In vitro pharmacological profile of KW-6356, a novel adenosine A2A receptor antagonist/inverse agonist

Y Ohno, M Suzuki, H Asada, T Kanda, M Saki… - Molecular …, 2023 - ASPET
… the inhibition of glutamate NMDA receptor (polyamine site), 1 … residues 1-316 of human A
2A receptor with residues Lys209… radioligands for the adenosine receptors were determined …

Adenosine A2A receptor antagonists: from caffeine to selective non‐xanthines

KA Jacobson, ZG Gao, P Matricon… - British journal of …, 2022 - Wiley Online Library
Adenosine acting at adenosine receptors provides an … 2A receptors modulate the activity of
excitatory glutamatergic … conserved residues including Asp52 2.50 , and replacement of these …

PET Imaging of the Interaction between Adenosine A2A and Dopamine D2 Receptors in Animal Models of Brain Diseases

K Prasad - 2023 - research.rug.nl
… to four subtypes of adenosine receptors, called A1, A2A, A2B … of these receptors in modulating
the excitatory glutamatergic … (aspartic/phosphorylated serine residues) in the Cterminal tail …

Biophysical Dissection of Isolated GPCRs: The Adenosine A2A Receptor under the Bistouries

JL Banères, T Botzanowski, JA Boutin, B Calamini… - Receptors, 2023 - mdpi.com
… high A 2A affinity antagonist at adenosine receptors [92], which … glutamate decarboxylase
(PGD). Accordingly, after the fusion of the 26-residue PGD-tag to the N-terminus of the receptor

Irreversible Antagonists for the Adenosine A2B Receptor

A Temirak, JG Schlegel, JH Voss, VJ Vaaßen… - Molecules, 2022 - mdpi.com
… It activates G protein-coupled adenosine receptor (AR) … Hence, we conclude that another
residue is responsible for … supplemented with 8 mM l-glutamine before use and split to 0.5 mio. …

The Signaling Pathways Involved in the Anticonvulsive Effects of the Adenosine A1 Receptor

J Spanoghe, LE Larsen, E Craey, S Manzella… - International journal of …, 2020 - mdpi.com
… of this review will focus on this adenosine receptor subtype. … EC) slices, adenosine-mediated
suppression of glutamatergic … the serine residues involved in receptor trafficking. A study in …

Oligomerization of the Human Adenosine A2A Receptor is Driven by the Intrinsically Disordered C-terminus

KDQ Nguyen, M Vigers, E Sefah, S Seppälä… - BioRxiv, 2020 - biorxiv.org
… -terminus of A 2A R and the third intracellular loop of D 2 R(66)… the homooligomerization of
the human adenosine A 2A R, a … cysteine residue C394 and a cluster of charged residues 355 …

A2A Adenosine Receptor Antagonists: Are Triazolotriazine and Purine Scaffolds Interchangeable?

A Spinaci, C Lambertucci, M Buccioni, D Dal Ben… - Molecules, 2022 - mdpi.com
… We employed the crystal structures of the human A 2A AR … and residue interaction forces
and the per-residue interaction … We focused on the above residues located in proximity of the …

Pharmacological and functional characterization of adenosine" A2" receptors as emerging targets in cerebral ischemia and oligodendrogliogenesis: an in vitro study

M Venturini - 2023 - flore.unifi.it
A2A adenosine receptors are highly conserved with 90% of … It is possible that other
mechanisms concur to the “residual … they inhibit glutamate release, adenosine potently increases …

Association Between Adenosine A2A Receptors and Connexin 43 Regulates Hemichannels Activity and ATP Release in Astrocytes Exposed to Amyloid-β Peptides

D Madeira, L Dias, P Santos, RA Cunha… - Molecular …, 2021 - Springer
… , ATP and glutamate) exchange with the extracellular medium. … phosphorylation at Ser368
residue in astrocytes challenged … and hippocampal glutamatergic neurons loss in human and …