• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

血小板血栓素合成的选择性抑制对血小板与内皮下相互作用的影响。

Effects of the selective inhibition of platelet thromboxane synthesis on the platelet-subendothelium interaction.

作者信息

De La Cruz J P, Villalobos M A, Escalante R, Guerrero A, Arrebola M M, Sánchez de La Cuesta F

机构信息

Department of Pharmacology and Therapeutics, School of Medicine, University of Málaga, 29071 Málaga, Spain.

出版信息

Br J Pharmacol. 2002 Dec;137(7):1082-8. doi: 10.1038/sj.bjp.0704963.

DOI:10.1038/sj.bjp.0704963
PMID:12429581
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1573583/
Abstract
  1. Drugs that inhibit TxA(2) synthesis are used to reduce platelet aggregation. The aim of this study was to compare the effects of a cyclo-oxygenase (COX) inhibitor (acetylsalicylic acid, ASA), a thromboxane synthetase (TxS) inhibitor (dazoxiben) and a dual TxS inhibitor and TxA(2) receptor blocker (DT-TX 30) on platelet aggregation and the platelet-subendothelium interaction in flow conditions. 2. The techniques used in this in vitro study were platelet aggregometry in whole blood, and measurement of platelet thromboxane B(2) and prostaglandin E(2) production and leucocyte production of 6-keto-PGF(1alpha). The platelet-subendothelium interaction was evaluated in rabbit aorta subendothelium preparations exposed to flowing blood at a shear stress of 800 s(-1). Morphometric methods were used to calculate the percentage of subendothelium occupied by platelets. 3. The 50% inhibitory concentration (IC(50)) of DT-TX 30 in whole blood was in the range of 10(-7) micro M (induced with collagen or arachidonic acid) to 10(-5) micro M (induced with thrombin) or 10(-4) (induced with ADP). IC(50) values under all experimental conditions were lower with DT-TX 30 than with ASA. For thromboxane B(2) the IC(50) were: ASA 0.84+/-0.05 micro M, dazoxiben 765+/-54 micro M, DT-TX 30 8.54+/-0.60 micro M. Prostaglandin E(2) was inhibited only by ASA (IC(50) 1.21+/-0.08 micro M). Leucocyte 6-keto-PGF(1alpha) was inhibited by ASA (IC(50) 6.58+/-0.76 micro M) and increased by dazoxiben and DT-TX 30. The greatest reduction in percentage subendothelial surface occupied by platelets after blood perfusion was seen after treatment with DT-TX 30 in the range of concentrations that inhibited collagen-induced platelet aggregation (control group: 31.20+/-3.8%, DT-TX 30 at 0.1 micro M: 10.71+/-0.55%, at 1.0 micro M: 6.53+/-0.44%, at 5.0 micro M; 1.48+/-0.07%). All three drugs reduced thrombus formation, although ASA (unlike dazoxiben or DT-TX 30) increased the percentage surface occupied by adhesions. 4. In conclusion, the effect of specific blockage of TxS together with blockage of membrane receptors for TxA(2) can surpass the effect of ASA in inhibiting the platelet-subendothelium interaction in flow conditions.
摘要
  1. 抑制血栓素A2（TxA2）合成的药物用于减少血小板聚集。本研究的目的是比较环氧化酶（COX）抑制剂（阿司匹林，ASA）、血栓素合成酶（TxS）抑制剂（达唑氧苯）以及双重TxS抑制剂和TxA2受体阻滞剂（DT-TX 30）在流动条件下对血小板聚集和血小板与内皮下相互作用的影响。2. 本体外研究采用的技术包括全血血小板聚集测定法，以及测量血小板血栓素B2和前列腺素E2的生成，还有白细胞生成6-酮-前列腺素F1α。在剪切应力为800 s(-1)的流动血液作用下，对兔主动脉内皮下制剂进行血小板与内皮下相互作用的评估。采用形态计量学方法计算血小板占据内皮下的百分比。3. DT-TX 30在全血中的50%抑制浓度（IC50）范围为10(-7) μM（由胶原或花生四烯酸诱导）至10(-5) μM（由凝血酶诱导）或10(-4)（由ADP诱导）。在所有实验条件下，DT-TX 30的IC50值均低于ASA。对于血栓素B2，IC50分别为：ASA 0.84±0.05 μM，达唑氧苯765±54 μM，DT-TX 30 8.54±0.60 μM。前列腺素E2仅被ASA抑制（IC50 1.21±0.08 μM）。白细胞6-酮-前列腺素F1α被ASA抑制（IC50 6.58±0.76 μM），而被达唑氧苯和DT-TX 可增加。在用抑制胶原诱导的血小板聚集的浓度范围内，DT-TX 30处理后，血液灌注后血小板占据内皮下表面的百分比降低最为显著（对照组：31.20±3.8%，0.1 μM的DT-TX 30：10.71±0.55%，1.0 μM：6.53±0.44%，5.0 μM：1.48±0.07%）。所有三种药物均减少血栓形成，尽管ASA（与达唑氧苯或DT-TX 30不同）增加了黏附占据的表面百分比。4. 总之，特异性阻断TxS并同时阻断TxA2的膜受体，在抑制流动条件下血小板与内皮下相互作用方面的效果可超过ASA。

