Literature DB >> 29031087

Characterization of the radiosynthesis and purification of [18F]THK-5351, a PET ligand for neurofibrillary tau.

Tobey J Betthauser1, Paul A Ellison2, Dhanabalan Murali2, Patrick J Lao3, Todd E Barnhart2, Shozo Furumoto4, Nobuyuki Okamura5, Sterling C Johnson6, Jonathan W Engle2, Robert J Nickles2, Bradley T Christian3.   

Abstract

This work characterizes the radiochemical synthesis, purification, and formulation of [18F]THK-5351, a tau PET radioligand, and develops an automated radiosynthesis routine (ELIXYS, Sofie Biosciences). Nucleophilic radiofluorination reaction was complete by 7min at 110°C with radiochemical yields proportional to precursor mass (0.1-0.5mg). Optimized HPLC purification produced radiotracer product with no chemical impurities observed on analytical HPLC in formulation. Automated radiosynthesis (ELIXYS), HPLC purification and formulation was completed in 86min producing formulated product suitable for human research use.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Alzheimer's disease; Automation; Formulation; Positron emission tomography; Radiochemical stability; Radiochemistry; THK; USP

Mesh：

Substances：

Year:  2017        PMID： 29031087      PMCID： PMC5673567          DOI： 10.1016/j.apradiso.2017.10.002

Source DB:  PubMed          Journal:  Appl Radiat Isot        ISSN： 0969-8043            Impact factor:   1.513


  16 in total

1.  Longitudinal changes of tau PET imaging in relation to hypometabolism in prodromal and Alzheimer's disease dementia.

Authors:  K Chiotis; L Saint-Aubert; E Rodriguez-Vieitez; A Leuzy; O Almkvist; I Savitcheva; M Jonasson; M Lubberink; A Wall; G Antoni; A Nordberg
Journal:  Mol Psychiatry       Date:  2017-05-16       Impact factor: 15.992

2.  In Vivo Comparison of Tau Radioligands 18F-THK-5351 and 18F-THK-5317.

Authors:  Tobey J Betthauser; Patrick J Lao; Dhanabalan Murali; Todd E Barnhart; Shozo Furumoto; Nobuyuki Okamura; Charles K Stone; Sterling C Johnson; Bradley T Christian
Journal:  J Nucl Med       Date:  2016-11-10       Impact factor: 10.057

3.  Tau imaging with [18 F]THK-5351 in progressive supranuclear palsy.

Authors:  A Ishiki; R Harada; N Okamura; N Tomita; C C Rowe; V L Villemagne; K Yanai; Y Kudo; H Arai; S Furumoto; M Tashiro; K Furukawa
Journal:  Eur J Neurol       Date:  2016-10-31       Impact factor: 6.089

4.  Structure-Activity Relationship of 2-Arylquinolines as PET Imaging Tracers for Tau Pathology in Alzheimer Disease.

Authors:  Tetsuro Tago; Shozo Furumoto; Nobuyuki Okamura; Ryuichi Harada; Hajime Adachi; Yoichi Ishikawa; Kazuhiko Yanai; Ren Iwata; Yukitsuka Kudo
Journal:  J Nucl Med       Date:  2015-12-23       Impact factor: 10.057

5.  Novel 18F-labeled arylquinoline derivatives for noninvasive imaging of tau pathology in Alzheimer disease.

Authors:  Nobuyuki Okamura; Shozo Furumoto; Ryuichi Harada; Tetsuro Tago; Takeo Yoshikawa; Michelle Fodero-Tavoletti; Rachel S Mulligan; Victor L Villemagne; Hiroyasu Akatsu; Takayuki Yamamoto; Hiroyuki Arai; Ren Iwata; Kazuhiko Yanai; Yukitsuka Kudo
Journal:  J Nucl Med       Date:  2013-07-15       Impact factor: 10.057

6.  Radiolysis of 2-[18F]fluoro-2-deoxy-D-glucose ([18F]FDG) and the role of ethanol and radioactive concentration.

Authors:  Mark S Jacobson; Heather R Dankwart; Douglas W Mahoney
Journal:  Appl Radiat Isot       Date:  2009-01-21       Impact factor: 1.513

7.  Fully automated production of diverse 18F-labeled PET tracers on the ELIXYS multireactor radiosynthesizer without hardware modification.

