A2A Adenosine Receptor Binding Parameters in Platelets from Patients Affected by Pathological Gambling

2011 ◽  
Vol 63 (3) ◽  
pp. 154-159 ◽  
Author(s):  
Claudia Martini ◽  
Simona Daniele ◽  
Michela Picchetti ◽  
Anna Panighini ◽  
Marina Carlini ◽  
...  
Keyword(s):  
Pathological Gambling ◽  
Receptor Binding ◽  
Adenosine Receptor ◽  
Binding Parameters ◽  
A2a Adenosine Receptor

scholarly journals Allosteric Antagonism of the A2A Adenosine Receptor by a Series of Bitopic Ligands

Cells ◽  
2020 ◽  
Vol 9 (5) ◽  
pp. 1200
Author(s):  
Zhan-Guo Gao ◽  
Kiran S. Toti ◽  
Ryan Campbell ◽  
R. Rama Suresh ◽  
Huijun Yang ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Adenosine Receptor ◽  
Radioligand Binding ◽  
Binding Properties ◽  
A2a Adenosine Receptor ◽  
Functional Antagonism ◽  
Allosteric Model ◽  
Schild Analysis ◽  
Hexamethylene Amiloride

Allosteric antagonism by bitopic ligands, as reported for many receptors, is a distinct modulatory mechanism. Although several bitopic A2A adenosine receptor (A2AAR) ligand classes were reported as pharmacological tools, their receptor binding and functional antagonism patterns, i.e., allosteric or competitive, were not well characterized. Therefore, here we systematically characterized A2AAR binding and functional antagonism of two distinct antagonist chemical classes. i.e., fluorescent conjugates of xanthine amine congener (XAC) and SCH442416. Bitopic ligands were potent, weak, competitive or allosteric, based on the combination of pharmacophore, linker and fluorophore. Among antagonists tested, XAC, XAC245, XAC488, SCH442416, MRS7352 showed Ki binding values consistent with KB values from functional antagonism. Interestingly, MRS7396, XAC-X-BY630 (XAC630) and 5-(N,N-hexamethylene)amiloride (HMA) were 9–100 times weaker in displacing fluorescent MRS7416 binding than radioligand binding. XAC245, XAC630, MRS7396, MRS7416 and MRS7322 behaved as allosteric A2AAR antagonists, whereas XAC488 and MRS7395 antagonized competitively. Schild analysis showed antagonism slopes of 0.42 and 0.47 for MRS7396 and XAC630, respectively. Allosteric antagonists HMA and MRS7396 were more potent in displacing [3H]ZM241385 binding than MRS7416 binding. Sodium site D52N mutation increased and decreased affinity of HMA and MRS7396, respectively, suggesting possible preference for different A2AAR conformations. The allosteric binding properties of some bitopic ligands were rationalized and analyzed using the Hall two-state allosteric model. Thus, fluorophore tethering to an orthosteric ligand is not neutral pharmacologically and may confer unexpected properties to the conjugate.

Modification of A-i and A2a adenosine receptor binding in aged striatum, hippocampus and cortex of the rat

Neuroreport ◽  
1995 ◽  
Vol 6 (11) ◽  
pp. 1583 ◽  
Author(s):  
Rodrigo A. Cunha ◽  
M. Dolores Constantino ◽  
Ana M. Sebastião ◽  
J. Alexandre Ribeiro
Keyword(s):  
Receptor Binding ◽  
Adenosine Receptor ◽  
A2a Adenosine Receptor

Ligand-Based Virtual Screening Using Tailored Ensembles: A Prioritization Tool for Dual A2A Adenosine Receptor Antagonists / Monoamine Oxidase B Inhibitors

2016 ◽  
Vol 22 (21) ◽  
pp. 3082-3096 ◽  
Author(s):  
Aliuska Morales Helguera ◽  
Yunierkis Perez-Castillo ◽  
M. Natália D.S. Cordeiro ◽  
Eduardo Tejera ◽  
César Paz-y-Miño ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Monoamine Oxidase ◽  
Adenosine Receptor ◽  
Monoamine Oxidase B ◽  
Receptor Antagonists ◽  
A2a Adenosine Receptor

scholarly journals Constitutive activity of the A2A adenosine receptor and compartmentalised cyclic AMP signalling fine-tune noradrenaline release

2012 ◽  
Vol 8 (4) ◽  
pp. 677-692 ◽  
Author(s):  
Edin Ibrisimovic ◽  
Helmut Drobny ◽  
Qiong Yang ◽  
Thomas Höfer ◽  
Stefan Boehm ◽  
...  
Keyword(s):  
Cyclic Amp ◽  
Noradrenaline Release ◽  
Adenosine Receptor ◽  
Constitutive Activity ◽  
A2a Adenosine Receptor ◽  
Fine Tune
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