Published in J Med Chem on December 10, 2009
Pharmacological and therapeutic effects of A3 adenosine receptor agonists. Drug Discov Today (2011) 1.44
Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions. J Med Chem (2012) 1.23
Novel Alexa Fluor-488 labeled antagonist of the A(2A) adenosine receptor: Application to a fluorescence polarization-based receptor binding assay. Biochem Pharmacol (2010) 1.01
The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs. Br J Pharmacol (2014) 0.99
2-Dialkynyl derivatives of (N)-methanocarba nucleosides: 'Clickable' A(3) adenosine receptor-selective agonists. Bioorg Med Chem (2009) 0.95
Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity. J Med Chem (2012) 0.92
Polyamidoamine (PAMAM) dendrimer conjugates of "clickable" agonists of the A3 adenosine receptor and coactivation of the P2Y14 receptor by a tethered nucleotide. Bioconjug Chem (2010) 0.89
Synthesis and pharmacological characterization of [(125)I]MRS5127, a high affinity, selective agonist radioligand for the A3 adenosine receptor. Biochem Pharmacol (2009) 0.86
Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions. ACS Med Chem Lett (2012) 0.86
Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element. ACS Med Chem Lett (2011) 0.84
Predicted structures of agonist and antagonist bound complexes of adenosine A3 receptor. Proteins (2011) 0.84
Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor. Biochem Pharmacol (2013) 0.82
Click modification in the N6 region of A3 adenosine receptor-selective carbocyclic nucleosides for dendrimeric tethering that preserves pharmacophore recognition. Bioconjug Chem (2012) 0.81
Fluorescent ligands for adenosine receptors. Bioorg Med Chem Lett (2012) 0.80
Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A3 adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts. BMC Pharmacol (2011) 0.79
Synthesis and biological evaluation of 2',4'- and 3',4'-bridged nucleoside analogues. Bioorg Med Chem (2011) 0.78
Lighting up G protein-coupled purinergic receptors with engineered fluorescent ligands. Neuropharmacology (2015) 0.76
Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists. J Med Chem (2016) 0.75
Synthesis and anti-renal fibrosis activity of conformationally locked truncated 2-hexynyl-N(6)-substituted-(N)-methanocarba-nucleosides as A3 adenosine receptor antagonists and partial agonists. J Med Chem (2014) 0.75
A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem (1976) 903.81
The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science (2008) 11.74
[3H]CGS 21680, a selective A2 adenosine receptor agonist directly labels A2 receptors in rat brain. J Pharmacol Exp Ther (1989) 4.18
Cyanine dye labeling reagents: sulfoindocyanine succinimidyl esters. Bioconjug Chem (1995) 3.90
The Sonogashira reaction: a booming methodology in synthetic organic chemistry. Chem Rev (2007) 3.76
125I-4-aminobenzyl-5'-N-methylcarboxamidoadenosine, a high affinity radioligand for the rat A3 adenosine receptor. Mol Pharmacol (1994) 2.65
A modification of a protein-binding method for rapid quantification of cAMP in cell-culture supernatants and body fluid. Anal Biochem (1990) 2.11
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary. J Med Chem (2002) 1.97
Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology (1997) 1.86
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. J Med Chem (2000) 1.65
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists. J Med Chem (2005) 1.54
Molecular probes for extracellular adenosine receptors. Biochem Pharmacol (1987) 1.47
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
Clinical evidence for utilization of the A3 adenosine receptor as a target to treat rheumatoid arthritis: data from a phase II clinical trial. J Rheumatol (2007) 1.38
Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells. FASEB J (2007) 1.32
ADOA3R as a therapeutic target in experimental colitis: proof by validated high-density oligonucleotide microarray analysis. Inflamm Bowel Dis (2006) 1.32
Protective roles of adenosine A1, A2A, and A3 receptors in skeletal muscle ischemia and reperfusion injury. Am J Physiol Heart Circ Physiol (2007) 1.31
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications. Bioorg Med Chem Lett (2001) 1.26
The A3 adenosine receptor agonist CP-532,903 [N6-(2,5-dichlorobenzyl)-3'-aminoadenosine-5'-N-methylcarboxamide] protects against myocardial ischemia/reperfusion injury via the sarcolemmal ATP-sensitive potassium channel. J Pharmacol Exp Ther (2007) 1.19
