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达曲班是一种血栓素受体拮抗剂,可保护心肌免受心肌缺血后的再灌注损伤,但对冠状动脉内皮无保护作用。

Daltroban, a thromboxane receptor antagonist, protects the myocardium against reperfusion injury following myocardial ischemia without protecting the coronary endothelium.

作者信息

Viehman G E, Ma X L, Lefer A M

机构信息

Department of Physiology, Jefferson Medical College, Thomas Jefferson University, Philadelphia, PA 19107.

出版信息

Methods Find Exp Clin Pharmacol. 1990 Dec;12(10):651-6.

PMID:1966110
Abstract

The effects of daltroban, a specific thromboxane receptor antagonist, were investigated in a model of myocardial ischemia consisting of 1.5 h of coronary artery occlusion followed by reperfusion for 4.5 h in anesthetized cats. Daltroban (1 mg/kg) was infused as a bolus 10 min prior to reperfusion of the left anterior descending (LAD) coronary artery. Daltroban infusion resulted in a significantly lower necrotic area expressed as a percentage of the myocardial area-at-risk compared to the MI + vehicle group. However, daltroban failed to retard increases in myeloperoxidase activity in the ischemic myocardium, indicating no reduction in neutrophil accumulation. Moreover, left anterior descending coronary artery ring preparations isolated from daltroban treated MI cats exhibited endothelial dysfunction following ischemia reperfusion. Thus, daltroban significantly protected the myocardium from reperfusion injury without protecting the coronary endothelium or retarding neutrophil accumulation.

摘要

在麻醉猫的心肌缺血模型中研究了特异性血栓素受体拮抗剂达曲班的作用。该模型包括冠状动脉闭塞1.5小时,随后再灌注4.5小时。在左前降支(LAD)冠状动脉再灌注前10分钟,静脉推注达曲班(1mg/kg)。与心肌梗死+赋形剂组相比,达曲班输注导致坏死面积占心肌危险面积的百分比显著降低。然而,达曲班未能抑制缺血心肌中髓过氧化物酶活性的增加,表明中性粒细胞聚集没有减少。此外,从接受达曲班治疗的心肌梗死猫分离的左前降支冠状动脉环制剂在缺血再灌注后表现出内皮功能障碍。因此,达曲班显著保护心肌免受再灌注损伤,但不能保护冠状动脉内皮或抑制中性粒细胞聚集。

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