Add to ORKGCentral adenosine A2A receptor is a promising target for drugs to treat Parkinson’s disease (PD), and the central blockade of adenosine A1 receptor improves cognitive function. In the present study, we investigated the effect of a novel adenosine A1 and A2A dual antagonist, 5-[5-amino-3-(4-fluorophenyl) pyrazin-2-yl]-1-isopropylpyridine-2(1H)-one (ASP5854), in ani-mal models of PD and cognition. The binding affinities of ASP5854 for human A1 and A2A receptors were 9.03 and 1.76 nM, respectively, with higher specificity and no species differ-ences. ASP5854 also showed antagonistic action on A1 and A2A agonist-induced increases of intracellular Ca 2 concentra-tion. ASP5854 ameliorated A2A agonist 2-[p-(2-carboxyethyl) phenethylamino]-5-N-eth...
In the past decades, many efforts were undertaken to develop ligands for the adenosine receptors, wi...
Adenosine A2A receptor antagonists have emerged as an attractive non-dopaminergic target in clinical...
Adenosine is an endogenous purine nucleoside that regulates several physiological functions, at the ...
Adenosine A(2A) receptors present in the central nervous system have been implicated in the modulati...
The drug treatment of Parkinson’s disease (PD) is accompanied by a loss of drug efficacy, the onset ...
The most effective treatment of Parkinson's disease (PD) is, at present, the dopamine precursor L-3,...
Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, A...
Adenosine receptors are G protein-coupled receptors (GPCRs) that mediate the physiological functions...
The adenosine A2A receptor has emerged as an attractive non-dopaminergic target in the pursuit of im...
Endogenous nucleoside adenosine modulates a number of physiological effects through interaction with...
Growing evidence emphasizes that the purine nucleoside adenosine plays an active role as a local reg...
The adenosine A2A receptor has emerged as an attractive non-dopaminergic target in the pursuit of im...
Adenosine A2A antagonists are believed to have therapeutic potential in the treatment of Parkinson’s...
Since the discovery of the biological effects of adenosine, the development of potent and selective ...
Several selective antagonists for adenosine A2A receptors (A2AR) are currently under evaluation in c...
In the past decades, many efforts were undertaken to develop ligands for the adenosine receptors, wi...
Adenosine A2A receptor antagonists have emerged as an attractive non-dopaminergic target in clinical...
Adenosine is an endogenous purine nucleoside that regulates several physiological functions, at the ...
Adenosine A(2A) receptors present in the central nervous system have been implicated in the modulati...
The drug treatment of Parkinson’s disease (PD) is accompanied by a loss of drug efficacy, the onset ...
The most effective treatment of Parkinson's disease (PD) is, at present, the dopamine precursor L-3,...
Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, A...
Adenosine receptors are G protein-coupled receptors (GPCRs) that mediate the physiological functions...
The adenosine A2A receptor has emerged as an attractive non-dopaminergic target in the pursuit of im...
Endogenous nucleoside adenosine modulates a number of physiological effects through interaction with...
Growing evidence emphasizes that the purine nucleoside adenosine plays an active role as a local reg...
The adenosine A2A receptor has emerged as an attractive non-dopaminergic target in the pursuit of im...
Adenosine A2A antagonists are believed to have therapeutic potential in the treatment of Parkinson’s...
Since the discovery of the biological effects of adenosine, the development of potent and selective ...
Several selective antagonists for adenosine A2A receptors (A2AR) are currently under evaluation in c...
In the past decades, many efforts were undertaken to develop ligands for the adenosine receptors, wi...
Adenosine A2A receptor antagonists have emerged as an attractive non-dopaminergic target in clinical...
Adenosine is an endogenous purine nucleoside that regulates several physiological functions, at the ...