ArticleProceedings of the National Academy of Sciences of the United States of America2008
Adenosine receptor antagonists alter the stability of human epileptic GABAA receptors.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 49 citations in OpenAlex.
- Direct energy consumption by inhibitory GABAFrontiers in neuroscience · 2026Article
- α4β2The Journal of physiology · 2025Article
- Regulation of GABAergic neurotransmission by purinergic receptors in brain physiology and disease.Purinergic signalling · 2025Review
- Selective modulation of epileptic tissue by an adenosine ABritish journal of pharmacology · 2024Article
- Exploration of chalcones and related heterocycle compounds as ligands of adenosine receptors: therapeutics development.Molecular diversity · 2022Review
- ATP and adenosine-Two players in the control of seizures and epilepsy development.Progress in neurobiology · 2021Review
- Role of Adenosine in Epilepsy and Seizures.Journal of caffeine and adenosine research · 2020Review
- G protein-coupled receptors in acquired epilepsy: Druggability and translatability.Progress in neurobiology · 2019Review
- The role of adenosine in epilepsy.Brain research bulletin · 2019Review
- The Taste of Caffeine.Journal of caffeine research · 2017Review
- Nitrobenzylthioinosine mimics adenosine to attenuate the epileptiform discharge of hippocampal neurons from epileptic rats.Oncotarget · 2017Article
- Adenosinergic signaling in epilepsy.Neuropharmacology · 2016Review
- When GABA Fails: Rundown on Chemokines.Epilepsy currents · 2014Article
- Article
- Homeostatic control of synaptic activity by endogenous adenosine is mediated by adenosine kinase.Cerebral cortex (New York, N.Y. : 1991) · 2014Article
- Functional interaction between pre-synaptic α6β2-containing nicotinic and adenosine A2A receptors in the control of dopamine release in the rat striatum.British journal of pharmacology · 2013Article
- Adenosine release during seizures attenuates GABAA receptor-mediated depolarization.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2012Article
- The role of extracellular adenosine in chemical neurotransmission in the hippocampus and Basal Ganglia: pharmacological and clinical aspects.Current topics in medicinal chemistry · 2011Review
- GABA(A) Receptors: Post-Synaptic Co-Localization and Cross-Talk with Other Receptors.Frontiers in cellular neuroscience · 2011Article
- Modulators of nucleoside metabolism in the therapy of brain diseases.Current topics in medicinal chemistry · 2011Review
Corrections and comments
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Authors and funding
16 authors at 5 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We examined how the endogenous anticonvulsant adenosine might influence gamma-aminobutyric acid type A (GABA(A)) receptor stability and which adenosine receptors (ARs) were involved. Upon repetitive activation (GABA 500 microM), GABA(A) receptors, microtransplanted into Xenopus oocytes from neurosurgically resected epileptic human nervous tissues, exhibited an obvious GABA(A)-current (I(GABA)) run-down, which was consistently and significantly reduced by treatment with the nonselective adenosine receptor antagonist CGS15943 (100 nM) or with adenosine deaminase (ADA) (1 units/ml), that inactivates adenosine. It was also found that selective antagonists of A2B (MRS1706, 10 nM) or A3 (MRS1334, 30 nM) receptors reduced I(GABA) run-down, whereas treatment with the specific A1 receptor antagonist DPCPX (10 nM) was ineffective. The selective A2A receptor antagonist SCH58261 (10 nM) reduced or potentiated I(GABA) run-down in approximately 40% and approximately 20% of tested oocytes, respectively. The ADA-resistant, AR agonist 2-chloroadenosine (2-CA) (10 microM) potentiated I(GABA) run-down but only in approximately 20% of tested oocytes. CGS15943 administration again decreased I(GABA) run-down in patch-clamped neurons from either human or rat neocortex slices. I(GABA) run-down in pyramidal neurons was equivalent in A1 receptor-deficient and wt neurons but much larger in neurons from A2A receptor-deficient mice, indicating that, in mouse cortex, GABA(A)-receptor stability is tonically influenced by A2A but not by A1 receptors. I(GABA) run-down from wt mice was not affected by 2-CA, suggesting maximal ARs activity by endogenous adenosine. Our findings strongly suggest that cortical A2-A3 receptors alter the stability of GABA(A) receptors, which could offer therapeutic opportunities.
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