ArticleACS chemical neuroscience2018
3-Substituted 1,5-Diaryl-1 H-1,2,4-triazoles as Prospective PET Radioligands for Imaging Brain COX-1 in Monkey. Part 1: Synthesis and Pharmacology.
Article in ACS chemical neuroscience, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers, 1 of them a synthesis that pooled it.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
27 citing papers in PubMed, 1 synthesis or guideline pooled it, 39 citations in OpenAlex.
- Radiopharmaceuticals for PET and SPECT Imaging: A Literature Review over the Last Decade.International journal of molecular sciences · 2022Pooled it
- PET measurement of cyclooxygenase-2 using a novel radioligand: upregulation in primate neuroinflammation and first-in-human study.Journal of neuroinflammation · 2020Trial
- [Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2026Article
- A comprehensive review ofMedicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- Synthetic Strategies to Access Fluorinated Azoles.European journal of organic chemistry · 2025Article
- Selective Mapping of Brain COX-1 with [11C]PS13: Pharmacokinetic Evidence from human PET Imaging.IBRO neuroscience reports · 2025Article
- Expanding tracer space for positron emission tomography with high molar activityNature communications · 2025Article
- [Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2025Article
- PET imaging of neuroinflammation: any credible alternatives to TSPO yet?Molecular psychiatry · 2025Review
- The Brain-Gut Axis, an Important Player in Alzheimer and Parkinson Disease: A Narrative Review.Journal of clinical medicine · 2024Review
- Isotopologues of potassium 2,2,2-trifluoroethoxide for applications in positron emission tomography and beyond.Nature communications · 2024Article
- The development status of PET radiotracers for evaluating neuroinflammation.Nuclear medicine and molecular imaging · 2024Review
- Whole-Body PET Imaging in Humans Shows ThatJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2023Article
- Cyclooxygenases as Potential PET Imaging Biomarkers to Explore Neuroinflammation in Dementia.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Review
- The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry · 2021Review
- NRM 2021 Abstract Booklet.Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism · 2021Article
- Is cyclooxygenase-1 involved in neuroinflammation?Journal of neuroscience research · 2021Review
- RepurposingJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2021Article
- Dynamics of Cyclooxygenase-1 Positive Microglia/Macrophage in the Retina of Pathological Model Mice as a Biomarker of the Retinal Inflammatory Diseases.International journal of molecular sciences · 2021Article
- Synthesis of [ACS chemical neuroscience · 2021Article
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
Cyclooxygenase-1 (COX-1) is a key enzyme in the biosynthesis of proinflammatory thromboxanes and prostaglandins and is found in glial and neuronal cells within brain. COX-1 expression is implicated in numerous neuroinflammatory states. We aim to find a direct-acting positron emission tomography (PET) radioligand for imaging COX-1 in human brain as a potential biomarker of neuroinflammation and for serving as a tool in drug development. Seventeen 3-substituted 1,5-diaryl-1 H-1,2,4-triazoles were prepared as prospective COX-1 PET radioligands. From this set, three 1,5-(4-methoxyphenyl)-1 H-1,2,4-triazoles, carrying a 3-methoxy (5), 3-(1,1,1-trifluoroethoxy) (20), or 3-fluoromethoxy substituent (6), were selected for radioligand development, based mainly on their high affinities and selectivities for inhibiting human COX-1, absence of carboxyl group, moderate computed lipophilicities, and scope for radiolabeling with carbon-11 ( t
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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.