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633 results on '"Scott, Peter J. H."'

155. Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging

Author

Bernard-Gauthier, Vadim, primary, Mossine, Andrew V., additional, Mahringer, Anne, additional, Aliaga, Arturo, additional, Bailey, Justin J., additional, Shao, Xia, additional, Stauff, Jenelle, additional, Arteaga, Janna, additional, Sherman, Phillip, additional, Grand’Maison, Marilyn, additional, Rochon, Pierre-Luc, additional, Wängler, Björn, additional, Wängler, Carmen, additional, Bartenstein, Peter, additional, Kostikov, Alexey, additional, Kaplan, David R., additional, Fricker, Gert, additional, Rosa-Neto, Pedro, additional, Scott, Peter J. H., additional, and Schirrmacher, Ralf, additional

Published
2018
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159. A Kinome-Wide Selective Radiolabeled TrkB/C Inhibitor for in Vitro and in Vivo Neuroimaging: Synthesis, Preclinical Evaluation, and First-in-Human

Author

Bernard-Gauthier, Vadim, primary, Bailey, Justin J., additional, Mossine, Andrew V., additional, Lindner, Simon, additional, Vomacka, Lena, additional, Aliaga, Arturo, additional, Shao, Xia, additional, Quesada, Carole A., additional, Sherman, Phillip, additional, Mahringer, Anne, additional, Kostikov, Alexey, additional, Grand’Maison, Marilyn, additional, Rosa-Neto, Pedro, additional, Soucy, Jean-Paul, additional, Thiel, Alexander, additional, Kaplan, David R., additional, Fricker, Gert, additional, Wängler, Björn, additional, Bartenstein, Peter, additional, Schirrmacher, Ralf, additional, and Scott, Peter J. H., additional

Published
2017
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162. A spot test for determination of residual TBA levels in 18F-radiotracers for human use using Dragendorff reagent

Author

Tanzey, Sean S., Mossine, Andrew V., Sowa, Alexandra R., Torres, Jovany, Brooks, Allen F., Sanford, Melanie S., and Scott, Peter J. H.

Abstract

When utilizing [18F]tetrabutylammonium fluoride ([18F]TBAF) in the synthesis of 18F-labeled radiotracers for clinical positron emission tomography (PET) imaging, it is necessary to confirm that residual TBA levels in formulated doses do not exceed established specifications (≤2.6 mg per patient dose). Historically this has been accomplished using HPLC, but this is time consuming for short-lived PET radiotracers and limited by the need for expensive equipment. This motivated us to introduce a TLC spot test for determining residual TBA, and we have developed a new method which employs the Dragendorff reagent. Herein we report details of the TLC method and use it to quantify residual TBA in different formulations of 6-[18F]fluoro-DOPA.

Published
2020
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165. Ring opening of epoxides with [18F]FeF species to produce [18F]fluorohydrin PET imaging agents.

Author

VerhoogAuthors contributed equally to this work., Stefan, Brooks, Allen F., Winton, Wade P., Viglianti, Benjamin L., Sanford, Melanie S., and Scott, Peter J. H.

Subjects
SPECIES, MOLECULES, TRICLOSAN
Abstract

A simple technique for the preparation of [18F]HF has been developed and applied to the generation of an [18F]FeF species for opening sterically hindered epoxides. This method has been successfully employed to prepare four drug-like molecules, including 5-[18F]fluoro-6-hydroxy-cholesterol, a potential adrenal/endocrine PET imaging agent. This easily automated one-pot procedure produces sterically hindered fluorohydrin PET imaging agents in good yields and high molar activities. [ABSTRACT FROM AUTHOR]

Published
2019
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166. C–H 18F-fluorination of 8-methylquinolines with Ag[18F]F.

Author

Lee, So Jeong, Brooks, Allen F., Ichiishi, Naoko, Makaravage, Katarina J., Mossine, Andrew V., Sanford, Melanie S., and Scott, Peter J. H.

