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


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 [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.

SUBMITTER: Whitmore CA 

PROVIDER: S-EPMC8070574 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature

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

Whitmore Clayton A CA   Boules Mariam I MI   Behof William J WJ   Haynes Justin R JR   Koktysh Dmitry D   Rosenberg Adam J AJ   Tantawy Mohammed N MN   Pham Wellington W  

Molecules (Basel, Switzerland) 20210410 8


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 activi  ...[more]

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