NBI 74330

A CXCR3 antagonist (Ki = 3.6 nM in a radioligand binding assay); inhibits CXCL10- or CXCL11-induced calcium mobilization in RBL cells expressing human CXCR3 (IC50 = 7 nM for both); inhibits CXCL11-induced chemotaxis of CXCR3-expressing H9 cells and PHA/IL-2 T cells (IC50s = 3.9 and 6.6 nM, respectively); reduces peritoneal lymphocyte migration in a mouse model of peritonitis at 100 mg/kg; reduces the size and number of aortic arch atherosclerotic lesions in Ldlr-/- mice; reduces spinal cord microglial activation and levels of CXCL4, CXCL9, and CXCL10 and decreases thermal and mechanical hyperalgesia in a rat model of chronic constriction injury-induced neuropathic pain