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists. J Med Chem (2007) 1.18
The cross-species A3 adenosine-receptor antagonist MRS 1292 inhibits adenosine-triggered human nonpigmented ciliary epithelial cell fluid release and reduces mouse intraocular pressure. Curr Eye Res (2005) 1.17
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system. Bioorg Med Chem (2008) 1.16
2-Chloro-N6-[3H]cyclopentyladenosine ([3H]CCPA)--a high affinity agonist radioligand for A1 adenosine receptors. Naunyn Schmiedebergs Arch Pharmacol (1989) 1.16
Functionalized congener approach to the design of ligands for G protein-coupled receptors (GPCRs). Bioconjug Chem (2009) 1.15
Adenosine receptors in colon carcinoma tissues and colon tumoral cell lines: focus on the A(3) adenosine subtype. J Cell Physiol (2007) 1.15
Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety. Bioorg Med Chem Lett (2005) 1.09
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorg Med Chem Lett (2008) 1.07
Synthesis of ethyl (1S,2R,3S,4S,5S)-2,3-O-(isopropylidene)-4-hydroxy-bicyclo[3.1.0]hexane-carboxylate from L-ribose: a versatile chiral synthon for preparation of adenosine and P2 receptor ligands. Nucleosides Nucleotides Nucleic Acids (2008) 1.07
Optimizing the immobilization of single-stranded DNA onto glass beads. J Biochem Biophys Methods (2001) 1.04
A3 adenosine receptors and mitogen-activated protein kinases in lung injury following in vivo reperfusion. Crit Care (2006) 1.03
2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. J Med Chem (2006) 1.02
Effector coupling of stably transfected human A3 adenosine receptors in CHO cells. Biochem Pharmacol (2002) 1.01
Adenosine induces airway hyperresponsiveness through activation of A3 receptors on mast cells. J Allergy Clin Immunol (2008) 1.01
The A3 adenosine receptor agonist CF502 inhibits the PI3K, PKB/Akt and NF-kappaB signaling pathway in synoviocytes from rheumatoid arthritis patients and in adjuvant-induced arthritis rats. Biochem Pharmacol (2008) 0.99
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists. J Med Chem (2008) 0.99
Activation of various subtypes of G-protein alpha subunits by partial agonists of the adenosine A1 receptor. Biochem Pharmacol (1998) 0.97
Synthesis and characterization of [76Br]-labeled high-affinity A3 adenosine receptor ligands for positron emission tomography. Nucl Med Biol (2009) 0.94
Computer aided comparative analysis of the binding modes of the adenosine receptor agonists for all known subtypes of adenosine receptors. J Mol Graph Model (2006) 0.93
Preparation and first evaluation of [(18)F]FE@SUPPY: a new PET tracer for the adenosine A(3) receptor. Nucl Med Biol (2008) 0.93
Syntheses of D- and L-cyclopentenone derivatives using ring-closing metathesis: versatile intermediates for the synthesis of D- and L-carbocyclic nucleosides. J Org Chem (2001) 0.92
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection. J Med Chem (2005) 0.89
Probing distal regions of the A2B adenosine receptor by quantitative structure-activity relationship modeling of known and novel agonists. J Med Chem (2008) 0.88
Novel strategies for the design of new potent and selective human A3 receptor antagonists: an update. Curr Med Chem (2006) 0.87
Medicinal chemistry of the A3 adenosine receptor: agonists, antagonists, and receptor engineering. Handb Exp Pharmacol (2009) 0.87
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists. Bioorg Med Chem (2009) 0.84
Synthesis and pharmacological characterization of [(125)I]MRS1898, a high-affinity, selective radioligand for the rat A(3) adenosine receptor. Purinergic Signal (2008) 0.82
Functionalized congeners of 1,4-dihydropyridines as antagonist molecular probes for A3 adenosine receptors. Bioconjug Chem (1999) 0.82
Generation of adenosine A3 receptor functionally humanized mice for the evaluation of the human antagonists. Biochem Pharmacol (2005) 0.80
Cannabinoids inhibit noradrenergic and purinergic sympathetic cotransmission in the rat isolated mesenteric arterial bed. Br J Pharmacol (2007) 0.80
Structure of an agonist-bound human A2A adenosine receptor. Science (2011) 6.21
Adenosine receptors as therapeutic targets. Nat Rev Drug Discov (2006) 6.15
