Synthesis and evaluation of 8-[131I]iodo-substituted imidazopyridine derivative as single photon emission computed tomography tracer for peripheral benzodiazepine receptors

Document Type

Article

Publication Date

11-1-2006

Abstract

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 SPECT radioligand for imaging of PBR.

Publication Source (Journal or Book title)

Chinese Chemical Letters

First Page

1435

Last Page

1438

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