相似文献

1
Effects of the selective inhibition of platelet thromboxane synthesis on the platelet-subendothelium interaction.血小板血栓素合成的选择性抑制对血小板与内皮下相互作用的影响。
Br J Pharmacol. 2002 Dec;137(7):1082-8. doi: 10.1038/sj.bjp.0704963.
2
Effects of camonagrel, a selective inhibitor of platelet thromboxane synthase, on the platelet-subendothelium interaction.血小板血栓素合酶选择性抑制剂卡莫格雷对血小板与内皮下相互作用的影响。
Pharmacology. 2003 Sep;69(1):44-50. doi: 10.1159/000071266.
3
The effect of a thromboxane synthetase inhibitor, dazoxiben, and acetylsalicylic acid on platelet function and prostaglandin metabolism.血栓素合成酶抑制剂达唑氧苯和乙酰水杨酸对血小板功能及前列腺素代谢的影响。
Thromb Haemost. 1983 Oct 31;50(3):703-6.
4
Thromboxane (Tx) A2 receptor blockade and TxA2 synthase inhibition alone and in combination: comparison of anti-aggregatory efficacy in human platelets.血栓素（Tx）A2受体阻断与TxA2合酶抑制单独及联合应用：对人血小板抗聚集疗效的比较
Br J Pharmacol. 1991 Feb;102(2):497-505. doi: 10.1111/j.1476-5381.1991.tb12200.x.
5
Effect of DT-TX 30, a combined thromboxane synthase inhibitor and thromboxane receptor antagonist, on retinal vascularity in experimental diabetes mellitus.血栓素合酶抑制剂与血栓素受体拮抗剂组合DT-TX 30对实验性糖尿病视网膜血管的影响
Thromb Res. 2000 Feb 1;97(3):125-31. doi: 10.1016/s0049-3848(99)00173-5.
6
Effects of Y-20811, a long-lasting thromboxane synthetase inhibitor, on thromboxane production and platelet function.长效血栓素合成酶抑制剂Y-20811对血栓素生成及血小板功能的影响。
Thromb Res. 1986 Aug 15;43(4):455-68. doi: 10.1016/0049-3848(86)90090-3.
7
DTTX30, a combined thromboxane receptor antagonist and thromboxane synthetase inhibitor, prevents coronary thrombosis in anesthetized dogs.DTTX30是一种血栓素受体拮抗剂和血栓素合成酶抑制剂的组合，可预防麻醉犬的冠状动脉血栓形成。
Basic Res Cardiol. 1997 Jun;92(3):181-90. doi: 10.1007/BF00788635.
8
Inhibition of platelet-vessel wall interactions by thromboxane receptor antagonism in a human in vitro system: potentiation of antiplatelet effects of aspirin.在人体体外系统中通过血栓素受体拮抗作用抑制血小板与血管壁的相互作用：增强阿司匹林的抗血小板作用
Eur J Clin Invest. 1998 Jul;28(7):562-8. doi: 10.1046/j.1365-2362.1998.00327.x.
9
In vitro antiplatelet profiles of the new thromboxane synthetase inhibitor sodium 2-(1-imidazolylmethyl)-4,5-dihydrobenzo[b]thiophene-6-carboxylate.新型血栓素合成酶抑制剂2-（1-咪唑基甲基）-4,5-二氢苯并[b]噻吩-6-羧酸钠的体外抗血小板特性
Arzneimittelforschung. 1991 May;41(5):506-10.
10
Potentiation by dazoxiben, a thromboxane synthetase inhibitor, of platelet aggregation inhibitory activity of a thromboxane receptor antagonist and of prostacyclin.血栓素合成酶抑制剂达唑昔班对血栓素受体拮抗剂和前列环素血小板聚集抑制活性的增强作用。
Eur J Pharmacol. 1982 Dec 3;85(3-4):331-3. doi: 10.1016/0014-2999(82)90220-5.

