Design, Synthesis, and Validation of a Novel [11C]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

doi:10.3390/molecules26082182

Open AccessArticle

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

by

Clayton A. Whitmore

^1,2,†,

Mariam I. Boules

^1,2,†,

William J. Behof

^1,2,

Justin R. Haynes

^1,2,

Dmitry Koktysh

^3,4,

Adam J. Rosenberg

^1,2

,

Mohammed N. Tantawy

^1,2 and

Wellington Pham

^{1,2,4,5,6,7,8,9,10,*}

¹

Vanderbilt University Medical Center, Vanderbilt University Institute of Imaging Science, Nashville, TN 37232, USA

²

Department of Radiology and Radiological Sciences, Vanderbilt University Medical Center, Nashville, TN 37232, USA

³

Department of Chemistry, Vanderbilt University, VU Station, Nashville, TN 37235, USA

⁴

Vanderbilt Institute of Nanoscale Science and Engineering, Vanderbilt University, Nashville, TN 37235, USA

⁵

Department of Biomedical Engineering, Vanderbilt University, Nashville, TN 37235, USA

⁶

Vanderbilt Brain Institute, Vanderbilt University, Nashville, TN 37232, USA

⁷

Vanderbilt Ingram Cancer Center, Nashville, TN 37232, USA

⁸

Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, TN 37232, USA

⁹

Vanderbilt Memory and Alzheimer’s Center, Vanderbilt University Medical Center, Nashville, TN 37212, USA

¹⁰

Institute of Imaging Science, Vanderbilt University, 1161, 21st Avenue South, Nashville, TN 37232, USA

^*

Author to whom correspondence should be addressed.

^†

These authors contribute equally to this work.

Molecules 2021, 26(8), 2182; https://doi.org/10.3390/molecules26082182

Submission received: 11 March 2021 / Revised: 3 April 2021 / Accepted: 7 April 2021 / Published: 10 April 2021

(This article belongs to the Special Issue Innovative Molecular Probes and Imaging Technology for the Detection of Alzheimer’s Disease and Dementia-Related Disorders)

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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.

Keywords: promethazine; PET imaging; Abeta; Alzheimer; autoradiography

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MDPI and ACS Style

Whitmore, C.A.; Boules, M.I.; Behof, W.J.; Haynes, J.R.; Koktysh, D.; Rosenberg, A.J.; Tantawy, M.N.; Pham, W. Design, Synthesis, and Validation of a Novel [¹¹C]Promethazine PET Probe for Imaging Abeta Using Autoradiography. Molecules 2021, 26, 2182. https://doi.org/10.3390/molecules26082182

AMA Style

Whitmore CA, Boules MI, Behof WJ, Haynes JR, Koktysh D, Rosenberg AJ, Tantawy MN, Pham W. Design, Synthesis, and Validation of a Novel [¹¹C]Promethazine PET Probe for Imaging Abeta Using Autoradiography. Molecules. 2021; 26(8):2182. https://doi.org/10.3390/molecules26082182

Chicago/Turabian Style

Whitmore, Clayton A., Mariam I. Boules, William J. Behof, Justin R. Haynes, Dmitry Koktysh, Adam J. Rosenberg, Mohammed N. Tantawy, and Wellington Pham. 2021. "Design, Synthesis, and Validation of a Novel [¹¹C]Promethazine PET Probe for Imaging Abeta Using Autoradiography" Molecules 26, no. 8: 2182. https://doi.org/10.3390/molecules26082182

APA Style

Whitmore, C. A., Boules, M. I., Behof, W. J., Haynes, J. R., Koktysh, D., Rosenberg, A. J., Tantawy, M. N., & Pham, W. (2021). Design, Synthesis, and Validation of a Novel [¹¹C]Promethazine PET Probe for Imaging Abeta Using Autoradiography. Molecules, 26(8), 2182. https://doi.org/10.3390/molecules26082182

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

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