ArticleEJNMMI radiopharmacy and chemistry2026
Radiosynthesis and preclinical evaluation of [
Article in EJNMMI radiopharmacy and chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
backgroundGlucagon-like peptide-1 receptor (GLP-1R) is a clinically validated therapeutic target for the treatment of obesity and type 2 diabetes. GLP-1Rs expressed in the central nervous system (CNS) regulate appetite and are therefore particularly important in the context of weight loss. There is thus an emerging need for efficient and brain-penetrating Positron Emission Tomography (PET) technologies to study the distribution of GLP-1R in the CNS and facilitate the development of novel GLP-1R-targeted therapeutics. However, currently established GLP-1R PET tracers are peptide-based and exhibit limited blood-brain barrier (BBB) penetration, restricting their use for imaging central GLP-1R expression. V-0219, a small molecule GLP-1R positive allosteric modulator, represents a potential scaffold for the development of BBB-penetrating PET tracers targeting incretin receptor systems in the brain.
resultsHere, we report the radiosynthesis and preclinical evaluation of [
conclusionTaken together, these findings demonstrate the feasibility of developing small-molecule-based PET tracers targeting incretin receptor systems, while highlighting the challenges associated with achieving sufficient in vivo specificity for brain GLP-1R imaging.
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