Potential Novel Compounds for the Imaging of Hypoxia Using SPECT
Objectives: Hypoxic tissue is of great significance in stroke and oncology. Unfortunately, imaging of hypoxia with nuclear medicine techniques is limited to the major cities, where Positron Emission Tomography (PET) scans can be performed. Single Photon Emission Computed Tomography (SPECT) is a nuclear medicine imaging technique that is widely available in many hospitals around Australia. 18F-SO201 has shown promising results as a stroke imaging agent for PET. The uptake of this agent in stroke affected areas of the brain is almost twice that of existing tracers. The faster uptake translates to a reduced scanning protocol. It is therefore of great interest to develop a derivative of the SO201 molecule as a SPECT imaging agent. Our initial approach is to develop 99m-Tc based derivatives of SO201.
Methods and results: Ligands incorporating the SO201 moeity were synthesised by alkylation of commercially available thioanilines. The ligands were reacted with either Re(CO)3(H2O)3 or Re(CO)5 using microwave or conventional heating to make the cold standard analogues for characterization. These ligands will then be reacted with radioactive 99m-Tc for investigation as potential hypoxic SPECT tracers.
Conclusion: A series of ligands have been synthesised for labelling with 99m-Tc with potential application in imaging of intracellular hypoxia.