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

Molecules

Dmitry Koktysh¹  MohammedN. Tantawy²  AdamJ. Rosenberg²  ClaytonA. Whitmore²  Wellington Pham²  MariamI. Boules²  WilliamJ. Behof²  JustinR. Haynes² 

[1] Department of Chemistry, Vanderbilt University, VU Station, Nashville, TN 37235, USA;Vanderbilt University Medical Center, Vanderbilt University Institute of Imaging Science, Nashville, TN 37232, USA;

关键词: promethazine;    PET imaging;    Abeta;    Alzheimer;    autoradiography;   

DOI  :  10.3390/molecules26082182

来源: DOAJ

【 摘 要 】

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

【 授权许可】

Unknown