ArticleACS chemical biology2014
Uncovering caffeine's adenosine A2A receptor inverse agonism in experimental parkinsonism.
Article in ACS chemical biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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
21 citing papers in PubMed, 41 citations in OpenAlex.
- Caffeine and Progression of Parkinson Disease: A Deleterious Interaction With Creatine.Clinical neuropharmacologyTrial
- Pleiotropic Bioactivity of Caterpillar Fungus, Orange Cordyceps, and Cordycepin: Insight from Integrated Network Pharmacology and Food and Drug Regulatory Framework.Pharmaceuticals (Basel, Switzerland) · 2026Review
- The Effects of Caffeine on Blood Platelets and the Cardiovascular System through Adenosine Receptors.International journal of molecular sciences · 2024Review
- Molecular Variability in Levodopa Absorption and Clinical Implications for the Management of Parkinson's Disease.Journal of Parkinson's disease · 2024Review
- Caffeine-folic acid-loaded-chitosan nanoparticles combined with methotrexate as a novel HepG2 immunotherapy targeting adenosine A2A receptor downstream cascade.BMC complementary medicine and therapies · 2023Article
- Sub-millisecond conformational dynamics of the ACommunications biology · 2023Article
- Investigating G-protein coupled receptor signalling with light-emitting biosensors.Frontiers in physiology · 2023Review
- AInternational review of neurobiology · 2023Article
- Nucleoside transporters and immunosuppressive adenosine signaling in the tumor microenvironment: Potential therapeutic opportunities.Pharmacology & therapeutics · 2022Review
- A NanoBRET-Based HInternational journal of molecular sciences · 2022Article
- Article
- Functional and Neuroprotective Role of Striatal Adenosine AJournal of caffeine and adenosine research · 2019Review
- Remote control of movement disorders using a photoactive adenosine AJournal of controlled release : official journal of the Controlled Release Society · 2018Article
- Triglyceride Form of Docosahexaenoic Acid Mediates Neuroprotection in Experimental Parkinsonism.Frontiers in neuroscience · 2018Article
- The Parkinson's disease-associated GPR37 receptor interacts with striatal adenosine AScientific reports · 2017Article
- Special Issue: Adenosine Receptors.Molecules (Basel, Switzerland) · 2017Article
- The Adenosinergic System as a Therapeutic Target in the Vasculature: New Ligands and Challenges.Molecules (Basel, Switzerland) · 2017Review
- Synthesis and Characterization of a New Bivalent Ligand Combining Caffeine and Docosahexaenoic Acid.Molecules (Basel, Switzerland) · 2017Article
- Neuroprotection by caffeine in the MPTP model of parkinson's disease and its dependence on adenosine A2A receptors.Neuroscience · 2016Article
- Optical probes based on G protein-coupled receptors - added work or added value?British journal of pharmacology · 2016Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 6 institutions in 4 countries.
Funding
Abstract
Caffeine, the most consumed psychoactive substance worldwide, may have beneficial effects on Parkinson's disease (PD) therapy. The mechanism by which caffeine contributes to its antiparkinsonian effects by acting as either an adenosine A2A receptor (A2AR) neutral antagonist or an inverse agonist is unresolved. Here we show that caffeine is an A2AR inverse agonist in cell-based functional studies and in experimental parkinsonism. Thus, we observed that caffeine triggers a distinct mode, opposite to A2AR agonist, of the receptor's activation switch leading to suppression of its spontaneous activity. These inverse agonist-related effects were also determined in the striatum of a mouse model of PD, correlating well with increased caffeine-mediated motor effects. Overall, caffeine A2AR inverse agonism may be behind some of the well-known physiological effects of this substance both in health and disease. This information might have a critical mechanistic impact for PD pharmacotherapeutic design.
Indexed as
Identifiers
What OpenQuestion holds
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.