CXCR1 and CXCR2 chemokine receptors, mainly activated by interleukin 8 (IL-8 or CXCL8), are expressed in a variety of cells including, leukocytes, fibroblasts, endothelial cells, and smooth muscle cells. Numerous intracellular mediators are activated by these G protein-coupled receptors based on several factors, including the nature of the ligand, its concentration, and the binding sites with the receptor, levels of the receptor, cell type, and stimulatory environment. Much focus is currently being directed towards CXCR1/2 inhibitors, as these receptors primarily induce the chemotaxis of leukocytes, especially neutrophils, during inflammation, a key process in cardiovascular disease (CVD) progression. CXCR1/2 inhibitors show beneficial effects in various animal models of CVD. These effects include reducing the atherosclerotic plaque area, improving the serum lipid profile, attenuation of the damage following ischemia-reperfusion, the regulation of blood pressure, and the restriction of cardiac remodeling. Based on these encouraging results, testing CXCR1/2 inhibitors in clinical trials could be of a great importance to limit the inflammatory complications associated with CVDs.

主要由白细胞介素 8（IL-8 或 CXCL8）激活的 CXCR1 和 CXCR2 趋化因子受体在多种细胞中表达，包括白细胞、成纤维细胞、内皮细胞和平滑肌细胞。许多细胞内介质被这些 G 蛋白偶联受体激活，这些因素基于多种因素，包括配体的性质、其浓度、与受体的结合位点、受体水平、细胞类型和刺激环境。目前，很多焦点都集中在 CXCR1/2 抑制剂上，因为这些受体主要在炎症期间诱导白细胞，尤其是中性粒细胞的趋化性，炎症是心血管疾病 (CVD) 进展的关键过程。CXCR1/2 抑制剂在各种 CVD 动物模型中显示出有益作用。这些作用包括减少动脉粥样硬化斑块面积，改善血脂谱，减轻缺血再灌注损伤，调节血压，限制心脏重构。基于这些令人鼓舞的结果，在临床试验中测试 CXCR1/2 抑制剂对于限制与 CVD 相关的炎症并发症可能非常重要。