Subjects
QUINOLINE derivatives, FLUORINATION, CARBON-hydrogen bonds, SUBSTITUTION reactions, RADIOCHEMISTRY
Abstract

This report describes a Pd-mediated C–H radiofluorination of 8-methylquinoline derivatives with no-carrier-added Ag[18F]F. To achieve this transformation, a new method was developed for the generation of Ag[18F]F using a sep-pak cartridge. The C–H radiofluorination was then optimized and applied to a series of substituted 8-methylquinoline derivatives. Finally, this method was fully automated using a radiochemistry synthesis module. [ABSTRACT FROM AUTHOR]

Published
2019
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167. Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging

Author

Bernard-Gauthier, Vadim, Mossine, Andrew V., Mahringer, Anne, Aliaga, Arturo, Bailey, Justin J., Shao, Xia, Stauff, Jenelle, Arteaga, Janna, Sherman, Phillip, Grand’Maison, Marilyn, Rochon, Pierre-Luc, Wängler, Björn, Wängler, Carmen, Bartenstein, Peter, Kostikov, Alexey, Kaplan, David R., Fricker, Gert, Rosa-Neto, Pedro, Scott, Peter J. H., and Schirrmacher, Ralf

Abstract

Changes in expression and dysfunctional signaling of TrkA/B/C receptors and oncogenic Trk fusion proteins are found in neurological diseases and cancers. Here, we describe the development of a first 18F-labeled optimized lead suitable for in vivo imaging of Trk, [18F]TRACK, which is radiosynthesized with ease from a nonactivated aryl precursor concurrently combining largely reduced P-gp liability and improved brain kinetics compared to previous leads while displaying high on-target affinity and human kinome selectivity.

Published
2024
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168. Synthesis of [18F]Arenes via the Copper-Mediated [18F]Fluorination of Boronic Acids

Author

Mossine, Andrew V., Brooks, Allen F., Makaravage, Katarina J., Miller, Jason M., Ichiishi, Naoko, Sanford, Melanie S., and Scott, Peter J. H.

Abstract

A copper-mediated radiofluorination of aryl- and vinylboronic acids with K18F is described. This method exhibits high functional group tolerance and is effective for the radiofluorination of a range of electron-deficient, -neutral, and -rich aryl-, heteroaryl-, and vinylboronic acids. This method has been applied to the synthesis of [18F]FPEB, a PET radiotracer for quantifying metabotropic glutamate 5 receptors.

Published
2024
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178. Automated synthesis of PET radiotracers by copper‐mediated 18F‐fluorination of organoborons: Importance of the order of addition and competing protodeborylation.

Author

Mossine, Andrew V., Brooks, Allen F., Bernard‐Gauthier, Vadim, Bailey, Justin J., Ichiishi, Naoko, Schirrmacher, Ralf, Sanford, Melanie S., and Scott, Peter J. H.

Subjects
POSITRON emission tomography, RADIOPHARMACEUTICALS, CHEMICAL synthesis, RADIOACTIVE tracers, DRUG development
Abstract

In this paper, we describe the use of Cu‐mediated [18F]fluorodeboronation for the automated production of positron emission tomography radiotracers suitable for clinical use. Two recurrent issues with the method, low radiochemical conversion on automation and protoarene byproduct purification issues, have been successfully addressed. The new method was utilized to produce sterile injectable doses of [18F]‐(±)‐IPMICF17, a positron emission tomography radiotracer for tropomyosin receptor kinase B/C, using an automated synthesis module. The product was isolated in 1.9 ± 0.1% isolated radiochemical yield, excellent radiochemical purity (>99%), and high specific activity (5294 ± 1227 Ci/mmol). Quality control testing confirmed that doses were suitable for clinical use. [ABSTRACT FROM AUTHOR]

Published
2018
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180. Identification of [18F]TRACK, a Fluorine-18-Labeled Tropomyosin Receptor Kinase (Trk) Inhibitor for PET Imaging.

