CXC chemokine receptor-3 (CXCR3) is a G-protein coupled receptor (GPCR) predominantly expressed on activated T lymphocytes that promote Th1 responses[3]. AMG 487 is the targeted blocker of chemokine receptor CXCR3 and improves inflammatory symptoms by blocking the inflammatory cycle[4]. AMG487 treatment in collagen-induced arthritis(CIA) mice decreased mRNA and protein expression levels of CXCR3, IL-17A, RORγt, and STAT3. Therefore, it can be concluded that the anti-arthritic effect of AMG487 is caused by the inhibitory action on IL-17A and by downregulating RORγt/STAT3 expression in CIA the model[5]. Pharmacological blockade of CXCR3 using local injection of its inhibitor, AMG487, into the anterior cingulate cortex (ACC) significantly attenuated hyperalgesia induced by chronic constriction injury and suppressed the phosphorylation of extracellular signal-regulated kinase (ERK)[6]. AMG487 application might alleviate PDGFR-β and occludin loss, and decreased the residual content of retinal albumin in the streptozocin-induced DR mouse model via the inhibition of oxidative and endoplasmic reticulum stress, in which p38 activation was also involved[7]. AMG487 significantly alleviated joint inflammation by decreasing GITR+CD25+, GITR+CD45+, GITR+IL-9+, GITR+NF-κB+ CD45+CD4+, CD45+CCR6+, CD45+IL-6+ cells, CD45+IL-17A+, and CD45+IL-21+, and increasing GITR+Foxp3+ and GITR+STAT6+ cells[8].
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