Literature DB >> 34291178

Performing radiosynthesis in microvolumes to maximize molar activity of tracers for positron emission tomography.

Maxim E Sergeev1,2, Mark Lazari1,2,3, Federica Morgia1,2, Jeffrey Collins1,2, Muhammad Rashed Javed1,2, Olga Sergeeva1,2, Jason Jones4, Michael E Phelps1,2,5, Jason T Lee1,2,5, Pei Yuin Keng1,2,5, R Michael van Dam1,2,3,4,5.   

Abstract

Positron emission tomography (PET) is a molecular diagnostic imaging technology to quantitatively visualize biological processes in vivo. For many applications, including imaging of low tissue density targets (e.g. neuroreceptors), imaging in small animals, and evaluation of novel tracers, the injected PET tracer must be produced with high molar activity to ensure low occupancy of biological targets and avoid pharmacologic effects. Additionally, high molar activity is essential for tracers with lengthy syntheses or tracers transported to distant imaging sites. We show that radiosynthesis of PET tracers in microliter volumes instead of conventional milliliter volumes results in substantially increased molar activity, and we identify the most relevant variables affecting this parameter. Furthermore, using the PET tracer [18F]fallypride, we illustrate that molar activity can have a significant impact on biodistribution. With full automation, microdroplet platforms could provide a means for radiochemists to routinely, conveniently, and safely produce PET tracers with high molar activity.

Year:  2018        PMID: 34291178      PMCID: PMC8291036          DOI: 10.1038/s42004-018-0009-z

Source DB:  PubMed          Journal:  Commun Chem        ISSN: 2399-3669


  45 in total

Review 1.  Positron emission tomography molecular imaging for drug development.

Authors:  Paul M Matthews; Eugenii A Rabiner; Jan Passchier; Roger N Gunn
Journal:  Br J Clin Pharmacol       Date:  2012-02       Impact factor: 4.335

Review 2.  A review of imaging agent development.

Authors:  Eric D Agdeppa; Mary E Spilker
Journal:  AAPS J       Date:  2009-05-05       Impact factor: 4.009

3.  Radiolabelling diverse positron emission tomography (PET) tracers using a single digital microfluidic reactor chip.

Authors:  Supin Chen; Muhammad Rashed Javed; Hee-Kwon Kim; Jack Lei; Mark Lazari; Gaurav J Shah; R Michael van Dam; Pei-Yuin Keng; Chang-Jin C J Kim
Journal:  Lab Chip       Date:  2014-03-07       Impact factor: 6.799

Review 4.  True radiotracers: are we approaching theoretical specific activity with Tc-99m and I-123?

Authors:  William C Eckelman; Mauro Bonardi; Wynn A Volkert
Journal:  Nucl Med Biol       Date:  2008-07       Impact factor: 2.408

5.  Noninvasive nuclear imaging enables the in vivo quantification of striatal dopamine receptor expression and raclopride affinity in mice.

Authors:  Kristina Fischer; Vesna Sossi; Andreas Schmid; Martin Thunemann; Florian C Maier; Martin S Judenhofer; Julia G Mannheim; Gerald Reischl; Bernd J Pichler
Journal:  J Nucl Med       Date:  2011-06-16       Impact factor: 10.057

6.  In vivo biodistribution of no-carrier-added 6-18F-fluoro-3,4-dihydroxy-L-phenylalanine (18F-DOPA), produced by a new nucleophilic substitution approach, compared with carrier-added 18F-DOPA, prepared by conventional electrophilic substitution.

Authors:  Willem-Jan Kuik; Ido P Kema; Adrienne H Brouwers; Rolf Zijlma; Kiel D Neumann; Rudi A J O Dierckx; Stephen G DiMagno; Philip H Elsinga
Journal:  J Nucl Med       Date:  2014-12-11       Impact factor: 10.057

Review 7.  Positron emission tomography microdosing: a new concept with application in tracer and early clinical drug development.

