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血栓素A2生成特异性抑制剂的测定

Determination of specific inhibitors of thromboxane A2 formation.

作者信息

Ladd N, Lewis G P

出版信息

Br J Pharmacol. 1980 May;69(1):3-5. doi: 10.1111/j.1476-5381.1980.tb10873.x.

DOI:10.1111/j.1476-5381.1980.tb10873.x
PMID:7378655
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2044183/
Abstract

Activation of platelets by contact with collagen leads to the simultaneous formation of a prostaglandin and thromboxane (TXA2), which can be assayed biologically with the superfused rabbit aorta and rat stomach strip. By this method it has been shown that a cyclo-oxygenase inhibitor, aspirin, inhibited formation of both prostaglandin and TXA2 while a specific TXA2 synthetase inhibitor, clotrimazole, inhibited only TXA2 formation. The method is suitable as a primary screen in the search for TXA2 specific synthetase inhibitors.

摘要

血小板与胶原蛋白接触后被激活,会同时生成前列腺素和血栓素(TXA2),这两种物质可用灌注的兔主动脉和大鼠胃条进行生物学检测。通过这种方法已表明,环氧化酶抑制剂阿司匹林可抑制前列腺素和TXA2的生成,而特异性TXA2合成酶抑制剂克霉唑仅抑制TXA2的生成。该方法适合作为寻找TXA2特异性合成酶抑制剂的初步筛选方法。

相似文献

1
Determination of specific inhibitors of thromboxane A2 formation.血栓素A2生成特异性抑制剂的测定
Br J Pharmacol. 1980 May;69(1):3-5. doi: 10.1111/j.1476-5381.1980.tb10873.x.
2
The effects of dipyridamole on TXA2 formation by horse platelet microsomes.双嘧达莫对马血小板微粒体形成血栓素A2的影响。
Prostaglandins Leukot Med. 1983 Feb;10(2):179-85. doi: 10.1016/s0262-1746(83)80008-0.
3
[Thrombocyte interaction with a collagen substrate: the role of thrombocyte-synthesized prostaglandin endoperoxides and thromboxane A2].[血小板与胶原底物的相互作用:血小板合成的前列腺素内过氧化物和血栓素A2的作用]
Biull Eksp Biol Med. 1984 Nov;98(11):563-6.
4
RCS from human platelets: is it only thromboxane?来自人血小板的活性氧物质:仅是血栓素吗?
Eur J Pharmacol. 1983 Nov 11;95(1-2):121-4. doi: 10.1016/0014-2999(83)90275-3.
5
Inhibition of thromboxane A2 biosynthesis in human platelets by burimamide.布立马胺对人血小板中血栓素A2生物合成的抑制作用。
Br J Pharmacol. 1980;71(1):157-64. doi: 10.1111/j.1476-5381.1980.tb10920.x.
6
The platelet-independent release of thromboxane A2 by Paf-acether from guinea-pig lungs involves mechanisms distinct from those for leukotriene.血小板激活因子从豚鼠肺中释放血栓素A2不依赖血小板,其机制与白三烯不同。
Br J Pharmacol. 1984 Jul;82(3):565-75. doi: 10.1111/j.1476-5381.1984.tb10795.x.
7
[The modification of the biosynthesis and effect of thromboxane A2 and prostacyclin by trapidil (Rocornal)].曲匹地尔(心可定)对血栓素A2和前列环素生物合成及作用的影响
Biomed Biochim Acta. 1983;42(2-3):283-99.
8
Effect of calcium concentration and inhibitors on the responses of platelets stimulated with collagen: contrast between human and rabbit platelets.钙浓度和抑制剂对胶原蛋白刺激的血小板反应的影响:人与兔血小板的对比
Comp Biochem Physiol A Comp Physiol. 1991;99(4):551-7. doi: 10.1016/0300-9629(91)90130-5.
9
Influence of selective thromboxane synthetase blocker CGS-13080 on thromboxane and prostacyclin biosynthesis in whole blood: evidence for synthesis of prostacyclin by leukocytes from platelet-derived endoperoxides.选择性血栓素合成酶阻滞剂CGS - 13080对全血中血栓素和前列环素生物合成的影响:白细胞从血小板衍生内过氧化物合成前列环素的证据。
J Lab Clin Med. 1985 Sep;106(3):246-52.
10
Differential effects of aspirin and indomethacin on platelet and leukocyte thromboxane A2 formation.阿司匹林和消炎痛对血小板及白细胞血栓素A2生成的不同作用。
Prostaglandins Leukot Med. 1985 Jun;18(3):379-91. doi: 10.1016/0262-1746(85)90071-x.

引用本文的文献

1
Prostaglandin endoperoxides, thromboxane A2 and adenosine diphosphate in collagen-induced aggregation of rabbit platelets.前列腺素内过氧化物、血栓素A2和二磷酸腺苷在胶原诱导的兔血小板聚集中的作用
Br J Pharmacol. 1982 Apr;75(4):623-31. doi: 10.1111/j.1476-5381.1982.tb09183.x.

本文引用的文献

1
Release of additional factors in anaphylaxis and its antagonism by anti-inflammatory drugs.过敏反应中其他因子的释放及其被抗炎药物的拮抗作用。
Nature. 1969 Jul 5;223(5201):29-35. doi: 10.1038/223029a0.
2
Thromboxanes: a new group of biologically active compounds derived from prostaglandin endoperoxides.血栓素:一类从前列腺素内过氧化物衍生而来的新型生物活性化合物。
Proc Natl Acad Sci U S A. 1975 Aug;72(8):2994-8. doi: 10.1073/pnas.72.8.2994.
3
Identification of an enzyme in platelet microsomes which generates thromboxane A2 from prostaglandin endoperoxides.在血小板微粒体中鉴定出一种可将前列腺素内过氧化物转化为血栓素A2的酶。
Nature. 1976 Jun 17;261(5561):558-60. doi: 10.1038/261558a0.
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In vivo method for quantitation for anti-platelet potency of drugs.
Naunyn Schmiedebergs Arch Pharmacol. 1978 Mar;302(1):25-30. doi: 10.1007/BF00586592.
5
Imidazole: a selective inhibitor of thromboxane synthetase.咪唑:一种血栓素合成酶的选择性抑制剂。
Prostaglandins. 1977 Apr;13(4):611-8. doi: 10.1016/0090-6980(77)90232-5.
6
ADP metabolism in vascular tissue, a possible thrombo-regulatory mechanism.血管组织中的ADP代谢,一种可能的血栓调节机制。
Thromb Res. 1979;14(6):901-14. doi: 10.1016/0049-3848(79)90008-2.