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内皮素-3:作为体内抗聚集肽的选择性

Endothelin-3: selectivity as an anti-aggregatory peptide in vivo.

作者信息

Lidbury P S, Thiemermann C, Thomas G R, Vane J R

机构信息

William Harvey Research Institute, St. Bartholomew's Hospital Medical College, London, U.K.

出版信息

Eur J Pharmacol. 1989 Jul 18;166(2):335-8. doi: 10.1016/0014-2999(89)90079-4.

DOI:10.1016/0014-2999(89)90079-4
PMID:2676565
Abstract

Endothelin-3 (1 nmol/kg) given i.v. to anaesthetised rabbits significantly inhibited ADP-induced ex vivo platelet aggregation, while causing only a transient decrease in blood pressure and no change in heart rate. Pretreatment with piroxicam (14 mumol/kg) abolished the anti-aggregatory effect. Thus, endothelin-3, while not inhibiting rabbit platelets in vitro, can induce the release of a cyclo-oxygenase produce, probably prostacyclin, which inhibits ex vivo aggregation. Unlike endothelin-1, this was achieved with minimal effect on the haemodynamics.

摘要

给麻醉的兔子静脉注射内皮素 -3(1纳摩尔/千克)可显著抑制二磷酸腺苷诱导的离体血小板聚集,同时仅引起血压短暂下降,心率无变化。用吡罗昔康(14微摩尔/千克)预处理可消除这种抗聚集作用。因此,内皮素 -3虽然在体外不抑制兔血小板,但可诱导环氧化酶产物(可能是前列环素)的释放,从而抑制离体血小板聚集。与内皮素 -1不同,这种作用对血流动力学的影响最小。

相似文献

1
Endothelin-3: selectivity as an anti-aggregatory peptide in vivo.内皮素-3:作为体内抗聚集肽的选择性
Eur J Pharmacol. 1989 Jul 18;166(2):335-8. doi: 10.1016/0014-2999(89)90079-4.
2
Endothelin-1 inhibits platelet aggregation in vivo: a study with 111indium-labelled platelets.内皮素-1在体内抑制血小板聚集:一项用铟-111标记血小板的研究。
Br J Pharmacol. 1990 Feb;99(2):303-8. doi: 10.1111/j.1476-5381.1990.tb14699.x.
3
Endothelin-1 releases prostacyclin and inhibits ex vivo platelet aggregation in the anesthetized rabbit.内皮素-1可释放前列环素并抑制麻醉兔的体外血小板聚集。
J Cardiovasc Pharmacol. 1989;13 Suppl 5:S138-41; discussion S142.
4
The endothelin ETB receptor agonist, IRL 1620, causes vasodilatation and inhibits ex vivo platelet aggregation in the anaesthetised rabbit.内皮素ETB受体激动剂IRL 1620可使麻醉兔血管舒张,并抑制离体血小板聚集。
Eur J Pharmacol. 1994 Jun 23;259(1):51-5. doi: 10.1016/0014-2999(94)90156-2.
5
Endothelins release tissue plasminogen activator and prostanoids.内皮素释放组织型纤溶酶原激活物和类前列腺素。
Eur J Pharmacol. 1990 Sep 21;186(2-3):205-12. doi: 10.1016/0014-2999(90)90435-9.
6
Mediation of endothelin-1-induced inhibition of platelet aggregation via the ETB receptor.内皮素-1通过ETB受体介导对血小板聚集的抑制作用。
Br J Pharmacol. 1993 Jun;109(2):530-4. doi: 10.1111/j.1476-5381.1993.tb13602.x.
7
Dissociation of the anti-ischaemic effects of cloricromene from its anti-platelet activity.氯克罗孟的抗缺血作用与其抗血小板活性的解离。
Br J Pharmacol. 1993 Sep;110(1):275-80. doi: 10.1111/j.1476-5381.1993.tb13805.x.
8
Prostacyclin mediates antiaggregatory and hypotensive actions of endothelin in anaesthetized beagle dogs.前列环素介导内皮素在麻醉比格犬体内的抗聚集和降压作用。
Br J Pharmacol. 1989 Sep;98(1):38-40. doi: 10.1111/j.1476-5381.1989.tb16859.x.
9
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.
10
Endothelin inhibits ex vivo platelet aggregation in the rabbit.
Eur J Pharmacol. 1988 Dec 6;158(1-2):181-2. doi: 10.1016/0014-2999(88)90273-7.

引用本文的文献

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The effect of methylmercury (CH3HgCl) on the production of endothelium-derived relaxing factor (EDRF) by cultured human umbilical vascular endothelial cells based on its anti-aggregatory effect on human platelets.基于甲基汞(CH3HgCl)对人血小板的抗聚集作用,研究其对培养的人脐血管内皮细胞产生内皮源性舒张因子(EDRF)的影响。
Cell Biol Toxicol. 1995 Dec;11(6):303-11. doi: 10.1007/BF01305903.
2
Effect of cadmium (CdCl2) on cell proliferation and production of EDRF (endothelium-derived relaxing factor) by cultured human umbilical arterial endothelial cells.镉(氯化镉)对培养的人脐动脉内皮细胞的细胞增殖及内皮源性舒张因子(EDRF)产生的影响。
Arch Toxicol. 1994;68(9):555-9. doi: 10.1007/s002040050113.
3
Endothelin and myocardial ischemia.
内皮素与心肌缺血
Cardiovasc Drugs Ther. 1994 Aug;8(4):589-99. doi: 10.1007/BF00877413.
4
Endothelins. Vascular actions and clinical implications.内皮素。血管作用及临床意义。
Drugs. 1993 Nov;46(5):795-804. doi: 10.2165/00003495-199346050-00001.
5
Effects of indomethacin on the regional haemodynamic responses to low doses of endothelins and sarafotoxin.吲哚美辛对低剂量内皮素和毒蜥毒素所致局部血流动力学反应的影响。
Br J Pharmacol. 1990 May;100(1):158-62. doi: 10.1111/j.1476-5381.1990.tb12069.x.
6
Endothelin-1 inhibits platelet aggregation in vivo: a study with 111indium-labelled platelets.内皮素-1在体内抑制血小板聚集:一项用铟-111标记血小板的研究。
Br J Pharmacol. 1990 Feb;99(2):303-8. doi: 10.1111/j.1476-5381.1990.tb14699.x.
7
Characteristics of endothelin-1 and endothelin-3 stimulation of phosphoinositide breakdown differ between regions of guinea-pig and rat brain.豚鼠和大鼠脑不同区域中内皮素-1和内皮素-3刺激磷酸肌醇分解的特征存在差异。
Naunyn Schmiedebergs Arch Pharmacol. 1990 Mar;341(3):268-71. doi: 10.1007/BF00169742.
8
In vitro inhibition by endothelins of thrombin-induced aggregation and Ca2+ mobilization in human platelets.内皮素对人血小板中凝血酶诱导的聚集和钙离子动员的体外抑制作用。
Br J Pharmacol. 1992 Aug;106(4):966-71. doi: 10.1111/j.1476-5381.1992.tb14443.x.