A novel N-methyl, N-phenyl-[6-chloro-2-(4-chlorophenyl)-8-iodoimidazo[1, 2-a]-pyridine-3-yl]acetamide (compound Ⅴ) was synthesized, radiolabelled with 131I and evaluated in vitro. In vitro cell uptake studies showed that MDA-MB-231 cells yield four-fold higher specific uptake of [131I]-compound Ⅵ than MCF-7 cells, corresponding to the increased expression of PBR in MDA-MB-231 cells. Blocking studies significantly reduced the MDA-MB-231 cells uptake of[131I]-compound Ⅵ. It indicated that [131I]-compound Ⅵ might be a potential SPECTradioligand for imaging of PBR.