ArticleBioorganic & medicinal chemistry2010
Synthesis and biodistribution of [11C]A-836339, a new potential radioligand for PET imaging of cannabinoid type 2 receptors (CB2).
Article in Bioorganic & medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
43 citing papers in PubMed.
- Whole-body biodistribution and radiation dosimetry of the cannabinoid type 2 receptor ligand [11C]-NE40 in healthy subjects.Molecular imaging and biology · 2013Trial
- Translational molecular imaging and drug development in multiple sclerosis.Theranostics · 2026Review
- Development of Carborane-Based Halogenated Naphthyridinone-Analogues as Cannabinoid Receptor Type 2 (CBChemMedChem · 2025Article
- Cannabinoid Receptor 2 (CB2) in Macrophages: A Promising Clinical Target for Immune Disorders.International journal of molecular sciences · 2025Review
- Development of Carborane-Based Benzothiazole Analogues as Cannabinoid Receptor Type 2 (CBACS omega · 2025Article
- PET imaging of neuroinflammation: any credible alternatives to TSPO yet?Molecular psychiatry · 2025Review
- Translational Preclinical PET Imaging and Metabolic Evaluation of a New Cannabinoid 2 Receptor (CBACS pharmacology & translational science · 2024Article
- The development status of PET radiotracers for evaluating neuroinflammation.Nuclear medicine and molecular imaging · 2024Review
- Synthesis, Structure-Activity Relationships, Radiofluorination, and Biological Evaluation of [Journal of medicinal chemistry · 2023Article
- First-in-human imaging using [European journal of nuclear medicine and molecular imaging · 2023Article
- Development of the High-Affinity Carborane-Based Cannabinoid Receptor Type 2 PET Ligand [Journal of medicinal chemistry · 2023Article
- Endocannabinoid System Biomarkers in Alzheimer's Disease.Cannabis and cannabinoid research · 2023Article
- PET Imaging in Animal Models of Alzheimer's Disease.Frontiers in neuroscience · 2022Review
- The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry · 2021Review
- Towards PET imaging of the dynamic phenotypes of microglia.Clinical and experimental immunology · 2021Review
- Development of [International journal of molecular sciences · 2021Article
- Cholesterol as a modulator of cannabinoid receptor CBScientific reports · 2021Article
- Positron Emission Tomography Imaging of the Endocannabinoid System: Opportunities and Challenges in Radiotracer Development.Journal of medicinal chemistry · 2021Review
- Inflammation in Experimental Models of α-Synucleinopathies.Movement disorders : official journal of the Movement Disorder Society · 2021Review
- CB2 Receptor in Microglia: The Guardian of Self-Control.International journal of molecular sciences · 2020Review
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
Recently, A-836339 [2,2,3,3-tetramethylcyclopropanecarboxylic acid [3-(2-methoxyethyl)-4,5-dimethyl-3H-thiazol-(2Z)-ylidene]amide] (1) was reported to be a selective CB2 agonist with high binding affinity. Here we describe the radiosynthesis of [11C]A-836339 ([11C]1) via its desmethyl precursor as a candidate radioligand for imaging CB2 receptors with positron-emission tomography (PET). Whole body and the regional brain distribution of [11C]1 in control CD1 mice demonstrated that this radioligand exhibits specific uptake in the CB2-rich spleen and little specific in vivo binding in the control mouse brain. However, [11C]1 shows specific cerebral uptake in the lipopolysaccharide (LPS)-induced mouse model of neuroinflammation and in the brain areas with Abeta amyloid plaque deposition in a mouse model of Alzheimer's disease (APPswe/PS1dE9 mice). These data establish a proof of principle that CB2 receptors binding in the neuroinflammation and related disorders can be measured in vivo.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.