ArticleActa pharmacologica Sinica2013
Modulation of A₂a receptor antagonist on D₂ receptor internalization and ERK phosphorylation.
Article in Acta pharmacologica Sinica, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 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
14 citing papers in PubMed, 29 citations in OpenAlex.
- Inhibition of Retinal AdoRA2a Activity Attenuates Myopia Progression.Investigative ophthalmology & visual science · 2026Article
- Stabilized DNature communications · 2025Article
- Unique effect of clozapine on adenosine ABiomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2023Article
- Enhancement of adenosine AFrontiers in neuroscience · 2022Article
- Potential Treat-to-Target Approach for Methamphetamine Use Disorder: A Pilot Study of Adenosine 2A Receptor Antagonist With Positron Emission Tomography.Frontiers in pharmacology · 2022Article
- NOX1/NADPH Oxidase Promotes Synaptic Facilitation Induced by Repeated DThe Journal of neuroscience : the official journal of the Society for Neuroscience · 2021Article
- Allosteric Interactions between Adenosine AInternational journal of molecular sciences · 2021Review
- Effects of an Adenosine AFrontiers in neuroscience · 2021Article
- Antipsychotic-Like Efficacy of Dopamine DMolecular neurobiology · 2018Article
- Essential Control of the Function of the Striatopallidal Neuron by Pre-coupled Complexes of Adenosine AFrontiers in pharmacology · 2018Article
- Reduced sleep duration mediates decreases in striatal D2/D3 receptor availability in cocaine abusers.Translational psychiatry · 2016Article
- Caffeine increases striatal dopamine D2/D3 receptor availability in the human brain.Translational psychiatry · 2015Article
- Intracellular calcium levels determine differential modulation of allosteric interactions within G protein-coupled receptor heteromers.Chemistry & biology · 2014Article
- An Adenosine AeNeuroArticle
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimTo explore the effects of heterodimerization of D2 receptor/A2a receptor (D2R/A2aR) on D2R internalization and D2R downstream signaling in primary cultured striatal neurons and HEK293 cells co-expressing A2aR and D2R in vitro.
methodsPrimary cultured rat striatal neurons and HEK293 cells co-expressing A2aR and D2R were treated with A2aR- or D2R-specific agonists. D2R internalization was detected using a biotinylation assay and confocal microscopy. ERK, Src kinase and β-arrestin were measured using Western blotting. The interaction between A2aR and D2R was detected using bioluminescence resonance energy transfer (BRET) and immunoprecipitation.
resultsD2R and A2aR were co-localized and formed complexes in striatal neurons, while both the receptors formed heterodimers in the HEK293 cells. In striatal neurons and the HEK293 cells, the D2R agonist quinpirole (1 μmol/L) marked increased Src phosphorylation and β-arrestin recruitment, thereby D2R internalization. Co-treatment with the A2aR antagonist ZM241385 (100 nmol/L) significantly attenuated these D2R-mediated changes. Furthermore, both ZM241385 (100 nmol/L) and the specific Src kinase inhibitor PP2 (5 μmol/L) blocked D2R-mediated ERK phosphorylation. Moreover, expression of the mutant β-arrestin (319-418) significantly attenuated D2R-mediated ERK phosphorylation in HEK293 cells expressing both D2R and A2aR, but not in those expressing D2R alone.
conclusionA2aR antagonist ZM241385 significantly attenuates D2R internalization and D2R-mediated ERK phosphorylation in striatal neurons, involving Src kinase and β-arrestin. Thus, A2aR/D2R heterodimerization plays important roles in D2R downstream signaling.
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.