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

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 an...

Descripción completa

Detalles Bibliográficos
Autores principales: Whitmore, Clayton A., Boules, Mariam I., Behof, William J., Haynes, Justin R., Koktysh, Dmitry, Rosenberg, Adam J., Tantawy, Mohammed N., Pham, Wellington
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8070574/
https://www.ncbi.nlm.nih.gov/pubmed/33920113
http://dx.doi.org/10.3390/molecules26082182
_version_ 1783683501943422976
author Whitmore, Clayton A.
Boules, Mariam I.
Behof, William J.
Haynes, Justin R.
Koktysh, Dmitry
Rosenberg, Adam J.
Tantawy, Mohammed N.
Pham, Wellington
author_facet Whitmore, Clayton A.
Boules, Mariam I.
Behof, William J.
Haynes, Justin R.
Koktysh, Dmitry
Rosenberg, Adam J.
Tantawy, Mohammed N.
Pham, Wellington
author_sort Whitmore, Clayton A.
collection PubMed
description 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.
format Online
Article
Text
id pubmed-8070574
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-80705742021-04-26 Design, Synthesis, and Validation of a Novel [(11)C]Promethazine PET Probe for Imaging Abeta Using Autoradiography Whitmore, Clayton A. Boules, Mariam I. Behof, William J. Haynes, Justin R. Koktysh, Dmitry Rosenberg, Adam J. Tantawy, Mohammed N. Pham, Wellington Molecules Article 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. MDPI 2021-04-10 /pmc/articles/PMC8070574/ /pubmed/33920113 http://dx.doi.org/10.3390/molecules26082182 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Whitmore, Clayton A.
Boules, Mariam I.
Behof, William J.
Haynes, Justin R.
Koktysh, Dmitry
Rosenberg, Adam J.
Tantawy, Mohammed N.
Pham, Wellington
Design, Synthesis, and Validation of a Novel [(11)C]Promethazine PET Probe for Imaging Abeta Using Autoradiography
title Design, Synthesis, and Validation of a Novel [(11)C]Promethazine PET Probe for Imaging Abeta Using Autoradiography
title_full Design, Synthesis, and Validation of a Novel [(11)C]Promethazine PET Probe for Imaging Abeta Using Autoradiography
title_fullStr Design, Synthesis, and Validation of a Novel [(11)C]Promethazine PET Probe for Imaging Abeta Using Autoradiography
title_full_unstemmed Design, Synthesis, and Validation of a Novel [(11)C]Promethazine PET Probe for Imaging Abeta Using Autoradiography
title_short Design, Synthesis, and Validation of a Novel [(11)C]Promethazine PET Probe for Imaging Abeta Using Autoradiography
title_sort design, synthesis, and validation of a novel [(11)c]promethazine pet probe for imaging abeta using autoradiography
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8070574/
https://www.ncbi.nlm.nih.gov/pubmed/33920113
http://dx.doi.org/10.3390/molecules26082182
work_keys_str_mv AT whitmoreclaytona designsynthesisandvalidationofanovel11cpromethazinepetprobeforimagingabetausingautoradiography
AT boulesmariami designsynthesisandvalidationofanovel11cpromethazinepetprobeforimagingabetausingautoradiography
AT behofwilliamj designsynthesisandvalidationofanovel11cpromethazinepetprobeforimagingabetausingautoradiography
AT haynesjustinr designsynthesisandvalidationofanovel11cpromethazinepetprobeforimagingabetausingautoradiography
AT koktyshdmitry designsynthesisandvalidationofanovel11cpromethazinepetprobeforimagingabetausingautoradiography
AT rosenbergadamj designsynthesisandvalidationofanovel11cpromethazinepetprobeforimagingabetausingautoradiography
AT tantawymohammedn designsynthesisandvalidationofanovel11cpromethazinepetprobeforimagingabetausingautoradiography
AT phamwellington designsynthesisandvalidationofanovel11cpromethazinepetprobeforimagingabetausingautoradiography

Ejemplares similares