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Literature DB >> 25431646

Microfluidic continuous-flow radiosynthesis of [¹⁸F]FPEB suitable for human PET imaging.

Steven H Liang¹, Daniel L Yokell², Raul N Jackson², Peter A Rice², Ronald Callahan¹, Keith A Johnson¹, David Alagille³, Gilles Tamagnan³, Thomas Lee Collier⁴, Neil Vasdev¹.

Abstract

The synthesis of fluorine-18 labeled 3-fluoro-5-[(pyridin-3-yl)ethynyl] benzonitrile ([18F]FPEB) for imaging metabotropic glutamate receptor subtype type 5 (mGluR5) was achieved with a commercial continuous-flow microfluidics device. This work represents the first positron emission tomography (PET) radiopharmaceutical that is suitable for human use with this technology. We also describe a validated synthesis of [18F]FPEB with a commercial reactor-based system.

Entities: Chemical Disease Gene Species

Year: 2014 PMID： 25431646 PMCID： PMC4243709 DOI： 10.1039/C3MD00335C

Source DB: PubMed Journal: Medchemcomm ISSN： 2040-2503 Impact factor: 3.597

19 in total

1. The up-regulation of metabotropic glutamate receptor 5 (mGluR5) in Down's syndrome brains.

Authors: A Oka; S Takashima
Journal: Acta Neuropathol Date: 1999-03 Impact factor: 17.088

Review 2. Micro-reactors for PET tracer labeling.

Authors: S Y Lu; V W Pike
Journal: Ernst Schering Res Found Workshop Date: 2007

Review 3. Microreactors for radiopharmaceutical synthesis.

Authors: Arkadij M Elizarov
Journal: Lab Chip Date: 2009-03-26 Impact factor: 6.799

4. Enhanced binding of metabotropic glutamate receptor type 5 (mGluR5) PET tracers in the brain of parkinsonian primates.

Authors: R Sanchez-Pernaute; J-Q Wang; D Kuruppu; L Cao; W Tueckmantel; A Kozikowski; O Isacson; A-L Brownell
Journal: Neuroimage Date: 2008-04-20 Impact factor: 6.556

5. Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers.

Authors: Terence G Hamill; Stephen Krause; Christine Ryan; Celine Bonnefous; Steve Govek; T Jon Seiders; Nicholas D P Cosford; Jeffrey Roppe; Ted Kamenecka; Shil Patel; Raymond E Gibson; Sandra Sanabria; Kerry Riffel; Waisi Eng; Christopher King; Xiaoqing Yang; Mitchell D Green; Stacey S O'Malley; Richard Hargreaves; H Donald Burns
Journal: Synapse Date: 2005-06-15 Impact factor: 2.562

6. Syntheses of mGluR5 PET radioligands through the radiofluorination of diaryliodonium tosylates.

Authors: Sanjay Telu; Joong-Hyun Chun; Fabrice G Siméon; Shuiyu Lu; Victor W Pike
Journal: Org Biomol Chem Date: 2011-08-16 Impact factor: 3.876

7. Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.

Authors: David Alagille; Herve DaCosta; Yelin Chen; Kamondanai Hemstapat; Alice Rodriguez; Ronald M Baldwin; P Jeffrey Conn; Jeffrey P Conn; Gilles D Tamagnan
Journal: Bioorg Med Chem Lett Date: 2011-04-20 Impact factor: 2.823

8. Syntheses of 11C- and 18F-labeled carboxylic esters within a hydrodynamically-driven micro-reactor.

Authors: Shui-Yu Lu; Paul Watts; Frederick T Chin; Jinsoo Hong; John L Musachio; Emmanuelle Briard; Victor W Pike
Journal: Lab Chip Date: 2004-09-28 Impact factor: 6.799

9. 18F-FPEB, a PET radiopharmaceutical for quantifying metabotropic glutamate 5 receptors: a first-in-human study of radiochemical safety, biokinetics, and radiation dosimetry.

