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

Autor:	Clayton A. Whitmore, Mariam I. Boules, William J. Behof, Justin R. Haynes, Dmitry Koktysh, Adam J. Rosenberg, Mohammed N. Tantawy, Wellington Pham
Jazyk:	angličtina
Rok vydání:	2021
Předmět:	promethazine PET imaging Abeta Alzheimer autoradiography Organic chemistry QD241-441
Zdroj:	Molecules, Vol 26, Iss 8, p 2182 (2021)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules26082182
Popis:	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.
Databáze:	Directory of Open Access Journals
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