ArticleNaunyn-Schmiedeberg's archives of pharmacology2013
In vitro pharmacological profile of the A2A receptor antagonist istradefylline.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 47 citations in OpenAlex.
- TTP protects against 6-OHDA-induced dopaminergic neurodegeneration via astrocytic Nrf2/HO-1 activation in cellular and rat models of Parkinson's disease.Metabolic brain disease · 2026Article
- Istradefylline modulates purinergic enzymes and reduces malignancy-associated factors in B16F10 melanoma cells.Purinergic signalling · 2023Article
- Molecular and Structural Insight into Adenosine AMolecular neurobiology · 2023Review
- Phenotypic Assessment of Pathogenic Variants inGenes · 2023Article
- Neuroprotection afforded by targeting G protein-coupled receptors in heteromers and by heteromer-selective drugs.Frontiers in pharmacology · 2023Review
- Discovery of Novel Dual Adenosine APharmaceuticals (Basel, Switzerland) · 2022Article
- Pathophysiological Role and Medicinal Chemistry of AMolecules (Basel, Switzerland) · 2022Review
- Expression of the Adenosine ABiomedicines · 2022Article
- ACurrent medicinal chemistry · 2022Review
- Istradefylline for OFF Episodes in Parkinson's Disease: A US Perspective of Common Clinical Scenarios.Degenerative neurological and neuromuscular disease · 2022Review
- Adenosine Receptor Antagonists to Combat Cancer and to Boost Anti-Cancer Chemotherapy and Immunotherapy.Cells · 2021Review
- Efficacy of Istradefylline, an Adenosine A2A Receptor Antagonist, as Adjunctive Therapy to Levodopa in Parkinson's Disease: A Pooled Analysis of 8 Phase 2b/3 Trials.Journal of Parkinson's disease · 2021Article
- A Pooled Analysis From Phase 2b and 3 Studies in Japan of Istradefylline in Parkinson's Disease.Movement disorders : official journal of the Movement Disorder Society · 2020Article
- Adenosine AInternational journal of molecular sciences · 2020Article
- Adenosine ACells · 2020Article
- Microbiota and Other Preventive Strategies and Non-genetic Risk Factors in Parkinson's Disease.Frontiers in aging neuroscience · 2020Article
- New Pharmacological Approaches to Treating Non-Motor Symptoms of Parkinson's Disease.Current pharmacology reports · 2016Article
- Adenosine 2A Receptor Antagonists for the Treatment of Motor Symptoms in Parkinson's Disease.Movement disorders clinical practice · 2015Review
- The role of adenosine A1 and A2A receptors in the caffeine effect on MDMA-induced DA and 5-HT release in the mouse striatum.Neurotoxicity research · 2015Article
- Antidepressant activity of the adenosine A2A receptor antagonist, istradefylline (KW-6002) on learned helplessness in rats.Psychopharmacology · 2014Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Adenosine A2A receptors are suggested to be a promising non-dopaminergic target for the treatment of Parkinson's disease (PD). Istradefylline is an adenosine A2A receptor antagonist that has been reported to exhibit antiparkinsonian activities in PD patients as well as both rodents and nonhuman primate models of PD. The aim of this study was to evaluate the in vitro pharmacological profile of istradefylline as an A2A receptor antagonist. Istradefylline exhibited high affinity for A2A receptors in humans, marmosets, dogs, rats, and mice. The affinities for the other subtypes of adenosine receptors (A1, A2B, and A3) were lower than that for A2A receptors in each species. Istradefylline demonstrated no significant affinity for other neurotransmitter receptors, including dopamine receptors (D1, D2, D3, D4, and D5). In addition, istradefylline hardly inhibited monoamine oxidase-A, monoamine oxidase-B, or catechol-O-methyl transferase. A kinetic analysis indicated that istradefylline reversibly binds to the human A2A receptors: The association reached equilibrium within 1 min, and the binding was also almost completely dissociated within 1 min. Istradefylline inhibited the A2A agonist CGS21680-induced accumulation of cAMP in the cultured cells and then shifted the concentration-response curve of CGS21680 to the right without affecting the maximal response of the agonist. These results indicate that istradefylline is a potent, selective, and competitive A2A receptor antagonist. The in vitro pharmacological profile of istradefylline helps to explain the in vivo profile of istradefylline and may be useful for clinical pharmacokinetic-pharmacodynamic considerations of efficacy and safety.
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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.