Authors: Dean F Wong; Rikki Waterhouse; Hiroto Kuwabara; Jongho Kim; James R Brašić; Wichana Chamroonrat; Michael Stabins; Daniel P Holt; Robert F Dannals; Terence G Hamill; P David Mozley
Journal: J Nucl Med Date: 2013-02-12 Impact factor: 10.057

10. Synthesis and preliminary biological evaluation of 3-[(18)F]fluoro-5-(2-pyridinylethynyl)benzonitrile as a PET radiotracer for imaging metabotropic glutamate receptor subtype 5.

Authors: Ji-Quan Wang; Werner Tueckmantel; Aijun Zhu; Daniela Pellegrino; Anna-Liisa Brownell
Journal: Synapse Date: 2007-12 Impact factor: 2.562

12 in total

Review 1. (11)C[double bond, length as m-dash]O bonds made easily for positron emission tomography radiopharmaceuticals.

Authors: Benjamin H Rotstein; Steven H Liang; Michael S Placzek; Jacob M Hooker; Antony D Gee; Frédéric Dollé; Alan A Wilson; Neil Vasdev
Journal: Chem Soc Rev Date: 2016-08-22 Impact factor: 54.564

2. Production of diverse PET probes with limited resources: 24 ¹⁸F-labeled compounds prepared with a single radiosynthesizer.

Authors: Jeffrey Collins; Christopher M Waldmann; Christopher Drake; Roger Slavik; Noel S Ha; Maxim Sergeev; Mark Lazari; Bin Shen; Frederick T Chin; Melissa Moore; Saman Sadeghi; Michael E Phelps; Jennifer M Murphy; R Michael van Dam
Journal: Proc Natl Acad Sci U S A Date: 2017-10-10 Impact factor: 11.205

Microfluidic continuous-flow radiosynthesis of [¹⁸F]FPEB suitable for human PET imaging.

1. The up-regulation of metabotropic glutamate receptor 5 (mGluR5) in Down's syndrome brains.

Review 2. Micro-reactors for PET tracer labeling.

Review 3. Microreactors for radiopharmaceutical synthesis.

4. Enhanced binding of metabotropic glutamate receptor type 5 (mGluR5) PET tracers in the brain of parkinsonian primates.

5. Synthesis, characterization, and first successful monkey imaging studies of metabotropic glutamate receptor subtype 5 (mGluR5) PET radiotracers.

6. Syntheses of mGluR5 PET radioligands through the radiofluorination of diaryliodonium tosylates.

7. Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series.

8. Syntheses of 11C- and 18F-labeled carboxylic esters within a hydrodynamically-driven micro-reactor.

9. 18F-FPEB, a PET radiopharmaceutical for quantifying metabotropic glutamate 5 receptors: a first-in-human study of radiochemical safety, biokinetics, and radiation dosimetry.

10. Synthesis and preliminary biological evaluation of 3-[(18)F]fluoro-5-(2-pyridinylethynyl)benzonitrile as a PET radiotracer for imaging metabotropic glutamate receptor subtype 5.

Review 1. (11)C[double bond, length as m-dash]O bonds made easily for positron emission tomography radiopharmaceuticals.

2. Production of diverse PET probes with limited resources: 24 ¹⁸F-labeled compounds prepared with a single radiosynthesizer.

3. Iodonium ylide-mediated radiofluorination of 18F-FPEB and validation for human use.

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

5. Total Radiosynthesis: Thinking outside "the box".

6. Synthesis of ¹⁸F-Arenes from Spirocyclic Iodonium(III) Ylides via Continuous-Flow Microfluidics.

7. Continuous-Flow Synthesis of N-Succinimidyl 4-[18F]fluorobenzoate Using a Single Microfluidic Chip.

8. Microfluidic radiosynthesis of [¹⁸F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors.

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

10. Development and implementation of ISAR, a new synthesis platform for radiopharmaceutical production.