International Union of Pharmacology LVIII: update on the P2Y G protein-coupled nucleotide receptors: from molecular mechanisms and pathophysiology to therapy. Pharmacol Rev (2006) 5.28
International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update. Pharmacol Rev (2011) 4.16
UDP acting at P2Y6 receptors is a mediator of microglial phagocytosis. Nature (2007) 3.78
Coordinated adenine nucleotide phosphohydrolysis and nucleoside signaling in posthypoxic endothelium: role of ectonucleotidases and adenosine A2B receptors. J Exp Med (2003) 3.71
Hematoxylin and eosin staining of tissue and cell sections. CSH Protoc (2008) 2.80
Characterization of the UDP-glucose receptor (re-named here the P2Y14 receptor) adds diversity to the P2Y receptor family. Trends Pharmacol Sci (2003) 2.37
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling. J Med Chem (2004) 2.15
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary. J Med Chem (2002) 1.97
Activation of Th1 and Tc1 cell adenosine A2A receptors directly inhibits IL-2 secretion in vitro and IL-2-driven expansion in vivo. Blood (2005) 1.84
N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors. Biochem Pharmacol (2003) 1.82
Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptors. J Med Chem (2002) 1.77
Structure-based discovery of A2A adenosine receptor ligands. J Med Chem (2010) 1.71
Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists. J Med Chem (2003) 1.70
Treatment of dry eye syndrome with orally administered CF101: data from a phase 2 clinical trial. Ophthalmology (2010) 1.70
2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists. J Med Chem (2003) 1.57
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists. J Med Chem (2005) 1.54
Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta (2010) 1.53
2-Chloro N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate is a selective high affinity P2Y(1) receptor antagonist. Br J Pharmacol (2002) 1.52
MRS2500 [2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in mice. J Pharmacol Exp Ther (2005) 1.51
Quantitation of the P2Y(1) receptor with a high affinity radiolabeled antagonist. Mol Pharmacol (2002) 1.49
Identification of essential residues involved in the allosteric modulation of the human A(3) adenosine receptor. Mol Pharmacol (2003) 1.46
Pharmacological and therapeutic effects of A3 adenosine receptor agonists. Drug Discov Today (2011) 1.44
Identification by site-directed mutagenesis of residues involved in ligand recognition and activation of the human A3 adenosine receptor. J Biol Chem (2002) 1.44
Human P2Y(6) receptor: molecular modeling leads to the rational design of a novel agonist based on a unique conformational preference. J Med Chem (2005) 1.43
Molecular Architecture of G Protein-Coupled Receptors. Drug Dev Res (1996) 1.39
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
Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y6 nucleotide receptors. Biochem Pharmacol (2004) 1.38
Exploring distal regions of the A3 adenosine receptor binding site: sterically constrained N6-(2-phenylethyl)adenosine derivatives as potent ligands. Bioorg Med Chem (2004) 1.34
Protective roles of adenosine A1, A2A, and A3 receptors in skeletal muscle ischemia and reperfusion injury. Am J Physiol Heart Circ Physiol (2007) 1.31
Induction of novel agonist selectivity for the ADP-activated P2Y1 receptor versus the ADP-activated P2Y12 and P2Y13 receptors by conformational constraint of an ADP analog. J Pharmacol Exp Ther (2004) 1.31
Conformational changes involved in G-protein-coupled-receptor activation. Trends Pharmacol Sci (2008) 1.29
Structure-activity relationships of uridine 5'-diphosphate analogues at the human P2Y6 receptor. J Med Chem (2006) 1.28
Targeted deletion of adenosine A(3) receptors augments adenosine-induced coronary flow in isolated mouse heart. Am J Physiol Heart Circ Physiol (2002) 1.27
Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists. J Med Chem (2002) 1.26
Digitoxin mimics gene therapy with CFTR and suppresses hypersecretion of IL-8 from cystic fibrosis lung epithelial cells. Proc Natl Acad Sci U S A (2004) 1.25
N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor. J Med Chem (2003) 1.25
Antiaggregatory activity in human platelets of potent antagonists of the P2Y 1 receptor. Biochem Pharmacol (2004) 1.25
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor. J Med Chem (2006) 1.25
