Published in ACS Chem Neurosci on June 21, 2011
An fMRI Study of SYN115 in Cocaine Dependent Subjects | NCT00783276
Inflammation in neurodegenerative diseases--an update. Immunology (2014) 1.30
G protein-coupled adenosine (P1) and P2Y receptors: ligand design and receptor interactions. Purinergic Signal (2012) 1.00
Effects of caffeine on alcohol consumption and nicotine self-administration in rats. Alcohol Clin Exp Res (2013) 0.94
Energy drinks mixed with alcohol: what are the risks? Nutr Rev (2014) 0.92
Lack of replication of the GRIN2A-by-coffee interaction in Parkinson disease. PLoS Genet (2014) 0.86
Can energy drinks increase the desire for more alcohol? Adv Nutr (2015) 0.79
Crystal structure of the adenosine A2A receptor bound to an antagonist reveals a potential allosteric pocket. Proc Natl Acad Sci U S A (2017) 0.75
Quantitative recording of rotational behavior in rats after 6-hydroxy-dopamine lesions of the nigrostriatal dopamine system. Brain Res (1970) 4.65
The role and regulation of adenosine in the central nervous system. Annu Rev Neurosci (2001) 4.17
6-Hydroxy-dopamine induced degeneration of central monoamine neurons. Eur J Pharmacol (1968) 2.81
Adenosine in the central nervous system: release mechanisms and extracellular concentrations. J Neurochem (2001) 2.63
Molecular cloning of the rat A2 adenosine receptor: selective co-expression with D2 dopamine receptors in rat striatum. Brain Res Mol Brain Res (1992) 1.96
Neuroprotection by caffeine and A(2A) adenosine receptor inactivation in a model of Parkinson's disease. J Neurosci (2001) 1.90
Adenosine: an endogenous inhibitor of neutrophil-mediated injury to endothelial cells. J Clin Invest (1986) 1.76
Immunohistochemical localization of adenosine A2A receptors in the rat central nervous system. J Comp Neurol (1998) 1.55
Randomized trial of the adenosine A(2A) receptor antagonist istradefylline in advanced PD. Neurology (2003) 1.50
Adenosine A(2A) receptor antagonist treatment of Parkinson's disease. Neurology (2003) 1.46
Adenosine receptors. J Biol Chem (1992) 1.44
Adenosine gates synaptic plasticity at hippocampal mossy fiber synapses. Proc Natl Acad Sci U S A (2003) 1.19
[3H]5'-N-ethylcarboxamide adenosine binds to both Ra and Ri adenosine receptors in rat striatum. Naunyn Schmiedebergs Arch Pharmacol (1984) 1.17
Adenosine A2A antagonist: a novel antiparkinsonian agent that does not provoke dyskinesia in parkinsonian monkeys. Ann Neurol (1998) 1.16
The effects of KW-3902, an adenosine A1-receptor antagonist,on diuresis and renal function in patients with acute decompensated heart failure and renal impairment or diuretic resistance. J Am Coll Cardiol (2007) 1.15
Adenosine receptor antagonists: translating medicinal chemistry and pharmacology into clinical utility. Chem Rev (2008) 1.14
A reassessment of risks and benefits of dopamine agonists in Parkinson's disease. Lancet Neurol (2009) 1.12
Neuroprotection by adenosine A2A receptor blockade in experimental models of Parkinson's disease. J Neurochem (2002) 1.10
Characterization of the potent and highly selective A2A receptor antagonists preladenant and SCH 412348 [7-[2-[4-2,4-difluorophenyl]-1-piperazinyl]ethyl]-2-(2-furanyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine] in rodent models of movement disorders and depression. J Pharmacol Exp Ther (2009) 1.09
Distribution of adenosine receptors in the postmortem human brain: an extended autoradiographic study. Synapse (1997) 1.09
Novel investigational adenosine A2A receptor antagonists for Parkinson's disease. Expert Opin Investig Drugs (2009) 1.09
Distribution of adenosine A2 receptor mRNA in the human brain. Neurosci Lett (1991) 1.08
1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-lesioned model of parkinson's disease, with emphasis on mice and nonhuman primates. Comp Med (2004) 1.06
Combined use of the adenosine A(2A) antagonist KW-6002 with L-DOPA or with selective D1 or D2 dopamine agonists increases antiparkinsonian activity but not dyskinesia in MPTP-treated monkeys. Exp Neurol (2000) 1.06
Antiparkinsonian effect of a new selective adenosine A2A receptor antagonist in MPTP-treated monkeys. Neurology (1999) 1.05
