Published in Mol Pharmacol on April 01, 1996
The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science (2008) 11.74
International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update. Pharmacol Rev (2011) 4.16
Community-wide assessment of GPCR structure modelling and ligand docking: GPCR Dock 2008. Nat Rev Drug Discov (2009) 2.23
The second extracellular loop of the dopamine D2 receptor lines the binding-site crevice. Proc Natl Acad Sci U S A (2004) 2.10
A candidate olfactory receptor subtype highly conserved across different insect orders. J Comp Physiol A Neuroethol Sens Neural Behav Physiol (2003) 2.08
Role of the extracellular loops of G protein-coupled receptors in ligand recognition: a molecular modeling study of the human P2Y1 receptor. Biochemistry (1999) 1.64
GPCR 3D homology models for ligand screening: lessons learned from blind predictions of adenosine A2a receptor complex. Proteins (2010) 1.57
The role of amino acids in extracellular loops of the human P2Y1 receptor in surface expression and activation processes. J Biol Chem (1999) 1.54
On the applicability of GPCR homology models to computer-aided drug discovery: a comparison between in silico and crystal structures of the beta2-adrenergic receptor. J Med Chem (2008) 1.46
Evaluation of homology modeling of G-protein-coupled receptors in light of the A(2A) adenosine receptor crystallographic structure. J Med Chem (2009) 1.38
Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: identification and characterization of essential amino acid residues. J Biol Chem (2010) 1.37
Two arginine-glutamate ionic locks near the extracellular surface of FFAR1 gate receptor activation. J Biol Chem (2008) 1.09
Ligand-dependent activation and deactivation of the human adenosine A(2A) receptor. J Am Chem Soc (2013) 1.02
Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain. J Med Chem (2013) 0.96
In silico analysis of the binding of agonists and blockers to the β2-adrenergic receptor. J Mol Graph Model (2011) 0.94
Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates. J Med Chem (2013) 0.94
Pharmacochemistry of the platelet purinergic receptors. Purinergic Signal (2011) 0.90
Homology modelling of the human adenosine A2B receptor based on X-ray structures of bovine rhodopsin, the beta2-adrenergic receptor and the human adenosine A2A receptor. J Comput Aided Mol Des (2009) 0.88
Computing highly correlated positions using mutual information and graph theory for G protein-coupled receptors. PLoS One (2009) 0.87
A new drug design targeting the adenosinergic system for Huntington's disease. PLoS One (2011) 0.85
Structural and energetic effects of A2A adenosine receptor mutations on agonist and antagonist binding. PLoS One (2014) 0.82
What can crystal structures of aminergic receptors tell us about designing subtype-selective ligands? Pharmacol Rev (2015) 0.82
Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists. ACS Med Chem Lett (2012) 0.79
Molecular dynamics simulation of the human adenosine A3 receptor: agonist induced conformational changes of Trp243. J Comput Aided Mol Des (2006) 0.78
A strategy using NMR peptide structures of thromboxane A2 receptor as templates to construct ligand-recognition pocket of prostacyclin receptor. BMC Biochem (2005) 0.78
Characterization of adenosine receptor in its native environment: insights from molecular dynamics simulations of palmitoylated/glycosylated, membrane-integrated human A(2B) adenosine receptor. J Mol Model (2012) 0.77
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor. ACS Med Chem Lett (2014) 0.76
Inhibition of platelet activation and thrombus formation by adenosine and inosine: studies on their relative contribution and molecular modeling. PLoS One (2014) 0.76
Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility. J Med Chem (2011) 0.75
