Design, Synthesis, and Validation of a Novel [<sup>11</sup>C]Promethazine PET Probe for Imaging Abeta Using Autoradiography
oleh: Clayton A. Whitmore, Mariam I. Boules, William J. Behof, Justin R. Haynes, Dmitry Koktysh, Adam J. Rosenberg, Mohammed N. Tantawy, Wellington Pham
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2021-04-01 |
Deskripsi
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 [<sup>11</sup>C]promethazine PET radioligand for future in vivo studies. The [<sup>11</sup>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.