引用本文的文献

1
Licochalcones extracted from Glycyrrhiza inflata inhibit platelet aggregation accompanied by inhibition of COX-1 activity.从胀果甘草中提取的光甘草定抑制血小板聚集，并伴有COX-1活性的抑制。
PLoS One. 2017 Mar 10;12(3):e0173628. doi: 10.1371/journal.pone.0173628. eCollection 2017.

本文引用的文献

1
Effect of aspirin on prostanoids and nitric oxide production in streptozotocin-diabetic rats with ischemic retinopathy.阿司匹林对链脲佐菌素诱导的缺血性视网膜病变糖尿病大鼠前列腺素和一氧化氮生成的影响。
Naunyn Schmiedebergs Arch Pharmacol. 2002 Feb;365(2):96-101. doi: 10.1007/s00210-001-0507-9. Epub 2001 Dec 14.
2
Methods and models to evaluate shear-dependent and surface reactivity-dependent antithrombotic efficacy.评估剪切依赖性和表面反应性依赖性抗血栓形成功效的方法和模型。
Thromb Res. 2001 Nov 1;104(3):149-74. doi: 10.1016/s0049-3848(01)00344-9.
3
Effect of dipyridamole and aspirin on the platelet-neutrophil interaction via the nitric oxide pathway.双嘧达莫和阿司匹林通过一氧化氮途径对血小板-中性粒细胞相互作用的影响。
Eur J Pharmacol. 2000 May 26;397(1):35-41. doi: 10.1016/s0014-2999(00)00245-4.
4
Effect of DT-TX 30, a combined thromboxane synthase inhibitor and thromboxane receptor antagonist, on retinal vascularity in experimental diabetes mellitus.血栓素合酶抑制剂与血栓素受体拮抗剂组合DT-TX 30对实验性糖尿病视网膜血管的影响
Thromb Res. 2000 Feb 1;97(3):125-31. doi: 10.1016/s0049-3848(99)00173-5.
5
Inhibition of platelet-vessel wall interactions by thromboxane receptor antagonism in a human in vitro system: potentiation of antiplatelet effects of aspirin.在人体体外系统中通过血栓素受体拮抗作用抑制血小板与血管壁的相互作用：增强阿司匹林的抗血小板作用
Eur J Clin Invest. 1998 Jul;28(7):562-8. doi: 10.1046/j.1365-2362.1998.00327.x.
6
DTTX30, a combined thromboxane receptor antagonist and thromboxane synthetase inhibitor, prevents coronary thrombosis in anesthetized dogs.DTTX30是一种血栓素受体拮抗剂和血栓素合成酶抑制剂的组合，可预防麻醉犬的冠状动脉血栓形成。
Basic Res Cardiol. 1997 Jun;92(3):181-90. doi: 10.1007/BF00788635.
7
Pulmonary pharmacology of DT-TX 30 SE, a potent selective combined thromboxane synthetase inhibitor and receptor antagonist, in guinea pigs.强效选择性血栓素合成酶抑制剂与受体拮抗剂DT-TX 30 SE在豚鼠体内的肺药理学研究
Jpn J Pharmacol. 1996 Jun;71(2):119-27. doi: 10.1254/jjp.71.119.
8
Effects of aspirin on platelet-neutrophil interactions. Role of nitric oxide and endothelin-1.阿司匹林对血小板-中性粒细胞相互作用的影响。一氧化氮和内皮素-1的作用。
Circulation. 1995 Apr 1;91(7):2080-8. doi: 10.1161/01.cir.91.7.2080.
9
Effects of triflusal and its main metabolite HTB on platelet interaction with subendothelium in healthy volunteers.曲氟尿苷及其主要代谢产物HTB对健康志愿者血小板与内皮下层相互作用的影响。
Eur J Clin Pharmacol. 1995;47(6):497-502. doi: 10.1007/BF00193701.
10
The electronic aggregometer: a novel device for assessing platelet behavior in blood.电子凝集仪：一种评估血液中血小板行为的新型设备。
J Pharmacol Methods. 1980 Feb;3(2):135-58. doi: 10.1016/0160-5402(80)90024-8.