Blocking striatal adenosine A2A receptors: a new strategy for basal ganglia disorders. Recent Pat CNS Drug Discov (2007) 1.02
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines. Bioorg Med Chem Lett (2006) 1.02
Recent progress in the discovery of adenosine A(2A) receptor antagonists for the treatment of Parkinson's disease. Curr Opin Drug Discov Devel (2010) 1.01
Effects of BG9719 (CVT-124), an A1-adenosine receptor antagonist, and furosemide on glomerular filtration rate and natriuresis in patients with congestive heart failure. J Am Coll Cardiol (2000) 0.99
Behavioural adverse effects of dopaminergic treatments in Parkinson's disease: incidence, neurobiological basis, management and prevention. Drug Saf (2009) 0.97
Subcellular localization of adenosine A(1) receptors in nerve terminals and synapses of the rat hippocampus. Brain Res (2003) 0.96
Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives. Bioorg Med Chem Lett (2008) 0.92
Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy. J Med Chem (2008) 0.92
Adenosine antagonists potentiate D2 dopamine-dependent activation of Fos in the striatopallidal pathway. Neuroscience (1995) 0.90
In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease. J Med Chem (2010) 0.87
COMT inhibitors in Parkinson's disease: can they prevent and/or reverse levodopa-induced motor complications? Neurology (2004) 0.87
Adenosine A2A receptors modify motor function in MPTP-treated common marmosets. Neuroreport (1998) 0.87
New developments in understanding the etiology of Parkinson's disease and in its treatment. Curr Opin Neurobiol (1998) 0.86
Pharmacological characterization of a novel, potent adenosine A1 and A2A receptor dual antagonist, 5-[5-amino-3-(4-fluorophenyl)pyrazin-2-yl]-1-isopropylpyridine-2(1H)-one (ASP5854), in models of Parkinson's disease and cognition. J Pharmacol Exp Ther (2007) 0.86
Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines. J Med Chem (2009) 0.85
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization. J Med Chem (2005) 0.84
The novel adenosine A2a receptor antagonist ST1535 potentiates the effects of a threshold dose of L-DOPA in MPTP treated common marmosets. Eur J Pharmacol (2006) 0.84
First visualization of adenosine A(2A) receptors in the human brain by positron emission tomography with [11C]TMSX. Synapse (2005) 0.83
Dopamine agonists in Parkinson's disease. Expert Rev Neurother (2008) 0.82
Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors. J Pharmacol Sci (2004) 0.82
Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines. Bioorg Med Chem Lett (2008) 0.82
Striatal adenosine A2A receptors--where are they? What do they do? Trends Pharmacol Sci (1998) 0.82
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents. J Med Chem (2008) 0.82
MAO-B inhibitors in Parkinson's disease. Adv Neurol (1993) 0.81
Characterization of the antiparkinsonian effects of the new adenosine A2A receptor antagonist ST1535: acute and subchronic studies in rats. Eur J Pharmacol (2007) 0.81
Brain adenosine A2A receptor occupancy by a novel A1/A2A receptor antagonist, ASP5854, in rhesus monkeys: relationship to anticataleptic effect. J Nucl Med (2008) 0.80
Selective lesion of central dopamine or noradrenaline neuron systems in the neonatal rat: motor behavior and monoamine alterations at adult stage. Behav Brain Res (1989) 0.80
Quantitative evaluation of MPTP-treated nonhuman parkinsonian primates in the HALLWAY task. J Neurosci Methods (2008) 0.80
Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines. Bioorg Med Chem Lett (2008) 0.79
Synthetic studies on selective adenosine A2A receptor antagonists: synthesis and structure-activity relationships of novel benzofuran derivatives. Bioorg Med Chem Lett (2009) 0.79
Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists. Bioorg Med Chem Lett (2008) 0.79
The novel adenosine A2a antagonist ST1535 potentiates the effects of a threshold dose of l-dopa in unilaterally 6-OHDA-lesioned rats. Brain Res (2006) 0.79
Adenosine A(2A) receptor antagonists KF17837 and KW-6002 potentiate rotation induced by dopaminergic drugs in hemi-Parkinsonian rats. Eur J Pharmacol (2000) 0.79