Author

Bernard-Gauthier, Vadim, Mossine, Andrew V., Mahringer, Anne, Aliaga, Arturo, Bailey, Justin J., Xia Shao, Stauff, Jenelle, Arteaga, Janna, Sherman, Phillip, Grand'maison, Marilyn, Rochon, Pierre-Luc, Wängler, Björn, Wängler, Carmen, Bartenstein, Peter, Kostikov, Alexey, Kaplan, David R., Fricker, Gert, Rosa-Neto, Pedro, Scott, Peter J. H., and Schirrmacher, Ralf

Published
2018
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186. Synthesis and Initial in Vivo Studies with [11C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3

Author

Li, Lei, primary, Shao, Xia, additional, Cole, Erin L., additional, Ohnmacht, Stephan A., additional, Ferrari, Valentina, additional, Hong, Young T., additional, Williamson, David J., additional, Fryer, Tim D., additional, Quesada, Carole A., additional, Sherman, Phillip, additional, Riss, Patrick J., additional, Scott, Peter J. H., additional, and Aigbirhio, Franklin I., additional

Published
2015
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193. High-Yielding Automated Convergent Synthesis of No-Carrier-Added [11C-Carbonyl]-Labeled Amino Acids Using the Strecker Reaction.

Author

Junhao Xing, Brooks, Allen F., Fink, Dylan, Huibin Zhang, Piert, Morand R., Scott, Peter J. H., and Xia Shao

Subjects
CHEMICAL synthesis, AMINO acid synthesis, RADIOACTIVE tracers
Abstract

A new variant of the Strecker synthesis using no-carrier-added [11C]cyanide for the synthesis of radiolabeled amino acids is described. The protocol is fully automated using a radiochemistry synthesis module and applied to the production of a number of new PET radiotracers. [11C-Carbonyl]sarcosine, [11C-carbonyl]methionine, [11Ccarbonyl]- N-phenylglycine, and [11C-carbonyl]glycine are all synthesized in moderate to good radiochemical yields. The synthesis of [11C-carbonyl] sarcosine has been validated for production of doses for clinical use, and preliminary evaluation of the new radiotracer in PC3 tumor-bearing mice is also reported. [ABSTRACT FROM AUTHOR]

Published
2017
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197. High Affinity Radiopharmaceuticals Based Upon Lansoprazole for PET Imaging of Aggregated Tau in Alzheimer’s Disease and Progressive Supranuclear Palsy: Synthesis, Preclinical Evaluation, and Lead Selection

Author

Fawaz, Maria V., primary, Brooks, Allen F., additional, Rodnick, Melissa E., additional, Carpenter, Garrett M., additional, Shao, Xia, additional, Desmond, Timothy J., additional, Sherman, Phillip, additional, Quesada, Carole A., additional, Hockley, Brian G., additional, Kilbourn, Michael R., additional, Albin, Roger L., additional, Frey, Kirk A., additional, and Scott, Peter J. H., additional

Published
2014
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200. Editorial: Positron Emission Tomography (PET) Imaging of Brain Biochemistry: Beyond High-Affinity Radioligands.

Author

Kilbourn, Michael R., Scott, Peter J. H., and Vasdev, Neil

Subjects
POSITRON emission tomography, BRAIN imaging, AMYLOID plaque, BIOCHEMISTRY, HUNTINGTON disease, TRANSLOCATOR proteins
Abstract

We are excited to watch the progress of not only the new radiotracers reported here, but also the many future ones sure to be developed as the improving methods for PET radiochemistry and I in vivo i radiotracer evaluation continue to produce unprecedented radiotracers to be translated to I in vivo i studies in the human brain. PET imaging of misfolded proteins has garnered enormous attention in recent years, yielding radiopharmaceuticals for imaging amyloid and tau in neurodegenerative disorders such as Alzheimer's disease and related dementias. Keywords: brain PET; neuroimaging; radiochemistry; radiopharmaceuticals; molecular imaging EN brain PET neuroimaging radiochemistry radiopharmaceuticals molecular imaging 1 2 2 05/05/22 20220503 NES 220503 The field of radiopharmaceutical chemistry devoted to the development of new neuroimaging agents for Positron Emission Tomography (PET) imaging began in earnest in the early 1980's and was for many years dominated by efforts targeting receptors for the major neurotransmitters such as biogenic amines, amino acids, and acetylcholine. [Extracted from the article]

Published
2022
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