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选择性雌激素受体调节剂 (SERMs)是一类在不同靶组织中可表现为雌激素激动剂或拮抗剂作用的化合物。雷洛昔芬是新一代SERMs代表药物。SERMs作用机制涉及雌激素受体、配体、应答元件、雌激素受体相关蛋白等方面。SERMs对于心血管疾病保护作用主要表现在对血脂的调节和对血管壁的直接作用。与激素替代疗法比较 ,SERMs对不同脂蛋白调节作用各异 ;SERMs具有调节血管壁增殖作用 ,其机制可能与eNOS(内皮一氧化氮合酶 )激活、Akt和ERK信号转导途径有关
Selective estrogen receptor modulators (SERMs) are a class of compounds that can act as estrogen agonists or antagonists in different target tissues. Raloxifene is a new generation of SERMs representative drugs. SERMs mechanism of action involves estrogen receptors, ligands, response elements, estrogen receptor-related proteins and so on. The protective effect of SERMs on cardiovascular diseases is mainly reflected in the regulation of blood lipids and the direct effect on the vessel wall. Compared with hormone replacement therapy, SERMs have different regulatory effects on different lipoproteins; SERMs can regulate the proliferation of vascular wall, and its mechanism may be related to the activation of eNOS (endothelial nitric oxide synthase), Akt and ERK signal transduction pathway