ArticleNuclear medicine communications2017
Pharmacologic characterizations of a P2X7 receptor-specific radioligand, [11C]GSK1482160 for neuroinflammatory response.
Article in Nuclear medicine communications, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
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Who cites it
34 citing papers in PubMed, 66 citations in OpenAlex.
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- Review
- Synthesis and in vitro evaluation of novel compounds and discovery of a promising iodine-125 radioligand for purinergic P2X7 receptor (P2X7R).Bioorganic & medicinal chemistry · 2025Article
- A current review on P2X7 receptor antagonist patents in the treatment of neuroinflammatory disorders: a patent review on antagonists.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- Unlocking the therapeutic potential of P2X7 receptor: a comprehensive review of its role in neurodegenerative disorders.Frontiers in pharmacology · 2024Review
- Leveraging the ATP-P2X7 receptor signalling axis to alleviate traumatic CNS damage and related complications.Medicinal research reviews · 2023Review
- Animal Models for the Investigation of P2X7 Receptors.International journal of molecular sciences · 2023Review
- An emerging master inducer and regulator for epithelial-mesenchymal transition and tumor metastasis: extracellular and intracellular ATP and its molecular functions and therapeutic potential.Cancer cell international · 2023Review
- Spotlight on P2X7 Receptor PET Imaging: A Bright Target or a Failing Star?International journal of molecular sciences · 2023Review
- PET Imaging of Fructose Metabolism in a Rodent Model of Neuroinflammation with 6-[Molecules (Basel, Switzerland) · 2022Article
- Novel brain PET imaging agents: Strategies for imaging neuroinflammation in Alzheimer's disease and mild cognitive impairment.Frontiers in immunology · 2022Review
- The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry · 2021Review
- Novel Thienopyrimidine-Based PET Tracers for P2YACS chemical neuroscience · 2021Article
- Towards PET imaging of the dynamic phenotypes of microglia.Clinical and experimental immunology · 2021Review
- PET Imaging of Neuroinflammation in Alzheimer's Disease.Frontiers in immunology · 2021Review
- Platelets in Multiple Sclerosis: Early and Central Mediators of Inflammation and Neurodegeneration and Attractive Targets for Molecular Imaging and Site-Directed Therapy.Frontiers in immunology · 2021Review
- Neuroinflammation in psychiatric disorders: PET imaging and promising new targets.The lancet. Psychiatry · 2020Review
- PET imaging of P2XJournal of neuroinflammation · 2020Article
- Advances in CNS PET: the state-of-the-art for new imaging targets for pathophysiology and drug development.European journal of nuclear medicine and molecular imaging · 2020Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
Abstract
objectiveThe P2X7 receptor (P2X7R) is a key regulatory element in the neuroinflammatory cascade that provides a promising target for imaging neuroinflammation. GSK1482160, a P2X7R modulator with nanomolar binding affinity and high selectivity, has been successfully radiolabeled and utilized for imaging P2X7 levels in a mouse model of lipopolysaccharide-induced systemic inflammation. In the current study, we further characterized its binding profile and determined whether [C]GSK1482160 can detect changes in P2X7R expression in a rodent model of multiple sclerosis.
methods[C]GSK1482160 was synthesized with high specific activity and high radiochemical purity. Radioligand saturation and competition binding assays were performed for [C]GSK1482160 using HEK293-hP2X7R living cells. Micro-PET studies were carried out in nonhuman primates. In vitro autoradiography and immunohistochemistry studies were then carried out to evaluate tracer uptake and P2X7 expression in experimental autoimmune encephalomyelitis (EAE) rat lumbar spinal cord at EAE-peak and EAE-remitting stages compared with sham rats.
results[C]GSK1482160 binds to HEK293-hP2X7R living cells with high binding affinity (Kd=5.09±0.98 nmol/l, Ki=2.63±0.6 nmol/l). Micro-PET studies showed high tracer retention and a homogeneous distribution in the brain of nonhuman primates. In the EAE rat model, tracer uptake of [C]GSK1482160 in rat lumbar spinal cord was the highest at the EAE-peak stage (277.74±79.74 PSL/mm), followed by the EAE-remitting stage(149.00±54.14 PSL/mm) and sham (66.37±1.48 PSL/mm). The tracer uptake correlated strongly with P2X7-positive cell counts, activated microglia numbers, and disease severity.
conclusionWe conclude that [C]GSK1482160 has the potential for application in monitoring neuroinflammation.
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