Citation: Bin LI, Jian Feng LI, Xiao Guang SUN, Gang HUANG. Synthesis and Evaluation of 8-[¹³¹I]Iodo-substituted Imidazopyridine Derivative as Single Photon Emission Computed Tomography Tracer for Peripheral Benzodiazepine Receptors[J]. Chinese Chemical Letters, ;2006, 17(11): 1435-1438. shu

Synthesis and Evaluation of 8-[¹³¹I]Iodo-substituted Imidazopyridine Derivative as Single Photon Emission Computed Tomography Tracer for Peripheral Benzodiazepine Receptors

1.
Department of Nuclear Medicine, Reiji Hospital, Medical School of Shanghai Jiaotong University, Shanghai 200127;
2.
Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200127

Received Date: 13 September 2006

Fund Project: The authors are thankful to Dr. Yun Jun GAO (Jilin University, Jilin, China) for his friendly assistance. This project was supported by the key subject of development foundation of Shanghai Municipal Education Committee, China (No. 04BA03).

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.
- Imidazo[1,2-a]pyridineacetamide,
- peripheral benzodiazepine receptors,
- synthesis,
- iododestannylation
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