Adenosine A2A
Effects of adenosine A2a receptor agonist and antagonist on cere-bellar nuclear factor-kBexpression preceded by MDMA toxicity
... Our data demonstrated the neurotoxic ef- fects of MDMA on cell death induced by this drug in the rat cerebellum. MDMA caused a significant increase in the number of dark cerebellar neurons compared to control. Dark ...
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Dual roles of the adenosine A2a receptor in autoimmune neuroinflammation
... We here report a profound and complex involvement of adenosine A2a receptor signaling in EAE, an animal model of multiple sclerosis. We show that A2aR is upregulated in the CNS tissue during experimental ...
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Adenosine A2A receptor antagonists act at the hyperoxic phase to confer protection against retinopathy
... vaso-obliteration and hypoxia-induced revascularization (Zhang et al. 2015). This proposal is further substantiated by a recent large prospective phase III clinical study “Caf- feine Therapy for Apnea of Prematurity” ...
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Adenosine A2A receptors promote collagen production by a Fli1 and CTGF mediated mechanism
... Transforming growth factor (TGF- b ) is known to be a critical regulator of matrix synthesis [26-28], and Fli1 is phosphorylated and acetylated following TGF- b 1 treat- ment in dermal fibroblasts [21,26-28]. On the ...
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Protection from pulmonary ischemia-reperfusion injury by adenosine A2A receptor activation
... We utilized 8–10 week old wild-type (WT) C57BL/6J mice (The Jackson Laboratory, Bar Harbor, ME) and A 2A AR knockout (KO) mice congenic to C57BL/6J [32]. Three groups of animals were studied (n = 6/group); a sham group, ...
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Characterization of the trigeminovascular actions of several adenosine A2A receptor antagonists in an in vivo rat model of migraine
... adenosine-induced dilation of endothelium-denuded middle meningeal arteries [18]. In these experiments, not only did caffeine (50 μM) or SCH58261 (1 μM) pre- vent the dural dilation, but a vasoconstriction to ...
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Human adenosine A2A receptor : molecular mechanism of ligand binding and activation
... A 2A R residues that directly interact with each ligand (distances < 4 Å) are indicated by filled cells and colored according to the ligand type with which they interact (agonists only, red; antagonists only, blue; ...
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The effect of an adenosine A2A agonist on intra-tumoral concentrations of temozolomide in patients with recurrent glioblastoma
... Overall, our study failed to demonstrate that brain interstitial temozolomide concentrations were increased by use of standard dose regadenoson; which we pre- specified as an increase in temozolomide brain concen- ...
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Cryo EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein
... map was very similar to the electron density map from the X-ray structure, despite the reported res- olutions being 4.1 A˚ and 3.4 A˚, respectively. This highlights the importance of the local resolution vs the global ...
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Test-retest variability of adenosine A2A binding in the human brain with 11C-TMSX and PET
... For BP ND values, the mean TRV was between ±10% using either cerebral cortex or cen- trum semiovale as a reference region, and always smaller than its standard deviation, further indicat[r] ...
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Adenosine A2A receptor activation reduces recurrence and mortality from Clostridium difficileinfection in mice following vancomycin treatment
... ATL 146e, was shown to reduce mortality in endotoxe- mia from LPS but not in E . coli septicemia unless anti- biotic was also given [19]. It is possible that adenosine is utilized by bacteria to enhance virulence ...
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Spare Adenosine A2a Receptors Are Associated with Positive Exercise Stress Test in Coronary Artery Disease
... It would have been expected that the presence of spare A 2A R would increase coronary blood flow in CAD patients as it would in an animal model, where an activation of only 5% of A 2A R present in the coronary system was ...
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Baicalin attenuates bleomycin-induced pulmonary fibrosis via adenosine A2a receptor related TGF-β1-induced ERK1/2 signaling pathway
... IPF. Adenosine, an endogenous intracellular purine nucleoside, is at low concentrations extracellularly under normal conditions, but released increasingly by cells during inflammation and tissue destruction [8, ...
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Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation
... potentiate adenosine- mediated activation of endogenous ARs in intact PC-12 ...enhanced adenosine-mediated cAMP production by PC-12 cells in a dose-dependent manner (Figure ...and adenosine was ...
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Adenosine A2 Receptor: Novel Target for the Management of Parkinsonism
... of adenosine A2A receptors in basal ganglia that are richly innervated by dopamine, and their antagonistic role towards the stimulation of dopamine receptors, have positioned A2A receptor antagonists ...
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Advances in Sickle Cell Therapies in the Hydroxyurea Era
... (2010) Adenosine A2A re- ceptors induced on iNKT and NK cells reduce pulmonary inflammation and injury in mice with sickle cell disease.. Field JJ, et alN[r] ...
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Effectiveness of Istradefylline for Fatigue and Quality of Life in Parkinson’s Disease Patients’ and of Their Caregivers’
... Adenosine A2A receptors are highly localized to the basal ganglia and are selectively localized on medium spiny neurons of the indirect output pathway, projecting from the striatum to the external globus ...
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Active state structures of G protein coupled receptors highlight the similarities and differences in the G protein and arrestin coupling interfaces
... Nonetheless, three new structures of GPCRs in an active state have been published during the last year, namely the adenosine A2A receptor A2AR bound to an engineered G protein, opsin bou[r] ...
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Commentary: Benzodiazepine (BZD) and Related BZD Receptor Agonists: Basic Science Reasons to Limit to Four Weeks or Less
... BZDs have little-known or underappreciated actions at receptors other than their well-known GABAA receptor action e.g., BZDs potentiate adenosine A2A receptor-mediated effects, alloste[r] ...
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A2A adenosine receptor modulates drug efflux transporter P glycoprotein at the blood brain barrier
... In brain endothelial cells, P-gp is localized in lipid raft, more specifically, in caveolae. Caveolae are specialized membrane (lipid) rafts that contain the caveolin protein and are characterized as flask-like ...
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