PET (positron emission tomography) tracers for imaging brain �-amyloid plaque have been developed and successfully applied in clinical studies of Alzheimer's disease. These include 2-arylbenzothiazole derivatives [11C]PIB and [18F]Flutemetamol developed at the University of Pittsburgh.  However, the need for a cyclotron and radiochemistry facility for tracer production has limited their widespread applicability. To circumvent these limitations, we aim at exploring Tc-99m labeled 2-arylbenzothiazoles for imaging �-amyloid plaques with the less expensive and more accessible imaging modality SPECT (single photon emission computed tomography). By using Re as a non-radioactive surrogate of Tc, we have synthesized a series of potent, compact and lipophilic Re 2-arylbenzothiazoles and selected the best candidate for labeling with Tc-99m. The design, synthesis, lipophilicity and binding affinities of Re 2-arylbenzothiazoles to aggregated �-amyloid peptides, and the radiolabeling, brain uptake and retention of the Tc-99m 2-arylbenzothiazole analog in mice will be presented.

Synthesis and structure-activity relationship of Tc/Re 2-arylbenzothiazoles as β-amyloid imaging agents

243rd National Meeting (2012)

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