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Mechanism of antiplatelet action of hypolipidemic, antidiabetic and antihypertensive drugs by PPAR activation PPAR agonists: New antiplatelet agents

机译:PPAR激活降血脂,降糖和降压药的抗血小板作用机理PPAR激动剂:新型抗血小板药

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Given the prevalence of cardiovascular disease in patients with cardiovascular risk factors (i.e., hypertension, diabetes, smoking and obesity) and that platelet activation plays an important pathogenic role in cardiovascular diseases, it is very important to identify the drugs that have multiple targets. In this sense, the present article describes the mechanism of antiplatelet action of hypolipidemic (statins and fibrates), antidiabetic (thiazolidinediones) and antihypertensive (nifedipine) drugs via peroxisome proliferator-activated receptor (PPAR) activation. The mechanism of antiplatelet action of the drugs is by direct activation of PPARs with the inhibition of cyclooxygenase-1, protein kinase C-alpha, calcium mobilization, thromboxane A2, sCD40L, platelet microparticles and cAMP-phosphodiesterase, and the stimulation of proteins kinase G and A Thus, these observations highlight PPARs as a novel therapeutic target for the treatment and prevention of cardiovascular diseases. (C) 2014 Elsevier Inc. All rights reserved.
机译:考虑到具有心血管危险因素(即高血压,糖尿病,吸烟和肥胖)的患者中普遍存在心血管疾病,并且血小板活化在心血管疾病中起重要的致病作用,因此确定具有多个靶标的药物非常重要。从这个意义上讲,本文描述了通过过氧化物酶体增殖物激活受体(PPAR)激活的降血脂药(他汀类药物和贝特类药物),抗糖尿病药(噻唑烷二酮类)和抗高血压药(硝苯地平)的抗血小板作用机制。药物的抗血小板作用机制是通过直接激活PPARs来抑制环氧合酶-1,蛋白激酶C-α,钙动员,血栓烷A2,sCD40L,血小板微粒和cAMP-磷酸二酯酶,以及刺激蛋白激酶G。因此,这些观察结果突出了PPARs作为治疗和预防心血管疾病的新型治疗靶标。 (C)2014 Elsevier Inc.保留所有权利。

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