ReviewAdvances in experimental medicine and biology2002
Interactions of flavones and other phytochemicals with adenosine receptors.
Review in Advances in experimental medicine and biology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
What it found
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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.
The trial behind it
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
26 citing papers in PubMed, 85 citations in OpenAlex.
- The effect of flavanol-rich cocoa on cerebral perfusion in healthy older adults during conscious resting state: a placebo controlled, crossover, acute trial.Psychopharmacology · 2015Trial
- Utilization of Cannabidiol in Post-Organ-Transplant Care.International journal of molecular sciences · 2025Review
- Biological Importance and Therapeutic Potential of Hispidol in Medicine: An Effective Aurone from Soybean.Current drug research reviews · 2025Article
- Possible Combinatorial Utilization of Phytochemicals and Extracellular Vesicles for Wound Healing and Regeneration.International journal of molecular sciences · 2024Review
- Natural flavonoids as potential therapeutics in the management of Alzheimer's disease: a review.3 Biotech · 2024Review
- In vivo phenotypic validation of adenosine receptor-dependent activity of non-adenosine drugs.Purinergic signalling · 2023Article
- Medicinal chemistry of P2 and adenosine receptors: Common scaffolds adapted for multiple targets.Biochemical pharmacology · 2021Review
- C3 amino-substituted chalcone derivative with selective adenosineChemicke zvesti · 2021Article
- Adenosine Receptor Ligands: Coumarin-Chalcone Hybrids as Modulating Agents on the Activity ofMolecules (Basel, Switzerland) · 2020Article
- Review
- Evaluation of Diuretic Activity and Phytochemical Contents of Aqueous Extract of the Shoot Apex ofJournal of experimental pharmacology · 2020Article
- Semisynthetic aurones inhibit tubulin polymerization at the colchicine-binding site and repress PC-3 tumor xenografts in nude mice and myc-induced T-ALL in zebrafish.Scientific reports · 2019Article
- Methoxy substituted 2-benzylidene-1-indanone derivatives as AMedChemComm · 2019Article
- Exploring Anti-Prion Glyco-Based and Aromatic Scaffolds: A Chemical Strategy for the Quality of Life.Molecules (Basel, Switzerland) · 2017Review
- A Potential Alternative against Neurodegenerative Diseases: Phytodrugs.Oxidative medicine and cellular longevity · 2016Review
- Flavonoid regulation of HCN2 channels.The Journal of biological chemistry · 2013Article
- Forging a modern generation of polyphenol-based therapeutics.British journal of pharmacology · 2013Article
- Insights into dietary flavonoids as molecular templates for the design of anti-platelet drugs.Cardiovascular research · 2013Review
- Ligand and structure-based methodologies for the prediction of the activity of G protein-coupled receptor ligands.Journal of computer-aided molecular design · 2009Article
- The interactions of flavonoids within neuronal signalling pathways.Genes & nutrition · 2007Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 3 institutions in 2 countries.
Funding
Abstract
Dietary flavonoids have varied effects on animal cells, such as inhibition of platelet binding and aggregation, inhibition of inflammation, and anticancer properties, but the mechanisms of these effects remain largely unexplained. Adenosine receptors are involved in the homeostasis of the immune, cardiovascular, and central nervous systems, and adenosine agonists/antagonists exert many similar effects. The affinity of flavonoids and other phytochemicals to adenosine receptors suggests that a wide range of natural substances in the diet may potentially block the effects of endogenous adenosine. We used competitive radioligand binding assays to screen flavonoid libraries for affinity and a computational CoMFA analysis of flavonoids to compare steric and electrostatic requirements for ligand recognition at three subtypes of adenosine receptors. Flavone derivatives, such as galangin, were found to bind to three subtypes of adenosine receptors in the microM range. Pentamethylmorin (Ki 2.65 microM) was 14- to 17-fold selective for human A3 receptors than for A1 and A2A receptors. An isoflavone, genistein, was found to bind to A1 receptors. Aurones, such as hispidol (Ki 350 nM) are selective A1 receptor antagonists, and, like genistein, are present in soy. The flavones, chemically optimized for receptor binding, have led to the antagonist, MRS 1067 (3,6-dichloro-2'-(isopropoxy)4'-methylflavone), which is 200-fold more selective for human A3 than A1 receptors. Adenosine receptor antagonism, therefore, may be important in the spectrum of biological activities reported for the flavonoids.
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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.