ArticleNuclear medicine and biology2014
Synthesis and evaluation of [(11)C]PyrATP-1, a novel radiotracer for PET imaging of glycogen synthase kinase-3β (GSK-3β).
Article in Nuclear medicine and biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 33 citations in OpenAlex.
- Current Landscape of Glycogen Synthase Kinase-3β PET Tracers: Progress, Limitations, and Perspectives-A Narrative Review.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Evaluation of [ACS chemical neuroscience · 2025Article
- Radiosynthesis and Evaluation ofACS pharmacology & translational science · 2025Article
- Synthesis and preliminary evaluation of novel PET probes for GSK-3 imaging.Scientific reports · 2024Article
- Radiosynthesis and evaluation of a novelAmerican journal of nuclear medicine and molecular imaging · 2024Article
- Development and Optimization ofACS pharmacology & translational science · 2023Review
- Harnessing dual-energy CT for glycogen quantification: a phantom analysis.Quantitative imaging in medicine and surgery · 2023Article
- PET imaging of glycogen synthase kinase-3 in pancreatic cancer xenograft mouse models.American journal of nuclear medicine and molecular imaging · 2022Article
- The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry · 2021Review
- Radiofluorination of oxazole-carboxamides for preclinical PET neuroimaging of GSK-3.Journal of fluorine chemistry · 2021Article
- Radiosynthesis and in Vivo Evaluation of [ACS chemical neuroscience · 2017Article
- Development of [ACS medicinal chemistry letters · 2017Article
- Failed PET Application Attempts in the Past, Can We Avoid Them in the Future?Molecular imaging and biology · 2016Article
- Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.Angewandte Chemie (International ed. in English) · 2016Article
- Synthesis of Diverse (11)C-Labeled PET Radiotracers via Direct Incorporation of [(11)C]CO2.Bioconjugate chemistry · 2016Article
- Synthesis and Evaluation of [(18)F]RAGER: A First Generation Small-Molecule PET Radioligand Targeting the Receptor for Advanced Glycation Endproducts.ACS chemical neuroscience · 2016Article
- Glycogen Synthase Kinase-3 (GSK-3)-Targeted Therapy and Imaging.Theranostics · 2016Review
- Recent Advances in the Development and Application of Radiolabeled Kinase Inhibitors for PET Imaging.Molecules (Basel, Switzerland) · 2015Review
- Synthesis and evaluation of [MedChemComm · 2015Article
- Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3.ACS medicinal chemistry letters · 2015Article
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7 authors at 1 institution in 1 country.
Funding
Abstract
introductionThe dysfunction of glycogen synthase kinase-3β (GSK-3β) has been implicated in a number of diseases, including Alzheimer's disease. The ability to non-invasively quantify GSK-3β activity in vivo is therefore of critical importance, and this work is focused upon development of inhibitors of GSK-3β radiolabeled with carbon-11 to examine quantification of the enzyme using positron emission tomography (PET) imaging.
methods(11)C PyrATP-1 was prepared from the corresponding desmethyl-piperazine precursor in an automated synthesis module. In vivo rodent and primate imaging studies were conducted on a Concorde MicroPET P4 scanner to evaluate imaging properties and in vitro autoradiography studies with rat brain samples were carried out to examine specific binding.
results2035±518MBq (55±14mCi) of [(11)C]PyrATP-1 was obtained (1%-2% non-corrected radiochemical yield at end-of-synthesis based upon [(11)C]CO2) with high chemical (>95%) and radiochemical (>99%) purities, and good specific activities (143±52GBq/μmol (3874±1424Ci/mmol)), n=5. In vivo microPET imaging studies revealed poor brain uptake in rodents and non-human primates. Pretreatment of rodents with cyclosporin A resulted in moderately increased brain uptake suggesting Pgp transporter involvement. Autoradiography demonstrated high levels of specific binding in areas of the rodent brain known to be rich in GSK-3β.
conclusion(11)C PyrATP-1 is readily synthesized using standard carbon-11 radiochemistry. However the poor brain uptake in rodents and non-human primates indicates that the radiotracer is not suitable for the purposes of quantifying GSK-3β in neurological and psychiatric disorders.
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