preparations of the cat eye.前列腺素E、F、A和B对猫眼括约肌、瞳孔开大肌及睫状肌标本的作用
Prostaglandins. 1975 Feb;9(2):157-66. doi: 10.1016/0090-6980(75)90020-9.

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.

DOI:10.1111/j.1476-5381.1981.tb16814.x
PMID:7248665
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2071689/
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。