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蒂卡格勒对心肌梗塞损伤的保护作用

Gemma Vilahur¹, Manuel Gutiérrez¹, Laura Casani¹

¹From Cardiovascular Research Center (CSIC-ICCC), IIB-HSCSP, Barcelona, Spain (G.V., L.C., L.V., L.B.); Radiology Unit, Hospital de la Santa Creu i Sant Pau (HSCSP), Barcelona, Spain (M.G., A.C., A.H.); Cardiology Unit. Hospital de la Santa Creu i Sant Pau (HSCSP), Barcelona, Spain (G.P.-L., F.C.); Cardiovascular and Metabolic Diseases, Innovative Medicines and Early Development Biotech Unit, AstraZeneca, Mölndal, Sweden (L.C.); and Cardiovascular Research Chair UAB (Autonomous University of Barcelona), Spain (L.B.).

|October 30, 2016

概括

与克洛皮多格勒相比,蒂卡格勒可显著减少肌心梗塞后的肌心损伤和. 这突显了蒂卡格勒罗除了抗血小板活性之外的心脏保护潜力.

科学领域:

心脏病学
药理学
生物化学

背景情况:

在心肌梗塞 (MI) 后,蒂卡格勒的临床结果优于克洛皮多格勒.
通过腺通路的潜在非目标效应是假设的.
需要阐明蒂卡格勒增强疗效的机制.

研究的目的:

为了比较心肌损伤减少的程度,Ticagrelor与克洛皮多格勒在MI后.
调查腺介导机制在蒂卡格勒勒心脏保护中的作用.
评估与每种药物相关的心肌中的分子变化.

主要方法:

猪经历了心肌梗塞 (MI) 并接受了安慰剂,克洛皮多格勒,提卡格勒或提卡格勒加上腺素受体抗剂.
进行心脏MRI,血小板聚合测定和心肌组织分析 (蛋白质表达,酶活性).
评估的特定蛋白质包括水素-4,AMP激活蛋白激酶和环氧激酶-2.

主要成果:

与安慰剂相比,蒂卡格勒和克洛皮多格勒都具有显著的抗血小板作用,并减少了心脏病发作的大小.
蒂卡格勒可以显著地减少心脏病发作的大小 (23. 5%比克洛皮多格勒更多) 和心肌胀 (24. 5%少).
阻断腺受体消除了蒂卡格勒罗的优越心脏保护作用,涉及腺通路和改变分子信号传递.

结论:

通过减少心脏病发作后的死亡损伤和瘤形成,提卡格雷勒具有显著的心脏保护作用.
这些有益作用通过依赖于腺的机制,独立于血小板抑制水平.
提卡的作用包括调节缺血性心肌中的水素-4 ,AMPK和COX-2信号.

关键词:

心脏成像技术心脏保护其他疾病心肌梗塞纯能P2Y受体对抗剂

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