Point mutations in the second extracellular loop of the histamine H2 receptor do not affect the species-selective activity of guanidine-type agonists. Naunyn Schmiedebergs Arch Pharmacol (2007) 0.75
Pharmacophore modeling of human adenosine receptor A(₂A) antagonists. J Mol Model (2010) 0.75
DNA sequencing with chain-terminating inhibitors. Proc Natl Acad Sci U S A (1977) 790.54
A cDNA cloning vector that permits expression of cDNA inserts in mammalian cells. Mol Cell Biol (1983) 18.32
Use of eukaryotic expression technology in the functional analysis of cloned genes. Methods Enzymol (1987) 12.66
[3H]CGS 21680, a selective A2 adenosine receptor agonist directly labels A2 receptors in rat brain. J Pharmacol Exp Ther (1989) 4.18
Cardiovascular purinoceptors. Physiol Rev (1990) 3.70
Identification of two serine residues involved in agonist activation of the beta-adrenergic receptor. J Biol Chem (1989) 3.51
Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists. J Med Chem (1994) 2.47
Pore loops: an emerging theme in ion channel structure. Neuron (1995) 2.09
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential. J Med Chem (1992) 2.01
Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. J Biol Chem (1995) 1.92
Adenosine A1 and A2 receptors: structure--function relationships. Med Res Rev (1992) 1.62
A2A adenosine receptors from rat striatum and rat pheochromocytoma PC12 cells: characterization with radioligand binding and by activation of adenylate cyclase. Mol Pharmacol (1992) 1.57
1.7 A X-ray structure of the periplasmic ribose receptor from Escherichia coli. J Mol Biol (1992) 1.51
Plasma membrane localization and functional rescue of truncated forms of a G protein-coupled receptor. J Biol Chem (1995) 1.33
Cloning, expression, and characterization of the unique bovine A1 adenosine receptor. Studies on the ligand binding site by site-directed mutagenesis. J Biol Chem (1992) 1.32
Structure and function in rhodopsin. Requirements of a specific structure for the intradiscal domain. J Biol Chem (1994) 1.30
Pharmacological characterization of the D2 dopamine receptor negatively coupled with adenylate cyclase in rat anterior pituitary. Mol Pharmacol (1983) 1.22
Probing of the location of the allosteric site on m1 muscarinic receptors by site-directed mutagenesis. Mol Pharmacol (1995) 1.19
Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor. EMBO J (1995) 1.19
Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors. J Biol Chem (1994) 1.16
A1 adenosine receptors. Two amino acids are responsible for species differences in ligand recognition. J Biol Chem (1994) 1.14
A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding. J Biol Chem (1994) 1.11
D2-dopamine receptor-mediated inhibition of cyclic AMP formation in striatal neurons in primary culture. Mol Pharmacol (1985) 1.11
The evolving model of calmodulin structure, function and activation. Structure (1995) 1.02
Glutamate 301 of the mouse gonadotropin-releasing hormone receptor confers specificity for arginine 8 of mammalian gonadotropin-releasing hormone. J Biol Chem (1994) 1.00
Molecular modeling of adenosine receptors. The ligand binding site on the rat adenosine A2A receptor. Eur J Pharmacol (1994) 0.99
Role of adenosine A2a receptors in the nucleus accumbens. Prog Neuropsychopharmacol Biol Psychiatry (1994) 0.97
Acidic residues in extracellular loops of the human Y1 neuropeptide Y receptor are essential for ligand binding. J Biol Chem (1994) 0.92
Adenosine agonists reduce conditioned avoidance responding in the rat. Pharmacol Biochem Behav (1993) 0.91
Muscarinic acetylcholine receptors: structural basis of ligand binding and G protein coupling. Life Sci (1995) 0.91
Identification of an adenosine receptor domain specifically involved in binding of 5'-substituted adenosine agonists. J Biol Chem (1994) 0.89
Crystal structure of RNase T1 complexed with the product nucleotide 3'-GMP. Structural evidence for direct interaction of histidine 40 and glutamic acid 58 with the 2'-hydroxyl group of the ribose. J Biol Chem (1994) 0.85
