細(xì)胞表面趨化因子受體2（CCR2）屬于G蛋白偶聯(lián)受體（GPCR）超家族成員，并且是單核細(xì)胞趨化蛋白1～4（MCP 1～4）的受體。MCP 1～4是促炎癥反應(yīng)的化學(xué)誘導(dǎo)物，CCR2和MCP-1在人類侵蝕性疾病模型如動(dòng)脈粥狀硬化、多發(fā)性硬化癥中均起顯著作用。大量研究證明CCR2和MCP-1拮抗劑可以減少臨床炎癥模型的發(fā)病率，這些化學(xué)拮抗劑的結(jié)構(gòu)多樣，主要包括γ-氨基丁酰胺類、甘胺酰胺類、噻唑類、吲哚類、二取代雙哌啶醇類、季銨鹽類和不飽和雜環(huán)類等，它們表現(xiàn)出不同的藥理活性。CCR2拮抗劑對(duì)各種與趨化因子相關(guān)的疾病具有較好的療效，部分藥物已經(jīng)進(jìn)入臨床試驗(yàn)階段，綜述CCR2及其受體拮抗劑的研究進(jìn)展。

CC Chemokine Receptor 2 (CCR2) is a member of the G protein-coupled receptor (GPCR) superfamily that serves as the receptor for monocyte chemoattractant proteins 1—4 (MCP-1 to -4), a group of pro-inflammatory chemotactic cytokines (chemokines). Many researches proved that CCR2 and the MCP-1 antagonist compound reduced the clinical inflammation model disease incidence rate, MCP-1 and CCR2 play the remarkable role in the human corrosive disease model like artery gruel shape hardening and the multiple scierosis. Its chemistry antagonist compound with the structural diversity, including 4-aminobutanamide antagonists, glycinamide antagonists, thiazole antagonists, indole antagonists, disubstituted piperidine alcohols antagonists, quaternary ammonium salts antagonists, and unsaturated heterocyclic antagonists, has displayed the different medicine activeness. CCR2 antagonists have good effect on various chemokine-related diseases, and some drugs have entered clinical trials. In this paper, CCR2 receptor antagonists aere reviewed.