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强效血小板活化因子(PAF)受体拮抗剂SR 27417对PAF诱导的牛血小板聚集的体外抑制作用。

In vitro inhibitory effect of SR 27417, a potent platelet-activating factor (PAF) receptor antagonist, on the PAF-induced bovine platelet aggregation.

作者信息

Bastos da Silva M, Delaunois A, Gustin P, Godeau J M, Lekeux P

机构信息

Département de physiologie, Faculté de Médecine Vétérinaire, Université de Liège, Sart Tilman, Belgium.

出版信息

Vet Res. 2000 Mar-Apr;31(2):267-72. doi: 10.1051/vetres:2000115.

DOI:10.1051/vetres:2000115
PMID:10779205
Abstract

The in vitro inhibitory effect of SR 27417, an antagonist of the platelet-activating factor (PAF) receptor, on PAF-induced platelet aggregation was studied in blood collected from seven healthy Friesien calves. Inhibitory effects of SR 27417 were determined at thirteen different concentrations (0.1-400 nM) by using the dose-response curves of PAF on calf platelet aggregation. In the presence of SR 27417, the maximal slopes of aggregation (%/min) induced by low and high concentrations of PAF were significantly different from the control values obtained without an antagonist at p < or = 0.05 and p < or = 0.01 respectively. In vitro PAF-induced calf platelet aggregation was dose-dependently inhibited by SR 27417. The drug inhibited PAF-induced platelet aggregation in a competitive reversible manner (pA2 = 10.46 +/- 2.36 mol x L(-1)). In conclusion, the results of our study showed that addition of SR 27417 to bovine platelet in vitro inhibits PAF-induced platelet aggregation.

摘要

在从七头健康的弗里斯兰小牛采集的血液中,研究了血小板活化因子(PAF)受体拮抗剂SR 27417对PAF诱导的血小板聚集的体外抑制作用。通过使用PAF对小牛血小板聚集的剂量反应曲线,在13种不同浓度(0.1 - 400 nM)下测定了SR 27417的抑制作用。在存在SR 27417的情况下,低浓度和高浓度PAF诱导的聚集最大斜率(%/分钟)与未使用拮抗剂时获得的对照值相比,分别在p≤0.05和p≤0.01时存在显著差异。体外PAF诱导的小牛血小板聚集受到SR 27417的剂量依赖性抑制。该药物以竞争性可逆方式抑制PAF诱导的血小板聚集(pA2 = 10.46±2.36 mol·L⁻¹)。总之,我们的研究结果表明,在体外向牛血小板中添加SR 27417可抑制PAF诱导的血小板聚集。

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