Effects of mono- and divalent ions on the binding of the adenosine analogue CGS 21680 to adenosine A2 receptors in rat striatum. Biochem Pharmacol (1992) 0.84
6agonist selectivity determinants in somatostatin receptor subtypes I and II. J Biol Chem (1994) 0.78
Genomic-sequence comparison of two unrelated isolates of the human gastric pathogen Helicobacter pylori. Nature (1999) 19.34
International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors. Pharmacol Rev (2001) 9.90
Nomenclature and classification of purinoceptors. Pharmacol Rev (1994) 5.32
VEGF enhances angiogenesis and promotes blood-brain barrier leakage in the ischemic brain. J Clin Invest (2000) 4.36
Direct observation of brownian motion of lipids in a membrane. Proc Natl Acad Sci U S A (1991) 3.91
Diffusion of injected macromolecules within the cytoplasm of living cells. Proc Natl Acad Sci U S A (1981) 3.61
NMDA receptors mediate calcium accumulation in myelin during chemical ischaemia. Nature (2005) 2.74
125I-4-aminobenzyl-5'-N-methylcarboxamidoadenosine, a high affinity radioligand for the rat A3 adenosine receptor. Mol Pharmacol (1994) 2.65
Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J Pharmacol Exp Ther (1991) 2.55
Hyperactivity and intact hippocampus-dependent learning in mice lacking the M1 muscarinic acetylcholine receptor. J Neurosci (2001) 2.54
Functionalized congeners of 1,3-dialkylxanthines: preparation of analogues with high affinity for adenosine receptors. J Med Chem (1985) 2.52
Structural mosaicism on the submicron scale in the plasma membrane. Biophys J (1998) 2.50
The Concise Guide to PHARMACOLOGY 2013/14: overview. Br J Pharmacol (2013) 2.48
Unconfined lateral diffusion and an estimate of pericellular matrix viscosity revealed by measuring the mobility of gold-tagged lipids. J Cell Biol (1993) 2.47
A rat model of focal embolic cerebral ischemia. Brain Res (1997) 2.44
Recommendations for standardization and phenotype definitions in genetic studies of osteoarthritis: the TREAT-OA consortium. Osteoarthritis Cartilage (2010) 2.39
Mice lacking the M3 muscarinic acetylcholine receptor are hypophagic and lean. Nature (2001) 2.39
Adenosine A3 receptor stimulation and cerebral ischemia. Eur J Pharmacol (1994) 2.33
The emerging normal and disease-related roles of anaplastic lymphoma kinase. Cell Mol Life Sci (2004) 2.19
Pronounced pharmacologic deficits in M2 muscarinic acetylcholine receptor knockout mice. Proc Natl Acad Sci U S A (1999) 2.16
Src deficiency or blockade of Src activity in mice provides cerebral protection following stroke. Nat Med (2001) 2.16
Spatial Fourier analysis of video photobleaching measurements. Principles and optimization. Biophys J (1991) 2.13
Functionalized congeners of adenosine: preparation of analogues with high affinity for A1-adenosine receptors. J Med Chem (1985) 2.12
2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors. J Med Chem (1994) 2.10
Towards a revised nomenclature for P1 and P2 receptors. Trends Pharmacol Sci (1997) 2.09
Enhancement of D1 dopamine receptor-mediated locomotor stimulation in M(4) muscarinic acetylcholine receptor knockout mice. Proc Natl Acad Sci U S A (1999) 1.93
Gamma-tocopherol prevents airway eosinophilia and mucous cell hyperplasia in experimentally induced allergic rhinitis and asthma. Clin Exp Allergy (2007) 1.93
Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. J Biol Chem (1995) 1.92
Short root mutant of Lotus japonicus with a dramatically altered symbiotic phenotype. Plant J (2000) 1.89
Spontaneous mutations that confer antibiotic resistance in Helicobacter pylori. Antimicrob Agents Chemother (2001) 1.88
A binding site model and structure-activity relationships for the rat A3 adenosine receptor. Mol Pharmacol (1994) 1.87
Cholinergic dilation of cerebral blood vessels is abolished in M(5) muscarinic acetylcholine receptor knockout mice. Proc Natl Acad Sci U S A (2001) 1.87
