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

利用放射自显影技术设计、合成和验证一种新型[(11)C]异丙嗪PET探针用于Aβ成像

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Abstract

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 [(11)C]promethazine PET radioligand for future in vivo studies. The [(11)C]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.

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