Synthesis and Evaluation of 8-[~(131)I]Iodo-substituted Imidazopyridine Derivative as Single Photon

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A novel N-methyl, N-phenyl-[6-chloro-2-(4-chlorophenyl)-8-iodoimidazo[1, 2-α]-pyridine-3-yl]acetamide (compoundⅤ) 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]-compoundⅥthan 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]-compoundⅥ. It indicated that [131I]-compoundⅥmight be a potential SPECT radioligand for imaging of PBR. A novel N-methyl, N-phenyl- [6-chloro-2- (4-chlorophenyl) -8-iodoimidazo [1,2-α] -pyridine-3-yl] acetamide in vitro cell uptake studies showed that MDA-MB-231 cells yield four-fold higher specific uptake of [131I] -compound VIthan MCF-7 cells, corresponding to the increased expression of PBR in MDA- . Blocking studies significantly reduced the MDA-MB-231 cells uptake of [131I] -compound VI. It indicated that [131I] -compound Ⅵ light be a potential SPECT radioligand for imaging of PBR.
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