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Caspase-3 is one of the executioner caspases activated as a result of apoptosis. Radiolabeled isatins bind to caspase-3 with high affinity and are potential tracers for use with positron emission tomography to image apoptosis. We compared the ability of two novel radiolabeled isatins, [¹⁸F]WC-IV-3 and [¹¹C]WC-98, to detect caspase-3 activation in a rat model of cycloheximide-induced liver injury.

Male Sprague-Dawley rats were treated with cycloheximide and then imaged with microPET 3 h later with [¹⁸F]WC-IV-3 and [¹¹C]WC-98. Biodistribution studies were also performed simultaneously, with caspase-3 activation verified by fluorometric enzyme assay and Western blots.

MicroPET imaging studies demonstrated similar behavior of both tracers but with a lower maximum peak with [¹¹C]WC-98 than with [¹⁸F]WC-IV-3. Biodistribution studies demonstrated increased uptake …