[3H]xanthine amine congener of 1,3-dipropyl-8-phenylxanthine: an antagonist radioligand for adenosine receptors. Proc Natl Acad Sci U S A (1986) 1.85
Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands. J Med Chem (2000) 1.85
Identification of potent, selective P2Y-purinoceptor agonists: structure-activity relationships for 2-thioether derivatives of adenosine 5'-triphosphate. J Med Chem (1993) 1.84
Competitive and selective antagonism of P2Y1 receptors by N6-methyl 2'-deoxyadenosine 3',5'-bisphosphate. Br J Pharmacol (1998) 1.80
Randomized controlled trial of sirolimus for renal transplant recipients at high risk for nonmelanoma skin cancer. Am J Transplant (2012) 1.80
Differential effects of P2-purinoceptor antagonists on phospholipase C- and adenylyl cyclase-coupled P2Y-purinoceptors. Br J Pharmacol (1994) 1.77
Coexpression studies with mutant muscarinic/adrenergic receptors provide evidence for intermolecular "cross-talk" between G-protein-linked receptors. Proc Natl Acad Sci U S A (1993) 1.75
Role of the extracellular loops of G protein-coupled receptors in ligand recognition: a molecular modeling study of the human P2Y1 receptor. Biochemistry (1999) 1.64
A mutational analysis of residues essential for ligand recognition at the human P2Y1 receptor. Mol Pharmacol (1997) 1.63
A physiological role of the adenosine A3 receptor: sustained cardioprotection. Proc Natl Acad Sci U S A (1998) 1.63
Adenosine A1 and A2 receptors: structure--function relationships. Med Res Rev (1992) 1.62
An oncogenic role of miR-142-3p in human T-cell acute lymphoblastic leukemia (T-ALL) by targeting glucocorticoid receptor-α and cAMP/PKA pathways. Leukemia (2011) 1.61
Deoxyadenosine bisphosphate derivatives as potent antagonists at P2Y1 receptors. J Med Chem (1998) 1.61
Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites. J Med Chem (1998) 1.61
Identification of receptors for neuromedin U and its role in feeding. Nature (2000) 1.60
A2A adenosine receptors from rat striatum and rat pheochromocytoma PC12 cells: characterization with radioligand binding and by activation of adenylate cyclase. Mol Pharmacol (1992) 1.57
Direct preconditioning of cultured chick ventricular myocytes. Novel functions of cardiac adenosine A2a and A3 receptors. J Clin Invest (1996) 1.57
A functionalized congener approach to adenosine receptor antagonists: amino acid conjugates of 1,3-dipropylxanthine. Mol Pharmacol (1986) 1.55
The role of amino acids in extracellular loops of the human P2Y1 receptor in surface expression and activation processes. J Biol Chem (1999) 1.54
Prevalence and predictors of depressive, anxiety and substance use disorders in HIV-infected and uninfected men: a longitudinal evaluation. Psychol Med (1997) 1.52
Probing the adenosine receptor with adenosine and xanthine biotin conjugates. FEBS Lett (1985) 1.52
Identification and molecular characterization of m3 muscarinic receptor dimers. J Biol Chem (1999) 1.51
Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. J Med Chem (1997) 1.51
Direct measurement of lateral transport in membranes by using time-resolved spatial photometry. Proc Natl Acad Sci U S A (1985) 1.51
Identification of the A2 adenosine receptor binding subunit by photoaffinity crosslinking. Proc Natl Acad Sci U S A (1989) 1.50
Molecular probes for extracellular adenosine receptors. Biochem Pharmacol (1987) 1.47
Visual sustained attention: image degradation produces rapid sensitivity decrement over time. Science (1983) 1.47
Apparent affinity of some 8-phenyl-substituted xanthines at adenosine receptors in guinea-pig aorta and atria. Br J Pharmacol (1987) 1.45
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. J Med Chem (2000) 1.44
Distinct pathways of desensitization of A1- and A2-adenosine receptors in DDT1 MF-2 cells. Mol Pharmacol (1991) 1.42
A new high affinity, iodinated adenosine receptor antagonist as a radioligand/photoaffinity crosslinking probe. Mol Pharmacol (1987) 1.42
