NUCL 5 |
| Sigma-2 receptors are over-expressed in many types of human cancer cells, including strongly metastatic breast cancer cell lines. Moreover, the sigma-2 subtype is over-expressed by ten-fold in growing cancer cells, which suggests a potential use of sigma-2 receptors as biomarkers of tumor proliferation. No endogenous ligands have been identified for sigma receptors, which complicates their characterization. Thus, the quest for selective ligands for the sigma-2 subtype receptor continues. Highly potent and selective ligand would help to map the distribution of sigma-2 receptors in the body, identify their function, and understand their role in cancer growth. Fluorine-18 labelled compound would present an advantage for PET imaging in terms of radionuclide properties. We report here the synthesis of N-[4-(3,4-dihydro-6,7-dimethoxy-1H-isoquinolin-N-yl)-butyl]-2,3-dimethoxy-5-fluoro-benzamide and its 18F-radiolabelled analogue via an aromatic electrophilic substitution reaction starting from the stannylated precursor. The binding properties of the product to sigma-2 receptors are being evaluated.
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Molecular Imaging
9:00 AM-11:50 AM, Sunday, August 19, 2007 Boston Park Plaza -- Stuart Rm, Oral
Division of Nuclear Chemistry & Technology |