3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists. Bioorg Med Chem Lett (2007) 0.78
Dopamine, but not norepinephrine or serotonin, reuptake inhibition reverses motor deficits in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated primates. J Pharmacol Exp Ther (2002) 0.78
Effect of locally infused 2-chloroadenosine, an A1 receptor agonist, on spontaneous and evoked dopamine release in rat neostriatum. Neurosci Lett (1995) 0.78
ST 1535: a preferential A2A adenosine receptor antagonist. Int J Neuropsychopharmacol (2005) 0.78
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists. Bioorg Med Chem (2010) 0.77
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides. Bioorg Med Chem (2009) 0.77
Synthetic studies on selective adenosine A2A receptor antagonists. Part II: synthesis and structure-activity relationships of novel benzofuran derivatives. Bioorg Med Chem Lett (2010) 0.77
Novel therapy in Parkinson's disease: adenosine A(2A) receptor antagonists. Expert Opin Drug Metab Toxicol (2011) 0.77
Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists. Bioorg Med Chem Lett (2013) 0.77
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs as adenosine A2A antagonists: the successful reduction of hERG activity. Part 2. Bioorg Med Chem Lett (2005) 0.76
A novel adenosine A(1) and A(2A) receptor antagonist ASP5854 ameliorates motor impairment in MPTP-treated marmosets: comparison with existing anti-Parkinson's disease drugs. Behav Brain Res (2008) 0.76
Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists. Bioorg Med Chem Lett (2008) 0.76
Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists. Bioorg Med Chem Lett (2008) 0.76
Optimization of arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists. Bioorg Med Chem Lett (2010) 0.76
Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists. Bioorg Med Chem Lett (2010) 0.76
Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones. Bioorg Med Chem Lett (2011) 0.76
Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives. Bioorg Med Chem Lett (2008) 0.76
Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists. Bioorg Med Chem Lett (2010) 0.76
Discovery of 2-aminoimidazopyridine adenosine A(2A) receptor antagonists. Bioorg Med Chem Lett (2010) 0.76
Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides. Bioorg Med Chem Lett (2009) 0.76
Synthesis and SAR studies of trisubstituted purinones as potent and selective adenosine A2A receptor antagonists. Bioorg Med Chem Lett (2009) 0.76
Synthesis of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists. Bioorg Med Chem Lett (2008) 0.76
2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability. Bioorg Med Chem Lett (2008) 0.75
Synthesis and biological evaluation of thiol-based inhibitors of glutamate carboxypeptidase II: discovery of an orally active GCP II inhibitor. J Med Chem (2003) 1.12
Regioselective preparation of 2-substituted 3,4-diaryl pyrroles: a concise total synthesis of ningalin B. J Org Chem (2002) 1.10
In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease. J Med Chem (2010) 0.87
Syntheses and in vitro evaluation of arylsulfone-based MMP inhibitors with heterocycle-derived zinc-binding groups (ZBGs). Bioorg Med Chem Lett (2007) 0.77
1-Hydroxy-2-pyridinone-based MMP inhibitors: synthesis and biological evaluation for the treatment of ischemic stroke. Bioorg Med Chem Lett (2007) 0.77
Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists. Bioorg Med Chem Lett (2013) 0.77
Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists. Bioorg Med Chem Lett (2010) 0.76
Design and characterization of optimized adenosine A₂A/A₁ receptor antagonists for the treatment of Parkinson's disease. J Med Chem (2012) 0.76
JNJ-40255293, a novel adenosine A2A/A1 antagonist with efficacy in preclinical models of Parkinson's disease. ACS Chem Neurosci (2014) 0.76
Optimization of arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists. Bioorg Med Chem Lett (2010) 0.76
Overcoming the genotoxicity of a pyrrolidine substituted arylindenopyrimidine as a potent dual adenosine A(2A)/A(1) antagonist by minimizing bioactivation to an iminium ion reactive intermediate. Chem Res Toxicol (2011) 0.75