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对大唑昔本进行人工循环中的血小板抑制作用研究。

Dazoxiben examined for platelet inhibitory effect in an artificial circulation.

作者信息

Goldman M, Hall C, Hawker R J, McCollum C N

出版信息

Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):61S-65S. doi: 10.1111/j.1365-2125.1983.tb02109.x.

DOI:10.1111/j.1365-2125.1983.tb02109.x
PMID:6681706
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1427697/
Abstract

1 Platelet inhibitory therapy may protect patency in prosthetic arterial grafts. 2 The effect of the thromboxane synthetase inhibitor dazoxiben (UK 37248) on 113Indium-labelled platelet deposition on Dacron arterial grafts was examined in an artificial circulation containing human blood which mimics the haemodynamics of femoropopliteal bypass. The influence of this drug on thromboxane production and platelet reactivity was measured during the experiment. The study was controlled and performed in two parts to assess in vitro and ex vivo drug effect. 3 Both in vitro and ex vivo dazoxiben reduced plasma thromboxane by about 80% and in citrated ex vivo blood increased mean (+/- s.e. mean) platelet aggregation threshold to collagen from control values of 4.8 +/- 1.7 mg/ml to 10.6 +/- 3.3 mg/ml (P less than 0.01). Dazoxiben, however, had no effect on platelet deposition on the arterial grafts. 4 Selective thromboxane inhibition failed to exert an antithrombotic effect in this model.

摘要
  1. 血小板抑制疗法可能会保护人工动脉移植物的通畅性。2. 在模拟股腘动脉旁路血流动力学的含人血人工循环中,研究了血栓素合成酶抑制剂达唑氧苯(UK 37248)对113铟标记的血小板在涤纶动脉移植物上沉积的影响。实验过程中测量了该药物对血栓素生成和血小板反应性的影响。该研究分为两部分进行对照,以评估体外和体内药物效果。3. 在体外和体内,达唑氧苯均使血浆血栓素降低约80%,在枸橼酸化的体内血液中,使胶原诱导的平均(±标准误)血小板聚集阈值从对照值4.8±1.7mg/ml提高到10.6±3.3mg/ml(P<0.01)。然而,达唑氧苯对动脉移植物上的血小板沉积没有影响。4. 在该模型中,选择性血栓素抑制未能发挥抗血栓作用。

相似文献

1
Dazoxiben examined for platelet inhibitory effect in an artificial circulation.对大唑昔本进行人工循环中的血小板抑制作用研究。
Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):61S-65S. doi: 10.1111/j.1365-2125.1983.tb02109.x.
2
Effects of thromboxane synthetase inhibition on arachidonate metabolism and platelet behaviour.血栓素合成酶抑制对花生四烯酸代谢及血小板行为的影响。
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Effect of dazoxiben on arterial graft thrombosis in the baboon.达唑氧苯对狒狒动脉移植物血栓形成的影响。
Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):57S-60S. doi: 10.1111/j.1365-2125.1983.tb02108.x.
4
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.
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6
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Br J Clin Pharmacol. 1983;15 Suppl 1(Suppl 1):79S-82S. doi: 10.1111/j.1365-2125.1983.tb02113.x.
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Inhibition of thromboxane and 12-HPETE formation by dazoxiben and its two thiophenic acid-substituted derivatives.
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The effects of dazoxiben, an inhibitor of thromboxane synthetase, on cold-induced forearm vasoconstriction and platelet behaviour in different individuals.
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Effect of the thromboxane synthetase inhibitor UK-37,248 (dazoxiben) upon platelet aggregation, coronary artery thrombosis and vascular reactivity.血栓素合成酶抑制剂UK-37,248(达唑氧苯)对血小板聚集、冠状动脉血栓形成及血管反应性的影响。
J Pharmacol Exp Ther. 1983 Dec;227(3):790-6.
10
Selective inhibition of thromboxane synthetase with dazoxiben - basis of its inhibitory effect on platelet adhesion.用达唑昔班选择性抑制血栓素合成酶——其对血小板黏附抑制作用的基础
Thromb Haemost. 1983 Apr 28;49(2):96-101.

本文引用的文献

1
UK-37, 248, a novel, selective thromboxane synthetase inhibitor with platelet anti-aggregatory and anti-thrombotic activity.UK-37,248,一种新型的选择性血栓素合成酶抑制剂,具有血小板抗聚集和抗血栓形成活性。
Thromb Res. 1981;23(1-2):145-62. doi: 10.1016/0049-3848(81)90247-4.
2
The interrelationship between thromboxane biosynthesis, aggregation and 5-hydroxytryptamine secretion in human platelets in vitro.体外人血小板中血栓素生物合成、聚集与5-羟色胺分泌之间的相互关系。
Thromb Haemost. 1980 Feb 29;43(1):38-40.
3
Prolongation of rat tail bleeding time caused by oral doses of a thromboxane synthetase inhibitor which have little effect on platelet aggregation.口服剂量的血栓素合成酶抑制剂可延长大鼠尾部出血时间,而该抑制剂对血小板聚集几乎没有影响。
Thromb Haemost. 1982 Feb 26;47(1):46-9.
4
Antithrombotic therapy for vascular prosthesis: an experimental model testing platelet inhibitory drugs.血管假体的抗血栓治疗:一种测试血小板抑制药物的实验模型
Surgery. 1980 Jun;87(6):668-76.
5
Thromboxane synthetase inhibition as antithrombotic strategy.抑制血栓素合成酶作为抗血栓形成策略。
Lancet. 1981 May 16;1(8229):1073-5. doi: 10.1016/s0140-6736(81)92241-8.
6
Pharmacologic control of thromboembolic complications of cardiac-valve replacement.
N Engl J Med. 1971 Jun 24;284(25):1391-4. doi: 10.1056/NEJM197106242842501.
7
Surface thrombogenicity of arterial prostheses.动脉假体的表面血栓形成性。
Surg Gynecol Obstet. 1973 Jan;136(1):12-6.
8
Influence of antiplatelet drugs on platelet-surface interactions.抗血小板药物对血小板-表面相互作用的影响。
Adv Exp Med Biol. 1978;102:265-83. doi: 10.1007/978-1-4757-1217-9_18.
9
PTFE (Goretex) femoropopliteal reconstruction for limb salvage.聚四氟乙烯(戈尔特斯)股腘动脉重建术用于肢体挽救。
Ann R Coll Surg Engl. 1979 Jul;61(4):301-3.
10
Prevention of arterial thromboembolism with acetylsalicylic acid. A controlled clinical study in patients with aortic ball valves.乙酰水杨酸预防动脉血栓栓塞。一项针对主动脉球瓣置换患者的对照临床研究。
Am Heart J. 1977 Jul;94(1):101-11. doi: 10.1016/s0002-8703(77)80351-7.