Design, Synthesis, and Validation of a Novel [11C]Promethazine PET Probe for Imaging Abeta Using Autoradiography

Promethazine, an antihistamine drug used in the clinical treatment of nausea, has been demonstrated the ability to bind Abeta in a transgenic mouse model of Alzheimer's disease. However, so far, all of the studies were performed in vitro using extracted tissues. In this work, we report the design and synthesis of a novel [C-11]promethazine PET radioligand for future in vivo studies. The [C-11]promethazine was isolated by RP-HPLC with radiochemical purity >95% and molar activity of 48 TBq/mmol. The specificity of the probe was demonstrated using human hippocampal tissues via autoradiography.

Automated summary

This study reports the design and synthesis of a novel [C-11]promethazine PET radioligand for future in vivo studies, with high radiochemical purity and molar activity. The specificity of the probe was demonstrated through autoradiography using human hippocampal tissues.