Authors:  Mats Bergström; Anders Grahnén; Bengt Långström
Journal:  Eur J Clin Pharmacol       Date:  2003-08-22       Impact factor: 2.953

8.  Syntheses and specific activity determinations of no-carrier-added (NCA) F-18-labeled butyrophenone neuroleptics--benperidol, haloperidol, spiroperidol, and pipamperone.

Authors:  C Y Shiue; J S Fowler; A P Wolf; M Watanabe; C D Arnett
Journal:  J Nucl Med       Date:  1985-02       Impact factor: 10.057

Review 9.  From Unorthodox to Established: The Current Status of (18)F-Trifluoroborate- and (18)F-SiFA-Based Radiopharmaceuticals in PET Nuclear Imaging.

Authors:  Vadim Bernard-Gauthier; Justin J Bailey; Zhibo Liu; Björn Wängler; Carmen Wängler; Klaus Jurkschat; David M Perrin; Ralf Schirrmacher
Journal:  Bioconjug Chem       Date:  2015-11-25       Impact factor: 4.774

10.  Tantalum [18O]water target for the production of [18F]fluoride with high reactivity for the preparation of 2-deoxy-2-[18F]fluoro-D-glucose.

Authors:  N Satyamurthy; Bernard Amarasekera; C William Alvord; Jorge R Barrio; Michael E Phelps
Journal:  Mol Imaging Biol       Date:  2002-01       Impact factor: 3.488

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  7 in total

1.  Economical Production of Radiopharmaceuticals for Preclinical Imaging Using Microdroplet Radiochemistry.

Authors:  Jia Wang; R Michael van Dam
Journal:  Methods Mol Biol       Date:  2022

2.  Microliter-scale reaction arrays for economical high-throughput experimentation in radiochemistry.

Authors:  Alejandra Rios; Travis S Holloway; Philip H Chao; Christian De Caro; Chelsea C Okoro; R Michael van Dam
Journal:  Sci Rep       Date:  2022-06-17       Impact factor: 4.996

3.  On-demand radiosynthesis of N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB) on an electrowetting-on-dielectric microfluidic chip for 18F-labeling of protein.

Authors:  Hee-Kwon Kim; Muhammad Rashed Javed; Supin Chen; Kirstin A Zettlitz; Jeffrey Collins; Anna M Wu; Chang-Jin C J Kim; R Michael van Dam; Pei Yuin Keng
Journal:  RSC Adv       Date:  2019-10-09       Impact factor: 4.036

4.  Sulfur [18F]Fluoride Exchange Click Chemistry Enabled Ultrafast Late-Stage Radiosynthesis.

Authors:  Qinheng Zheng; Hongtao Xu; Hua Wang; Wen-Ge Han Du; Nan Wang; Huan Xiong; Yuang Gu; Louis Noodleman; K Barry Sharpless; Guang Yang; Peng Wu
Journal:  J Am Chem Soc       Date:  2021-02-25       Impact factor: 15.419

5.  Synthesis of [18F]PS13 and Evaluation as a PET Radioligand for Cyclooxygenase-1 in Monkey.

Authors:  Carlotta Taddei; Cheryl L Morse; Min-Jeong Kim; Jeih-San Liow; Jose Montero Santamaria; Andrea Zhang; Lester S Manly; Paolo Zanotti-Fregonara; Robert L Gladding; Sami S Zoghbi; Robert B Innis; Victor W Pike
Journal:  ACS Chem Neurosci       Date:  2021-01-25       Impact factor: 5.780

6.  Multi-GBq production of the radiotracer [18F]fallypride in a droplet microreactor.

Authors:  Jia Wang; Philip H Chao; Roger Slavik; R Michael van Dam
Journal:  RSC Adv       Date:  2020-02-24       Impact factor: 4.036

7.  A novel multi-reaction microdroplet platform for rapid radiochemistry optimization.

Authors:  Alejandra Rios; Jia Wang; Philip H Chao; R Michael van Dam
Journal:  RSC Adv       Date:  2019-07-01       Impact factor: 4.036

  7 in total

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