Effects of a new PAR1 antagonist, F 16618, on smooth muscle cell contraction

被引：7

作者：

Bocquet, Arnaud ^{[1
]}

Letienne, Robert ^{[1
]}

Sablayrolles, Sylvie ^{[1
]}

De Vries, Luc ^{[1
]}

Perez, Michel ^{[1
]}

Le Grand, Bruno ^{[1
]}

机构：

[1] Ctr Rech Pierre Fabre, F-81106 Castres, France

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 2009年 / 611卷 / 1-3期

关键词：

PAR1; antagonist; Vessel; Vasoconstriction; PROTEINASE-ACTIVATED RECEPTORS; ENDOTHELIUM-DEPENDENT RELAXATION; SUBARACHNOID HEMORRHAGE; CORONARY-ARTERY; UP-REGULATION; THROMBIN; EXPRESSION; MECHANISM; ANGIOPLASTY; RESPONSES;

D O I：

10.1016/j.ejphar.2009.03.056

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

This study evaluated the effects of two PAR1 antagonists on vessels contracted by SFLLR. ER 121958 antagonized the SFLLR-induced contraction on rat denuded superior mesenteric artery and pig coronary artery in a non-competitive manner (IC50 values were 22 [7.5-43.6] nM and 2.9 [2.09-4.02] nM, respectively). F 16618 inhibited the SFLLR-induced superior mesenteric arteries and coronary arteries contraction in a competitive manner (pA(2) values of 7.3 and 6.2, respectively). PAR1 antagonists do not affect vessel resting tension or haemodynamic parameters in anaesthetized rats. Thus, PARI antagonists could have beneficial effects against vasospasm due to vessel injury. (C) 2009 Elsevier B.V. All rights reserved.

引用

页码：60 / 63

页数：4

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