ArticleACS pharmacology & translational science2026
A Holistic Approach to Identifying a Positron Emission Tomography (PET) Tracer Candidate for In Vivo Imaging of Purinergic P2X7 Receptor in Neuroinflammation.
Article in ACS pharmacology & translational science, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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Who cites it
1 citing paper in PubMed.
- Benzamide derivatives as allosteric ligands of the human and rat P2X7 receptor.Purinergic signalling · 2026Article
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24 authors.
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Abstract
The central role of neuroinflammation in the pathogenesis of neurodegenerative diseases and brain disorders has spurred the development of Positron Emission Tomography (PET) radiotracers to investigate neuroimmune mechanisms noninvasively in vivo. Because it is expressed in glia, the purinergic P2X7 receptor (P2X7R) is a validated target for in vivo imaging of neuroinflammation, an alternative to the 18 kDa translocator protein, which is currently the standard target for neuroinflammation in clinical practice. However, clinically validated P2X7R PET radiotracers remain needed. The present study aimed to identify a novel molecular scaffold for developing an effective P2X7R PET radiotracer, starting from three chemotypes with antagonist activity in the nanomolar range at human P2X7R, to exploit structural diversity and meet the multidimensional key attributes that a CNS PET radiotracer must have. Thus, we evaluated the selected chemotypes across a range of properties, including radioligand binding affinity at the human P2X7 receptor, off-target selectivity, in vitro metabolic stability, and nonspecific binding to brain tissue. Our study pointed to compound
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