Uncovering Caffeine's Adenosine A2A Receptor Inverse Agonism in ...

Beneficial Effect of a Selective Adenosine A2A Receptor Antagonist ...

Consumption of caffeine, a non-selective adenosine A2A receptor (A2AR) antagonist, reduces the risk of developing Alzheimer's disease (AD) and mitigates ...

Adenosine 2A Receptor Antagonists for the Treatment of Motor ...

Theophylline is a methylxanthine that, as with caffeine, antagonizes both A1 and A2 receptors and is a nonselective phosphodiesterase inhibitor.

Neuronal A2A receptor exacerbates synapse loss and memory ...

Early pathological upregulation of adenosine A2A receptors (A2ARs), one of the caffeine targets, by neurons is thought to be involved in the ...

Structures of Human A1 and A2A Adenosine Receptors with ...

(Congreve et al., 2012), caffeine (Dore´ et al., 2011), xanthine amine congener XAC (Dore´ et al., 2011), and an inverse agonist antibody ...

Caffeine, Adenosine Receptors and Estrogen in Toxin Models of ...

Number of pages: 27. Keywords: Adenosine A2A receptor, Dopamine, Gender, Methylxanthine, Ovariectomy,. Striatum. Acknowledgements: We thank Angela Scibelli for ...

Istradefylline – a first generation adenosine A 2A antagonist for the ...

Adenosine A2A receptor antagonists in parkinson's disease: progress in clinical trials from the newly approved istradefylline to drugs in early development and ...

KD-64 – a new selective A2A adenosine receptor antagonist has ...

Obesity was induced in mice by high-fat diet and the tested compounds (KD-. 33. 64 and caffeine) were administrated for 21 days. KD-64 showed ...

Functional and Neuroprotective Role of Striatal Adenosine A 2A ...

In the striatum, adenosine A2A receptors (A2AR) are mainly expressed within the soma and dendrites of the striatopallidal neuron.

Caffeine acts through neuronal adenosine A2A receptors to prevent ...

3F); this finding is compatible with the synaptic atrophy known to occur in chronic stress (18, 19). This prophylactic effect on pharmacological ...

Caffeine, Adenosine Receptors, and Synaptic Plasticity - CiteSeerX

... adenosine A2A receptor antagonists. These effects of low micromolar concentration of caffeine (30 µM) are maintained in aged animals, which is important ...

Neuroprotection by caffeine and more specific A2A receptor ...

The authors review the evidence that caffeine and more specific antagonists of the adenosine A 2A receptor protect dopaminergic neurons in several toxin models ...

Protective Agents in Parkinson's Disease: Caffeine and Adenosine ...

Based on several findings suggesting that the adenosinergic system is one of the most interesting in the field of neuroprotection in ...

KD-64—A new selective A2A adenosine receptor antagonist ... - PLOS

Although, contrary to caffeine, KD-64 did not reduce diet-induced obesity in mice, it improved glucose tolerance. Thus, the activity of the selective adenosine ...

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine ...

The adenosine class of heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors (GPCRs) mediates the important role ...

Pathways and Mechanism of Caffeine Binding to Human Adenosine ...

Caffeine (CFF) is a common antagonist to the four subtypes of adenosine G-protein-coupled receptors (GPCRs), which are critical drug targets for treating ...

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Uncovering caffeine's adenosine a2A receptor inverse agonism in experimental parkinsonism. A C S Chemical Biology, 9(11), 2496-2501. doi:10.1021/cb5005383.

Adenosine A1-A2A receptor heteromers - IMR Press

Caffeine is a non-selective adenosine receptor antagonist, with reported similar in vitro affinities for A1, A2A and A2B receptors and with lower affinity for ...

Adenosine receptor - Wikipedia

The adenosine receptors are commonly known for their antagonists caffeine, theophylline, and theobromine, whose action on the receptors produces the ...

3RFM: Thermostabilised adenosine A2A receptor in ... - RCSB PDB

Here we report the structures of a thermostabilized adenosine A(2A) receptor in complex with the xanthines xanthine amine congener and caffeine.

the implications of adenosine 2A receptor antagonism

Aim of the study: This review aims to outline the action mechanism of A2AR antagonism on motor performance, and thus evaluate the suggested ...