PET and SPECT radiotracers

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Early diagnosis of CNS disorders
In recent years, several PET tracers for monitoring the activity and expression of P-gp at the BBB have been tested. P-gp substrates such as [11C]verapamil and [11C]loperamide can be employed to visualize P-gp activity, but they display a low baseline uptake in the brain and formation of radiolabeled metabolites which hamper the interpretation of PET data. P-gp inhibitors such as [11C]elacridar, [11C]laniquidar and [11C]tariquidar have been tested to investigate Pgp expression and the results need further investigation. Recently, we developed MC18, MC266 and MC80, characterized as inhibitor, substrate and inducer of P-gp by in vitro and ex vivo assays. These molecules 11C radiolabelled have been evaluated in vivo.
PET radiotracers could be employed for various purposes:
1 P-gp inhibitors to monitor decreased expression of P-gp at the BBB in neurodegenerative disorders such as Alzheimer’s and Parkinson’s diseases;
2 P-gp substrates with a high baseline uptake to monitor increased expression of P-gp in epileptic foci.