Rapid identification of functionally critical amino acids in a G protein-coupled receptor. Nat Methods (2007) 1.24
Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions. J Med Chem (2012) 1.23
Keynote review: allosterism in membrane receptors. Drug Discov Today (2006) 1.22
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. J Med Chem (2005) 1.21
Quantification of Gi-mediated inhibition of adenylyl cyclase activity reveals that UDP is a potent agonist of the human P2Y14 receptor. Mol Pharmacol (2009) 1.20
Controlling murine and rat chronic pain through A3 adenosine receptor activation. FASEB J (2012) 1.20
Emerging adenosine receptor agonists. Expert Opin Emerg Drugs (2007) 1.19
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists. J Med Chem (2007) 1.18
Structure activity and molecular modeling analyses of ribose- and base-modified uridine 5'-triphosphate analogues at the human P2Y2 and P2Y4 receptors. Biochem Pharmacol (2005) 1.18
Progress in the pursuit of therapeutic adenosine receptor antagonists. Med Res Rev (2006) 1.18
Paraffin embedding tissue samples for sectioning. CSH Protoc (2008) 1.18
The cross-species A3 adenosine-receptor antagonist MRS 1292 inhibits adenosine-triggered human nonpigmented ciliary epithelial cell fluid release and reduces mouse intraocular pressure. Curr Eye Res (2005) 1.17
Systematic investigation of polyamidoamine dendrimers surface-modified with poly(ethylene glycol) for drug delivery applications: synthesis, characterization, and evaluation of cytotoxicity. Bioconjug Chem (2008) 1.17
Development of selective agonists and antagonists of P2Y receptors. Purinergic Signal (2008) 1.17
Identification of an agonist-induced conformational change occurring adjacent to the ligand-binding pocket of the M(3) muscarinic acetylcholine receptor. J Biol Chem (2005) 1.17
CysLT1 leukotriene receptor antagonists inhibit the effects of nucleotides acting at P2Y receptors. Biochem Pharmacol (2005) 1.17
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system. Bioorg Med Chem (2008) 1.16
Structural determinants of efficacy at A3 adenosine receptors: modification of the ribose moiety. Biochem Pharmacol (2004) 1.16
Activity of Novel Adenine Nucleotide Derivatives as Agonists and Antagonists at Recombinant Rat P2X Receptors. Drug Dev Res (2000) 1.16
UDP is a competitive antagonist at the human P2Y14 receptor. J Pharmacol Exp Ther (2008) 1.13
Toward multivalent signaling across G protein-coupled receptors from poly(amidoamine) dendrimers. Bioconjug Chem (2008) 1.13
Stimulation of the P2X7 receptor kills rat retinal ganglion cells in vivo. Exp Eye Res (2010) 1.12
Small molecule blockers of the Alzheimer Abeta calcium channel potently protect neurons from Abeta cytotoxicity. Proc Natl Acad Sci U S A (2009) 1.12
Structure-activity relationship of uridine 5'-diphosphoglucose analogues as agonists of the human P2Y14 receptor. J Med Chem (2007) 1.12
P2Y6 nucleotide receptor activates PKC to protect 1321N1 astrocytoma cells against tumor necrosis factor-induced apoptosis. Cell Mol Neurobiol (2003) 1.11
Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives. Mol Pharmacol (2002) 1.11
2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors. Biochem Pharmacol (2004) 1.11
Demystifying the three dimensional structure of G protein-coupled receptors (GPCRs) with the aid of molecular modeling. Chem Commun (Camb) (2003) 1.10
UDP-glucose acting at P2Y14 receptors is a mediator of mast cell degranulation. Biochem Pharmacol (2009) 1.10
Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety. Bioorg Med Chem Lett (2005) 1.09
Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists. Bioorg Med Chem (2008) 1.08
[32P]2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate ([32P]MRS2500), a novel radioligand for quantification of native P2Y1 receptors. Br J Pharmacol (2006) 1.07
Behavioral characterization of mice lacking the A3 adenosine receptor: sensitivity to hypoxic neurodegeneration. Cell Mol Neurobiol (2003) 1.07
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorg Med Chem Lett (2008) 1.07
Structure-activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists. Bioorg Med Chem (2004) 1.07
Synthesis of ethyl (1S,2R,3S,4S,5S)-2,3-O-(isopropylidene)-4-hydroxy-bicyclo[3.1.0]hexane-carboxylate from L-ribose: a versatile chiral synthon for preparation of adenosine and P2 receptor ligands. Nucleosides Nucleotides Nucleic Acids (2008) 1.07