Authors:  Mark Lazari; Jeffrey Collins; Bin Shen; Mohammed Farhoud; Daniel Yeh; Brandon Maraglia; Frederick T Chin; David A Nathanson; Melissa Moore; R Michael van Dam
Journal:  J Nucl Med Technol       Date:  2014-07-17

8.  18F-THK5351: A Novel PET Radiotracer for Imaging Neurofibrillary Pathology in Alzheimer Disease.

Authors:  Ryuichi Harada; Nobuyuki Okamura; Shozo Furumoto; Katsutoshi Furukawa; Aiko Ishiki; Naoki Tomita; Tetsuro Tago; Kotaro Hiraoka; Shoichi Watanuki; Miho Shidahara; Masayasu Miyake; Yoichi Ishikawa; Rin Matsuda; Akie Inami; Takeo Yoshikawa; Yoshihito Funaki; Ren Iwata; Manabu Tashiro; Kazuhiko Yanai; Hiroyuki Arai; Yukitsuka Kudo
Journal:  J Nucl Med       Date:  2015-11-05       Impact factor: 10.057

9.  Tau positron emission tomographic imaging in aging and early Alzheimer disease.

Authors:  Keith A Johnson; Aaron Schultz; Rebecca A Betensky; J Alex Becker; Jorge Sepulcre; Dorene Rentz; Elizabeth Mormino; Jasmeer Chhatwal; Rebecca Amariglio; Kate Papp; Gad Marshall; Mark Albers; Samantha Mauro; Lesley Pepin; Jonathan Alverio; Kelly Judge; Marlie Philiossaint; Timothy Shoup; Daniel Yokell; Bradford Dickerson; Teresa Gomez-Isla; Bradley Hyman; Neil Vasdev; Reisa Sperling
Journal:  Ann Neurol       Date:  2015-12-15       Impact factor: 10.422

10.  Longitudinal Assessment of Tau Pathology in Patients with Alzheimer's Disease Using [18F]THK-5117 Positron Emission Tomography.

Authors:  Aiko Ishiki; Nobuyuki Okamura; Katsutoshi Furukawa; Shozo Furumoto; Ryuichi Harada; Naoki Tomita; Kotaro Hiraoka; Shoichi Watanuki; Yoichi Ishikawa; Tetsuro Tago; Yoshihito Funaki; Ren Iwata; Manabu Tashiro; Kazuhiko Yanai; Yukitsuka Kudo; Hiroyuki Arai
Journal:  PLoS One       Date:  2015-10-13       Impact factor: 3.240
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  3 in total

1.  In Vivo Characterization and Quantification of Neurofibrillary Tau PET Radioligand 18F-MK-6240 in Humans from Alzheimer Disease Dementia to Young Controls.

Authors:  Tobey J Betthauser; Karly A Cody; Matthew D Zammit; Dhanabalan Murali; Alexander K Converse; Todd E Barnhart; Charles K Stone; Howard A Rowley; Sterling C Johnson; Bradley T Christian
Journal:  J Nucl Med       Date:  2018-05-18       Impact factor: 10.057

2.  Automation of a Positron-emission Tomography (PET) Radiotracer Synthesis Protocol for Clinical Production.

Authors:  Eric Schopf; Christopher M Waldmann; Jeffrey Collins; Christopher Drake; Roger Slavik; R Michael van Dam
Journal:  J Vis Exp       Date:  2018-10-26       Impact factor: 1.355

3.  Strategy for Screening of Antioxidant Compounds from Two Ulmaceae Species Based on Liquid Chromatography-Mass Spectrometry.

Authors:  Joong Yeun Won; Su Young Son; Sunmin Lee; Digar Singh; Sarah Lee; Jong Seok Lee; Choong Hwan Lee
Journal:  Molecules       Date:  2018-07-23       Impact factor: 4.411
  3 in total

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