Species differences in structure-activity relationships of adenosine agonists and xanthine antagonists at brain A1 adenosine receptors. FEBS Lett (1986) 1.42
Mechanism of carbon dioxide-catalyzed oxidation of tyrosine by peroxynitrite. Biochemistry (1996) 1.41
G protein-dependent activation of phospholipase C by adenosine A3 receptors in rat brain. Mol Pharmacol (1995) 1.40
M(2) and M(4) receptor knockout mice: muscarinic receptor function in cardiac and smooth muscle in vitro. J Pharmacol Exp Ther (2000) 1.40
Haploidentical hematopoietic stem cell transplantation without in vitro T-cell depletion for the treatment of hematological malignancies. Bone Marrow Transplant (2006) 1.38
A new rat model of thrombotic focal cerebral ischemia. J Cereb Blood Flow Metab (1997) 1.35
Induction of cortical oscillations in spreading cells by depolymerization of microtubules. Cell Motil Cytoskeleton (2001) 1.35
Modelling the P2Y purinoceptor using rhodopsin as template. Drug Des Discov (1995) 1.35
Plasma membrane localization and functional rescue of truncated forms of a G protein-coupled receptor. J Biol Chem (1995) 1.33
Hydrophilic side chains in the third and seventh transmembrane helical domains of human A2A adenosine receptors are required for ligand recognition. Mol Pharmacol (1996) 1.33
Cloning, expression, and characterization of the unique bovine A1 adenosine receptor. Studies on the ligand binding site by site-directed mutagenesis. J Biol Chem (1992) 1.32
Acyclic and cyclopropyl analogues of adenosine bisphosphate antagonists of the P2Y1 receptor: structure-activity relationships and receptor docking. J Med Chem (2001) 1.32
The A2 adenosine receptor: guanine nucleotide modulation of agonist binding is enhanced by proteolysis. Mol Pharmacol (1991) 1.32
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists. J Med Chem (1998) 1.32
Behavioral effects of A1- and A2-selective adenosine agonists and antagonists: evidence for synergism and antagonism. J Pharmacol Exp Ther (1991) 1.31
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. J Med Chem (1998) 1.31
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. J Med Chem (1996) 1.31
Elucidating the role of muscarinic receptors in psychosis. Life Sci (2001) 1.29
Activation of hippocampal adenosine A3 receptors produces a desensitization of A1 receptor-mediated responses in rat hippocampus. J Neurosci (1997) 1.29
Vagal tone dominates autonomic control of mouse heart rate at thermoneutrality. Am J Physiol Heart Circ Physiol (2008) 1.28
Identification of potent P2Y-purinoceptor agonists that are derivatives of adenosine 5'-monophosphate. Br J Pharmacol (1996) 1.27
A novel cardioprotective function of adenosine A1 and A3 receptors during prolonged simulated ischemia. Am J Physiol (1997) 1.27
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications. Bioorg Med Chem Lett (2001) 1.26
Molecular dynamics simulation of a synthetic ion channel. Biophys J (1998) 1.26
Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors. J Med Chem (1995) 1.26
[3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors. Biochem Pharmacol (2001) 1.25
Identification of a receptor/G-protein contact site critical for signaling specificity and G-protein activation. Proc Natl Acad Sci U S A (1995) 1.25
Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists. J Med Chem (1999) 1.25
Molecular modeling of adenosine receptors. I. The ligand binding site on the A1 receptor. Drug Des Discov (1992) 1.25
Identification and characterization of a second melanin-concentrating hormone receptor, MCH-2R. Proc Natl Acad Sci U S A (2001) 1.24
Induction of apoptosis in HL-60 human promyelocytic leukemia cells by adenosine A(3) receptor agonists. Biochem Biophys Res Commun (1996) 1.23
Truncated V2 vasopressin receptors as negative regulators of wild-type V2 receptor function. Biochemistry (1998) 1.21