Adenosine A2A receptor
Dual roles of the adenosine A2a receptor in autoimmune neuroinflammation
... of adenosine A2a receptor signaling in EAE, an animal model of multiple ...the receptor lead to a stronger acti- vation of the immune system, reflected by a marked Th17 ...
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Effects of adenosine A2a receptor agonist and antagonist on cere-bellar nuclear factor-kBexpression preceded by MDMA toxicity
... of A2a-R on the NF-kB expression in the rat cerebellum after ...an A2a- R agonist, increased NF-kB expression in the rat cerebellum that previously received MDMA ...The adenosine A2a ...
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Characterization of the trigeminovascular actions of several adenosine A2A receptor antagonists in an in vivo rat model of migraine
... agonist CGS21680 (10 μg/kg, i.v., n = 24; the optimal dose as determined in 7 pilot experiments, data not shown). Dural vasodilator responses remained unchanged after re- peated treatment for 4 times (data not shown) and ...
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Structure activity relationships of the sustained effects of adenosine A2A receptor agonists driven by slow dissociation kinetics
... slow A2A agonist dissociation kinetics have been cited as a potential mechanism to achieve a desirable clinical response for topically applied drugs (Mantell et ...for A2A where the receptor has been ...
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Suppression of inflammation by low dose methotrexate is mediated by adenosine A2A receptor but not A3receptor activation in thioglycollate induced peritonitis
... Methotrexate is an effective disease-modifying drug widely used in low doses at weekly intervals for the control of rheu- matoid arthritis and psoriasis with a relatively safe profile com- pared with other therapies ...
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Adenosine A2A receptor activation reduces recurrence and mortality from Clostridium difficileinfection in mice following vancomycin treatment
... novo adenosine synthesis ...normal adenosine homeo- stasis, extracellular adenosine concentrations can be lower than 1 μM ...and adenosine secretion in inflammatory and other cell ...
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Cryo EM structure of the adenosine A2A receptor coupled to an engineered heterotrimeric G protein
... Nb35), which was then subtracted from the original particles. The resulting particles were used to produce an accurate map of the micelle and thioredoxin, which was then used to perform signal sub- traction of the ...
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Adenosine A2A receptor antagonists act at the hyperoxic phase to confer protection against retinopathy
... GFAP expression in the avascular area. Analysis showed that OIR markedly reduced GFAP-positive cells, as ex- pected, but KW6002 partially reversed this reduction of astrocyte function in retina compared to the ...
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Effects of adenosine A2A receptor activation and alanyl glutamine in Clostridium difficile toxin induced ileitis in rabbits and cecitis in mice
... shown to decrease inflammatory responses and improved survival in mouse models of endotoxemia and sepsis [40,41]. Several experimental studies have shown that alanyl-glutamine is at least as effective as glutamine in ...
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Caffeine and a selective adenosine A2A receptor antagonist induce sensitization and cross-sensitization behavior associated with increased striatal dopamine in mice
... following chronic treatment. Chronic treatment with a selective adenosine A 1 antagonist DPCPX did not demon- strate locomotor sensitization. Our results suggest that chronic administration of low dosages of ...
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Activation of microglial cells triggers a release of brain-derived neurotrophic factor (BDNF) inducing their proliferation in an adenosine A2A receptor-dependent manner: A2A receptor blockade prevents BDNF release and proliferation of microglia
... including adenosine [5]. The relation between adenosine and neuroinflammation is heralded by the key role of adenosine A 2A receptors (A 2A R) ...
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Large-scale functional expression of WT and truncated human adenosine A2A receptor in Pichia pastoris bioreactor cultures
... functional receptor from the flask ...functional receptor for the first 4 hours post induction (Figure 3A) while after this time functional expression increased rapidly, as measured at 14 ...measurable ...
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Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation
... release adenosine during normal metabolic ...hypoxia, adenosine production and release are elevated [3-5]. Endogenous adenosine is rapidly degraded and therefore its presence is limited to sites of ...
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Human adenosine A2A receptor : molecular mechanism of ligand binding and activation
... the receptor, and the position of NECA (shown as sticks) is essentially identical in both states (Carpenter et ...the receptor an outward movement of H6 by 14 Å (indicated by a red arrow) is required to ...
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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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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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Effectiveness of Istradefylline for Fatigue and Quality of Life in Parkinson’s Disease Patients’ and of Their Caregivers’
... selective adenosine A2A receptor antagonist, for the treatment of non-motor symptoms and quality of life (QoL) in Parkinson’s disease (PD) patients with and QoL in their ...
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A New Class of Fluorinated A(2A) Adenosine Receptor Agonist with Application to Last-Step Enzymatic [F-18]Fluorination for PET Imaging
... where adenosine is responsible for regulating the vasodilation of the coronary arteries, thus mediating coronary blood ...flow. Adenosine receptors are also significant in particular regions of the brain ...
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Impaired vasocontractile responses to adenosine in chorionic vessels of human term placenta from pregnant women with pre existing and gestational diabetes
... to adenosine of chorionic vessels (arteries and veins) from both GDM and T1DM, suggesting a systemic alteration of adenosine signalling in the fetoplacental circulation in maternal ...a ...
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Human mesenchymal stromal cells inhibit platelet activation and aggregation involving CD73-converted adenosine
... A2AR: Adenosine 2A receptor; ADA: Adenosine deaminase; ADP: Adenosine diphosphate; ALP: Alkaline phosphatase; AMP: Adenosine monophosphate; AMP-CP: α , β -Methyleneadenosine 5 ′ ...
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